维药瘤果黑种草籽化学成分研究

为研究维药瘤果黑种草籽的化学成分,采用硅胶、ODS柱色谱等方法分离纯化,分离并鉴定了16个化合物,利用理化性质及波谱方法鉴定化学成分的结构分别为:Nigeglanine(1)、附子碱(2)、L-色氨酸(3)、L-色氨酸甲酯(4)、5,7-二羟基-异苯并呋喃酮(5)、豆甾醇(6)、豆甾醇-3-O-β-D-葡萄糖苷(7)、β-谷甾醇(8)、β-胡萝卜苷(9)、亚油酸(10)、邻苯二甲酸二丁酯(11)、棕榈酸(12)、十六烷酸1-甘油酯(13)、硬酯酸(14)、硬酯酸2-甘油酯(15)和蔗糖(16)。其中化合物3～5、7、9、11和15为首次从该种药材中得到。     

喜光花叶的化学成分研究(Ⅲ)

从喜光花Actephila merrilliana叶中分离得到11个化合物,通过理化方法和波谱数据分别鉴定为5,5’-dimethoxy-alloagerasasin(1)、对羟基苯甲醛(2)、丁香酸(3)、正十八烷酸(4)、反式桂皮酸(5)、对甲氧基苯甲酸(6)、间苯二酚(7)、邻苯二甲酸(8)、邻羟基苯甲酸(9)、对羟基苯甲酸(10)以及戊二酸(11),以上所有化合物均首次从该属植物中分离得到。     

河南蹄叶橐吾根的化学成分研究

从蹄叶橐吾根乙醇提取物中分离得到11种化合物,经理化和波谱分析分别鉴定为原儿茶醛(1)、7-羟基-色原酮(2)、咖啡酸(3)、阿魏酸(4)、1,5-二咖啡酰奎宁酸(5)、当归酸(6)、β-谷甾醇(7)、胡萝卜苷(8)、蜂斗菜素(9)、异蜂斗菜素(10)及正三十五烷(11)。其中酚类化合物1～5、倍半萜类化合物9～10及脂烃11为首次从该植物中分离得到。     

刺山柑化学成分研究

采用硅胶、聚酰胺和Sephadex LH-20等色谱方法从维吾尔药刺山柑中分离得到11个化学成分,通过理化手段及波谱技术分别鉴定为正二十八烷(1)、β-胡萝卜苷(2)、正二十八烷醇(3)、正三十二烷酸(4)、正十六烷酸(5)、琥珀酸(6)、原儿茶酸(7)4、-羟基-5-甲基呋喃-3-羧酸(8)、山萘酚3-O-β-D-芸香糖苷(9)、芦丁(10)和水苏碱(11)。其中化合物13、和4为首次从该属植物中分离得到。     

肾蕨的化学成分研究

从肾蕨乙醇提取物中分离得到6个化合物,根据理化和光谱分析,鉴定为β-谷甾醇(1)、羊齿-9(11)-烯(2)、齐墩果酸(3)、肉豆蔻酸十八烷基酯(4)、正三十一烷酸(5)和正三十烷醇(6),化合物3～6为首次从该植物中分离得到。     

桑白皮的化学成分研究

采用硅胶和凝胶柱层析方法对桑白皮(Cortex Mori)的化学成分进行分离纯化,并根据理化性质和光谱数据分析鉴定得到11个化合物,分别是:羟基白藜芦醇(Hydroxyresveratrol,1),桑叶苷A(mulberroside A,2),熊果酸(ursolic acid,3),3-乙酰基-α-香树酯醇(3-acetyl-α-amyranol,4),熊果烷(ursane,5),β-谷甾醇(β-sitosterol,6),胡萝卜苷(daucosterol,7),十六碳烷酸(palmitic acid,8),十八碳烷酸(stearic acid,9),二十六烷酸-α-单甘油酯(α-glycerol monohexacosanoate,10),二十八烷酸-α-单甘油酯(α-glycerol monooctacosanoate,11)。其中化合物5、8～11均为首次从桑白皮中获得。     

