Xue-Qin Ma

The genus Desmodium (Fabaceae)-traditional uses in Chinese medicine, phytochemistry and pharmacology.

ETHNOPHARMACOLOGICAL RELEVANCE Plants of the genus Desmodium (Fabaceae), such as Desmodium styracifolium (Osbeck) Merr. and Desmodium gyrans (L. f.) DC., have a long history of medical use in Traditional Chinese Medicine to treat various ailments including rheumatism, pyrexia, dysentery, wounds, cough, malaria, hepatitis, hemoptysis, etc. In the theory of Traditional Chinese Medicine, most species have the effect of relieving internal heat or fever, neutralizing toxins, inhibiting pain, invigorating blood circulation, suppressing cough and alleviating dyspnea. MATERIALS AND METHODS A bibliographic investigation was accomplished by analyzing secondary sources including Chinese Herbal Classics, and worldwide accepted scientific databases (Pubmed, Scopus and Web of Science, SciFinder) were scrutinized for the available information on the ethnopharmacological uses in Chinese medicine, phytochemistry, pharmacology and toxicology of Desmodium species. RESULTS The genus Desmodium is a large member of the Papilionaceae (Fabaceae) family. It contains about 350 plant species used for both feeding stuffs and herbal medicines, of which only about 30 species have been phytochemically or pharmacologically investigated. Desmodium plant extracts, as well as the active principles, have been experimentally studied for their anti-inflammatory, cytotoxic, antidiabetic, antinephrolithic, antibacterial, and nootropic activities in vitro or in vivo. And so far, a total of 212 compounds have been isolated from 15 Desmodium species and characterized mainly as flavonoids and alkaloids, followed by terpenoids, steroids, phenols, phenylpropanoids, glycosides and a number of volatile oils. The remaining unrevealed species are recorded chiefly in Asia and Africa being used in empirical treatment for various diseases. CONCLUSIONS Desmodium species have long been used in TCM to treat various ailments. Available scientific references revealed that the traditional medical uses of some important Desmodium species in TCM have been evaluated by modern pharmacological studies. As literature demonstrated, flavonoids and alkaloids are perhaps responsible for most of the activities shown by the plants of this genus. Further studies are still required to reveal the structure-activity relationship of these active constituents.

Cytotoxic phenylpropanoid glycosides from Fagopyrum tataricum (L.) Gaertn.

Fagopyrum tataricum (L.) Gaertn (tartary buckwheat) is an ancient dicotyledonous crop belonging to Polygonaceae family. Besides its benefits for human consumption, tartary buckwheat is also an important folk medicine in China for its antioxidant, antitumour, hypotensive, hypoglycaemic and hypolipidaemic activities. Phytochemical investigation of the ethyl acetate fraction of tartary buckwheat roots led to the isolation of seven new phenylpropanoid glycosides, tatarisides A-G (1-7), together with a known phenylpropanoid glycoside, diboside A (8). Their structures were elucidated by means of spectroscopic methods. All compounds (1-8) were evaluated for their cytotoxic activity against four human cancer cell lines (A-549, HCT116, ZR-75-30 and HL-60). Tatariside C (3) was the most active compound with IC50 values of 6.44-7.49μg/ml against the four tested cell lines.

Anti-arthritic activity of Xanthium strumarium L. extract on complete Freund׳s adjuvant induced arthritis in rats

ETHNOPHARMACOLOGICAL RELEVANCE Xanthium strumarium L. fruit (Xanthiu fruit) has been traditionally used as a medicinal herb in China for the treatment of many ailments including rheumatoid arthritis. However, the anti-arthritic activity of Xanthium strumarium fruit has still not been demonstrated. In the present study, we confirmed that the extract of Xanthium strumarium (EXS) prevents rheumatoid arthritis induced by Complete Freund׳s Adjuvant (CFA) in rats. MATERIALS AND METHODS Male Wistar rats (160±10 g) were immunized by intradermal injection of 0.1 mL of CFA into the left hind metatarsal footpad. EXS was administered orally at a dose of 300 and 75 mg/kg once a day after the induction of adjuvant arthritis. Methotrexate (3 mg/kg, twice a week) was used as a positive control. Paw swelling, arthritic score, body weight loss, spleen index, thymus index, serum cytokines, inflammatory mediators and histological change were measured. The chemical profile of EXS was analyzed by HPLC-DAD. RESULTS We found that the EXS significantly suppressed paw swelling and arthritic score, increased body weight loss and decreased the thymus index. The overproduction of TNF-α and IL-1β were remarkably suppressed in the serum of all EXS-treated rats, and in contrast IL-10 was markedly increased. The level of COX-2 and 5-LOX was also decreased with EXS treatment. Ten phenolic acid derivatives were identified from 14 detected peaks by HPLC-DAD with the reference substances and verified by LC-MS. CONCLUSIONS These results suggest the potential effect of EXS as an anti-arthritis agent towards CFA-induced arthritis in rats. Xanthium strumarium has the potential to be regarded as a candidate for use in general therapeutics and as an immune-modulatory medicine in rheumatoid arthritis.

