Herbal Science Research - anti-inflammatory

Some phytochemical, pharmacological and toxicological properties of ginger (Zingiber officinale Roscoe): A review [...]

Site Editor — Fri, 02 Nov 2007 15:49:24 -0700

Some phytochemical, pharmacological and toxicological properties of ginger (Zingiber officinale Roscoe): A review of recent research.: Food Chem Toxicol. 2007 Sep 18; Ali BH, Blunden G, Tanira MO, Nemmar A

Ginger (Zingiber officinale Roscoe, Zingiberacae) is a medicinal plant that has been widely used in Chinese, Ayurvedic and Tibb-Unani herbal medicines all over the world, since antiquity, for a wide array of unrelated ailments that include arthritis, rheumatism, sprains, muscular aches, pains, sore throats, cramps, constipation, indigestion, vomiting, hypertension, dementia, fever, infectious diseases and helminthiasis. Currently, there is a renewed interest in ginger, and several scientific investigations aimed at isolation and identification of active constituents of ginger, scientific verification of its pharmacological actions and of its constituents, and verification of the basis of the use of ginger in some of several diseases and conditions. This article aims at reviewing the most salient recent reports on these investigations. The main pharmacological actions of ginger and compounds isolated therefrom include immuno-modulatory, anti-tumorigenic, anti-inflammatory, anti-apoptotic, anti-hyperglycemic, anti-lipidemic and anti-emetic actions. Ginger is a strong anti-oxidant substance and may either mitigate or prevent generation of free radicals. It is considered a safe herbal medicine with only few and insignificant adverse/side effects. More studies are required in animals and humans on the kinetics of ginger and its constituents and on the effects of their consumption over a long period of time.

Comparison of glucosamine sulfate and a polyherbal supplement for the relief of osteoarthritis of the knee [...]

Site Editor — Fri, 02 Nov 2007 15:31:58 -0700

Comparison of glucosamine sulfate and a polyherbal supplement for the relief of osteoarthritis of the knee: a randomized controlled trial [ISRCTN25438351].:
BMC Complement Altern Med. 2007 Oct 31;7(1):34 Authors: Mehta K, Gala J, Bhasale S, Naik S, Modak M, Thakur H, Deo N, Miller MJ

ABSTRACT: BACKGROUND: The efficacy and safety of a dietary supplement derived from South American botanicals was compared to glucosamine sulfate in osteoarthritis subjects in a Mumbai-based multi-center, randomized, double-blind study. METHODS: Subjects (n=95) were screened and randomized to receive glucosamine sulfate (n= 47, 1500 mg/day) or reparagen (n=48, 1800 mg/day), a polyherbal consisting of 300 mg of vincaria (Uncaria guianensis) and 1500 mg of RNI 249 (Lepidium meyenii) administered orally, twice daily. Primary efficacy variable was response rate based on a 20% improvement in WOMAC pain scores. Additional outcomes were WOMAC scores for pain, stiffness and function, visual analog score (VAS) for pain, with assessments at 1, 2, 4, 6 and 8 weeks. Tolerability, investigator and subject global assessments and rescue medication consumption (paracetamol) were measured together with safety assessments including vital signs and laboratory based assays. RESULTS: Subject randomization was effective: age, gender and disease status distribution was similar in both groups. The response rates (20% reduction in WOMAC pain) were substantial for both glucosamine (89%) and reparagen (94%) and supported by investigator and subject assessments. Using related criteria response rates to reparagen were favorable when compared to glucosamine. Compared to baseline both treatments showed significant benefits in WOMAC and VAS outcomes within one week (P<0.05), with a similar, progressive improvement over the course of the 8 week treatment protocol (45-62% reduction in WOMAC or VAS scores). Tolerability was excellent, no serious adverse events were noted and safety parameters were unchanged. Rescue medication use was significantly lower in the reparagen group (p <0.01) at each assessment period. Serum IGF-1 levels were unaltered by treatments. CONCLUSION: Both reparagen and glucosamine sulfate produced substantial improvements in pain, stiffness and function in subjects with osteoarthritis. Response rates were high and the safety profile was excellent, with significantly less rescue medication use with reparagen. Reparagen represents a new natural productive alternative in the management of joint health. Trial registration: Current Controlled Trials ISRCTN25438351.

PMID: 17974032 [PubMed - as supplied by publisher]

Epigallocatechin gallate affects human dendritic cell differentiation and maturation.

Site Editor — Mon, 22 Oct 2007 18:26:50 -0700

Epigallocatechin gallate affects human dendritic cell differentiation and maturation.: J Allergy Clin Immunol. 2007 Oct 10; Authors: Yoneyama S, Kawai K, Tsuno NH, Okaji Y, Asakage M, Tsuchiya T, Yamada J, Sunami E, Osada T, Kitayama J, Takahashi K, Nagawa H

BACKGROUND: Epigallocatechin gallate (EGCG), a component of green tea catechin with the strongest biological activity, has been focused in recent years because of its anti-inflammatory and immunomodulatory activities. Dendritic cells (DCs) are professional antigen-presenting cells, capable of priming naive T cells, and play the key roles in the activation of T-cell-mediated immune responses. OBJECTIVE: We aimed to investigate the effect of EGCG on human monocyte-derived DCs (MODCs) and, consequently, on the T-cell-mediated immune response. METHODS: The induction of apoptosis, and the detailed phenotypic and functional changes of MODCs, generated by culture of peripheral blood monocytes in the presence of GM-CSF and IL-4, induced by EGCG was investigated and compared with the effects of dexamethasone. RESULTS: Epigallocatechin gallate induced apoptosis and affected the phenotype of the developing DCs. The expressions of CD83, CD80, CD11c, and MHC class II, which are molecules essential for antigen presentation by DCs, were downregulated by EGCG. EGCG also suppressed the endocytotic ability of immature DCs, whereas dexamethasone-treated DCs had higher endocytotic ability than control DCs. Most importantly, mature DCs treated with EGCG inhibited stimulatory activity toward allogeneic T cells while secreting high amounts of IL-10. CONCLUSION: Epigallocatechin gallate induces immunosuppressive alterations on human MODCs, both by induction of apoptosis and suppression of cell surface molecules and antigen presentation. CLINICAL IMPLICATIONS: These alterations should be considered promising new immunosuppressive and anti-inflammatory agents to treat autoimmune and allergic diseases and to prevent the graft rejection in organ transplantation.

PMID: 17935769 [PubMed - as supplied by publisher]

B vitamins and berries and age-related neurodegenerative disorders.

