Promising activity of Anthemis austriaca Jacq. on the endometriosis rat model and isolation of its active constituents

Anthemis austriaca Jacq. flowers are traditionally used to alleviate abdominal pain, hemorrhoids, ovary diseases and pneumonia. This study aimed to investigate the effects of A. austriaca flowers, which are frequently used in gynecological disorders, on the rat endometriosis model. The rat endometriosis model was used to evaluate the potential activity of the plant in endometriosis. The dried plant material was extracted with n-hexane, ethyl acetate (EtOAc), and methanol (MeOH), successively. The obtained extracts from A. austriaca flowers were applied to the rats. The adhesion scores, endometrial foci areas, and cytokine levels of the peritoneal fluids were measured on surgical induction of endometriosis in rats. The adhesion scores, endometriotic volume, and cytokine levels of the peritoneal fluids were reduced in the EtOAc, MeOH, and buserelin acetate-treated (reference) groups. The MeOH extract reduced the adhesion scores and endometrial foci areas from 3.1 to 1.1 (p < 0.01) and from 86.4 to 40.5 (p < 0.01), respectively and also the MeOH extract reduced tumor necrosis factor (TNF)-α, vascular endothelial growth factor (VEGF), and interleukin (IL)-6 levels of the peritoneal fluids from 13.7 to 3.8 (p < 0.01), from 28.4 to 16.3 (p < 0.05) and from 50.2 to 24.3 (p < 0.01), respectively. Therefore, isolation studies were conducted on the EtOAc and MeOH extracts. After the MeOH extract was fractionated using RP-18 column, the obtained subfractions were evaluated again on the endometriosis rat model. Subfractions A and C of the MeOH extract displayed statistically significant activity on the endometriosis rat model. Phytochemical investigation resulted in the isolation of 4-β-D-glucopyranosyloxy-6-methyl-2H-pyran-2-one (1) from Fr. A and quercetin (2), apigenin-7-O-(3″-O-acetyl)-β-D-glucopyranoside (3), apigenin-7-O-(6″-O-acetyl)-β-D-glucopyranoside (4), apigenin-7-O-β-D-glucopyranoside (5), quercetin-7-O-β-D-glucopyranoside (6) from Fr. C. Moreover, β-sitosterol-3-O-β-D-glucopyranoside (7) was isolated from the EtOAc extract. As a conclusion, the MeOH extract obtained from A. austriaca flowers contributed to the regression of endometriosis. In addition, flavonoids and sterols of the plant were detected as the possible compounds responsible for the activity.     

Cytotoxic and potential anticancer constituents from the stems of Schisandra pubescens

Abstract

Context: The diethyl ether extract of the stems of Schisandra pubescens Hemsl. et Wils. (Schisandraceae) was found to exhibit cytotoxic activity in vitro. However, investigations of the bioactive constituents of this plant have been very limited.

Objective: Elucidation of the cytotoxic constituents of S. pubescens was performed.

Methods: Repeated silica gel column chromatography and preparative TLC were used for the chemical investigation of the diethyl ether extract of S. pubescens stems. All isolates were evaluated for their in vitro cytotoxicity against A549, PC-3, KB and KBvin human cancer cell lines.

Results: Nine known compounds were obtained, including four lignans, epischisandrone (1), tigloylgomisin P (2), cagayanone (3) and (?)-gomisin L₂ (4), together with five triterpenoids, micranoic acid B (5), lancifodilactone H (6), coccinic acid (7), schisanlactone B (8) and anwuweizonic acid (9). Compounds 2–6 and 8 showed moderate to marginal cytotoxicity, with GI₅₀ values of 11.83–35.65?μM.

Conclusion: The isolation of 1–9 from S. pubescens and the cytotoxicities of 3–6 are first reported. Compounds 2–6 and 8 could be the active principles responsible for the anticancer effects of S. pubescens.     

