棉毛橐吾根茎中化学成分研究

采用硅胶、Sephadex LH-20凝胶、Toyopearl HW-40凝胶及Diaion HP-20树脂等色谱方法从云南丽江棉毛橐吾中分离得到化合物18个,通过理化手段及波谱技术分别鉴定为:呋喃艾里莫芬-14β,6α-内酯(1)、β-谷甾醇(2)、惕格酸(3)、棕榈酸(4)、十九烷酸甲酯(5)、艾里莫芬-7(11)-烯-12,8α(14β,6α)-二内酯(6)、8β-甲氧基艾里莫芬-7(11)-烯-12,8α(14β,6α)-二内酯(7)、1-O-十六烷酰基甘油酯(8)、8β-羟基艾里莫芬-7(11)-烯-12,8α(14β,6α)-二内酯(9)、对羟基桂皮酸甲酯(10)、对羟基苯乙酮(11)、伞形花内酯(12)、3,4-二羟基苯乙酮(13)、胡萝卜苷(14)、1,5-二咖啡酰奎宁酸(15)、对羟基桂皮酸(16)、咖啡酸(17)及七叶内酯(18),其中化合物4~5,8,10,13,15及17,18为首次从该植物中分离得到。     

甘肃产蓝萼香茶菜二萜化学成分研究

对甘肃天水小陇山产蓝萼香茶菜进行二萜化学成分研究。采用硅胶柱色谱法分离纯化,通过薄层色谱及波谱法进行结构鉴定,SRB法分别对分离化合物进行了体外细胞毒活性测试。共鉴定出5个二萜化合物,它们分别为:1α,6,11β,15β-四乙酰基-6,7-断裂-7,20-内酯-对映-贝壳杉-16-烯(1α,6,11β,15β-tetraacetoy-6,7-seco-7,20-olide-ent-kaur-16-en,Ⅰ),6β,11α-二羟基-6,7-断裂-6,20-环氧-1α,7-内酯-对映-贝壳杉-16-烯-15-酮(6β,11α-di-hydroxy-6,7-seco-6,20-epoxy-1α,7-olide-ent-kaur-16-en-15-one,Ⅱ),6β,7β,14β-三羟基-1α-乙酰氧基-7α,20-环氧-对映-贝壳杉-16烯-15-酮(6β,7β,14β-trihydroxy-1α-acetoxy-7α,20-epoxy-ent-kaur-16-en-15-one,Ⅲ),6β,11α,15α-三羟基-6,7-断裂-6,20-环氧-1α,7-内酯-对映-贝壳杉-16-烯(6β,11α,15α-trihydroxy-6,7-seco-6,20-epoxy-1α,7-olide-ent-kaur-16-en,Ⅳ),1α,6β,7β,14β-四羟基-7α,20-环氧-对映-贝壳杉-16-烯-15-酮(1α,6β,7β,14β-tetrahydroxy-7α-20-ep-oxy-ent-kaur-16-en-15-one,Ⅴ)。化合物Ⅲ、Ⅳ、Ⅴ均为首次从该植物中分离得到,并且以上5个二萜化合物对人肝癌细胞株Bel-7402和人卵巢癌细胞株HO-8910均显示了良好的细胞毒活性。     

Two New Triterpenoid Saponins from Akebia quinata （Thunb.） Decne.

Two new triterpenoid saponins, hederagenin 3-O-α-L-arabinopyranosyl-（1→〉2）-α-L-arabinopyranoside named akeboside La （compound 1）, oleanolic acid 3-O-α-L-arabinopyranosyl-（1→〉2）-β-D-glucopyranoside named akeboside Lb （compound 2）, along with five known saponins, oleanolic acid 3-O-α-L-rhamnopyranosyl-（1→〉2）-α-L- arabinopyranoside （compound 3）, hederagenin 3-O-α-L-rhamnopyranosyl-（1→〉2）-α-L-arabinopyranoside （compound 4）, oleanolic acid 3-O-β-D-xylopyranosyl-（1→〉3）-α-L-rhamnopyranosyl-（1→〉2）-α-L-arabinopyranoside （compound 5）, 3-O-α-L-rhamnopyranosyl-（1→〉2）-α-L-arabinopyranosyl oleanolic acid 28-O-α-L-rhamnopyranosyl-（1→〉4）-α-D- glucopyranosyl-（1→〉6）-β-D-glucopyranoside （compound 6）, 3-O-α-L-rhamnopyranosyl-（1→〉2）-α-L-arabinopyranosyl hederagenin 28-α-L-rhamnopyranosyl-（1→〉4）-β-D-glucopyranosyl-（1→〉6）-β-D-glucopyranoside （compound 7） were isolated from the n-butanol part of the 80% ethanol extracts of the dried stems of Akebia quinata （Thunb.） Decne. Compound 5 was isolated from plants of genus Akebia for the first time. The structures were elucidated on the basis of physicochemical properties and spectral data.     