Site Editor — Mon, 22 Oct 2007 18:20:48 -0700

B vitamins and berries and age-related neurodegenerative disorders.: Evid Rep Technol Assess (Full Rep). 2006 Apr;(134):1-161 Authors: Balk E, Chung M, Raman G, Tatsioni A, Chew P, Ip S, DeVine D, Lau J

OBJECTIVES: To assess the effects, associations, mechanisms of action, and safety of B vitamins and, separately, berries and their constituents on age-related neurocognitive disorders-primarily Alzheimer's (AD) and Parkinson's disease (PD). DATA SOURCES: MEDLINE and CAB Abstracts. Additional studies were identified from reference lists and technical experts. REVIEW METHODS: Vitamins B1, B2, B6, B12, and folate, and a dozen types of berries and their constituents were evaluated. Human, animal, and in vitro studies were evaluated. Outcomes of interest from human studies were neurocognitive function or diagnosis with AD, cognitive decline, PD, or related conditions. Intervention studies, associations between dietary intake and outcomes, and associations between B vitamin levels and outcomes were evaluated. Specific mechanisms of action were evaluated in animal and in vitro studies. Studies were extracted for study design, demographics, intervention or predictor, and neurocognitive outcomes. Studies were graded for quality and applicability. RESULTS: In animal studies, deficiencies in vitamins B1 or folate generally cause neurological dysfunction; supplementation with B6, B12, or folate may improve neurocognitive function. In animal experiments folate and B12 protect against genetic deficiencies used to model AD; thiamine and folate also affect neurovascular function and health. Human studies were generally of poor quality. Weak evidence suggests possible benefits of B1 supplementation and injected B12 in AD. The effects of B6 and folate are unclear. Overall, dietary intake studies do not support an association between B vitamin intake and AD. Studies evaluating B vitamin status were mostly inadequate due to poor study design. Overall, studies do not support an association between B vitamin status and age-related neurocognitive disorders. Only one study evaluated human berry consumption, finding no association with PD. Animal studies of berries have almost all been conducted by the same research group. Several berry constituents have been shown to affect brain and nerve tissue function. Blueberry and strawberry extract were protective of markers of disease, although effects on neurocognitive tests were less consistent. Berry extracts may protect against the deleterious effects of compounds associated with AD. Reporting of adverse events was uncommon. When reported, actual adverse events from B vitamins were rare and minor. CONCLUSIONS: The current research on B vitamins is largely inadequate to confidently assess their mechanisms of action on age-related neurocognitive disorders, their associations with disease, or their effectiveness as supplements. B vitamin supplementation may be of value for neurocognitive function, but the evidence is inconclusive.

PMID: 17628125 [PubMed - indexed for MEDLINE]

[Research on different processings of Scutellaria baicalensis Georgi]

Site Editor — Mon, 22 Oct 2007 18:19:21 -0700

[Research on different processings of Scutellaria baicalensis Georgi]: Zhong Yao Cai. 2006 Sep;29(9):893-5 Authors: Song SH, Wang BL, Feng JK, Wang ZZ

OBJECTIVE: Comparing the different processings of S. baicalensis Georgi with fresh herb. METHODS: Watering, cooking and steaming method were adopted and the contents of flavonoids was determined by HPLC. RESULTS: Cooking and steaming method could not only intenerate the slices, but also destroy the activity of enzyme. So different means could be choosen according to practice. CONCLUSION: Among them, cooking method with 1 time volume of water, heating 10 min, drying at 80 degrees C and steaming method taking 20 min, drying at 80 degrees C is proper.

PMID: 17212039 [PubMed - indexed for MEDLINE]

Anti-inflammatory properties and regulatory mechanism of a novel derivative of artemisinin in [...] autoimmune encephalomyelitis

Site Editor — Mon, 22 Oct 2007 18:09:34 -0700

Anti-inflammatory properties and regulatory mechanism of a novel derivative of artemisinin in experimental autoimmune encephalomyelitis.: J Immunol. 2007 Nov 1;179(9):5958-65 Authors: Wang Z, Qiu J, Guo TB, Liu A, Wang Y, Li Y, Zhang JZ

Ethyl 2-[4-(12-beta-artemisininoxy)]phenoxylpropionate (SM933) is a novel derivative of artemisinin, an herbal compound approved for the treatment of malaria. In this study, we show that SM933 has unique anti-inflammatory properties through regulation of signaling pathways, leading to amelioration of experimental autoimmune encephalomyelitis. The anti-inflammatory properties of SM933 were characterized by inhibition of encephalitogenic T cell responses that were altered to exhibit a Th2 immune deviation and reduced activity and concentration of NO and inducible NO synthase. The observed effect of SM933 was mediated through regulatory mechanisms involving the NFkappaB and the Rig-G/JAB1 signaling pathways. SM933 was found to inhibit the activity of NFkappaB by up-regulating IkappaB, which accounted for various down-stream anti-inflammatory actions. Furthermore, it up-regulated Rig-G through the action of IFN-alpha and prevented JAB1, a master cell cycle regulator, from entering the nucleus to promote p27 degradation, resulting in down-regulation of CDK2 and cyclin A and cell cycle progression. Regulation of the Rig-G/JAB1 pathway by SM933 led to altered cell cycle activity of encephalitogenic T cells as a result of its selective effect on activated, but not resting, T cells. The study indicates that SM933 is a novel anti-inflammatory agent acting through defined signaling mechanisms and provides regulatory mechanisms required for effective drug targeting in treatment of autoimmune disease and inflammation.

PMID: 17947669 [PubMed - in process]

[STW 5/Iberogast: multi-target-action for treatment of functional dyspepsia and irritable bowel syndrome]

Site Editor — Sun, 21 Oct 2007 05:52:12 -0700

[STW 5/Iberogast: multi-target-action for treatment of functional dyspepsia and irritable bowel syndrome]: Wien Med Wochenschr. 2007;157(13-14):301-7 Authors: Allescher HD, Wagner H

Functional gastro-intestinal diseases such as functional dyspepsia and irritable bowel syndrome are a therapeutic challenge, as they are not only characterized by a multitude of symptoms, some of them with severe consequences for affected patients, but are also caused by a multitude of factors. The clinical efficacy of the therapeutics STW 5/Iberogast in these diseases has been proven in a number of randomized prospective clinical studies. Several preclinical studies suggest that its efficacy could be due to its complex composition of nine standardized herbal extracts, which act differently on multiple sites. This principle, which is quite popular in clinical medicine, was introduced as a multi-target therapy for functional bowel disorders. Components of STW 5/Iberogast reduce gastro-intestinal hypersensitivity and act spasmolytic on spastic, tonicising on atonic gastro-intestinal muscle. In addition a stimulating effect on reduced mucus-secretion, an inhibitory effect on enhanced gastric acid secretion and an anti-inflammatory effect have been shown. These effects could explain the clinical efficacy of STW5/Iberogast in a large range of symptoms.

