Purification and structure determination of gelatinase and collagenase inhibitors from Viola patrinii fermentation extracts

Investigation of collagenase and gelatinase inhibitory natural components afforded two isoflavonoids. Two isoflavonoids, tectorigenin-7-O-β-D-glucoside (1) and luteolin-7-O-β-D-glucuronopyranoside (2), were isolated from ethyl acetate fraction of Viola patrinii fermentation extracts (VPFE). Of these, compounds 1 and 2 exhibited collagenase inhibitory activity (IC₅₀) at a concentration of less than 1.5?μM, and compound 2 showed gelatinases A and B inhibitory activity (IC₅₀) at 0.3?μM and 0.8?μM, respectively.     

BREAST CANCER: AETIOLOGICAL FACTORS AND ASSOCIATIONS (A POSSIBLE PROTECTIVE ROLE OF PHYTOESTROGENS)

Background : In spite of many known and suspected factors associated with the risk of breast cancer there has until recently been no explanation for its continuing increase in women of Western societies over recent decades or why there has not been an equivalent increase in women of most Asian and other less Westernized societies. It has long been suspected that a significant factor has been an increasing change of diet in Western societies from one predominantly vegetarian to one with a high content of meat and dairy products as well as ‘refined’ foods. Although diet has long been suspected there has otherwise been no real explanation as to the mechanism of the change in incidence of breast cancer. Methods : A comprehensive literature review has been made of aetiological factors and associations concerning breast cancer to determine whether any consistent trend can explain the rising incidence in Western societies. Results : There are a number of likely contributory factors but there is now accumulating evidence that the single most important difference is that people having a vegetarian diet have a high intake of legumes and other plant foods containing a variety of lignans and isoflavonoids. These appear to have an important role as nature'sex hormone modulators. These agents appear to be biologically active in a number of ways not yet completely understood but they do have both a weak oestrogenic effect and an anti-oestrogenic competitive effect, thus reducing the potential carcinogenic action of prolonged oestrogen activity. A probable additional benefit of such diets could be the role of dietary fibre. Conclusions : A major problem of Western diets may not be the presence of meat or dairy products in the diet but the absence of desirable ingredients of vegetarian diets, namely dietary fibre and certain plant lignans and isoflavonoids. A modification of diet to include a greater proportion of fibre and soy or other leguminous plant food should be studied. Alternatively addition of more fibre and lignans and especially isoflavonoids to traditional Western diets would seem worthy of serious investigation. Such influences appear to have their greatest impact early in life and therefore could be especially important for girls and young women in Western societies.     

射干异黄酮分散片的制备和质量考察

目的研究射干异黄酮分散片的制备工艺及质量。方法以崩解时间为指标,采用正交设计法考察处方组分和筛选处方,并对优选处方的3批样品进行崩解时限、溶出度、分散均匀性等质量评价。结果优选的射干分散片处方为:12%交联聚乙烯吡咯烷酮(内加:外加=2:1),14%预胶化淀粉(内加:外加=2:1),3%微粉硅胶。射干分散片可在30 s内完全崩解,在45 m in内可释放完全,分散均匀性等符合分散片各项质量指标。结论本实验制备的射干分散片崩解快,溶出度高,制备工艺较简单,适用于工业化生产。     

野葛化学成分研究

目的研究野葛(Pueraria lobata)根的化学成分。方法利用溶剂提取,硅胶柱色谱和凝胶色谱等手段进行分离、纯化,根据理化性质和波谱数据进行结构鉴定。结果分离鉴定了14个化合物,分别为大豆苷元(1),芒柄花苷(2),大豆苷(3), 3′-甲氧基葛根素(4),葛根素(5),葛苷B(6),大豆苷元-8-C-芹菜糖基-(1-6)-葡萄糖苷(7), 3′-羟基葛根素(8),葛根素木糖苷(9),大豆苷元-7,4′-O-二葡萄糖苷(10),葛根素-4′-O-葡萄糖苷(11),美佛辛-4′-O-葡萄糖苷(12), sissotorin(13),葛苷C(14)。结论化合物11和13为首次从野葛的根中分离得到。     

交趾黄檀异黄酮类化学成分研究

目的研究交趾黄檀Dalbergia cochinchinensis中异黄酮类化学成分。方法采用正、反相以及凝胶柱色谱等方法进行分离纯化,通过理化性质及波谱分析进行结构鉴定。结果从交趾黄檀心材70%乙醇提取物中分离得到14个异黄酮类成分,分别鉴定为紫苜蓿酮(1)、7-羟基-2′,4′-二甲氧基异黄烷(2)、4,7,2′-三羟基-4′-甲氧基异黄烷醇(3)、5,7-二羟基-2′,3′,4′-三甲氧基二氢异黄酮(4)、芒柄花黄素(5)、2′-羟基芒柄花黄素(6)、2′,5,7-三羟基-4′-甲氧基异黄酮(7)、染料木黄酮(8)、3′-O-methylviolanone(9)、3-hydroxyvestitone(10)、鹰嘴豆芽素A(11)、后莫弗里素(12)、美迪紫檀素(13)、isodarparvinol B(14)。结论化合物3、4、12为首次从该属植物分离得到,化合物1~2、6~11、13~14首次从该植物分离得到。     