小花草玉梅化学成分研究

目的：研究银莲花属植物小花草玉梅的化学成分。方法：采用硅胶柱色谱,凝胶柱色谱,反相柱色谱并结合制备高效液相色谱等技术分离纯化单体化合物,并根据理化性质及光谱数据鉴定结构。结果：分离并鉴定了4个化合物,分别是常春藤皂苷元-28-O-β-D-吡喃葡萄糖酯苷（1）、3-O-β-D-吡喃葡萄糖-（1→2）-α-L-吡喃阿拉伯糖-齐墩果酸皂苷元-28-O-α-L-吡喃鼠李糖-（1→4）-β-D-吡喃葡萄糖-（1→6）-β-D-吡喃葡萄糖酯苷（2）、3-O-β-D-吡喃葡萄糖-（1→2）-α-L-吡喃阿拉伯糖-常春藤皂苷元-28-O-α-L-吡喃鼠李糖-（1→4）-β-D-吡喃葡萄糖-（1→6）-β-D-吡喃葡萄糖酯苷（3）和3-O-β-D-吡喃核糖-（1→3）-α-L-吡喃鼠李糖-（1→2）-α-L-吡喃阿拉伯糖-常春藤皂苷元-28-O-α-L-吡喃鼠李糖-（1→4）-β-D-吡喃葡萄糖-（1→6）-β-D-吡喃葡萄糖酯苷（4）。结论：化合物1为首次从银莲花属植物中分离得到,2-4为首次从小花草玉梅中分离得到。     

珍珠菜中黄酮及Megastigmane类化学成分研究北大核心CSCD

对珍珠菜Lysimachia clethroides的化学成分进行研究。应用硅胶、Sephadex LH-20和制备型HPLC等柱色谱技术进行分离纯化,并运用现代波谱技术（ESI-MS,^1H-NMR,^13C NMR）进行结构鉴定。从珍珠菜中分离得到12个化合物,分别鉴定为山柰酚（1）、槲皮素（2）、cinchonain Ib（3）、芹菜素-6-C-β-D-吡喃木糖基-8-C-α-L-吡喃阿拉伯糖苷（4）、芹菜素-6,8-二-C-α-L-吡喃阿拉伯糖苷（5）、芹菜素-6-C-α-L-吡喃阿拉伯糖基-8-C-β-D-吡喃木糖苷（6）、芹菜素-6,8-二-C-β-D-吡喃木糖苷（7）、芹菜素-6-C-β-L-吡喃阿拉伯糖基-8-C-β-D-吡喃葡萄糖苷（8）、芹菜素-6-C-α-L-吡喃阿拉伯糖基-8-C-β-D-吡喃葡萄糖苷（9）、芹菜素-6-C-β-D-吡喃葡萄糖基-8-C-α-L-吡喃阿拉伯糖苷（10）、blumenol A（11）、（3S,5R,6R,7E,9S）-大柱香波龙-7-烯-3,5,6,9-四醇-3-O-β-D-吡喃葡萄糖苷（12）。化合物3-8和11-12为首次从该属植物中分离得到。体外活性测试结果显示化合物1-12均没有明显的细胞毒活性（IC50〉10 μM）。     