PMID: 17704976 [PubMed - indexed for MEDLINE]

Phytodolor--effects and efficacy of a herbal medicine.

Site Editor — Sun, 21 Oct 2007 05:50:54 -0700

Phytodolor--effects and efficacy of a herbal medicine.: Wien Med Wochenschr. 2007;157(13-14):343-7 Authors: Gundermann KJ, Müller J

Herbal antirheumatics are successfully used in painful inflammatory or degenerative rheumatic diseases. One of these herbal medicines is Phytodolor (STW 1), a fixed combination of extracts from aspen leaves and bark (Populus tremula), common ash bark (Fraxinus excelsior), and golden rod herb (Solidago virgaurea). Its effects as well as those of its components have been verified in experimental and human pharmacological investigations. The mode of action of STW 1 includes antiinflammatory, antioedematous, antioxidative and analgesic properties, and it is considered to be broader than that of synthetic antirheumatics. Open clinical studies and randomised, placebo- or verum-controlled double-blind trials, performed in different subtypes of rheumatic diseases, confirm the pharmacological evidence of efficacy, such as by reducing the intake of non-steroidal antiinflammatory drugs (NSAIDs). STW 1 has a high drug safety. CONCLUSION: Phytodolor (STW 1) is a reasonable alternative to NSAIDs and to cyclooxygenase(COX)-2-inhibitors such as rofecoxib.

PMID: 17704984 [PubMed - indexed for MEDLINE]

Use of herbal preparations in the treatment of oxidant-mediated inflammatory disorders.

Site Editor — Sun, 21 Oct 2007 05:41:39 -0700

Use of herbal preparations in the treatment of oxidant-mediated inflammatory disorders.: Complement Ther Med. 2007 Sep;15(3):207-16 Authors: Kaplan M, Mutlu EA, Benson M, Fields JZ, Banan A, Keshavarzian A

Complementary and alternative medicine (CAM) use has increased in popularity in recent years and herbal therapy alone is now a billion dollar market. For centuries herbs have been used as food and for medicinal purposes. Various herbs have been identified as possessing anti-inflammatory and antioxidative properties, and they are currently being used to treat inflammatory disorders as well as those caused by reactive oxygen species (ROS). Asthma, Alzheimer's disease, inflammatory bowel disease (IBD), rheumatoid arthritis (RA), and atherogenesis are all disorders where inflammation and ROS are involved in their pathogenesis. This review examines the pathogenesis of the above mentioned ROS-mediated inflammatory disorders, as well as discusses the antioxidant and anti-inflammatory mechanisms of various herbs and the clinical trials where herbs have been used to treat these disorders.

PMID: 17709066 [PubMed - indexed for MEDLINE]

[...] Nonpharmacological and Nonsurgical Interventions for Patients With Rheumatoid Arthritis: An Overview of Systematic Reviews

Site Editor — Thu, 04 Oct 2007 05:42:36 -0700

Effectiveness of Nonpharmacological and Nonsurgical Interventions for Patients With Rheumatoid Arthritis: An Overview of Systematic Reviews.: Phys Ther. 2007 Sep 25; Authors: Christie A, Jamtvedt G, Dahm KT, Moe RH, Haavardsholm EA, Hagen KB

CONCLUSIONS:based on systematic reviews of randomized controlled trials are considered to provide the highest level of evidence about the effectiveness of an intervention. This overview summarizes the available evidence from systematic reviews on the effects of nonpharmacological and nonsurgical interventions for rheumatoid arthritis (RA). Systematic reviews of studies of patients with RA (aged >18 years) published between 2000 and 2007 were identified by comprehensive literature searches. Methodological quality was independently assessed by 2 authors, and the quality of evidence was summarized by explicit methods. Pain, function, and patient global assessment were considered primary outcomes of interest. Twenty-eight systematic reviews were included in this overview. High-quality evidence was found for beneficial effects of joint protection and patient education, moderate-quality evidence was found for beneficial effects of herbal therapy (gamma-linolenic acid) and low-level laser therapy, and low-quality evidence was found for the effectiveness of the other interventions. The quality of evidence for the effectiveness of most nonpharmacological and nonsurgical interventions in RA is moderate to low.

PMID: 17906290 [PubMed - as supplied by publisher]

Carpal tunnel syndrome, diabetic neuropathy, fibromyalgia, glucosamine and chondroitin, hypnosis [...], marijuana for pain.

Site Editor — Thu, 04 Oct 2007 05:30:00 -0700

Carpal tunnel syndrome, diabetic neuropathy, fibromyalgia, glucosamine and chondroitin, hypnosis in pain management, marijuana for pain.: J Pain Palliat Care Pharmacother. 2007;21(2):61-7 Authors: Fishman SM

This feature presents information for patients in a question and answer format. It is written to simulate actual questions that many pain patients ask and to provide answers in a context and language that most pain patients will comprehend. Issues addressed in this issue are carpel tunnel syndrome, fibromyalgia, glucosamine and chondroitin, hypnosis, marijuana.

PMID: 17844729 [PubMed - indexed for MEDLINE]

Wound healing activity of Matricaria recutita L. extract.

Site Editor — Thu, 04 Oct 2007 05:28:53 -0700

Wound healing activity of Matricaria recutita L. extract.: J Wound Care. 2007 Jul;16(7):298-302 Authors: Nayak BS, Raju SS, Rao AV

OBJECTIVE: To evaluate the wound healing activity of M. recutita (chamomile) extract in rats. METHOD: Wound healing activity was determined using excision, incision and dead space wound models.The animals were divided into two groups of six for each model: animals in the test group were treated with the aqueous extract of M. recutita (120mg/kg/day), which was mixed in their drinking water. Animals in the control group were maintained with plain drinking water. Healing was assessed by the rate of wound contraction, period of epithelialisation, wound-breaking strength, granulation tissue weight and hydoxyproline content.Antimicrobial activity of the extract against various microorganisms was assessed. RESULTS: On day 15 animals in the test group exhibited a greater reduction in the wound area when compared with the controls (61 % versus 48%), faster epithelialisation and a significantly higher wound-breaking strength (p<0.002). In addition, wet and dry granulation tissue weight and hydroxyproline content were significantly higher. CONCLUSION: The increased rate of wound contraction, together with the increased wound-breaking strength, hydroxyproline content and histological observations, support the use of M. recutita in wound management. However, this needs to be studied further before it can be considered for clinical use.

