宾川獐牙菜碳苷类成分的研究

目的研究宾川獐牙菜Swertia binchuanensis T.N.Ho et S.W.Liu碳苷类成分。方法宾川獐牙菜95%乙醇提取物的乙酸乙酯和正丁醇部位通过硅胶、大孔吸附树脂、Sephadex LH-20、MCI柱进行分离纯化,根据理化性质和波谱数据鉴定所得化合物的结构。结果从中分离出6个化合物,分别鉴定为6-C-β-D-吡喃葡萄糖-4',5-二羟基-7-甲氧基黄酮(1)、6-C-β-D-吡喃葡萄糖-4',5,7-三羟基黄酮(2)、6-C-β-D-吡喃葡萄糖-5,7,3',4'-四羟基黄酮(3)、2-C-β-D-吡喃葡萄糖-1,3,6,7-四羟基口山酮(4)、5,7,3',4'-四羟基黄酮(5)、3,5,7,3',4'-五羟基黄酮(6)。结论所有化合物均为首次从该植物中分离得到。     

黔产宽叶缬草的RAPD分析

目的探讨黔产宽叶缬草在分子水平上的遗传多样性。方法试剂盒法提取20份宽叶缬草样本的总DNA,扩增多态性(RAPD)技术从40个随机引物中筛选出13个,对总DNA样品进行扩增,Popgene 1.32和NTSYS 2.10e软件分析样本的Nei’s、Shannon’s多样性指数以及Jaccard遗传相似性系数,UPGMA法进行聚类分析。结果 20份宽叶缬草样本中共扩增出102条清晰条带,其中88条具有多态性,多态率为86.27%,Nei’s和Shannon’s多样性指数分别为0.303 0和0.453 7,Jaccard遗传相似系数在0.411 8~0.882 4之间。另外,UPGMA聚类分析可将来自剑河县的13份样本聚为一类,江口县的7份样本聚为另一类,而且剑河地区又分为栽培与野生样本2个分支。结论黔产宽叶缬草种水平上具有较高的遗传多样性,其RAPD标记可用于遗传多样性研究,为今后开发该植物的选种与育种工作奠定基础。     

Acylated flavone C-glycosides from Trollius ledebouri

Six new acylated flavone C-glycosides, 2'-O-(2'-methylbutyryl)isoswertisin (1), 3'-O-(2'"-methylbutyryl)isoswertisin (2), 2'-O-(2'"-methylbutyryl)vitexin (3), 2'-O-(2'"-methylbutyryl)orientin (4), 2'-O-(3'",4'"-dimethoxybenzoyl)vitexin (5), and 2'-O-(3'",4'"-dimethoxybenzoyl)orientin (6), and the known flavone C-glycoside, isoswertisin, were isolated from the flowers of Trollius ledebouri. The structures of 1-6 were elucidated by spectroscopic methods.     

Sucrose esters and xanthone C-glycosides from the roots of Polygala sibirica.

Six new sucrose esters, sibiricoses A(1)-A(6) (1-6), two new xanthone C-glycosides, sibiricaxanthones A (7) and B (8), and a new acetophenone glycoside, sibiricaphenone (9), were isolated from the roots of Polygala sibirica together with six known glycosides. The structures of new compounds were elucidated on the basis of chemical and spectroscopic evidence. The structure of the known xanthone glycoside, polygalaxanthone III (10), was revised.     