小果南烛三萜类化学成分研究

羊毛甾烷三萜是南烛属植物主要活性成分之一。为进一步研究南烛属植物功效物质基础,结合民族民间对小果南烛的应用实际,该文利用硅胶、MCI、Sephadex LH-20、半制备高效液相色谱等植物化学技术手段对该植物95%乙醇提取物进行分离、纯化,综合理化性质和波谱数据对其化合物进行鉴定。结果表明:从小果南烛的茎、叶提取物中分离得到14个三萜及其皂苷,分别鉴定为mollic acid 3-O-α-Larabinopyranoside (1)、mollic acid 3-O-β-D-glucopyranoside (2)、cycloart-3,7-dihydroxy-24-en-28-oic acid (3)、白桦脂酸(4)、1β,3α,11α-trihydroxy-urs-12-ene (5)、oleanderolide (6)、(Z)-马斯里酸-3-O-对香豆酸酯(7)、木栓酮(8)、坡模酸(9)、2α,3α-二羟基乌苏-12-烯-28-酸(10)、科罗索酸(11)、齐墩果酸(12)、熊果酸(13)、委陵菜酸(14)。其中,化合物1-7为首次从南烛属植物分离得到,化合物8-11,14为首次从小果南烛植物中分离得到。     

大叶土蜜树化学成分及抗神经炎活性研究

为研究大叶土蜜树(Bridelia retusa)茎的化学成分及其抗神经炎活性,采用色谱技术从大叶土蜜树茎部分95%乙醇提取物中分离得到11个化合物。通过核磁共振波谱、质谱以及与文献数据比较,化合物结构鉴定为没食子酸(1)、木栓酮(2)、阿魏酸二十七烷脂(3)、芥子醛(4)、丁香醛(5)、丁香脂素(6)、补骨脂素(7)、补骨脂酚(8)、二十五烷酸(9)、亚油酸(10)和1-Linoleoylglycerol(11)。其中化合物3～11为首次从土蜜树属中分离得到。对化合物1～11的抗神经炎活性进行评价,发现化合物4、5、10和11对LPS诱导BV-2细胞NO生成具有显著抑制作用,其IC50分别为12. 57、8. 41、5. 86、5. 86μM。     

珍珠菜的化学成分研究(英文)

从珍珠菜(Lysimachia clethroidesDuby)的70%丙酮提取物中分离得到11个化合物,经理化性质及波谱数据分析分别鉴定为23-羟基乌苏酸(1)、Isotachioside(2)、对羟基苯甲酸(3)、3-甲氧基-4-羟基苯甲酸(4)、原儿茶酸(5)、3,5-二羟基苯甲酸(6)、甲基-α-D-呋喃果糖苷(7)、尿苷(8)、β-谷甾醇(9)、胡萝卜苷(10)和齐墩果酸(11)。化合物1、2、4、7和8为首次从该属植物中分离得到,化合物3、5、6、9~11为首次从该种植物中分离得到。     

攀援孔药花化学成分研究

从攀援孔药花全草95%乙醇提取物中首次分离得到19个化合物,通过波谱数据或与已知物对照,它们分别鉴定为:(2S,3S,4R)-2-[(2R)-2-羟基-二十一酰胺基]-二十一烷-1,3,4-三醇(1)、(2S,3S,4R)-2-二十四酰胺基-十八烷-1,3,4-三醇(2)、胡萝卜甙(3)、β-谷甾醇(4)、(20S,22E,24R)-5α,8α-表二氧-麦角甾-6,22-二烯-3β-醇(5)、6β-羟基-豆甾-4-烯-3-酮(6)、十六烷酸-1-甘油酯(7)、桦木酸(8)、大黄素(9)、二十二烷酸-1-甘油酯(10)、对羟基苯甲醛(11)、十七烷酸-1-甘油酯(12)、金色酰胺醇乙酸酯(13)、十九烷酸-1-甘油酯(14)、棕榈酸(15)(、E)-p-香豆酸(16)、(22E,24S)-24-甲基-5α-胆甾-7,22-二烯-3β,5α,6β-三醇(17)、2-去氧-β-蜕皮激素(18)和auranamide(19)。     

