Objective To explore the protective effect of active component of Eclipta on hepatic injury induced by Concanavalin A(ConA) in mice.Methods Mouse hepatic injury models were established by injection of ConA(15 mg/kg) via tail vein.The effect of Eclipta extracts on serum alanine aminotransferase(ALT) and liver histology in both normal mice and hepatic injury mice was examined.A pure compound was obtained by means of bioactivity-guided isolation,and IR, ~(13)C-NMR,~1H-NMR,~1H-~(13)C HMBC and ~1'H-~(13)C HMQC were used for structural identification.Results Eclipta extracts decreased serum ALT in hepatic injury mice induced by ConA,and demonstrated anti-apoptosis effect induced by ConA in hepatocytes.Wedelolactone,a coumarin,was isolated from Eclipta,and its structure was identified on the basis of spectroscopic analysis.Wedelolactone inhibited ConA-induced T cell proliferation selectively,and completely antagonized the effect of ConA at the concentration of 10μg/mL.Conclusion Eclipta herb has hepatoprotective effect. Wedelolactone,the anti-inflammatory and anti-apoptosis active component of Eclipta,might serve as a lead compound for developing new antiinflammatory drugs.

A series of lipoamino acids were synthesized and their neuroprotective effect against brain ischemia induced by oxygen-glucose deprivation (OGD) on rat cerebral slices was evaluated. Among these compounds, N-stearoyl-L-tyrosine (4), N-stearoyl-L-serine (5) and N-stearoyl-L-threonine (6) exhibited good neuroprotective activity. We found that the neuroprotective activity of lipoamino acids depended on the acyl group, the presence of a free carboxylic function and a free hydroxyl group at the branched chain of the amino acids. The results also showed that 5 was the most active compound, protecting rat brain slices against OGD as well as hydrogen peroxide (H2O2) insult at the range of 1–10 M.

Objective To evaluate the strengthening and restoring effects and hepatoprotective effect of Eclipta extracts.Methods Sixty Kunming mice were randomly divided into control group,low-dose Eclipta group,high-dose Eclipta group,cyclophosphamide(CY) group,low-dose Eclipta CY group and high-dose Eclipta CY group(n=10).Eclipta 8 g·kg-1·d-1 or 4 g·kg-1·d-1 were administered by oral gavage for 7 d.Immunosuppression mouse models were established by intraperitoneal injection of 0.05 g/kg CY on the fourth day of administration.The effects of Eclipta extracts on thymus index,spleen index and carbon clearance index in both normal mice and immunosuppression mice induced by CY were tested,and those on proliferation of lymphocyte and T cells induced by ConA were examined.Based on these data,strengthening and restoring effects of Eclipta were observed.Besides,70 Kunming mice were randomly divided into control group,low-dose Eclipta group,high-dose Eclipta group,CCl4 group,DDB group,low-dose Eclipta CCl4 group and high-dose Eclipta CCl4 group.20 g·kg-1·d-1 and 10 g·kg-1·d-1 Eclipta were administered by oral gavage for 7 d.Hepatic injury mouse models were established by intraperitoneal injection of 10 mL/kg CCl4 2 h after the last administration.The effects of Eclipta extracts on serum ALT,MDA,TP and T-Bil levels in both normal mice and hepatic injury mice induced by CCl4 was tested,and those on the viability of the primary culture hepatocytes were determined.Based on these data,hepatoprotective effect of Eclipta was observed. Results Eclipta extracts increased thymus index and carbon clearance index in both normal mice and immunosuppression mice induced by CY,promoted proliferation of lymphocyte and proliferation of T cells induced by ConA,reduced serum ALT and MDA levels in hepatic injury mice,and improved the viability of the primary culture hepatocytes. Conclusion Eclipta herb has strengthening and restoring effects and hepatoprotective effect.

Muscarinic M2 receptor antagonists with high subtype selectivity (M2/M1) will decrease the toxicity in central nervous system in treatment of AD. The exploration of quantitative structure-selectivity relationship (QSSR) to muscarinic M2 receptor antagonists will provide design information for drug with fewer side effects. In this paper, CoMFA models of pK(i)(M1), pK(i)(M2) wand p[K-i(M2)/K-i(M1)] (pK(i)(M2) - pK(i)(M1)) were used to study the subtype selectivity (M2/M1) of piperidinyl piperidine derivatives as muscarinic M2 subtype receptor antagonists. The parameters of the three models are: 0.633, 0.636 and 0.726 for cross-validated r(2) (r(cv)(2)), 0.109, 0.204 and 0.09 for the Standard error of estimate (SD), respectively. The results show the model of p[K-i(M2)/K-i(M1)] is the best one for design of piperidinyl piperidine derivatives as muscarinic antagonists with high subtype selectivity (M2/M1). (c) 2007 Elsevier Ltd. All rights reserved.