Anti-inflammatory and hepatoprotective effects of total flavonoid C-glycosides from Abrus mollis extracts

The aim of this study was to evaluate the anti-inflammatory and hepatoprotective effects of the total flavonoid C-glycosides isolated from Abrus mollis extracts（AME）. In the anti-inflammatory tests, xylene-induced ear edema model in mice and carrageenan-induced paw edema model in rats were applied. The hepatoprotective effects of AME were evaluated with various in vivo models of acute and chronic liver injury, including carbon tetrachloride（CCl4）-induced hepatitis in mice, D-galactosamine（D-GalN）-induced hepatitis in rats, as well as CCl4-induced hepatic fibrosis in rats. In the acute inflammation experiment, AME significantly suppressed xylene-induced ear edema and carrageenan-induced paw edema, respectively. In the acute hepatitis tests, AME significantly attenuated the excessive release of ALT and AST induced by CCl4 and D-GalN. In CCl4-induced hepatic fibrosis model, AME alleviated liver injury induced by CCl4 shown by histopathological sections of livers and improved liver function as indicated by decreased liver index, serum ALT, AST, TBIL, and ALP levels and hydroxyproline contents in liver tissues, and increased serum ALB and GLU levels. These results indicated that AME possesses potent anti-inflammatory activity in acute inflammation models and hepatoprotective activity in both acute and chronic liver injury models. In conclusion, AME is a potential anti-inflammatory and hepatoprotective agent and a viable candidate for treating inflammation, hepatitis, and hepatic fibrosis.     

Cytotoxic principles from the sap of Kalmia latifolia

Examination of the sap of Kalmia latifolia has revealed Grayanotoxin I (1), phloretin (3), and 2',6'-dihydroxy-4-methoxyacetophenone (5) as cytotoxic components. Twenty-one dihydrochalcones have been synthesized and tested for cytotoxic activity. 2'3,3'4,4'-Pentahydroxydihydrochalcone (8) has been found to be cytotoxic and to have marginal activity in vivo. Seven new dihydrochalcones are described.     

Alvaradoins E-N, antitumor and cytotoxic anthracenone C-glycosides from the leaves of Alvaradoa haitiensis

Bioactivity-directed fractionation of an extract of the leaves of Alvaradoa haitiensis, using the KB (human oral epidermoid carcinoma) cell line, led to the isolation and identification of 10 new anthracenone C-glycosides, alvaradoins E-N (1-10), along with the known compound chrysophanol (11). The cytotoxicity of all compounds was evaluated, and preliminary structure-activity relationships are suggested. The most potent compounds in the in vitro assays (1 and 2) were evaluated in vivo versus the P388 (murine lymphocytic leukemia) model, and alvaradoin E (1) showed antileukemic activity (125% T/C) at a dose of 0.2 mg kg-1 per injection when administered intraperitoneally.     

不同产地显齿蛇葡萄中二氢杨梅素测定

目的研究国内各主产区显齿蛇葡萄中二氢杨梅素的含有量差别,初步研究藤茶原料的资源特点。方法以超声波辅助提取、高效液相色谱法测定二氢杨梅素。结果显齿蛇葡萄不同样品的二氢杨梅素含有量为2.50%³9.50%。结论不同地区显齿蛇葡萄中二氢杨梅素量有较明显的差别,其中武夷山脉(黎川县)、武陵山区(来凤县、酉阳县)、佛顶山(石阡县)的二氢杨梅素含有量普遍较高,罗霄山脉(大余县、衡东县)、南岭(连州市、恭城县、平乐县)同期相对偏低。     

Diuretic Activity of Extracts from Astydamia latifolia,Forsskaolea angustifolia and Ceterach aureum in Rats

We have confirmed the diuretic properties attributed to three endemic species from the Canary Islands. The plants chosen were Astydamia latifolia (L.f.), Forsskaolea angustifolia (Retz) and Ceterach aureum (Cav.) Buch. and Paronychia canariensis . The results confirm a diuretic activity probably due to high content of potassium salts     

海南大叶冬青中2种活性成分的含量研究

目的建立同时测定海南大叶冬青叶中苦丁苷A、D含量的高效液相色谱法。方法色谱柱:Dikma Diamonsil C18(4.6mm×250mm,5μm)色谱柱;流动相:乙腈-水(36:64);流速:1.0mL.min-1;测定波长苦丁苷A为228nm,苦丁苷D为261nm,柱温40℃。结果线性范围苦丁苷A为0.190～5.80μg(r=0.9999);苦丁苷D为0.236～7.100μg(r=0.9999);平均回收率(n=6)分别为99.3%(RSD=1.6%)和99.2%(RSD=1.3%)。结论该法稳定,重现性好,操作简单,是测定大叶冬青中苦丁苷A和D的较理想方法。     

