常用中药Xi莶研究进展

Xi签中已分离鉴定42个成分,其中17个是新二萜类化合物,我研究组确定了17个新成分中的10个,并对3个指定错了的化学结构给予了评论和改正。     

毛梗豨莶乙酸乙酯部位化学成分及生物活性研究

毛梗豨莶草(Siegesbeckia glabresce)的乙酸乙酯萃取部位具有显著的抑制细胞坏死性凋亡(necroptosis)的活性。为明确毛梗豨莶草的活性成分,该研究采用正相硅胶柱色谱谱(二氯甲烷∶甲醇20∶1～0∶1)、反相ODS柱色谱(30%～100%甲醇)、Sephadex LH-20柱色谱、重结晶等方法对毛梗豨莶草乙酸乙酯萃取部位进行了化学成分分离和纯化,并根据理化性质和波谱数据进行了结构鉴定。结果表明:从毛梗豨莶乙酸乙酯部位分离并鉴定了9个化合物,分别为3,7-二甲氧基槲皮素(1)、芹菜素(2)、奥卡宁(3)、okanin-4’-O-β-D-6″-trans-p-coumaroylglucoside(4)、1H-Indole-3-carbaldehyde(5)、对羟基苯甲醛(6)、3,5-二甲氧基-4-羟基苯甲醛(7)、3,4-divanillyltetrahydrofuran(8)、buddlenol D(9)。除化合物1和化合物6外,其余7个化合物均为首次从豨莶属植物中分离得到。     

中国被毛孢液体发酵的化学成分

本文采用反相硅胶、正相硅胶和Sephadex LH-20凝胶等层析技术对中国被毛孢液体发酵的化学成分进行研究。经1D-NMR(1H NMR、13C NMR、DEPT)、2D-NMR(HSQC、HMBC、1H,1H-COSY)和ESI-MS、HR-EI-MS解析鉴定,从其菌丝体中分离到腺苷(1)、2'-脱氧腺苷(2)、2,3-二羟基丙基壬烷酸酯(3)和4-羟基-6-戊基-四氢吡喃-2-酮(4),从发酵液中分离到4-甲基-1H-咪唑-5-乙醇(5)。化合物3和5首次以天然产物形式分离得到。     

两头毛的化学成分及药理作用研究进展

本文综述了两头毛的化学成分和药理作用的研究进展。两头毛中主要含有生物碱、黄酮类、甾醇、三萜类和神经酰胺等多种化学成分。药理学方面研究证明：两头毛具有抗炎,抗氧化,抑菌,神经营养等活性,在临床上,两头毛作为治疗肝炎和痢疾的药物。     

毛剪秋罗的化学成分研究

从毛剪秋罗(Lychnis coronaria(L.)Desr.)全草的乙醇提取物中分离鉴定了11个已知化合物,经波谱分析确定其结构分别为tricin 7-O-glucopyranoside(1),(+)-isoscoparin(2),epoxyactinidionoside(3), 1α, 20R- hydroxyecdysone ( 4 ), ecdysterone ( 5 ), polypoding B ( 6 ), ecdysterone 22-O-β-D-glucopyranoside(7), stigmast-5-ene-3-one(8), taraxerol ( 9 ), a-tocopherol (10), dehydrodiconiferyl alcohol 4-O-β-D-gluoopyranoside(11).此外,还分离得到β-谷甾醇和胡萝卜苷.以上化合物均为首次从该植物中分离得到.     

毛裂蜂斗菜化学成分的研究

从毛裂蜂斗菜（ｐｄｔａｓｉｌｅｘ ｔｒｉｃｈｏｌｏｂｕｓ Ｆｒａｎｃｈ。）的石油醚提取物中首次分离得到６个化合物,运用ＩＲ,ＥＩ－ＭＳ,ＨＲＭＳ,＾１Ｈ ＮＭＲ,＾１３Ｃ ＮＭＲ,ＤＥＰＴ等光谱方法确定了它们的结构。它们分别是：Ａ１－β－谷甾醇;Ａ２,三十二碳酸,Ａ３,羽扇豆醇;Ａ４,Ｂａｋｋｅｎｏｌｉｄｅ－Ｂ;Ａ５,Ｂａｋｋｅｎｏｌｉｄｅ－Ｄ和Ａ６,ａｋｋｅｎｏｌｉｄｅ－Ｅ。     

毛球莸和小叶灰毛莸的化学成分

从毛球莸中分离出4个化合物,经MS、~1H-NMR和~(13)C-NMR等波谱分析方法分别鉴定为刺槐素(Ⅰ),香叶木素(Ⅱ),赪桐甾醇(Ⅲ)和一个环烯醚萜甙——8-acetyl ha-pagide。从小叶灰毛莸中除分离到上述环烯醚萜甙,还另外获得一个环烯醚萜甙ajugoside(Ⅴ)。     