PMID: 17708380 [PubMed - indexed for MEDLINE]

Incensole Acetate, [...] Isolated from Boswellia Resin, Inhibits Nuclear Factor (NF)-kappa B Activation.

Site Editor — Thu, 27 Sep 2007 19:02:56 -0700

Incensole Acetate, a Novel anti-inflammatory compound Isolated from Boswellia Resin, Inhibits Nuclear Factor (NF)-kappa B Activation.: Mol Pharmacol. 2007 Sep 25; Authors: Moussaieff A, Shohami E, Kashman Y, Fride E, Schmitz ML, Renner F, Fiebich BL, Munoz E, Ben-Neriah Y, Mechoulam R

Boswellia resin is a major anti-inflammatory agent in herbal medical tradition, as well as a common food supplement. Its anti-inflammatory activity has been attributed to boswellic acid and its derivatives. Here, we re-examined the anti-inflammatory effect of the resin, using IkappaBalpha degradation in TNFalpha-stimulated HeLa cells as a read-out for a bioassay-guided fractionation. We thus isolated two novel NF-kappaB inhibitors from the resin, their structures elucidated as incensole acetate (IA) and its non-acetylated form, incensole (IN). IA inhibited TAK/TAB-mediated IkappaB kinase (IKK) activation loop phosphorylation, resulting in the inhibition of cytokine and LPS mediated NF-kappaB activation. It had no effect on IKK activity in vitro, nor did it suppress IkappaBalpha phosphorylation in costimulated T-cells, indicating that the kinase inhibition is neither direct, nor is it affecting all NF-kappaB activation pathways. The inhibitory effect appears specific as IA did not interfere with TNFalpha-induced activation of JNK and p38 MAPK. IA treatment had a robust anti-inflammatory effect in a mouse inflamed paw model. Cembrenoid diterpenoids, and specifically IA and its derivatives may thus constitute a potential novel group of NF-kappaB inhibitors, originating from an ancient anti-inflammatory herbal remedy.

PMID: 17895408 [PubMed - as supplied by publisher]

A comprehensive review on nettle effect and efficacy profiles, Part I: herba urticae.

Site Editor — Wed, 26 Sep 2007 19:17:00 -0700

A comprehensive review on nettle effect and efficacy profiles, Part I: herba urticae. Chrubasik JE, Roufogalis BD, Wagner H, Chrubasik SA. Phytomedicine. 2007 Jun;14(6):423-35.

Nettle herb is recommended for complaints associated with rheumatoid arthritis, osteoarthritis and urinary tract infections. We therefore conducted a comprehensive review of the literature to summarize the pharmacological and clinical effects of this plant material. Although clinical and experimental studies suggest that nettle herb has some anti-inflammatory properties, clinical evidence beyond doubt is lacking. Nettle preparations exert a number of promising in vitro and in vivo effects, however, further studies are needed to support these results and to find out if these effects are surrogates for clinical relevant effects in humans.

PMID: 17493795 [PubMed - indexed for MEDLINE]

A randomized, placebo-controlled, double-blind clinical trial of curcuminoids in oral lichen planus.

Site Editor — Wed, 26 Sep 2007 19:01:00 -0700

A randomized, placebo-controlled, double-blind clinical trial of curcuminoids in oral lichen planus.: Phytomedicine. 2007 Aug;14(7-8):437-46 Authors: Chainani-Wu N, Silverman S, Reingold A, Bostrom A, Mc Culloch C, Lozada-Nur F, Weintraub J

We studied the efficacy of curcuminoids in the treatment of oral lichen planus (OLP), a chronic, mucocutaneous, immunological disease. Curcuminoids are components of turmeric (Curcuma longa) that have anti-inflammatory activity. Turmeric has been used in Ayurveda (Indian traditional medicine) for centuries. A randomized, double-blind, placebo-controlled trial was conducted. In all, 100 consecutive, eligible patients with OLP presenting to the oral medicine clinic at the University of California, San Francisco, were to be selected. Two interim analyses were to be conducted during the trial. The trial was conducted between February 2003 and September 2004. The first interim analysis was conducted in October 2004 using data from the first 33 subjects. Study subjects were randomized to receive either placebo or curcuminoids at 2000 mg/day for 7 weeks. In addition, all subjects received prednisone at 60 mg/day for the first 1 week. The primary outcome was a change in symptoms from baseline. Secondary outcomes were changes in clinical signs and occurrence of side effects. The first interim analysis did not show a significant difference between the placebo and curcuminoids groups. Conditional power calculations suggested a less than 2% chance that the curcuminoids group would have a significantly better outcome as compared with the placebo group if the trial were continued to completion. Therefore, the study was ended early for futility. Reaching a conclusion regarding the efficacy of curcuminoids based on the results of this study is not possible as it was ended early for futility. Curcuminoids at this dose were well tolerated and the results suggest that for future studies a larger sample size, a higher dose and/or longer duration of curcuminoids administration should be considered; however, for the next step, an RCT of a shorter duration, using a higher dose of curcuminoids, and without an initial course of prednisone, should be considered.

PMID: 17604143 [PubMed - indexed for MEDLINE]

[Effect of chinese herbs in enhancing prednisone for treatment of refractory rheumatoid arthritis]

Site Editor — Sat, 22 Sep 2007 18:15:33 -0700

[Effect of chinese herbs in enhancing prednisone for treatment of refractory rheumatoid arthritis]: Zhongguo Zhong Xi Yi Jie He Za Zhi. 2007 Aug; 27(8): 742-4 Liu W, Liu XY, Wang Y

OBJECTIVE: To investigate the Chinese herbal medicine in enhancing effect of prednisone for treatment of refractory rheumatoid arthritis (RA). METHODS: One hundred and twenty patients with refraetory RA were assigned to two groups, the treated group was orally administered with Qingbi Tablet, a patent Chinese herbal preparation formulated based on the clearing heat and removing toxic substances principle, and the control group was treated with intramuscular injection of amethopterin (MTX), oral intake of voltaren 75 mg and hydroxychloroquine 0.2 g once a day. Besides prednisone was given to all patients orally, the initiating dosage used in the treated group was lesser than that in the control group. The clinical index, dosage and adverse reaction of prednisone were recorded every 2 weeks. RESULTS: The curative effect evaluated by American College of Rheumatology (ACR) standard showed no statistical difference between the two groups (P > 0.05). Either clinical or laboratory indexes were improved significantly in both groups (P < 0.05), but the improvement in resting pain, patient's self-evaluation and doctor's evaluation in the treated group were better than those in the control group, showing statistical difference (P < 0.05). The 20-week total amount of prednisone used in the treated group was less than that in the control group (32,935 mg vs. 51,170 mg), while the dosage of prednisone used in various observation time points between the two groups was also significantly different respectively (P < 0.05), the former was less than the latter. CONCLUSION: Chinese herbal medicine can enhance the effect of prednisone in patients of refractory RA and alleviate the adverse reactions of prednisone.