Inhibitory effects of the root extract of Litsea cubeba (lour.) pers. on adjuvant arthritis in rats.

ETHNOPHARMACOLOGICAL RELEVANCE The dried root of Litsea cubeba (Lour.) Pers. (Family Lauraceae) has long been used as a folk remedy in Traditional Chinese Medicine (TCM) and Dai Ethnopharmacy for the treatment of rheumatic diseases in southwestern China. AIM OF THE STUDY This study investigated the preventive efficacy of Litsea cubeba root in treating rheumatoid arthritis using Freunds complete adjuvant (CFA) induced arthritis (AA) in rat model. MATERIALS AND METHODS Arthritis was induced in male Wistar rats by immunization with CFA. Ethanol extract (EELC) and water extract (WELC) of Litsea cubeba root both at 50mg/kg and 200mg/kg were orally administered from a day after the induction of arthritis. Paw swelling, arthritic score, body weight growth rate, index of thymus and spleen were observed, and the production of TNF-α, IL-1β, IL-6 and IL-10 in serum were measured by enzyme-linked immunosorbent assay. The expression levels of inflammatory enzymes like cyclooxygenase and lipoxygenase were also measured by enzyme-linked immunosorbent assay. Moreover, histological changes in the ankle joint were analyzed in AA rats. RESULTS Both EELC and WELC significantly suppressed paw swelling and arthritic score, increased the loss in body weight and decreased the index of thymus. Histopathological improvement in joint architecture was also observed in EELC, WELC-treated AA rats. The expression levels of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) were decreased on treatment with EELC and WELC. Furthermore, the overproduction of TNF-α, IL-1β and IL-6 were remarkably attenuated in serum of all Litsea cubeba-treated rats, however, IL-10 was markedly increased at doses of 50mg/kg of EELC and WELC. CONCLUSIONS These results indicate that extract of Litsea cubeba root significantly attenuates adjuvant arthritis in rats by decreasing the levels of TNF-α, IL-1β and IL-6 and increasing of IL-10 in serum as well as down-regulate the levels of inflammatory enzymes such as COX-2 and 5-LOX. This suggests that Litsea cubeba root might be used as a therapeutic agent for the treatment of human arthritis.

Labdane-type diterpenoids from the fruits of Vitex trifolia.

Seven new labdane-type diterpenoids, vitextrifolins A-G (1-7), along with eight previously reported analogues, were isolated from the fruits of Vitex trifolia. The structures of 1-7 were elucidated by spectroscopic data interpretation. The isolates were evaluated for their cytotoxicity against four human cancer cell lines (A549, HCT116, HL-60, and ZR-75-30), but all were inactive (IC(50) < 5 μg/mL).

Antiosteoporotic activity and constituents of Podocarpium podocarpum

Our study aimed to investigate the antiosteoporotic properties of the ethanol extract of Podocarpium podocarpum (DC.) Yang et Huang (PE) in ovariectomized (OVX) rats and to characterize the active constituents. As a result, PE significantly inhibited the increased urinary Ca excretion and activity of bone resorption markers including tartrate-resistant acid phosphatase (TRAP), deoxypyridinoline crosslinks and cathepsin K in OVX rats, whereas exhibited little effects on the body, uterus and vagina weight. Detailed micro-CT analysis showed that PE notably enhanced bone quality, with increased bone mineral content (BMC), bone volume fraction (BVF), connectivity density (CD), tissue mineral content (TMC), tissue mineral density (TMD) and trabecular number (Tb. N), and decreased trabecular separation (Tb. Sp), in OVX animal. Those findings implied that PE had notable antiosteoporotic effect, especially effective in preventing bone resorption, with little side-effects on reproductive tissue. Further chemical investigation led to the isolation of 17 flavonoids, most of which showed significantly stimulatory effect on osteoblastic proliferation, ALP activity and mineralized nodes formation as well as inhibitory effect on osteoclastic TRAP activity in osteoblastic and osteoclastic cells. Our results indicated that PE, with abundant flavonoids, had remarkable antiosteoporotic activity and therefore can be a promising candidate for the treatment of postmenopausal osteoporosis induced by estrogen deficiency through herbal remedy.