中国特有药用植物铁破锣中的新皂甙类成分

从铁破锣（Beesia calthaefolia(Maxim.)Ulbr.根茎中分离得到5个化合物（1－5）,经化学和波谱学方法鉴定,其中2个为有机酸－铁破锣酸（beesic acid,9-phenyl-2E,4E,6E,8E-nontetraenoic acid,1)和香草酸（2）;3个为齐墩果酸型三萜皂甙：oleanolic acid-3-o－α-Larabinopyranosyl-－28－O-α-L-rhamnopyranosyl-(1→4）-β-D-glucopyranosyl-（1→6）-β-D-glucopyranosyl ester(3),hederasaponin B(oleanolic acid-3-O-α-L-rhamnopyranosyl-(1→2)-α－L-arabinopyranosly-28-Oα-L-rhamnopyranosyl-(1→4)-β-D-glucopyranosyl-(1→6）－β－D－glucopyranosyl ester,4)和铁破锣皂甙Q（beesioside Q,oleanolic acid-3-O-β-D-glucopyranosyl-(1→3）－α－L-rhamnopyranosyl-(1→2)-α-L-arabinopyranolsyl-28-O-α-L-rhamnopyranosyl-(1→4)-β-D-glucopyranosyl-(1→6）－β－D－glucopyranosyl ester,5)。化合物1系首次从自然界中分离得到,化合物5为新化合物。     

D-葡萄糖苷酶抑制剂的研究

用高灵敏度的荧光法研究了13种糖类化合物对α或β-D-葡萄糖苷酶的抑制作用．实验结果表明：5-氨基-5-脱氧-D-吡喃葡萄糖-1-磺酸铵盐（1）、5-氨基-5-脱氧-D-吡喃葡萄糖-1-磺酸（2）、5-氨基-5-脱氧-D-葡萄糖-1．亚硫酸加成物（3）等三种氮杂糖对α或β-D-葡萄糖苷酶均呈现竞争性抑制作用．化合物（1）的Kiα＝372μmol／L;Kiβ＝6．38μmol/L．化合物（2）的Kiα＝34．4μmol／L;Kiβ＝6．84μmol／L．化合物（3）的Kiα＝47．2μmol/L;Kiβ＝11．9μmol/L．上述三个化合物对β-D-葡萄糖苷酶的抑制作用都强子α-D-葡萄糖苷酶．尤其对化合物（1）,其Kiα／Kiβ＝58．3,表明其抑制糖苷酶活性有较好的选择性．     

绿玉树化学成分研究北大核心CSCD

采用正反相硅胶、Sephadex LH-20和HPLC等色谱手段对绿玉树Euphorbia tirucalli化学成分进行分离纯化,从绿玉树地上部分70%丙酮提取物中分离得到12个化合物。利用MS、1H NMR和13C NMR等现代波谱技术确定化合物结构为4α-去氧-巴豆醇-13-乙酸酯（1）、对映-3β,13S-二羟基-16-烯-14-阿替森酮（2）、羊毛甾醇（3）、3-表-粘霉烯醇（4）、齐墩果烷-9（11）,12-二烯-3-酮（5）、β-香树烯酮（6）、齐墩果烷-18-烯-3-酮（7）、无羁萜（8）、4-豆甾烯-3-酮（9）、β-谷甾醇（10）、山奈酚-3-O-α-L-鼠李糖苷（11）和东莨菪内酯（12）。其中,化合物1、2、5-7、9和12为首次从该植物中分离得到。     

土木香化学成分的研究

采用硅胶柱色谱、制备薄层色谱、制备高效液相、葡聚糖凝胶SephadexLH-20等方法进行分离纯化,根据光谱数据进行结构鉴定。从乙醇提取物中分离得到了8个化合物,分别鉴定为：异土木香内酯（1）,11,13-二氢异土木香内酯（2）,土木香内酯（3）,β-谷甾醇（4）,3-hydroxy-11,13-dihydroisoalantolactone（5）,macrophyllilae-toneE（6）,HIS-12-en-18-H-3-O-β-D-glucopyranoside（7）,caffeic acid anhydride（8）。化合物7和8系首次从该属植物中分离得到。     

中华小苦荬萜类化学成分的研究(英文)

从中华小苦荬全草的乙酸乙酯提取物中分离得到8个萜类化合物,通过波谱方法及文献对照分别鉴定为β-香树脂素(1),3β-羟基-20(30)-蒲公英甾烯(2),熊果-12-烯-3β-醇(3),羽扇豆醇(4),10-羟基艾里莫芬-7(11)-烯-12,8α-内酯(5),乌苏-12,20(30)-二烯-3β,28-二醇(6),3β,8α-二羟基-6β-当归酰基艾里莫芬-7(11)-烯-12,8β-内酯(7)和乌苏酸(8),化合物1～8均首次从该植物中分离得到。     

Sesquiterpene lactones,flavonoids and anthraquinones from Asphodeline globifera and Asphodeline Damascena

The known compounds chrysoeriol, apigenin, luteolin, acacetin, scutellarein, 6-methoxyluteolin, apigenin 7-glucoside, luteolin 7-glucoside, esculetin, chrysophanol, asphodeline, mircocarpin, sitosterol, 1-β-acetoxyeudesman-4(15),7(11)dien-2α,12-olide and 1-β-acetoxy-8β-hydroxyeudesman-4(15),7(11)-dien-8α,12-olide were isolated from Asphodeline globifera and A. damascena. A new sesquiterpene lactone 1-β-acetoxy-8β-ethoxyeudesman-4(15),7(11)dien-8α, 12-olide was also characterized. These are the first reports of sesquiterpene lactones in Asphodeline and in the Liliaceae.     