Alkamides from Echinacea inhibit cyclooxygenase-2 activity in human neuroglioma cells.

Site Editor — Sat, 22 Sep 2007 17:45:09 -0700

Alkamides from Echinacea inhibit cyclooxygenase-2 activity in human neuroglioma cells.: Biochem Biophys Res Commun . 2007 Aug 24; 360(2): 441-6 Hinz B, Woelkart K, Bauer R

During past years inhibition of the cyclooxygenase-2 (COX-2) enzyme has been proven as an effective strategy to suppress pain and inflammation. Based on this and other mechanistic findings, interest has also renewed in the molecular pathways underlying the anti-inflammatory effects of herbal drugs. The present study addressed this issue and investigated the impact of several polyunsaturated alkamides isolated from a CO2 extract of the roots of Echinacea angustifolia DC. on both activity and expression of COX-2. A 48-h treatment of H4 human neuroglioma cells with the CO2 extract led to a significant suppression of prostaglandin (PG) E2 formation. Analysis of eight different alkamides revealed a contribution of undeca-2Z-ene-8,10-diynoic acid isobutylamide (A5), dodeca-2E-ene-8,10-diynoic acid isobutylamide (A7), and dodeca-2E,4Z-diene-8,10-diynoic acid 2-methylbutylamide (A8) to this response. Using an established short-term COX-2 activity assay, all three alkamides were shown to interfere with COX-2 activity. In contrast, none of the COX-2-suppressing nor any other tested alkamide was found to inhibit COX-2 mRNA and protein expression. Instead, increased COX-2 mRNA and protein levels were registered in the presence of the CO2 extract and most of the analyzed alkamides which caused, however, no stimulation of PG formation. Overall, our results suggest that certain alkamides derived from E. angustifolia roots may contribute to the pharmacological action of the herbal extract by inhibiting COX-2-dependent PGE2 formation at sites of inflammation.

A review of the efficacy and safety of devil's claw for pain [...]

Site Editor — Sat, 22 Sep 2007 17:34:55 -0700

A review of the efficacy and safety of devil's claw for pain associated with degenerative musculoskeletal diseases, rheumatoid, and osteoarthritis.: Holist Nurs Pract. 2007 Jul-Aug;21(4):203-7 Authors: Denner SS

Harpagophytum procumbens, known as devil's claw, has been used traditionally for the treatment of pain, fevers, and dyspepsia. Recently, it has become popular for the treatment of rheumatoid and osteoarthritis. Studies have yet to establish a clear mechanism of action; however, current research is focusing on pro-inflammatory mediators as well as on potential antioxidant characteristics.

PMID: 17627199 [PubMed - indexed for MEDLINE]

Interleukin-1 genotype-selective inhibition of inflammatory mediators by a botanical: a nutrigenetics proof of concept.

Site Editor — Sat, 22 Sep 2007 17:12:00 -0700

Interleukin-1 genotype-selective inhibition of inflammatory mediators by a botanical: a nutrigenetics proof of concept.: Nutrition. 2007 Sep 18; Authors: Kornman K, Rogus J, Roh-Schmidt H, Krempin D, Davies AJ, Grann K, Randolph RK

OBJECTIVE: Although observational studies have shown that genotype may influence nutritional effects on target outcomes, there are few reported studies that stratified subjects by genotype before a nutritional intervention. This proof-of-concept trial determined whether specifically formulated botanical mixtures reduced inflammation in individuals with genetic variations that predispose to overexpression of interleukin-1beta (IL-1beta) and early heart disease. METHODS: Healthy adults with elevated C-reactive protein (CRP) were stratified into genetic groups based on being positive (IL1(Pos)) or negative (IL1(Neg)) for the at-risk IL-1 gene variations. IL1(Pos) (n = 39) and IL1(Neg) (n = 40) subjects were then randomized to the candidate botanical formulation or placebo. The botanical formulation included rose hips, a blueberry and blackberry mixture, and a grapevine extract. RESULTS: At 12 wk of dosing with the botanical formulation, IL-1beta gene expression by stimulated peripheral blood mononuclear cells was significantly lower than at baseline and significantly lower than placebo in IL1(Pos) and IL1(Neg) subjects. Mean IL-1beta gene expression treatment effect over the 12-wk period was greater in IL1(Pos) than in IL1(Neg) subjects. At 12 wk of dosing the botanical mixture produced no mean change in serum CRP levels. However, in IL1(Pos) subjects, significantly more subjects achieved a reduction in CRP with the botanical mixture than with placebo. No CRP effect was observed in the IL1(Neg) subjects. CONCLUSION: This study represents one of a few prospective clinical trials in which genetic variations were shown to differentially influence nutrient effects on outcomes.

PMID: 17884346 [PubMed - as supplied by publisher]

Alkamides from Echinacea inhibit cyclooxygenase-2 activity in human neuroglioma cells.

