鬼臼类植物内生真菌的分离及其抗癌活性研究

通过对三属四种鬼臼类植物地下茎内生真菌的分离,发现鬼臼类植物地下茎中内生真菌的物种类型极其丰富,主要分布在地下茎的表皮层和维管组织中,来源于外界环境.通过对包括鬼臼类植物在内的7种植物内生真菌的抗癌活性测定,发现内生真菌的抗癌活性与宿主有密切有关系,鬼臼类植物地下茎内生真菌含有较高比例的抗癌活性菌株.宿主种类、地理位置都会影响内生真菌的分布,进而影响活性菌株出现的频率.通过对所有鬼臼类植物地下茎内生真菌次生代谢产物的深入分析,并没有发现产生鬼臼毒素的内生真菌,鬼臼类植物地下茎内生真菌的抗癌活性成分是独立产生的.     

Peptaibols from two unidentified fungi of the order Hypocreales with cytotoxic,antibiotic, and anthelmintic activities

As part of an ongoing investigation of filamentous fungi for anticancer leads, an active culture was identified from the Mycosynthetix library (MSX 70741, of the order Hypocreales, Ascomycota). The fungal extract exhibited cytotoxic activity against the H460 (human nonsmall cell lung carcinoma) cell line, and bioactivity‐directed fractionation yielded peptaibols 1–12 and harzianums A (13) and B (14). Structure elucidation of 1–12 was facilitated by high‐resolution MS/MS using higher‐energy collisional dissociation and by high field NMR (950 MHz). The absolute configuration was determined by Marfey's analysis of the individual amino acids; the time required for such analysis was decreased via the development of a 10‐min ultra performance liquid chromatography method. The isolated peptaibols (1–12), along with three other peptaibols isolated and elucidated from a different fungus (MSX 57715) of the same order (15–17), were examined for activity in a suite of biological assays, including those for cytotoxic, antibacterial, and anthelmintic activities. Copyright © 2012 European Peptide Society and John Wiley & Sons, Ltd.     

Synthesis and in vitro antitumor activity of novel alkenyl derivatives of pyridoxine,bioisosteric analogs of feruloyl methane

Two series of novel pyridoxine-based azaheterocyclic analogs of feruloyl methane (Dehydrozingerone, DZG) were synthesized, and their biological activity against a panel of tumor and normal cell lines was evaluated in vitro. The most active compounds possessed expressed cytotoxic activity, which was comparable to cytotoxic activity of doxorubicin and significantly higher than that of DZG, and a remarkable selectivity for the studied cancer cell lines as compared to the normal cells. The leading compound and DZG initiated arrest of the cell cycle in the G2/M phase, preventing normal division and further transition of daughter cells to the G0/G1 phase. Similar to DZG, but with higher efficiency, the leading compound was able to inhibit migration activity and, therefore, invasiveness of tumor cells. It also increased concentration of reactive oxygen species in tumor cells, induced depolarization of mitochondrial membranes and initiated apoptosis accompanied by disruption of integrity of cytoplasmic cell membranes. By contrast to DZG, the leading compound did not possess antioxidant properties. The obtained data make the described chemotype a promising starting point for the development of new anticancer agents.     

Zerumbone induced apoptosis in liver cancer cells via modulation of Bax/Bcl-2 ratio

Background  

Zerumbone is a cytotoxic component isolated from Zingiber zerumbet Smith, a herbal plant which is also known as lempoyang. This new anticancer bioactive compound from Z. zerumbet was investigated for its activity and mechanism in human liver cancer cell lines.     