Spectroscopic characterization and antiproliferative activity on HepG2 human hepatoblastoma cells of flavonoid C-glycosides from Petrorhagia velutina

Eight flavonoid C-glycosides, including three new analogues, have been isolated from leaf and root methanolic extracts of Petrorhagia velutina, a Mediterranean herbaceous plant. The antiproliferative activity against human hepatoblastoma cancer cell line HepG2 has been analyzed by the MTT (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide) test. Isoorientin (4) significantly reduces the proliferation of HepG2 cells as determined by the complete conversion of the tetrazolium probe into formazan after 48 h of exposure.     

Antiulcer and antimicrobial activity of Anogeissus latifolia

Ethnobotanically, the bark of Anogeissus latifolia (Roxb. ex DC.) Wall. ex Guill. and Perr.(Combretaceae) has been reported to be used in the treatment of various disorders including stomach and skin diseases. We studied the antiulcer potential and antimicrobial activity of the 50% aqueous alcoholic extract in order to validate ethnobotanical claims regarding the plant use in the above-mentioned disorders. Gastroprotective potential of the Anogeissus latifolia extract (ALE) (100 and 200mg/kg/body weight) was studied on aspirin, cold-resistant stress (CRS), pylorus ligated (PL) and ethanol-induced ulcers. Status of the antioxidant enzymes superoxide dismutase (SOD) and catalase along with lipid peroxidation (LPO) was also studied in CRS-induced ulcers. The results of the present study showed for the first time that the ALE possessed gastroprotective activity as evidenced by its significant inhibition in the formation of ulcers induced by physical and chemical agents with a maximum of 84.16% curation (200mg/kg body weight) in CRS-induced ulcers. ALE decreased LPO and SOD with concomitant increase in catalase activity in CRS-induced ulcers. Moderate antibacterial activity and antifungal activity was also observed. High performance thin layer chromatography (HPTLC) showed the presence of gallic acid and ellagic acid (0.95%, w/w, 0.25%, w/w, respectively) in the plant. These findings could justify, at least partially, the inclusion of this plant in the management of gastric disorders in traditional medicine.     

HPLC法测定不同产地大叶冬青叶中4种三萜类成分的含量

目的建立HPLC法测定大叶冬青叶中羽扇豆醇、豆甾醇、α-香树脂素和苦丁冬青苷D含量的方法,对比分析26批来自不同产地及不同采收期大叶冬青叶中4种成分的含量,为其质量标准的完善提供参考。方法采用YMC-ODS C18(4.6 mm×250 mm,5μm)色谱柱,以甲醇(A)-0.4%磷酸水溶液(B)为流动相等度洗脱,流速1 mL·min^-1,检测波长205 nm,柱温30℃,进样量20μL,建立同时测定羽扇豆醇、豆甾醇、α-香树脂素含量的方法;以乙腈(A)-0.4%磷酸水溶液(B)为流动相等度洗脱,流速1 mL·min^-1,检测波长254 nm,柱温30℃,进样量10μL,建立测定苦丁冬青苷D含量的方法。结果在上述色谱条件下羽扇豆醇、豆甾醇、α-香树脂素分离度良好,分别在质量浓度18.88~906.00μg·mL^-1(r=1.000 0,n=6)、15.06~723.00μg·mL^-1(r=0.999 9,n=6)、22.75~1 092.00μg·mL^-1(r=0.999 9,n=6)呈良好的线性关系,平均加样回收率(n=6)分别为100.43%(RSD=1.96%)、98.72%(RSD=0.88%)、102.86%(RSD=2.47%)。苦丁冬青苷D在质量浓度9.55~573.00μg·mL^-1(r=0.9999,n=6)呈良好的线性关系,平均加样回收率为101.35%(RSD=0.25%)。结论所建立的测定方法简单方便、结果准确、重复性好,可用于测定大叶冬青叶中羽扇豆醇、豆甾醇、α-香树脂素和苦丁冬青苷D的含量,为大叶冬青质量标准的建立提供理论依据。不同产地及不同采收时期大叶冬青叶中4种三萜类成分含量存在明显差异。     