薏苡糠壳的化学成分及其种子萌发活性研究

为了解薏苡(Coixlachryma-jobi)糠壳的化学成分,利用多种柱色谱技术对其乙醇提取物乙酸乙酯萃取部位进行分离,经波谱数据分析鉴定了15个化合物,分别为香豆酸(1)、香豆酸甲酯(2)、2-羟乙基-香豆酸酯(3)、咖啡酸甲酯(4)、阿魏酸甲酯(5)、(E)-3-(4-甲氧基苯基)丙烯酸(6)、2,3-二羟基-1-(4-羟基-3-甲氧基苯基)-1-丙酮(7)、2,3-二羟基-1-(4-羟基-3,5-二甲氧基苯基)-1-丙酮(8)、对羟基苯甲酸(9)、3-羟基-4-甲氧基苯甲酸(10)、1,3,5-三甲氧基苯(11)、methyl (3-hydroxy-2-oxo-2,3-dihydroindol-3-yl)-acetate (12)、尿囊素(13)、2-(2-羟乙基)-3-甲基反丁烯二酸(14)和油酸(15),其中化合物3、7、12、13和14为首次从薏苡中分离得到。活性测试结果表明,化合物1、2、9、10和11对种子萌发具有较强的抑制作用。     

苦槛蓝叶的黄酮类成分及其荔枝霜疫霉抑制活性研究

为了解苦槛蓝(Myoporum bontioides)的化学成分,采用色谱分离法从叶中分离得到11个化合物,分别鉴定为：5, 7, 3?-三羟基-4?-甲氧基黄酮(1)、3, 5, 7, 4?-四羟基-3?-甲氧基黄酮(2)、5, 7, 4?-三羟基-3?, 5?-二甲氧基黄酮(3)、木犀草素(4)、山奈酚(5)、鼠李黄素(6)、5, 7-二羟基二氢黄酮(7)、7, 4?-二羟基二氢黄酮(8)、5, 7, 3?, 4?-四羟基二氢黄酮(9)、5-O-乙酰基-3, 7, 3?, 4?-四羟基二氢黄酮(10)和7-甲氧基香橙素(11)。除化合物4、7、11之外,其他化合物均为首次从苦槛蓝叶中分离得到。菌丝生长速率法测试表明化合物4、7~9和11对荔枝霜疫霉菌具有较好的抑菌活性。     

铁皮石斛内生真菌次生代谢产物研究

为了解铁皮石斛(Dendrobium officinale)内生真菌Phyllosticta aristolochiicola的次生代谢产物,从该真菌中分离得到15个化合物,经波谱分析分别鉴定为N-methyl-2-pyrolidinone (1)、环-(甘氨酸-L-脯氨酸)(2)、环-(D-丙氨酸-L-脯氨酸)(3)、环-(L-缬氨酸-L-脯氨酸)(4)、环-(L-亮氨酸-L-脯氨酸)(5)、cyclo-(L-Leu-D-4-hydroxyprolinyl)(6)、环-(L-苯丙氨酸-L-脯氨酸)(7)、环-(L-苯丙氨酸-L-4-羟基脯氨酸)(8)、环-(L-酪氨酸-L-脯氨酸)(9)、环-(L-苯丙氨酸-L-亮氨酸)(10)、啤酒甾醇(11)、对羟基苯乙醇(12)、对羟基苯乙酸(13)、(2S,3R)-1-(4-羟基苯基)丁烷-2,3-二醇(14)和(2R,3S)-1-苯基丁烷-2,3-二醇(15)。采用MTS法检测抗肿瘤活性表明,化合物2、10和14对HL-60、A-549、SMMC-7721、MCF-7和SW-480细胞株具有一定的抑制活性。     

Biotransformation of gallic acid by <Emphasis Type="Italic">Beauveria sulfurescens</Emphasis> ATCC 7159