Maximization of minority classes in core collections designed for association studies

Core collections are nowadays widely employed in diverse studies on plant genetics. The more extensively used method to build core collections (maximization strategy) is based on the selection, from a global collection, of those accessions which maximize the number of different alleles and phenotypic classes (classes’ richness). However, different core collections should be created for different types of studies, and though several years ago most of core collections were developed to make the characterization and use of germplasm collections easier with a smaller sample size, for either conservation or breeding purposes, today, they are widely employed for association studies that are broadly applied in plant genetic improvement. Following the M strategy, some alleles or phenotypic classes often appear in a very low frequency, which may reduce the power of the analysis, avoiding the detection of real associations (false negatives). In this work, we propose and evaluate a new way to build core collections using the maximization strategy in several sequential steps, to maximize the frequency of minority classes, thus increasing the statistical power of the association study.     

上海辰山植物园植物收集的现状和展望

上海辰山植物园于2005年开始筹建,与此同时启动了的植物收集工作。本文就辰山植物园基本情况、植物收集中长远规划、进展及技术策略进行了论述。活植物收集和标本收集是辰山植物园植物收集工作的两个方面。活植物收集包括以华东植物区系植物为主的物种收集和以上海适生的观赏植物为主的园艺品种收集,如鸢尾属、绣球属、荚蒾属、锦带属和绣线菊属的观赏园艺品种。截止到2010年,辰山植物园共收集了9000种和园艺品种。其中,华东植物区系物种有1700种,来自世界范围专业苗圃的园艺品种有2800个,另有4500种和品种是种植于温室的热带和亚热带植物。目前共收集了近10000份标本,多数为研究和活植物收集的凭证标本,全部存放于上海辰山植物园标本馆（CSH）。     

上海辰山植物园植物收集的现状和展望

上海辰山植物园于2005年开始筹建,与此同时启动了的植物收集工作。本文就辰山植物园基本情况、植物收集中长远规划、进展及技术策略进行了论述。活植物收集和标本收集是辰山植物园植物收集工作的两个方面。活植物收集包括以华东植物区系植物为主的物种收集和以上海适生的观赏植物为主的园艺品种收集,如鸢尾属、绣球属、荚蓬属、锦带属和绣线菊属的舭赏园艺品种。截止到2010年,辰山植物园共收集了9000种和园艺品种。其中,华东植物区系物种有1700种,来自世界范围专业苗圃的园艺品种有2800个,另有4500种和品种是种植于温室的热带和亚热带植物。目前共收集了近10000份标本,多数为研究和活植物收集的凭证标本,全部存放于上海辰山植物园标本馆（CSH）。     

美国在华采集竹类植物标本的历史(1840-2010年)

植物标本采集是植物学研究的重要内容, 与植物引种密切相关。自19世纪以来, 美国植物采集者在全球尤其是中国进行了广泛的植物采集。在众多的植物类群中, 中国的竹类植物引起了美国采集者的极大关注, 并开展了大量调查研究和标本采集工作。研究美国植物采集者在中国采集竹类植物标本的历史, 对了解竹类植物从中国引种到美国的历史具有重要意义。本文基于国内外有关美国在华采集的竹类植物标本数据, 对其学名、采集地、采集人以及采集时间进行整理校对, 分析了美国采集者在华采集竹类植物标本的历史。结果表明: 1840-2010年, 美国在华共采集竹类植物标本960号2,238份, 隶属于25属120种(含变种和变型), 分别占中国竹类属和种数的73.5%和22.5%; 有45位(支)采集者(采集队), 在这些采集者中莫古礼最为重要; 采集地涉及20个省级行政区; 采集时间前后跨度约170年, 主要集中在20世纪上半叶。     

Isoarnottinin 4'-glucoside, a glycosylated coumarin from Prangos uloptera, with biological activity

Coumarins are a well-known group of natural products distributed in the plant kingdom especially in the family Apiaceae with various biological activities. Isoarnottinin 4'-glucoside is a simple glycosylated coumarin found previously in a few genera of Apiaceae, and its biological activities have not been previously described in details. In the present paper, the compound was isolated from Prangos uloptera (Apiaceae) leaves using HPLC techniques. Antimicrobial, phytotoxic and cytotoxic activities of the compound were evaluated by disk diffusion, lettuce assay and MTT method. Our results indicated that the compound has high antibacterial effect against Erwinia carotovora, a common plant pathogen with MIC value of 100 microg/mL. The compound also exhibited significant phytotoxic activity against lettuce and modest cytotoxic activity against HeLa cell line with IC50 of 0 .84 mg/mL. It could be concluded that isoamottinin 4'-glucoside may play phytoalexin or allelopathic role for plant and may be a candidate for an antibacterial agent or a bioherbicide.     