There is conflict between the education reform and present system of the medical chemistry courses, because there are some obvious drawbacks in the system. Two courses in the system are basic chemistry and organic chemistry, which are taught periodically. This system divides the whole content into separated courses. In some cases those two courses are repetition of each other. It prevents medical students from holding the basic knowledge of chemistry systematically and comprehensively. The solution is, with the modern technology of education, to combine two courses to form a new system of medical chemistry in order to train creative talent for medicine.

<正> 鸦胆子 Brucea javanica(L.)Merr.中的某些苦木素类成分具有抗疟、抗肿瘤和抗阿米巴痢疾的作用。作者又从该植物种子中分离得到2个新的苦木素 javanicolide C(1)和D(2)和5个新的苦木素葡糖苷javanico-side B～F(3～7),还分得8个已知的苦木素和19个已知的苦木素葡糖苷。干燥粉碎的鸦胆子种子用热甲醇提取,

缬草属植物V．laxiflora DC．是一种草本灌木，在智利民间用于杀死消化道内寄生虫和镇静等。作者从该植物地上部分和根分离得到一个新的虹彩内酯、一新的木脂素和11个已知化合物，初步研究了它们的抗结核杆菌活性。

目的研究鳢肠属植物鳢肠水溶性部位的化学成分及其药理活性.方法通过溶剂提取法和色谱技术分离化学成分,运用光谱手段进行结构鉴定,利用C6细胞和PC12细胞观察鳢肠水溶性成分对细胞增殖活性的抑制作用.结果从该部位分离得到3个三萜皂苷,分别为3-O-β-D-吡喃葡糖刺囊酸(Ⅰ)、3-O-β-D-吡喃葡糖刺囊酸-28-O-β-D-吡喃葡糖苷(Ⅱ)和3-O-(2-O-硫酰基-β-D-吡喃葡糖)刺囊酸(Ⅲ),还分离得到了豆甾醇(Ⅳ)和蟛蜞菊内酯(Ⅴ);化合物Ⅰ具有抑制C6细胞和PC12细胞增殖的活性.结论化合物Ⅰ是鳢肠水溶性部位抑制细胞增殖的活性成分.

Objective To investigate the chemical constituents from hydrophilic fractions of Eclipta prostrata L. and their pharmacological effects. Methods Constituents were isolated by means of extraction and chromatographic separations, identified by spectral analysis, and their bioactivity was evaluated on glioma C6 cells and PC12 cells. Results Five compounds were isolated and identified as: 3-O-β-D- glucopyranosyl-echinocystic acid (Ⅰ) , 3-O-β-D-glucopyranosyl-echinocystic acid-28-O-β-D-glucopyranoside (Ⅱ ) , 3-O-( 2-O-sulfuryl-β-D-glucopyranosyl) -echi-nocystic acid ( Ⅲ ) , stigmasterol ( Ⅳ ) and wedelolactone ( Ⅴ ) ; compound I could inhibit the proliferation of C6 cells and PC12 cells. Conclusion Compound I is the active constituent in hydrophilic fractions of E. prostrata for the inhibitory effect to cell proliferation.

缬草属植物V.laxiflora DC.是一种草本灌木,在智利民间用于杀死消化道内寄生虫和镇静等.作者从该植物地上部分和根分离得到一个新的虹彩内酯、一新的木脂素和11个已知化合物,初步研究了它们的抗结核杆菌活性.

美丽山竹子(拟)Garcinia speciosa广泛分布于印度、缅甸和泰国.作者从具抗HIV-1活性的该植物树皮甲醇粗提物的乙酸乙酯部位分得3个新的原萜烷型三萜garciosaterpene A(1)、B(2)、C(3)和1个新的二香叶基二苯酮garciosaphenone A(4)以及4个已知化合物,并对它们进行了抗HIV-1试验.

Objective To explore the feasibility of reform on teaching chemistry in medical college. Methods A series of reform measures were taken in lecture notes teaching, forms and methods as well as experiments. Results Students obtained higher grades in the examination after reform. Conclusion The teaching reform is good for the improvement of the learning abilities of the students.