钩毛茜草蒽醌类化学成分的研究

为研究我国特有植物钩毛茜草(Rubia oncotricha)的化学成分,该文将钩毛茜草70%乙醇提取物采用硅胶、凝胶柱色谱等进行分离纯化,并对所得化合物进行结构鉴定。结果表明:从钩毛茜草中共分离了15个蒽醌类化合物,分别是2-methyl-1,3,6-trihydroxy-9,10-anthraquinone-3-O-(6′-O-acetyl)-α-rhamnosyl(1→2)-β-glucoside(1)、2-methyl-1,3,6-trihydroxy-9,10-anthraquinone-3-O-α-rhamnosyl(1→2)-β-glucoside(2)、2-methyl-1,3,6-trihydroxy-9,10-anthraquinone-3-O-(3′-O-acetyl)-α-rhamnosyl(1→2)-β-glucoside(3)、2-methyl-1,3,6-trihydroxy-9,10-anthraquinone-3-O-β-glucoside(4)、1,3,6-trihydroxy-2-hydroxymethyl-9,10-anthraquinone-3-O-(6′-O-acetyl)-β-D-glucopyranoside(5)、2-methyl-1,3,6-trihydroxy-9,10-anthraquinone-3-O-(6′-O-acetyl)-β-D-glucopyranoside(6)、大黄素甲醚-8-O-β-D-葡萄糖苷(7)、大黄素-8-O-β-D-葡萄糖苷(8)、digiferruginol-11-O-β-gentiobioside(9)、2-methyl-1,3,6-trihydroxy-9,10-anthraquinone-3-O-(6′-O-acetyl)-β-D-xylopyranosyl-(1→2)-β-D-glucopyranoside(10)、6-hydroxyrubiadin(11)、1,2-二羟基蒽醌(12)、大黄酚(13)、6-hydroxyxanthopurpurin(14)、1,3-二羟基蒽醌(15)。化合物7、8、14为首次从茜草属植物中分离得到,化合物1-6、9、10、12、13为首次从该药材中分离得到。     

大丁草属植物的化学成分和药理活性研究

本文概述了大丁草属植物的化学成分和药理活性研究。着重介绍了其中所含的香豆素类化合物的化学结构特点、光谱特征及生物活性。     

腺梗豨莶的新双色满

作者从腺梗莶的乙醚抽出物中分到一个新的双色满成分 ,基于光谱分析和应用二维核磁共振技术 ,它的化学结构已被确定为 3,3’ 双 (3,4 二氢化 6 甲氧基 2H 1 苯并吡喃 )或 3,3’ 双 (6 甲氧基色满 )。     

In vitro anti-inflammatory activity of 3-O-methyl-flavones isolated from Siegesbeckia glabrescens

Four flavones, 3,4'-O-dimethylquercetin (1), 3,7-O-dimethylquercetin (2), 3-O-methylquercetin (3) and 3,7,4'-O-trimethylquercetin (4) were isolated as the inhibitors of nitric oxide production in activated microglia (IC(50) values: 11.1, 4.2, 3.8, and 25.1 microM, respectively). They suppressed the expression of protein and mRNA of inducible nitric oxide synthase. Furthermore, compounds 2 and 3 showed scavenging activity of peroxynitrite with SC(50) values of 1.75 and 0.77 microM, respectively.     

PTP1B inhibitory activity of kaurane diterpenes isolated from Siegesbeckia glabrescens

Protein tyrosine phosphatase 1B (PTP1B) is considered as a therapeutic target for the treatment of diabetes and obesity. In our preliminary screening study, a MeOH extract of the aerial part of Siegesbeckia glabrescens was found to inhibit PTP1B activity at 30 microg/mL. Bioassay-guided fractionation led to the isolation of two active diterpenes, ent-16betaH, 17-isobutyryloxy-kauran-19-oic acid (1) and ent-16betaH, 17-acetoxy-18-isobutyryloxy-kauran-19-oic acid (2), along with ent- 16betaH, 17-hydroxykauran-19-oic acid (3). Compounds 1 and 2 inhibited the PTP1B activity with IC50 values of 8.7 +/- 0.9 and 30.6 +/- 2.1 microM, respectively. Kinetic studies suggest that both 1 and 2 are non-competitive inhibitors of PTP1B. However, compound 3 substituted with a hydroxyl group at C-17 in kaurane-type showed no inhibitory effects towards PTP1B.     

Chemical Constituents of Siegesbeckia orientalis L.

The aerial parts of Siegesbeckia have been used as the traditional Chinese medicine in the treatment of rheumatic arthritis, hypertension, malaria, neurasthenia, and snakebite. In order to find new and bioactive compounds, the chemical constituents of the aerial parts of S. orientalis L. were investigated and two new compounds, namely β-D-glucopyranosyl-ent-2-oxo-15,16-dihydroxy-pimar-8（14）-en-19-oic-late （compound 1 ） and [1 （10） E,4Z]-8β-angeloyloxy-9α-methoxy-6α, 15-dihydroxy-14-oxogermacra-1 （10）,4,11 （13）-trien-12-oic acid 12,6-1actone （compound 2）, as well as five known ent-pimarane diterpenes （compounds 3-7） were isolated. The structures of the two new compounds were identified by their physicochemical properties and spectral analysis, particularly oneand two-dimensional nuclear magnetic resonance spectral methods.     