Studies on the Constituents of Aristolochia versicolar S. M. Hwang

Twenty-four constituents were isolated from the root of Aristolochia versicolar S. M. Hwang (collected from Guangxi province, China). Ten of them (two novel sesquiterpene lacrones and eight known compounds) were reported recently. This paper deals with the other eight compounds. From the petroleum ether extraction a sesquiterpene lactone, C15H20O2, mp. 94–95℃ [α]D36 –49˚ (C=1.8, EtOH), confirmed to be isoaristolactone, was obtained from plants for the first time. On the basis of spectral analysis (UV, IR, 1HNMR, 13CNMR, MS) and chemical reactions its structure was determined as B2. From the petroleum enter unsoluble sec- tion 6-methoxyaristolic acid methyl ester (D1), aristolic acid (D3), 6-methoxyaristolic acid (ari- stolinic acid) (D4f), 6-methoxyaristolochic acid methyl ester (D4y), aristolochic acid A(D5), β-sitosterol-D-glucoside (D10) and allantoin (C2) were isolated and identified. Dx, Ds, and Ds show ed antifertility activity in mice.     

Four new sesquiterpene polyol esters from Celastrus angulatus

Celastrus species, such as Celastrus angulatus, has been demonstrated to be very rich in natural sesquiterpene polyol esters sharing the β-dihydroagarofuran skeleton, some of which showed various biological activities. In this paper, four new sesquiterpene polyol esters, named as angulatins K-N (1–4), along with three known ones, 1β-acetoxy-9β-benzoxy-4α, 6α-dihydroxy-8α, 15-diisobutanoyloxy-2β-(α-methyl)-butanoyloxy-β-dihydroagarofuran, angulatin A, and celangulin III, were isolated from the root bark of C. angulatus. The structures of the new compounds were elucidated by extensive spectroscopic methods, mainly including HR-MS and 1D and 2D NMR techniques.     

A germacranolide sesquiterpene lactone suppressed inducible nitric oxide synthase by downregulating NF-κB activity

A germacranolide sesquiterpene lactone, 2α,5-epoxy-5,10-dihydroxy-6α-angeloyloxy-9β-(3-methylbutyloxy)-germacran-8α,12-olide (EDAG), isolated from Carpesium triste var. manshuricum, showed inhibitory activity in the production of nitric oxide (NO) and the expression of inducible nitric oxide synthase (iNOS) mRNA and protein in LPS-activated macrophage cells. Molecular analysis reveals that these suppressive effects are correlated with the inhibition of NF-κB activation by EDAG. Immunoblotting showed that EDAG suppressed the LPS-induced degradation of I-κBα and decreased nuclear translocation of p65. Furthermore, EDAG showed reduced phosphorylation of ERK1/2 and p38 MAPK, whereas activation of JNK was not changed. These data suggest, at least in part, that EDAG utilizes the signal cascades of ERK1/2, p38 MAPK, and NF-κB for the suppression of iNOS gene expression.     

Microbial transformation of the sesquiterpene lactone tagitinin C by the fungus Aspergillus terreus

The biotransformation of the sesquiterpene lactone tagitinin C by the fungus Aspergillus terreus MT 5.3 yielded a rare derivative that was elucidated by spectrometric methods. The fungus led to the formation of a different product through an unusual epoxidation reaction between C4 and C5, formation of a C3,C10 ether bridge, and a methoxylation of the C1 of tagitinin C. The chemical structure of the product, namely 1β-methoxy-3α-hydroxy-3,10β-4,5α-diepoxy-8β-isobutyroyloxygermacr-11(13)-en-6α,12-olide, is the same as that of a derivative that was recently isolated from the flowers of a Brazilian population of Mexican sunflower (Tithonia diversifolia), which is the source of the substrate tagitinin C. The in vitro cytotoxic activity of the substrate and the biotransformed product were evaluated in HL-60 cells using an MTT assay, and both compounds were found to be cytotoxic. We show that soil fungi may be useful in the biotransformation of sesquiterpene lactones, thereby leading to unusual changes in their chemical structures that may preserve or alter their biological activities, and may also mimic plant biosynthetic pathways for production of secondary metabolites.     