Site Editor — Fri, 13 Jul 2007 18:39:55 -0700

Alkamides from Echinacea inhibit cyclooxygenase-2 activity in human neuroglioma cells.: >Biochem Biophys Res Commun. 2007 Jun 19; Hinz B, Woelkart K, Bauer R

During past years inhibition of the cyclooxygenase-2 (COX-2) enzyme has been proven as an effective strategy to suppress pain and inflammation. Based on this and other mechanistic findings, interest has also renewed in the molecular pathways underlying the anti-inflammatory effects of herbal drugs. The present study addressed this issue and investigated the impact of several polyunsaturated alkamides isolated from a CO(2) extract of the roots of Echinacea angustifolia DC on both activity and expression of COX-2. A 48-h treatment of H4 human neuroglioma cells with the CO(2) extract led to a significant suppression of prostaglandin (PG) E(2) formation. Analysis of eight different alkamides revealed a contribution of undeca-2Z-ene-8,10-diynoic acid isobutylamide (A5), dodeca-2E-ene-8,10-diynoic acid isobutylamide (A7), and dodeca-2E,4Z-diene-8,10-diynoic acid 2-methylbutylamide (A8) to this response. Using an established short-term COX-2 activity assay, all three alkamides were shown to interfere with COX-2 activity. In contrast, none of the COX-2-suppressing nor any other tested alkamide was found to inhibit COX-2 mRNA and protein expression. Instead, increased COX-2 mRNA and protein levels were registered in the presence of the CO(2) extract and most of the analyzed alkamides which caused, however, no stimulation of PG formation. Overall, our results suggest that certain alkamides derived from E. angustifolia roots may contribute to the pharmacological action of the herbal extract by inhibiting COX-2-dependent PGE(2) formation at sites of inflammation.

In vitro and in vivo antiallergic effects of Glycyrrhiza glabra and its components.

Site Editor — Fri, 13 Jul 2007 18:29:45 -0700

In vitro and in vivo antiallergic effects of Glycyrrhiza glabra and its components.: Planta Med. 2007 Mar;73(3):257-61 Authors: Shin YW, Bae EA, Lee B, Lee SH, Kim JA, Kim YS, Kim DH

Licorice (Glycyrrhiza glabra L., Leguminosae) is frequently used in traditional medicine to treat inflammatory and allergic diseases. In this study, the main components (glycyrrhizin, 18beta-glycyrrhetinic acid, isoliquiritin, and liquiritigenin) were isolated from licorice, and their anti-allergic effects, such as antiscratching behavior and IgE production-inhibitory activity, were evaluated both in vitro and in vivo. Liquiritigenin and 18beta-glycyrrhetinic acid most potently inhibited the degranulation of RBL-2H3 cells induced by IgE with the antigen (DNP-HSA) and rat peritoneal mast cells induced by compound 48/80. Liquiritigenin and 18beta-glycyrrhetinic acid potently inhibited the passive cutaneous anaphylactic reaction as well as the scratching behavior in mice induced by compound 48/80. These components inhibited the production of IgE in ovalbumin-induced asthma mice but liquiritigenin had little effect. This suggests that the antiallergic effects of licorice are mainly due to glycyrrhizin, 18beta-glycyrrhetinic acid, and liquiritigenin, which can relieve IgE-induced allergic diseases such as dermatitis and asthma.

PMID: 17327992 [PubMed - indexed for MEDLINE]

Induction of apoptosis by ginger in HEp-2 cell line is mediated by reactive oxygen species.

Site Editor — Fri, 13 Jul 2007 18:10:37 -0700

Induction of apoptosis by ginger in HEp-2 cell line is mediated by reactive oxygen species.: Basic Clin Pharmacol Toxicol. 2007 May;100(5):302-7 Authors: Vijaya Padma V, Arul Diana Christie S, Ramkuma KM

Ginger (Zingiber officinale Roscoe, Zingiberaceae) is a commonly used medicinal herb throughout the world. Although some studies have demonstrated its antitumour activities on cancer cells in vitro and in vivo, the exact mechanism is not fully elucidated. Hence, the present study was designed to examine the in vitro cytotoxic activities of saline extract prepared from ginger extract on HEp-2 cell line. The cytotoxic effect of the drug was confirmed by 3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay and cell counting and estimation of protein, DNA and RNA. Meanwhile, propidium iodide staining and agarose gel electrophoresis were performed for determining the induction of apoptosis. In addition, superoxide radical generation, nitrite formation and glutathione studies show involvement of free radicals. The present results show that the extract exerts dose-dependent suppression of cell proliferation; the IC(50) value was found to be 900 microg/ml. At a dose of 250 microg/ml, marked morphological changes including cell shrinkage and condensation of chromosomes were observed. Agarose gel electrophoresis of DNA from HEp-2 cells treated with 250 microg/ml ginger powder for 24 hr showed marked DNA ladder pattern. The involvement of free radicals was confirmed by increased superoxide production, decreased nitrate formation and depletion of glutathione in ginger-treated cells. Further screening of active components using gas chromatography-mass spectrometry analyses showed the presence of clavatol, geraniol and pinostrobin in the extract. The results of the present study suggest that ginger might be useful as a potential antitumour agent.

PMID: 17448115 [PubMed - indexed for MEDLINE]

[Effect of glucocorticoid with traditional Chinese medicine in severe acute aespiratory syndrome (SARS)]

Site Editor — Fri, 13 Jul 2007 18:01:18 -0700

[Effect of glucocorticoid with traditional Chinese medicine in severe acute respiratory syndrome (SARS)]: Zhongguo Zhong Yao Za Zhi. 2005 Dec;30(23):1874-7 Authors: Liu BY, He LY, Liang ZW, Tong XY, Hu JQ, Jiao Q, Ni Q, Liu XM, Xie YM, Li P, Gao FZ, Wen TC, Liu WM

OBJECTIVE: To evaluate the effects of traditional Chinese medicine in 461 cases of severe acute respiratory syndrome(SARS) on glucocorticoid's dosage. METHOD: By using the polycentric nonrandomized concurrent controled trial and under the condition of glucocorticoid use, the patierts were divided into two groups: the integrated traditional Chinese and western mendicine(ITCWM) and simplicity western mendicine alone(WM). The observation indexes were time in hospital, pneumonia duration, mortality, glucocorticoid's gross dosage, glucocorticoid's average dosage of days and glucocorticoid use time. RESULT: In the ITCWM group, average time in hospital was shortened (P = 0.058), pneumonia duration was shortened (P = 0.057), mortality fell (P = -0.001). The median of glucocorticoid' s gross dosage was 1,277.0 mg x d(-1) in the ITCWM group, and that was 1,680.0 mg x d(-1) in the WM group (P = 0.083). The median of glucocorticoid's average dosage of days was 84.40 mg x d(-1) in the ITCWM group, and that was 115.33 mg x d(-1) in the WM group (P = 0.025). According to the analysis of 461 cases divided by stages and different ponderance, within 7 days after illness, in the ITCWM group, the glucocorticoid' s average dosage decreased. In the common type, the dosage in the ITCWM and in the WM was 146.43 mg x d(-1), and 183.64 mg x d(-1), respectively (P = 0.057), in the severe type, that was 137.71 and 177.86 mg x d(-1), respectively (P = 0.001). CONCLUSION: Compared with the group of simplicity western mendicine, in the group of integratived Chinese and western mendicine, time in hospital shorten, pneumonia duration shorten, mortality fall, simultaneity, glucocorticoid's average dosage is decreased. The use of TCM in the forepart of treatment can be capable of decreasing glucocorticoid's dosage.

