OBJECTIVE: To investigate the time- and dose-dependent effects of 3, 5, 2', 4'-tetrahydroxy chalcone (P40) on the levels of uric acid and the contents of hepatic xanthine dehydrogenase (XDH) and xanthine oxidase (XOD) in the hyperuricemic mice induced by potassium oxonate. METHODS: The hyperuricemic mice were induced by an intraperitoneal injection of uricase inhibitor potassium oxonate. Serum uric acid levels were determined by using tie phosphotungstic acid method. The contents of hepatic XOD and XDH were determined using commercially available Elisa kits. Allopurinol was as a positive control. RESULTS: When orally administrated to the oxonate-induced hyperuricemic mice, compound P40 at doses of 0.5, 1.0, 2.0, 4.0 mg · kg-1 and the allopurinol at a doses of 1.0 mg · kg-1 significantly decreased the uric acid levels and reduced the concentration of XOD compared with model group. As for the study of time-dependent effects: after administration of allopurinol 30 min or P40 60 min effectively reduced serum uric acid levels compared to the model group, respectively. Administration with P40 and allopurinol for 15, 30, 60, 90 min can reduce the concentration of XDH and XOD, compared with model group. CONCLUSION: P40 could reduce the serum uric acid levels in oxonate-induced hyperuricemic mice by reducing the contents of hepatic XDH/XOD.

Objective: To study the chemical constituents in the whole herb of Lycopodium japonicum. Methods: The constituents were isolated and purified by silica gel and semi-preparative HPLC, and their structures were elucidated by means of physicochemical properties and spectroscopic analysis. All the isolated compounds were evaluated using relevant in vitro anti-inflammatory assay against LPS-induced NO releases. Results: Nineteen compounds were isolated from the whole herb of L. japonicum, and identified as lycoposerramine-M N-oxide (1), acetyllycoposerramine-M (2), lycopodine (3), lycoposerramine-M (4), miyoshianine-C (5), 12-epilycodoline N-oxide (6), gnidioidine (7), lycoposerramine-K (8), lucidioline (9), 4α-hydroxyanhydrolycodoline (10), flabelline (11), hydroxypropyllycodine (12), lycodine (13), des-N-methyl-α-obscurine (14), α-obscurine (15), des-N-methyl-β-obscurine (16), lycoflexine (17), lycoflexine N-oxide (18), and fawcettidine (19). Compound 5 and 18 could inhibit the release of nitric oxide (NO) in the RAW264.7 cell line stimulated by lipopolysaccaride. The IC50 values of 5 and 18 are 31.82 and 40.69 μmol/L, respectively. Conclusion: Compound 1 is a new compound, named lycoposerramine-M N-oxide, compounds 2, 6, 11, 12, 16, 18, and 19 are isolated from this plant for the first time. Compounds 5 and 18 exhibit the potent inhibitory activity.

This study was to investigate the chemical constituents of the aerial part of Zygophyllumfabago, by phytochemical methods. The compounds were isolated by silica gel and Sephadex LH-20 column chromatographies from the EtOAc extract. Their structures were characterized by various spectroscopic data (1H-NMR, 13C-NMR, MS) and comparison with the literature. As a result, thirteen compounds were isolated and their structures were identified as 1-hydroxyhinesol(1), hinesol(2), atractylenolactam(3), beta-eudesmol (4), 5alpha-hydroperoxy-beta-eudesmol(5), 12-hydroxy-valenc-1(10)-en-2-one(6), pubinernoid A(7), (6S,7E)-6-hydroxy-4,7-megastigmadien-3,9-dione(8), 3-hydroxy-5alpha, 6alpha-epoxy-beta-ionone (9), (3S,5R, 6S, 7E)-3, 5, 6-trihydroxy-7-megastigmen-9-one(10), (6R,7E,9R)-9-hydroxy-4,7-megastigmadien-3-one(11), (S)-3-hydroxy-beta-ionone(12), and blumenol A(13). Compounds 1-7 were sesquiterpenoids and 8-13 were megastigmane type norsesquiterpenoids. All the compounds were obtained from Z. fabago for the first time, and compound 1 was a new natural product.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization ; Terpenes ; chemistry ; isolation & purification ; Zygophyllum ; chemistry