Preparative-scale fermentation of gallic acid (3,4,5-trihydroxybenzoic acid) (1) with Beauveria sulfurescens ATCC 7159 gave two new glucosidated compounds, 4-(3,4-dihydroxy-6-hydroxymethyl-5-methoxy-tetrahydro-pyran-2-yloxy)-3-hydroxy-5-methoxy-benzoic acid (4), 3-hydroxy-4,5-dimethoxy-benzoic acid 3,4-dihydroxy-6-hydroxymethyl-5-methoxy-tetrahydro-pyran-2-yl ester (7), along with four known compounds, 3-O-methylgallic acid (2), 4-O-methylgallic acid (3), 3,4-O-dimethylgallic acid (5), and 3,5-O-dimethylgallic acid (6). The new metabolite genistein 7-O-β-D-4″-O-methyl-glucopyranoside (8) was also obtained as a byproduct due to the use of soybean meal in the fermentation medium. The structural elucidation of the metabolites was based primarily on 1D-, 2D-NMR, and HRFABMS analyses. Among these compounds, 2, 3, and 5 are metabolites of gallic acid in mammals. This result demonstrated that microbial culture parallels mammalian metabolism; therefore, B. sulfurescens might be a useful tool for generating mammalian metabolites of related analogs of gallic acid (1) for complete structural identification and for further use in investigating pharmacological and toxicological properties in this series of compounds. In addition, a GRE (glucocorticoid response element)-mediated luciferase reporter gene assay was used to initially screen for the biological activity of the 6 compounds, 2–6 and 8, along with 1 and its chemical O-methylated derivatives 9–13. Among the 12 compounds tested, 11–13 were found to be significant, but less active than the reference compounds of methylprednisolone and dexamethasone.     

New lanostane-type triterpenoids, inonotsutriols D, and E, from Inonotus obliquus

Two new lanostane-type triterpenoids, inonotsutriols D (1) and E (2), were isolated from the sclerotia of Inonotus obliquus (Pers.: Fr.) Pil. (Japanese name: kabanoanatake; Russian name: chaga). Their structures were determined to be lanost-8-ene-3β,22R,24R-triol (1) and lanost-8-ene-3β,22R,24S-triol (2) on the basis of spectral data, including 2D NMR analysis. In addition, major compounds, inotodiol (3), trametenolic acid (4), 3β-hydroxylanosta-8,24-dien-21-al (5), 21-hydroxylanosterol (6), inonotsuoxide A (7) and inonotsuoxide B (8) were identified, and all compounds, except 2, were evaluated for their cancer cell growth inhibitory activity against P388, HL-60, L1210 and KB cell lines.     

Hydroxylation of steroids by Fusarium oxysporum, Exophiala jeanselmei and Ceratocystis paradoxa

The potential of Fusarium oxysporum var. cubense UAMH 9013 to perform steroid biotransformations was reinvestigated using single phase and pulse feed conditions. The following natural steroids served as substrates: dehydroepiandrosterone (1), pregnenolone (2), testosterone (3), progesterone (4), cortisone (5), prednisone (6), estrone (7) and sarsasapogenin (8). The results showed the possible presence of C-7 and C-15 hydroxylase enzymes. This hypothesis was explored using three synthetic androstanes: androstane-3,17-dione (9), androsta-4,6-diene-3,17-dione (10) and 3α,5α-cycloandrost-6-en-17-one (11). These fermentations of non-natural steroids showed that C-7 hydroxylation was as a result of that position being allylic. The evidence also pointed towards the presence of a C-15 hydroxylase enzyme.The eleven steroids were also fed to Exophialajeanselmei var. lecanii-corni UAMH 8783. The results showed that the fungus appears to have very active 5α and 14α-hydroxylase enzymes, and is also capable of carrying out allylic oxidations.Ceratocystis paradoxa UAMH 8784 was grown in the presence of the above-mentioned steroids. The results showed that monooxygenases which effect allylic hydroxylation and Baeyer–Villiger rearrangement were active. However, redox reactions predominated.     