PMID: 16499032 [PubMed - indexed for MEDLINE]

Curcumin and autoimmune disease.

Site Editor — Fri, 13 Jul 2007 17:48:50 -0700

Curcumin and autoimmune disease.: Adv Exp Med Biol. 2007;595:425-51 Authors: Bright JJ

The immune system has evolved to protect the host from microbial infection; nevertheless, a breakdown in the immune system often results in infection, cancer, and autoimmune diseases. Multiple sclerosis, rheumatoid arthritis, type 1 diabetes, inflammatory bowel disease, myocarditis, thyroiditis, uveitis, systemic lupus erythromatosis, and myasthenia gravis are organ-specific autoimmune diseases that afflict more than 5% of the population worldwide. Although the etiology is not known and a cure is still wanting, the use of herbal and dietary supplements is on the rise in patients with autoimmune diseases, mainly because they are effective, inexpensive, and relatively safe. Curcumin is a polyphenolic compound isolated from the rhizome of the plant Curcuma longa that has traditionally been used for pain and wound-healing. Recent studies have shown that curcumin ameliorates multiple sclerosis, rheumatoid arthritis, psoriasis, and inflammatory bowel disease in human or animal models. Curcumin inhibits these autoimmune diseases by regulating inflammatory cytokines such as IL-1beta, IL-6, IL-12, TNF-alpha and IFN-gamma and associated JAK-STAT, AP-1, and NF-kappaB signaling pathways in immune cells. Although the beneficial effects of nutraceuticals are traditionally achieved through dietary consumption at low levels for long periods of time, the use of purified active compounds such as curcumin at higher doses for therapeutic purposes needs extreme caution. A precise understanding of effective dose, safe regiment, and mechanism of action is required for the use of curcumin in the treatment of human autoimmune diseases.

PMID: 17569223 [PubMed - in process]

Effect of cooking on garlic (Allium sativum L.) antiplatelet activity and thiosulfinates content.

Site Editor — Mon, 11 Jun 2007 06:15:12 -0700

Effect of cooking on garlic (Allium sativum L.) antiplatelet activity and thiosulfinates content.: J Agric Food Chem. 2007 Feb 21;55(4):1280-8 Authors: Cavagnaro PF, Camargo A, Galmarini CR, Simon PW

The raw form of garlic and some of its preparations are widely recognized as antiplatelet agents that may contribute to the prevention of cardiovascular disease. Herein, we examined the in-vitro antiaggregatory activity (IVAA) of human blood platelets induced by extracts of garlic samples that were previously heated (in the form of crushed versus uncrushed cloves) using different cooking methods and intensities. The concentrations of allicin and pyruvate, two predictors of antiplatelet strength, were also monitored. Oven-heating at 200 degrees C or immersing in boiling water for 3 min or less did not affect the ability of garlic to inhibit platelet aggregation (as compared to raw garlic), whereas heating for 6 min completely suppressed IVAA in uncrushed, but not in previously crushed, samples. The latter samples had reduced, yet significant, antiplatelet activity. Prolonged incubation (more than 10 min) at these temperatures completely suppressed IVAA. Microwaved garlic had no effect on platelet aggregation. However, increasing the concentration of garlic juice in the aggregation reaction had a positive IVAA dose response in crushed, but not in uncrushed, microwaved samples. The addition of raw garlic juice to microwaved uncrushed garlic restored a full complement of antiplatelet activity that was completely lost without the garlic addition. Garlic-induced IVAA was always associated with allicin and pyruvate levels. Our results suggest that (1) allicin and thiosulfinates are responsible for the IVAA response, (2) crushing garlic before moderate cooking can reduce the loss of activity, and (3) the partial loss of antithrombotic effect in crushed-cooked garlic may be compensated by increasing the amount consumed.

Induction of cyclooxygenase-2 by ginsenoside Rd via activation of CCAAT-enhancer binding proteins and cyclic AMP [...]

Site Editor — Wed, 30 May 2007 01:11:34 -0700

Induction of cyclooxygenase-2 by ginsenoside Rd via activation of CCAAT-enhancer binding proteins and cyclic AMP response binding protein.: Biochem Biophys Res Commun. 2007 May 22; Authors: Jeong HG, Pokharel YR, Han EH, Kang KW

Panax ginseng is a widely used herbal medicine in East Asia and is reported to have a variety of pharmacological effects against cardiovascular diseases and cancers. Here we show a unique effect of ginsenoside Rd (Rd) on cyclooxygenase-2 (COX-2) expression in RAW264.7 macrophages. Rd (100mug/ml), but not other ginsenosides induced COX-2 and increased prostaglandin E(2) production. Gel shift and Western blot analyses using nuclear fractions revealed that Rd increased both the DNA binding of and the nuclear levels of CCAAT/enhancer binding protein (C/EBP)alpha/beta and cyclic AMP response element binding protein (CREB), but not of p65, in RAW264.7 cells. Moreover, Rd increased the luciferase reporter gene activity in cells transfected with a 574-bp mouse COX-2 promoter construct. Site-specific mutation analyses confirmed that Rd-mediated transcriptional activation of COX-2 gene was regulated by C/EBP and CREB. These results provide evidence that Rd activated C/EBP and CREB, and that the activation of C/EBP and CREB appears to be essential for induction of COX-2 in RAW264.7 cells.

Evidence of effectiveness of herbal antiinflammatory drugs in the treatment of painful osteoarthritis and chronic low back pain.

Site Editor — Fri, 11 May 2007 15:46:07 -0700

Evidence of effectiveness of herbal antiinflammatory drugs in the treatment of painful osteoarthritis and chronic low back pain.: Phytother Res. 2007 Apr 20; Authors: Chrubasik JE, Roufogalis BD, Chrubasik S

Treatment with herbal medicines is very popular in Europe. In order to get information on the evidence of effectiveness of oral herbal medicines in the treatment of pain in the joints or lower back, OVID(MEDLINE), PUBMED and COCHRANE COLLABORATION LIBRARY were searched back to 1985 for systematic reviews. The level of evidence of effectiveness was defined as strong - at least two confirmatory studies demonstrating a clinical relevant effect, moderate - one confirmatory study with a clinical relevant effect and/or multiple exploratory studies of good quality; otherwise the evidence was insufficient or conflicting in the case of inconsistent findings.Fifteen systematic reviews were identified. The evidence of effectiveness was strong for a proprietary unsaponifiable avocado soybean fraction and Harpagophytum preparations containing >50 mg harpagoside in the daily dosage, moderate for ginger and a proprietary rose hip and seed powder, insufficient for Boswellia serrata gum resin and other herbal preparations and inconsistent for a proprietary willow bark extract.Further rigorous studies are required to confirm the usefulness of herbal medicines in the treatment of osteoarthritic complaints and chronic low back pain in order to enable acceptance of the herbal medicines into the treatment guidelines. Copyright (c) 2007 John Wiley & Sons, Ltd.