阿魏属植物化学成分研究进展

目的对阿魏属植物近10年来研究所得到的化学成分进行综述。方法通过查阅国内外相关文献,总结珍稀中药阿魏及阿魏来源植物的化学成分的研究进展,按照化合物的结构类型对其化学成分进行分类。结果阿魏属植物含有多种化学成分,主要含有香豆素类、倍半萜香豆素类、倍半萜类、芳香族类和含硫化合物等。结论为进一步研究、开发和利用阿魏属植物资源提供参考。     

款冬花的化学成分研究

目的：研究款冬花的化学成分。方法利用硅胶柱、高效液相等色谱技术对款冬花甲醇提取物进行分离纯化,通过波谱数据鉴定结构。结果从款冬花中共分得5个化合物,分别鉴定为：款冬酮（1）、14- acetoxy -7β-（4- methylsenecioyloxyl）-1α-（2＇- methylbutyryloxy）- notonipetranone（2）、6- acetyl -2,2- dimethylchroman -4- one（3）、3,4- epoxy -1,8- diangeloyloxy bisabola -7（14）-10- dien -2- one（4）以及橐吾香附酮醇（5）。结论化合物3～5为首次从该植物中分离得到。     

宽叶金粟兰化学成分的研究

目的研究宽叶金粟兰根的化学成分。方法利用多种柱色谱方法进行分离纯化，根据光谱数据和理化性质进行结构鉴定。结果从宽叶金粟兰根中分离鉴定了8个化合物，分别是：curcolonol (I)，zedoarofuran (II)，shizukanolide E (III)，异秦皮啶-7-O-葡糖苷(IV)，伞形花内酯苷(V)，异秦皮啶-3-β-D-芹菜糖(1→3)-β-D-葡糖苷(VI)，β-谷甾醇(VII)，胡萝卜苷(VIII)。结论异秦皮啶-7-O-β-D-芹菜糖(1→3)-β-D-葡糖苷(VI)为新化合物，命名为宽叶金粟兰苷，化合物I和II为首次从该属植物中分离得到。     

黄槿化学成分和药理活性研究进展

黄槿为《全国中草药汇编》收载的两种半红树植物之一,具有清热解毒的功效,在海南黎族聚集地区作为药物使用.有关黄槿的化学成分研究起始于20世纪60年代,至今从中分离得到了大量的三萜、黄酮、倍半萜和酰胺类化合物,其中木栓烷型三萜和高度氧化的倍半萜类成分是该药用植物的特征性成分.药理研究主要集中在抗炎、抗肿瘤和抗氧化活性.现就...     

丁座草的化学成分研究

目的 研究丁座草块茎的化学成分。方法用色谱方法分离丁座草块茎的乙醇提取物。结果 共分离得到8个化合物，根据理化性质及各种光谱技术进行结构鉴定，分别为α-香树素（Ⅰ）、3β-乙酰氧基-熊果-28，13-内酯（11）、3β-乙酰氧基-熊果-11（12）-烯-28，13-内酯（Ⅲ）、3β-乙酰熊果酸（Ⅳ）、3β-乙酰齐墩果酸（V）、β-谷甾醇（Ⅵ）、熊果酸（Ⅶ）、（＋）-松脂素单葡萄糖苷（Ⅷ）。结论 化合物Ⅰ～Ⅲ为首次从该属植物中分离得到。     

海刀豆化学成分的分离鉴定和活性评价Δ

目的 对采自福建漳州沿海红树林伴生植物海刀豆进行化学成分和生物活性研究。方法 采用硅胶柱层析、Sephadex LH-20凝胶层析、薄层层析、MCI微孔树脂层析以及HPLC高效液相色谱等方法对海刀豆的乙酸乙酯提取物进行分离纯化,通过波谱数据分析及文献比较对化合物进行结构鉴定,并用MTT法初步评价其细胞毒活性。结果 从该植物的乙酸乙酯提取物中分离到10个化合物,分别鉴定为3,7-二羟基-6-甲氧基黄酮(1)、毛蕊异黄酮(2)、芒柄花素(3)、乌苏酸(4)、木栓酮(5)、羽扇豆醇(6)、β-谷甾醇(7)、β-胡萝卜苷(8)、二十六烷酸(9)和二十四烷酸(10)。结论 化合物1-2、4-10均为首次从海刀豆中分离得到。     