Marmycins A and B, cytotoxic pentacyclic C-glycosides from a marine sediment-derived actinomycete related to the genus Streptomyces

Two new cytotoxic quinones of the angucycline class, marmycins A and B ( 1, 2), were isolated from the culture broth of a marine sediment-derived actinomycete related to the genus Streptomyces. The gross structures and absolute configurations of both compounds were determined by spectroscopic and crystallographic methods. Marmycin A ( 1) displayed significant cytotoxicity against several cancer cell lines, some at nanomolar concentrations; while compound 2, a chloro analogue of 1, was less potent. For marmycin A ( 1), tumor cell cytotoxicity appeared to coincide with induction of modest apoptosis and arrest in the G1 phase of the cell cycle.     

Antileishmanial compounds from Cordia fragrantissima collected in Burma (Myanmar)

A methanol extract of the wood of Cordia fragrantissima, collected in Burma (Myanmar), was found to exhibit significant activity against Leishmania major. Bioassay-guided fractionation of this extract using several chromatographic techniques afforded three new compounds (1-3) and five known compounds (4-8). The structures of the new compounds were revealed on the basis of spectroscopic data interpretation and by X-ray crystallographic analysis. Interestingly, the new compounds, despite the presence of asymmetric carbons, were found to be racemates. The activities of the isolates from C. fragrantissima and several derivatives were evaluated against the promastigote forms of Leishmania major, L. panamensis, and L. guyanensis.     

Cytotoxic lignans from the stems of Helicteres hirsuta collected in Indonesia

Cytotoxicity-guided fractionation of the stems of Helicteres hirsuta, of Indonesian origin, led to the isolation and identification of six lignans, namely, (+/-)-pinoresinol, (+/-)-medioresinol, (+/-)-syringaresinol, (-)-boehmenan, (-)-boehmenan H and (+/-)-trans-dihydrodiconiferyl alcohol. Of these isolates, (+/-)-pinoresinol exhibited potent cytotoxic effects when evaluated against a small panel of cancer cell lines.     

Antimicrobial ambiguines from the cyanobacterium Fischerella sp. collected in Israel

Bioassay-guided fractionation of the 7:3 MeOH/water extract of a cultured cyanobacterium strain identified as Fischerella sp. yielded nine isonitrile-containing alkaloids. Three of the compounds, ambiguine H isonitrile (1), ambiguine I isonitrile (2), and ambiguine J isonitrile (3), are new, while the other six, 12-epi-hapalindole H, ambiguine A isonitrile, ambiguine B isonitrile, ambiguine D isonitrile, ambiguine E isonitrile, and ambiguine F isonitrile, have been previously isolated from Fischerella ambigua. The structures of the compounds were determined by 1D and 2D NMR techniques and mass spectrometric data. Ambiguine H isonirile and ambiguine I isonirile possess antibacterial and antimycotic activity.     

Antifertility effects of some coumarins isolated from Ruta chalepensis and R. chalepensis var. latifolia in rodents

Crude extracts of Ruta chalepensis and R. chalepensis var. latifolia showed antifertility activity in female rats. In order to establish the active constituents which may be responsible for this effect, a group of selected coumarins and alkaloids were tested in vivo. Although chalepensin, bergaptol, chalepin and xanthatoxin showed antifertility activity, 70% of the test animals developed cystic and atretic follicles in their ovaries and glomerulocapsular adhesion and segmental fusion was observed in the kidneys. No harmful effect was observed in the brain. Alkaloids in this study showed no antifertility activity.