To study insulino-mimetic effects of bis(alpha-furancarboxylato) oxovanadium (IV) (BFOV), a orally active antidiabetic vanadyl complex, on glucose uptake and lipogenesis in isolated rat adipocytes were determined by using 2-deoxy-D-[3H]-glucose and D-[3H]-glucose, respectively. Lipolysis was assayed by free fatty acids (FFA) released from isolated rat adipocytes treated with epinephrine. The results showed that BFOV, similar to insulin, concentration-dependently significantly enhanced the uptake of 2-deoxy-D-[3H]-glucose and the transformation from D-[3H]-glucose to lipid in isolated rat adipocytes, with the EC50 values of (0.31 +/- 0.08) mmol L(-1) and (0.49 +/- 0.12) mmol L(-1), respectively. Moreover, BFOV markedly inhibited FFA release from isolated rat adipocytes treated with epinephrine, and the IC50 value was (0.30 +/- 0.20) mmol L(-1). BFOV had insulino-mimetic effects such as enhancing glucose uptake and lipogenesis, as well as inhibiting lipolysis.
Adipocytes ; drug effects ; metabolism ; Animals ; Blood Glucose ; drug effects ; Hypoglycemic Agents ; pharmacology ; Insulin ; pharmacology ; Lipogenesis ; drug effects ; Male ; Organometallic Compounds ; pharmacology ; Rats ; Rats, Sprague-Dawley

Garcinia mangostana L. is a common tropical plant,which is also called mangosteen. Its exocarp is used as a tradi?tional medicine in India,Thailand,Myammar and other Southeast Asian countries. In recent years,systematic studies on the chemi?cal constituents of the plant have shown that G. mangostana contains various xanthone compounds in a large amount. Many studies have shown that these compounds display many pharmacological activities,such as antioxidant,antiproliferative,pro-apoptosis,anti-inflammation and antibacterial activities,which has attracted great attention in the medical community. This paper reviews the main chemical constituents of G. mangostana and their pharmacological effects.

This study was aimed to investigate the prophylactic effect of Toll like receptor (TLR)5 agonist flagellin on acute graft versus host disease (aGVHD) after allogeneic hematopoietic stem cell transplantation (allo-HSCT) and its possible mechanism. The animal model with allo-HSCT aGVHD was established by using purebred mice (male mouse C57BL/6 as donor, female mouse BALB/c as recipient) with complete-unidentical major histocompatibility antigen. The recipient mice were randomly divided into 3 groups: group 1 in which mice were injected with high purity (95%) flagellin before and after allo-HSCT respectively, group 2 in which mice received allo-HSCT without injection of flagellin, group 3 in which mice were radiated alone. The aGVHD features of mice in group 1 and 2 were observed and compared. The results showed that the typical symptoms of aGVHD appeared in transplanted mice. The death peak of mice in group 2 appeared at day 4-5 after transplantation. The aGVHD symptoms were obviously alleviated and the mean survival time was prolonged significantly in mice group 1 as compared with mice in group 2 (P < 0.05). The comparison of WBC count in peripheral blood of mice in 3 groups before transplantation showed no significant difference (P > 0.05), while WBC count of mice in group 1 and 2 showed the significant difference at days 14 and 21 after transplantation (P < 0.05). The pathological appearances of aGVHD in mice of group 1 were obviously reduced as compared with mice in group 2. The flow cytometric detection of Treg cell/CD4(+) T cell levels at different time before and after transplantation demonstrated that the Treg cell level in mice of group 1 at weeks 2-4 after transplantation significantly increased as compared with mice in group 2 (P < 0.05). It is concluded that flagellin can effectively prevent the aGVHD occurrence after allo-HSCT, reduce the symptoms and pathological changes of aGVHD, obviously prolong mean survival time of mice in group 1. The mechanism of flagellin effect may be associated to increase of Treg cell level in mice after allo-HSCT.
Animals ; Female ; Flagellin ; therapeutic use ; Graft vs Host Disease ; prevention & control ; Hematopoietic Stem Cell Transplantation ; adverse effects ; methods ; Male ; Mice ; Mice, Inbred BALB C ; Mice, Inbred C57BL ; T-Lymphocytes, Regulatory ; Toll-Like Receptor 6 ; agonists ; Transplantation, Homologous