Phenylpropanoids from Podocarpium podocarpum

Abstract Context: Podocarpium podocarpum (DC.) Yang et Huang (Leguminoseae) is a very important Podocarpium species with significant anti-inflammatory, analgesic and anti-pyretic activities, which has not yet been subjected to adequate phytochemical investigation. Objective: To isolate and identify bioactive compounds from P. podocarpum. Materials and methods: Ethanol extract of the whole plant of P. podocarpum was subjected to repeated column chromatography. Chemical structures of the compounds were identified by 1D, 2D-NMR spectra and MS data. Human cervical carcinoma (HeLa) and pancreatic carcinoma (PANC-1) cell lines were employed to evaluate the in vitro cytotoxic activity of the isolated constituents at six concentrations (0.001, 0.01, 0.1, 1.0, 10.0, 100.0 μg/ml). Results: A new phenylpropanoid glycoside, podocarioside A (1), together with four known compounds, (E)-3-(4-hydroxy-3-propoxyphenyl) acrylic acid (2), schizandrin (3), dehydrodiconiferyl alcohol (4) and dihydrodehydrodiconiferyl alcohol (5), were isolated from P. podocarpum. Compounds 1, 3 and 4 showed moderate cytotoxic against HeLa cells with IC50 values of 38.62, 8.64 and 5.85 μg/mL, respectively, while none exhibited toxicity against PANC-1 cells. Discussion and conclusion: This is the first report on the isolation and identification of bioactive compounds from P. podocarpum. In vitro cytotoxic assay of the isolated constituents establishes the potential of those components as antitumor agents.

Kaempferitrin prevents bone lost in ovariectomized rats.

BACKGROUND Podocarpium podocarpum (DC.), an edible and medicinal plant popularly used for the treatment of bruises and fracture in Chinese folk medicine, has been proved to possess significant antiosteoporotic effect in our latest research. PURPOSE Our study aimed to investigate the in vitro and in vivo antiosteoporotic effect of kaempfertrin (KN), a principal flavonoid in P. podocarpum obtained through bio-guided isolation. METHODS An ovariectomized (OVX) rat model of osteoporosis as well as in vitro osteoblast and osteoclast cell lines were employed to evaluate the antiosteoporotic potency of KN. RESULTS KN significantly improved the bone mass and microarchitecture in OVX rats, with little estrogen-like side effect compared with estradiol valerate. KN also exhibited stimulatory effect on osteoblastic cells and inhibitory action on osteoclastic cells, which down-regulated the phosphorylation level of I-κB. CONCLUSION KN possessed significant antiosteoporotic activity. Combined with its limited estrogen-like side effect, KN can be regarded as an idealistic antiosteoporotic candidate for human osteoporosis diseases.

Lignans and phenylpropanoids from Fagopyrum tataricum roots

0009-3130/12/4802-0303 2012 Springer Science+Business Media, Inc. 1) Department of Pharmacognosy, School of Pharmacy, Second Military Medical University, Shanghai 200433, P. R. China, fax: +86 21 81871300; +86 21 81871309, e-mail: qinsmmu@126.com; zheng_chengjian@hotmail.com; 2) Department of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, 350108, P. R. China; 3) Department of Pharmaceutical Analysis, School of Pharmacy, NingXia Medical Univercity, 1160 Shenli Street, Yinchuan 750004, P. R. China. Published in Khimiya Prirodnykh Soedinenii, No. 2, March–April, 2012, pp. 271–272. Original article submitted December 25, 2010. Chemistry of Natural Compounds, Vol. 48, No. 2, May, 2012 [Russian original No. 2, March–April, 2012]