PTP1B inhibitory activity of kaurane diterpenes isolated from Siegesbeckia glabrescens

Protein tyrosine phosphatase 1B (PTP1B) is considered as a therapeutic target for the treatment of diabetes and obesity. In our preliminary screening study, a MeOH extract of the aerial part of Siegesbeckia glabrescens was found to inhibit PTP1B activity at 30 μg/mL. Bioassay‐guided fractionation led to the isolation of two active diterpenes, ent-16βH,17-isobutyryloxy-kauran-19-oic acid (1) and ent-16βH,17-acetoxy-18-isobutyryloxy-kauran-19-oic acid (2), along with ent-16βH,17-hydroxy-kauran-19-oic acid (3). Compounds 1 and 2 inhibited the PTP1B activity with IC₅₀ values of 8.7 ± 0.9 and 30.6 ± 2.1 μM, respectively. Kinetic studies suggest that both 1 and 2 are non-competitive inhibitors of PTP1B. However, compound 3 substituted with a hydroxyl group at C-17 in kaurane-type showed no inhibitory effects towards PTP1B.     

Non-specific immune response and disease resistance induced by Siegesbeckia glabrescens against Vibrio parahaemolyticus in Epinephelus bruneus

The immunomodulatory effect of Siegesbeckia glabrescens extract-supplementation diets on innate immune response and disease resistance of kelp grouper, Epinephelus bruneus against Vibrio parahaemolyticus at weeks 1, 2, and 4 is reported. The serum lysozyme activity was significantly enhanced with any enriched diet from weeks 1-4 when compared to control diet (0%). The alternative complement haemolytic activities significantly were enhanced with all enriched diets on weeks 2 and 4 whereas the cellular reactive oxygen species (ROS) was significantly enhanced only with 1.0% and 2.0% diets. The reactive nitrogen intermediate (RNI) value was significantly enhanced with any enriched diet on weeks 2 and 4, but on first week it did not differ from control. The myeloperoxidase (MPO) production significantly increased with 1.0% and 2.0% diets from second week onwards; with other enriched diets the increase manifested on fourth week; but during first week it did not vary from that of the control with any enriched diet. The protection in terms of cumulative mortality was the least being 25% and 20% when fed with 1.0% and 2.0% diets. The present results indicate that feeding kelp grouper with S. glabrescens extract enriched diet at 1.0% and 2.0% levels significantly enhance the immunological parameters, increase the disease resistance and minimize the cumulative mortality in E. bruneus against V. parahaemolyticus.     

Diterpenoids from Neoboutonia glabrescens (Euphorbiaceae)

Glabrescin, a daphnane diterpenoid, neoboutonin, a degraded diterpenoid with a novel skeleton, and neoglabrescins A and B, two rhamnofolane derivatives, have been isolated from the stem bark of Neoboutonia glabrescens Prain (Euphorbiaceae), together with the known tigliane derivative, baliospermin, and the known daphnane, montanin. Other constituents include squalene, 3-acetylaleuritolic acid, oleanolic acid and sitosterol, and the phenolic compounds 9-methoxy-1,7-dimethylphenanthrene and 2,3,8-tri-O-methylellagic acid. The structures were assigned on the basis of spectral studies and comparison with published literature data. The structures of neoglabrescins A and B were derived for their acetylated derivatives and, in the case of neoglabrescin A, confirmed by X-ray crystallographic analysis.     

Nitric oxide inhibitory constituents from Siegesbeckia pubescens

Two new sesquiterpenoids (1 and 2) and a new ent-pimarane type diterpenoid (3), together with eighteen known compounds (4–21), were isolated from the whole plants of Siegesbeckia pubescens. The structures of the new compounds were determined on the basis of 1D-, 2D NMR and HRESIMS data. All compounds were evaluated for their inhibitory effects on LPS-induced nitric oxide production in RAW 264.7 macrophages. Of these, highly oxygenated germacrane type sesquiterpenoids (1–2 and 13–14) showed significant inhibitory effects with IC₅₀ values ranging from 3.9 to 16.8 μM.     

Brassica glabrescens,eine neue Art aus Nordost-Italien

Abstract

The new endemic species Brassica glabrescens Poldini is described from the Friuli, Italy. It is a perennial caespitose hemicryptophyte belonging to sect. Brassicaria (Godr.) Coss. (= Oreobrassica Prantl), which shows close affinity to the very complex species B. repanda (Willd.) DC. and particularly to its subsp. saxatilis (DC.) Heywood from South France.     

ent-Pimarane Diterpenes from the Aerial Parts of Siegesbeckia pubescens

Five new ent-pimarane diterpenes ( 1 – 5 ) and five known analogs ( 6 – 10 ) were isolated from the aerial parts of Siegesbeckia pubescens. Their structures, including absolute configurations, were determined by comprehensive spectroscopic methods especially 1D and 2D NMR and quantum chemical electronic circular dichroism calculations. All the isolated compounds were evaluated for their cytotoxicity against human BT549, A549 and H157 cancer cell lines. Among them, compounds 1 and 2 showed mild cytotoxicity against lung cancer cell lines H157 with IC₅₀ values of 16.35±2.59 and 18.86±4.83 μM, respectively.