Honokiol up-regulates prostacyclin synthease protein expression and inhibits endothelial cell apoptosis.

Site Editor — Wed, 21 Feb 2007 18:07:40 -0800

Honokiol up-regulates prostacyclin synthease protein expression and inhibits endothelial cell apoptosis.: Eur J Pharmacol. 2007 Jan 5;554(1):1-7 Authors: Zhang X, Chen S, Wang Y

Honokiol is a bioactive compound extracted from the Chinese medicinal herb Magnolia officinalis. We recently demonstrated that honokiol inhibited arterial thrombosis through stimulation of prostacyclin (PGI2) generation and endothelial cell protection. The current study is designed to investigate its mechanism of stimulation of PGI2 generation and cell protection. 6-keto-PGF1alpha, the stable metabolite of PGI2, in the media of rat aortic endothelial cells was measured with radioimmunoassay kits. Indomethacin, an inhibitor of cyclooxygenase (COX) and tranylcypromine, a prostacyclin synthease inhibitor were used to ascertain the target enzyme affected by honokiol. Prostacyclin synthease protein levels in endothelial cells were determined by Western blot analysis using an anti-PGI2 synthease rabbit polyclonal antibody. Flow cytometry was used to quantify the apoptotic cells and spectrophotometry was used to test the caspase-3 activity. Honokiol (0.376-37.6 microM) increased the level of 6-keto-PGF1alpha in the media of normal endothelial cells. It counteracted the inhibitory effect of tranylcypromine on the PGI2 generation, but did not influence the effect of indomethacin; evidently, honokiol up-regulated the expression of prostacyclin synthease in the endothelial cells. These effects showed perfect concentration-dependent behavior. In addition, at lower concentration (0.376-3.76 microM), honokiol significantly decreased the percentage of apoptotic endothelial cells induced by oxidized low-density lipoprotein (ox-LDL) and significantly lowered the activity of caspase-3 stimulated by ox-LDL. A high dose of honokiol (37.6 microM), however, failed to influence either of them. In conclusion, honokiol augments PGI2 generation in normal endothelial cells; its effect on PGI2 generation attributes to up-regulation of prostacyclin synthease expression; its cell protection may be correlated with its inhibition on apoptosis of endothelial cells. These findings have partly revealed the molecular mechanism of honokiol on inhibiting arterial thrombosis.

Willow Leaves' Extracts Contain Anti-Tumor Agents Effective against Three Cell Types.

Site Editor — Thu, 01 Feb 2007 16:58:34 -0800

Willow Leaves' Extracts Contain Anti-Tumor Agents Effective against Three Cell Types.: PLoS ONE. 2007;2:e178 Authors: El-Shemy HA, Aboul-Enein AM, Aboul-Enein KM, Fujita K

Many higher plants contain novel metabolites with antimicrobial, antifungal and antiviral properties. However, in the developed world almost all clinically used chemotherapeutics have been produced by in vitro chemical synthesis. Exceptions, like taxol and vincristine, were structurally complex metabolites that were difficult to synthesize in vitro. Many non-natural, synthetic drugs cause severe side effects that were not acceptable except as treatments of last resort for terminal diseases such as cancer. The metabolites discovered in medicinal plants may avoid the side effect of synthetic drugs, because they must accumulate within living cells. The aim here was to test an aqueous extract from the young developing leaves of willow (Salix safsaf, Salicaceae) trees for activity against human carcinoma cells in vivo and in vitro. In vivo Ehrlich Ascites Carcinoma Cells (EACC) were injected into the intraperitoneal cavity of mice. The willow extract was fed via stomach tube. The (EACC) derived tumor growth was reduced by the willow extract and death was delayed (for 35 days). In vitro the willow extract could kill the majority (75%-80%) of abnormal cells among primary cells harvested from seven patients with acute lymphoblastic leukemia (ALL) and 13 with AML (acute myeloid leukemia). DNA fragmentation patterns within treated cells inferred targeted cell death by apoptosis had occurred. The metabolites within the willow extract may act as tumor inhibitors that promote apoptosis, cause DNA damage, and affect cell membranes and/or denature proteins.

Anti-inflammatory, anti-tumor-promoting, and cytotoxic activities of constituents of marigold (Calendula officinalis) flowers.

Site Editor — Thu, 01 Feb 2007 16:54:10 -0800

Anti-inflammatory, anti-tumor-promoting, and cytotoxic activities of constituents of marigold (Calendula officinalis) flowers.: J Nat Prod. 2006 Dec;69(12):1692-6 Authors: Ukiya M, Akihisa T, Yasukawa K, Tokuda H, Suzuki T, Kimura Y

Ten oleanane-type triterpene glycosides, 1-10, including four new compounds, calendulaglycoside A 6'-O-methyl ester (2), calendulaglycoside A 6'-O-n-butyl ester (3), calendulaglycoside B 6'-O-n-butyl ester (5), and calendulaglycoside C 6'-O-n-butyl ester (8), along with five known flavonol glycosides, 11-15, were isolated from the flowers of marigold (Calendula officinalis). Upon evaluation of compounds 1-9 for inhibitory activity against 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation (1 microg/ear) in mice, all of the compounds, except for 1, exhibited marked anti-inflammatory activity, with ID50 values of 0.05-0.20 mg per ear. In addition, when 1-15 were evaluated against the Epstein-Barr virus early antigen (EBV-EA) activation induced by TPA, compounds 1-10 exhibited moderate inhibitory effects (IC50 values of 471-487 mol ratio/32 pmol TPA). Furthermore, upon evaluation of the cytotoxic activity against human cancer cell lines in vitro in the NCI Developmental Therapeutics Program, two triterpene glycosides, 9 and 10, exhibited their most potent cytotoxic effects against colon cancer, leukemia, and melanoma cells.