HPLC同时测定不同产地葛根中6种主要异黄酮类成分的含量

目的:建立同时测定葛根药材中6种主要异黄酮类成分含量的HPLC方法.方法:采用RP-HPLC法,Kromasil C18(4.6 mm×250 mm,5μm)柱;流动相:甲醇-0.1％枸橼酸溶液,梯度洗脱;流速1.0 mL· min-1,柱温30℃,检测波长250 nm.结果:3’-羟基葛根素、葛根素、大豆苷、染料木苷、芒柄花苷、大豆苷元的线性范围分别为76.2～1 016,65.8 ～1 316,85.6 ～1712,49.98 ～499.8,21.94 ～219.4,48.5 ～485 ng,相关系数(R2)均大于0.999 6,6种成分的平均加样回收率分别为99.73％(RSD 0.6％),100.48％ (RSD 1.11％),100.37％ (RSD 0.79％),100.28％(RSD 1.07％),99.96％ (RSD 1.22％),97.36％(RSD 1.59％).结论:方法简便快速,重复性良好,结果准确可靠,可用于葛根药材中6种主要异黄酮类成分的含量测定.     

Tyrosinase inhibitory constituents from the stems of Maackia fauriei

Bioassay‐guided investigation of the stems of Maackia fauriei led to the isolation of seven flavonoid constituents, formononetin (1), genistein (2), daidzein (3), texasin (4), tectorigenin (5), odoratin (6) and mirkoin (7). Their structures were elucidated on the basis of spectral studies as well as by comparison with literature data. Tyrosinase inhibition activities were carried out on the isolated compounds. Among these, mirkoin (7) was identified as a potent tyrosinase inhibitor. It inhibited mushroom tyrosinase with an IC₅₀ value of 0.005 mm , which is ten times more active than kojic acid (IC₅₀ = 0.045 mm ). The inhibition kinetics, analysed by Lineweaver‐Burk plots, indicated mirkoin (7) to be a competitive inhibitor of tyrosinase when l ‐tyrosinase was used as a substrate. The results suggest that hydroxyl groups at C‐4′ in the B ring of flavonoids play an important role in the tyrosinase inhibition activities. Interestingly, compounds 4–7 were isolated for the first time from this plant. Copyright © 2009 John Wiley & Sons, Ltd.     

黄豆渣中异黄酮的提取分离研究

 目的 对黄豆渣中异黄酮的提取分离进行研究,以利于综合开发大豆资源。方法 以异黄酮提取率及提取物中异黄酮含量为指标,采用正交试验法考察诸因素对提取的影响。提取物经丙酮除杂,醋酸乙酯萃取,提取分离总异黄酮;总异黄酮用10%HCl回流水解,提取分离异黄酮苷元,用HPLC检测结果。结果 提取异黄酮的最佳条件为一定量脱脂黄豆渣,每次用4倍量乙醇提取1 h,提取3次,提取率为1.14%;所得总异黄酮含量为25.6%,产率为1.05%;异黄酮苷元产率为0.4%,含量为46.5%。结论 以黄豆渣为原料生产异黄酮成本低,变废为宝,具有实际意义。     

Antithrombogenic and Antiplatelet Activities of Extract from <Emphasis Type="Italic">Maackia amyrensis</Emphasis> Wood

Antithrombogenic and antiplatelet effects of a new drug, containing isoflavonoids (extract from the wood of Maackia amyrensis, a Far Eastern plant), were studied. A course (200 mg/kg intragastrically during 14 days) of Maackia amyrensis extract prevented intravascular clotting, initiated by application of 10% iron chloride solution on the vessel. The drug increased antiaggregant activity of the vascular wall and potentiated endothelium-dependent vasodilatation in ovariectomied rats. The reference drug ethinylestradiol (25 μg/kg intragastrically during 14 days) potentiated the antiaggregant effect of the endothelium, but was inferior to Maackia amyrensis extract in the capacity to induce endothelium-dependent vasodilatation in ovariectomied rats. Translated from Byulleten’ Eksperimental’noi Biologii i Meditsiny, Vol. 147, No. 2, pp. 164-167, February, 2009     

Antibacterial activity of flavonoids from the stem bark of Erythrina caffra thunb.

The antibacterial activity of the stem bark of Erythrina caffra Thunb. was investigated against different bacterial strains. The antibacterial activity was determined by a micro broth dilution assay. Antibacterial compounds were isolated and identified using a Bruker Avance III LPO NMR spectrometer. Four known flavonoids, abyssione‐V 4′‐O‐methyl ether, 6,8‐diprenylgenistein, alpinumisoflavone and burttinone, were isolated. All the compounds were active against both Gram‐negative and Gram‐positive bacteria. The minimum inhibitory concentration values obtained (MIC) ranged from 3.9 μg/mL to 125 μg/mL. This is the first report of antibacterial activity of burttinone and the isolation of these compounds from E. caffra. Copyright © 2010 John Wiley & Sons, Ltd.