Isoarnottinin 4′-glucoside, a glycosylated coumarin from Prangos uloptera, with biological activity

Coumarins are a well-known group of natural products distributed in the plant kingdom especially in the family Apiaceae with various biological activities. Isoarnottinin 4′-glucoside is a simple glycosylated coumarin found previously in a few genera of Apiaceae, and its biological activities have not been previously described in details. In the present paper, the compound was isolated from Prangos uloptera (Apiaceae) leaves using HPLC techniques. Antimicrobial, phytotoxic and cytotoxic activities of the compound were evaluated by disk diffusion, lettuce assay and MTT method. Our results indicated that the compound has high antibacterial effect against Erwinia carotovora, a common plant pathogen with MIC value of 100 μg/ml. The compound also exhibited significant phytotoxic activity against lettuce and modest cytotoxic activity against HeLa cell line with IC₅₀ of 0.84 mg/ml. It could be concluded that isoarnottinin 4′-glucoside may play phytoalexin or allelopathic role for plant and may be a candidate for an antibacterial agent or a bioherbicide.     

Synthesis,Biological Activity Evaluation and Molecular Docking of Imidazole Derivatives Possessing Hydrazone Moiety

In an attempt to identify potential active anticancer agents with low cytotoxic properties and CA inhibitors, a new series of hybrid compounds incorporating imidazole ring and hydrazone moiety as part of their structure were synthesized by aza-Michael addition reaction followed by intramolecular cyclization. The structure of synthesized compounds was elucidated using various spectral techniques. Synthesized compounds were evaluated for their in vitro anticancer (prostate cell lines; PC3) and CA inhibitory (hCA I and hCA II) activity. Among them, some compound displayed remarkable anticancer activity and CA inhibitory activity with K_i values in range of 17.53±7.19–150.50±68.87 nM against cytosolic hCA I isoform associated with epilepsy, and 28.82±14.26–153.27±55.80 nM against dominant cytosolic hCA II isoforms associated with glaucoma. Furthermore, the theoretical parameters of the bioactive molecules were calculated to establish their drug-likeness qualities. The proteins used for the calculations are prostate cancer protein (PDB ID: 3RUK and 6XXP). ADME/T analysis was carried out to examine the drug properties of the studied molecules.     

Two new flavonol glycosides as DNA topoisomerase I poisons

Flavonoids are secondary plant metabolites whose anticancer properties are actually being studied from an epidemiological and pharmacological point of view. They are believed to be implicated in the lower risk of some forms of cancer observed in Asian countries, due to their capacity to control cell proliferation, to act on certain regulatory enzymes as protein kinases or topoisomerases. Based on these precedents, three flavonols isolated from a cytotoxic butanol extract from Retama sphaerocarpa Boissier have been assessed to study their topoisomerase I and II activity. Two new rhamnazin glycosides were found to have the ability to stabilize the cleavage complex human DNA topoisomerase I at concentrations in the 100-250 microM range, acting as topoisomersase I poisons.     

Collections of pathogenic viruses for addressing general biologic problems

Development of the theory and practice of building and maintenance of collections of reference cultures of pathogens strains is actual in conservation of a biodiversity, and as for maintenance with standardized superfine starting materials fundamental and applied researches in fields of microbiology, an immunology, biotechnology, ecology, and biosafety. Various approaches to taxonomy of viruses, and also definition of concepts "strain" and "species" are discussed in the article. Formulations of the concepts most conforming to museum collections activity are given. The methodology of collecting pathogens, including fifteen-year experience of maintenance of the National collection of hemorrhagic fever viruses belonging to group I of pathogenicity, is summarized. The systemic approach is suggested as a basis of methodology of collecting. Selection of pathogen species and their specific strains according to purpose and on the basis of complex study of their biological and other characteristics, as well as standardization and unification of methods of pathogens maintenance and preparing on their basis working materials, diagnostic kits and other preparations, create a real basis of optimization, unification and continuity of the subsequent applied researches. The offer about formation at the state level of a new independent direction--pathogens collecting with establishment of federal centers based on pathogens' classes has been made.     