Anti-inflammatory sesquiterpene lactones from the flower of Vernonia cinerea

Bioassay-guided fractionation of the hexane extract from the flowers of Vernonia cinerea (Asteraceae) led to the isolation of a new sesquiterpene lactone, 8α-hydroxyhirsutinolide (2), and a new naturally occurring derivative, 8α-hydroxyl-1-O-methylhirsutinolide (3), along with seven known compounds (1 and 4-9). The structures of the new compounds were determined by 1D and 2D NMR experiments and by comparison with the structure of compound 1, whose relative stereochemistry was determined by X-ray analysis. The isolated compounds were evaluated for their cancer chemopreventive potential based on their ability to inhibit nitric oxide (NO) production and tumor necrosis factor alpha (TNF-α)-induced NF-κB activity. Compounds 1, 2, 4, 5, and 9 inhibited TNF-α-induced NF-κB activity with IC(50) values of 3.1, 1.9, 0.6, 5.2, and 1.6μM, respectively; compounds 4 and 6-9 exhibited significant NO inhibitory activity with IC(50) values of 2.0, 1.5, 1.2, 2.7, and 2.4μM, respectively.     

A new neolignan glucoside from hairy roots of Cichorium intybus

A new neolignan glucoside was isolated from hairy roots of Cichorium intybus. Its structure was determined as (7S, 8R)-3′-demethyl-dehydrodiconiferyl alcohol-3′-O-β-glucopyranoside based on a combination of 1D and 2D NMR techniques and CD data. In addition, further water soluble constituents, including four known phenolic compounds and one known sesquiterpene lactone glucoside, were isolated from the same source.     

Chlorinated and diepoxy withanolides from Withania somnifera and their cytotoxic effects against human lung cancer cell line

Phytochemical studies on the aerial parts of Withania somnifera L. Dunal. (Solanaceae) led to the isolation of a chlorinated steroidal lactone (27-acetoxy-4β,6α-dihydroxy-5β-chloro-1-oxowitha-2,24-dienolide), a diepoxy withanolide (5β,6β,14α,15α-diepoxy-4β,27-dihydroxy-1-oxowitha-2,24-dienolide), and withaferin A. Their structures were elucidated by using spectroscopic techniques. All three compounds exhibited a growth inhibition and cytotoxic activity against human lung cancer cell line (NCI-H460), with withaferin A being the most potent (GI(50)=0.18 μg/mL and LC(50)=0.45 μg/mL) among three compounds tested.     

Chlorinated Withanolides from Withania somnifera

A chlorinated withanolide, 6α-chloro-5β,17α-dihydroxywithaferin A (1), and nine known withanolides, 6α-chloro-5β-hydroxywithaferin A (2), (22R)-5β-formyl-6β,27-dihydroxy-1-oxo-4-norwith-24-enolide, withaferin A, 2,3-dihydrowithaferin A, 3-methoxy-2,3-dihydrowithaferin A, 2,3-didehydrosomnifericin, withanone, withanoside IV and withanoside X, were isolated from Withania somnifera (Solanaceae). All structures were elucidated on the basis of spectroscopic methods (IR, HRESIMS, 1D/2D NMR). X-ray crystallography confirmed the absolute configuration of 1.     

Three new dihydroagarofuran sesquiterpenoids from Celastrus orbiculatus

Three new β-dihydroagarofuran sesquiterpene polyesters, 1β-acetoxy-8α,9β-dibenzoyloxy-13-nicotinoyloxy-β-dihydroagarofuran (1), 1β,2β-diacetoxy-9α-benzoyloxy-13-nicotinoyloxy-β-dihydroagarofuran (2), and 6α,8α,9β,13-tetraacetoxy-1β-cinnamoyloxy-2β,4α-dihydroxy-β-dihydroagarofuran (3) were isolated from the fruits of Celastrus orbiculatus Thunb. Their structures were determined by means of extensive spectroscopic analyses (IR, ESIMS, HRESIMS, 1D and 2D NMR).