Objective:To investigate the effect of mangiferin on the mRNA expression of phosphoribosylpyrohoosphate synthetase (PRPS), phosphate ribose pyrophosphate amide transferase (PRPPAT) in liver and hypoxanthine-guanine phosphate transfer enzyme (HGPRT) in brain of hyperuricemic mice induced by potassium oxonate. Method:Hyperuricemic mice were induced through intraperitoneal injection with uricase inhibitor potassium oxonate. The serum uric acid level was determined by the phosphotungstic acid method. The mRNA expression levels of PRPS and PRPPAT in liver as well as HGPRT in brain of hyperuricemic mice were measured by reverse transcriptase polymerase chain reaction (RT-PCR). Result:An intraperitoneal injection with potassium oxonate caused a marked increase in serum uric acid level, compared with normal control group (P<0.05). Intragastric administration with mangiferin at the doses of 1.5, 3.0, 6.0 mg·kg^-1 was able to significantly reduce serum uric acid levels, compared with hyperuricemic control group (P<0.05,P<0.01); Moreover, the increase in the mRNA expression levels of PRPS and PRPPAT in liver, as well as the decrease in the mRNA expression of HGPRT in brain were observed in hyperuricemic control group, but with no statistically difference. Mangiferin has no impact on the mRNA expressions of PRPS, PRPPAT and HGPRT, compared with hyperuricemic control group. Conclusion:The hyporuricemic effect of mangiferin might not be related with PRPS, PRPPAT and HGPRT in therapeutic dose.

To study the constituents of Karelinia caspia (Pall.) Less, three phenylpropanoid derivatives and other compounds were isolated by silica gel, RP-18 chromatographic methods. Compound 1 was a new phenylpropanoid glycoside named as kareline A. Their structures were determined by spectroscopic analysis, including 1D- and 2D-NMR and mass spectrometry.

In order to find out the composition, characteristics and traditional utilization characteristics of Dai medicine and promote the rational protection, inheritance and utilization of the resources and traditional knowledge of Dai medicine in China, the resources of traditional Dai medicine have been investigated systematically and the traditional knowledge of Dai medicine have been analyzed in the article. We found out that there were altogether 1 077 kinds of traditional Dai medicine in China and among which 272 were the first time recorded in the condition of Dai folk medical uses. There were 1 053 plant medicines which belong to 169 family and 694 genus. These plant medicines mainly distributed in the southern, west southern and east southern area of Yunnan province, the southern area of Guangxi, Guangdong, Guizhou, Sichuan, Fujian province and tropical, subtropical district as Taiwan, and more than 94.49% plant medicines could be found in Yunnan province. From the point of plant life form, they were major herbaceous or shrubby plants; When it is used as medicinal part, root and rhizome of plants account for the highest proportion, the next were whole plant and leaves. From nature, flavor and channel tropism points of view, the largest proportion of Dai medicines were cool, bitter-tasted and possesses water element. In terms of treatment of disease types, most of the drugs can treat gastrointestinal diseases, next were drugs that could be used to treat upper respiratory infection, traumatological and rheumatic diseases, urinary infection, gynecological diseases, hepatopathy, puerperium fever and diseases caused by poisonous insects and beast of prey bite. The study revealed that the resources of traditional Dai medicine and traditional knowledge of application were abundant in China, but the resources of traditional Dai medicine and traditional knowledge of application were faced with the risk of gradually reduce and loss. The article suggested that we should take measures to strengthen the study of protection and utilization of important traditional Dai medicine and endangered resources along with the protection and transmission of traditional knowledge of Dai nationalistic medicine.