Cytotoxic constituents of propolis inducing anticancer effects: a review

Objectives Propolis is a honeybee product used extensively in traditional medicine for its antioxidant, anti‐inflammatory, immunomodulatory and anticancer effects. Propolis exhibits a broad spectrum of biological activities because it is a complex mixture of natural substances. In this review, the antitumour effects of propolis extracts and its constituents (e.g. flavonoids, terpenes and caffeic acid phenethyl ester) are discussed. Key findings The effect of propolis on experimental carcinogenesis is discussed, as well as its possible mechanisms of action against tumours, involving apoptosis, cell cycle arrest and interference on metabolic pathways. Propolis seems to be efficient against different tumour cells both in vitro and in vivo, which suggests its potential in the development of new anticancer drugs. Summary Propolis extracts may be important economically and would allow a relatively inexpensive cancer treatment. Preclinical investigations are needed to further elucidate the benefits of propolis and its antitumour properties.     

藤苦参的化学成分与药理作用研究进展

藤苦参Streptocaulon griffithii是我国傣族传统用药,在民间应用广泛,极具开发前景。藤苦参含有多种生物活性成分,包括强心甾、三萜、有机酸、木脂素、苯环衍生物等。药理研究表明,藤苦参及其有效成分具有显著的抗肿瘤、促进创伤愈合、抗癫痫等药理作用。对藤苦参化学成分及药理作用进行综述,旨在为进一步开发和临床应用提供参考。     

Cytotoxic constituents ofPsoralea corylifolia

A coumestan derivative, psoralidin (1) was found to be a cytotoxic principle of the seeds of Psoralea corylifolia L. (Leguminosae) with the IC50 values of 0.3 and 0.4 microg/ml against the HT-29 (colon) and MCF-7 (breast) human cancer cell lines, respectively. A coumarin, angelicin (2) was also isolated as a marginally cytotoxic agent along with an inactive compound, psoralen (3) from the plant. The isolates 1-3 were not active against the A541 (lung) and HepG2 (liver hepatoma) cancer cell lines.     

Cytotoxic constituents fromSolanum lyratum

Activity-guided fractionation of the ethanol extract of the whole plant from Solanum lyratum resulted in the isolation of a new pregnane derivative glycoside, 16-dehydropregnenolone 3-O-alpha-L-rhamnopyranosyl-(1 --> 2)-beta-D-glucopyranosid uronic acid (2), as well as other six known compounds: 16-dehydropregnenolone (1), allopregenolone (3), protocatechuic acid (4), vanillic acid (5), caffeic acid (6), and scopoletin (7). The structures of the isolated compounds were elucidated on the basis of their spectral data and chemical evidences. Compounds 1, 3, 4 were isolated for the first time from this plant. Cytotoxic activities of the isolated compounds were evaluated. Compound 1 exhibited significant cytotoxic activity against A375-S2, HeLa, SGC-7901, and Bel-7402 with IC50 values of 13.1 +/- 0.9, 21.5 +/- 1.0, 40.2 +/- 0.7, and 49.8 +/- 1.2 microg/mL, respectively.     

软枣猕猴桃的化学成分和药理活性研究进展

软枣猕猴桃为猕猴桃科猕猴桃属多年生落叶藤本植物,在我国东北三省的分布最为广泛.其果实、根、茎叶均可入药,具有抗肿瘤、抗辐射、提高免疫功能等药理活性.研究表明,软枣猕猴桃全株含有挥发油、三萜、黄酮、多糖等化学成分.综述了近年来从软枣猕猴桃果实、根、茎叶中分离到的挥发油类、三萜类、黄酮类等化学成分,及其肿瘤抑制、抗辐射、提...     