A new epoxidic ganoderic acid and other phytoconstituents from Ganoderma lucidum

A new epoxidic ganoderic acid, 8α,9α-epoxy-3,7,11,15,23-pentaoxo-5α-lanosta-26-oic acid (1), together with the known compounds 3β-hydroxy-7,11,15,23-tetraoxo-5α-lanosta-8-en-26-oic acid (2), ergosta-7,22-diene-3β-yl pentadecanoate (3), ergosta-7,22-diene-3β-ol (4), β-sitosterol (5), fatty acids (6–10), fatty acid ester (11) and octadecane (12) were isolated from the fruiting bodies of Ganoderma lucidum from south India. Their structures were determined by ¹H, ¹³C, ¹³C DEPT, ¹H–¹H COSY, HMBC, HSQC, NOESY NMR, FT-IR, UV–vis and FABMS spectral analysis. Compounds (1–3) exhibited good antifungal activity against Candida albicans in disc diffusion assay (100 μg/disc). Steroid ester (3) showed moderate anti-inflammatory activity (59.7% inhibition, 100 mg/kg body weight) in carrageenan-induced paw edema.     

Biotransformation of pseudolaric acid B by Chaetomium globosum

Pseudolaric acid B (1) is a natural product with potent antifungal activity. We discovered that pseudolaric acid B did not kill but only suppress the growth of the filamentous fungus Chaetomium globosum. It was proposed that pseudolaric acid B was converted to metabolites with decreased antifungal activities. In this study, a scaled-up biotransformation of pseudolaric acid B by C. globosum produced five metabolites, including three new compounds, pseudolaric acid I (2), pseudolaric acid B 18-oyl-alanine (4) and pseudolaric acid B 18-oyl-serine (6), together with two known compounds, pseudolaric acid F (3) and pseudolaric acid B 18-oyl-glycine (5). The structures were characterized by NMR and MS spectroscopy. The major biotransformation reaction was conjugation with amino acids. None of the metabolites showed inhibitory effects on the growth of Candida albicans. The results suggested that biotransformation might be a detoxification process for fungi to resist antifungal drugs.     

油榄仁果实化学成分的研究

为了解油榄仁(Terminalia bellirica Roxb.)的化学成分,从油榄仁果实的乙酸乙酯提取物中分离得到11个化合物,通过波谱分析,分别鉴定为:表松脂酚(1)、(–)-芝麻素(2)、麻醉椒苦素(3)、二氢醉椒素(4)、异香兰素(5)、3,4-二羟基苯甲酸(6)、没食子酸(7)、没食子酸甲酯(8)、没食子酸乙酯(9)、3,4,8,9,10-五羟基二苯骈[b,d]吡喃-6-酮(10)、polystachyol(11),其中化合物1~6、10和11为首次从油榄仁果实中分离得到。     

柯拉斯那沉香的生物活性成分研究

为了解柯拉斯那(Aquilaria crassna)的化学成分,从其所产沉香中分离得到10个化合物,经波谱分析分别鉴定为:6,8-羟基-2-(2-苯乙基)色酮(1),6,8-二羟基-2-[2-(4-甲氧基苯)乙基]色酮(2),rel-(1a R,2R,3R,7b S)-1a,2,3,7b-tetrahydro-2,3-dihydroxy-5-(2-phenylethyl)-7H-oxireno[f][1]benzopyran-7-one(3),rel-(1a R,2R,3R,7b S)-1a,2,3,7b-tetrahydro-2,3-dihydroxy-[2-(4-methoxyphenyl)-ethyl]-7H-oxireno[f][1]benzopyran-7-one(4),rel-(1a R,2R,3R,7b S)-1a,2,3,7b-tetrahydro-2,3-dihydroxy-5-[2-(3-hydroxy-4-methoxyphenyl)-ethyl]-7H-oxireno[f][1]benzopyran-7-one(5),oxidoagarochromone B(6),oxidoagarochromone C(7),(5S,6R,7S,8R)-2-[2-(3′-hydroxy-4′-methoxyphenyl)ethyl]-5,6,7,8-tetrahydroxy-5,6,7,8-tetrahydrochromone(8),6,7-cis-dihydroxy-2-(2-phenylethyl)-5,6,7,8-tetrahydrochromone(9),N-trans-feruloyltyramine(10)。化合物3~5和8~10为首次从柯拉斯那沉香中分离得到。化合物1,3,6,7,9和10对乙酰胆碱酯酶具有一定的抑制活性,化合物4对人慢性髓原白血病细胞株K-562和人胃癌细胞株SGC-7901均具有较小的抑制作用,化合物1和3对人肝癌细胞株BEL-7402也有抑制活性。