Free radical scavenging activity and chemical constituents of Urvillea ulmaceae

The methanol extract of Urvillea ulmaceae Kunth (Sapindaceae) aerial parts and the hexane, ethyl acetate, and hydromethanol fractions were evaluated for their free radical scavenging activity with the DPPH assay. Among all the tested fractions, the ethyl acetate fraction was the most active, exhibiting an IC₅₀ of 16.33?μg/mL, comparable to that of the commercial antioxidant BHT. Fractionation of the ethyl acetate fraction through chromatographic methods afforded trans-N-methyl-5-hydroxypipecolic acid, epicatechin, and proanthocyanidin A2 as the main constituents. Epicatechin and proanthocyanidin A2 showed potent DPPH radical scavenging activity, with IC₅₀ values of 18.34 and 11.45?μg/mL, respectively. A new compound, trans-N-methyl-5-hydroxypipecolic acid, did not show any antioxidant effect (IC₅₀?>?500?μg/mL).     

白狼毒化学成分和生物活性研究进展

白狼毒作为有毒中药,具有抗结核、抗癌、抗白血病、细胞毒、免疫调节等活性.本文综述了近10年来狼毒大戟和月腺大戟中80多个成分的化学研究,为白狼毒临床应用的安全有效和进一步深入研究提供参考.     

Cytotoxic ring A-seco triterpenoids from the stem bark of Dysoxylum lukii

Abstract

A chemical investigation of the 70% ethanol extract from the stem bark of Dysoxylum lukii afforded three new ring A-seco triterpenoids, dysoxylukiines A–C (1–3). Their structures were elucidated on the basis of extensive 1D and 2D NMR (COSY, HMQC, HMBC, and NOESY) analyses. The isolated compounds were evaluated in vitro for cytotoxic properties. Consequently, compound 3 exhibited modest cytotoxic activities against four osteosarcoma cell lines (SOSP-9607, MG-63, Saos-2, and M663) with IC₅₀ values less than 10 μM.     

丁座草的化学成分研究

目的研究丁座草Boschniakia himalaicaHook.f.et Thoms.块茎的化学成分。方法采用柱色谱分离,通过理化性质和光谱分析确定化合物的结构。结果与结论从丁座草块茎的乙醇提取物中,共分离得到7个化合物,鉴定了5个化合物,分别为3β-乙酰熊果酸(3β-acetoxyurs-12-en-28-oic acid,Ⅰ)、3β-乙酰齐墩果酸(3β-acetyloleanolic acid,Ⅱ)、β-谷甾醇(β-sitosterol,Ⅲ)、熊果酸(ursolic acid,Ⅳ)、( )-松脂素单葡萄糖苷[( )-pinoresinol monoglucoside,Ⅴ]。化合物Ⅰ为首次从该属植物中分离得到,化合物Ⅱ和Ⅲ为首次从该植物中分离得到。     

Cytotoxic constituents of the octocoralDendronephthya gigantea

A known monoalkyl glycerol ether, (+/-)-1-nonadecyloxy-2,3-propanediol (1) was isolated from the ethyl acetate extract of a soft coral Dendronephthya gigantea as a weakly cytotoxic constituent against four human cancer cell lines, A549, HT-29, HT-1080, and SNU-638. In addition, a known ceramide, (2S,3R,4E,8E)-N-hexadecanoyl-2-amino-4,8-octadecadiene-1,3-diol (2), was also isolated as an inactive constituent. This is the first report on the isolation of the compounds 1 and 2 from the octocoral, Dendronephthya species.     

Sesquiterpenoids and other constituents from the flower buds of Tussilago farfara

One new norsesquiterpenoid, namely tussfarfarin A (1), and four new artifacts resulting from extraction procedure, namely tussfarfarin B (2), 6-(1-ethoxyethyl)-2,2-dimethylchroman-4-ol (3), 5-ethoxymethyl-1H-pyrrole-2-carbaldehyde (4), and 3β-hydroxy-7α-ethoxy-24β-ethylcholest-5-ene (5), along with 18 known compounds, were isolated from the flower buds of Tussilago farfara. Their structures were elucidated by extensive spectroscopic analysis.