Constituents and biological activities from Muehlenbeckia hastulata

Muehlenbeckia hastulata (J. E.Sm.) Johnst. used mainly for its abortive properties was found active for oxytoxic and analgesic activities in a biological activity screening (oxytoxic, analgesic, antimicrobial, cytotoxic and xanthine oxidase assay). Epicatechin, emodin-8-glycoside and rutin were isolated from the aerial part and the root of the plant.     

Semisynthesis of some novel thiourea and carbamimidothioic acid derivatives using natural alkaloid L-norephedrine and their anticancer activity

A novel series of thiourea and carbamimidothioic acid derivatives was synthesized using natural alkaloid L-norephedrine as a starting material. Structures of the newly synthesized compounds were confirmed by analytical and spectral data. The synthesized compounds were evaluated in vitro for anticancer activity against the human breast (MCF-7), human liver (HEPG2), and human colon (HCT116) cancer cell lines. Best activity of the synthesized compounds was expressed against HEPG2, however, none of the compounds exceeded the IC₅₀ of doxorubicin. The corresponding N-(1-(2-chloroacetoxy)-1-phenylpropan-2-yl)-N′-p-tolylcarbamimidothioic acid was the most potent compound and exhibited higher cytotoxic activity against the human colon cancer cell line (HCT116) when compared with the reference drug doxorubicin. Also, this compound was the most active against the MCF-7 cell line but less active than the positive control.     

One pot synthesis and anticancer activity of dimeric phloroglucinols

A series of dimeric phloroglucinol compounds were synthesized in a single step using commercially available phloroglucinol and methanesulfonic acid. Based on the reported anticancer activity of plant derived dimeric phloroglucinols, these synthesized compounds were evaluated for their in vitro anti-proliferative activities against various cancer cell lines. Several compounds demonstrated in vitro cytotoxic effects across a wide array of tumor cell types. The compound 29 with pyridin-3-yl group on linker methylene and two diisovaleryl phloroglucinol moieties was found to be the most active in all the five cancer cell lines having a low IC(50) of 5.5 μM in colon cancer cell lines (HCT116).     

Synthesis, biological evaluation and molecular docking of aryl hydrazines and hydrazides for anticancer activity

Aryl hydrazine and hydrazide analogues were synthesized based on p-tolyl hydrazine, isolated as a breakdown product of a secondary metabolite from the mushroom, Agaricus bisporus, and tested to be highly active molecule than 5-fluorouracil in in vitro anticancer studies. The synthesized analogues were tested for anticancer activity using NCI protocol. Anolgues 12 and 15 emerged as molecules with significant in vitro anticancer activity. Molecular docking study revealed the binding orientations of aryl hydrazines and hydrazides analogues in the active sites of thymidylate synthase.     

海南文昌清澜港红树林真菌抗B16肿瘤细胞活性菌株的筛选

从海南文昌清澜港红树林采集78份植物组织和土壤样品。对样品进行真菌分离, 共分离得到真菌608株, 采用目测法对其体外抗肿瘤细胞活性进行检测, 发现81株红树林真菌对小鼠黑色素瘤B16细胞有不同程度的抑制作用, 占总分离菌株的13.32%。结果表明, 从红树植物杯萼海桑中分离得到真菌菌株的数量最多, 而从红树植物银叶树分离得到的抗肿瘤细胞活性菌株数量最多。     

海南文昌清澜港红树林真菌抗B16肿瘤细胞活性菌株的筛选

从海南文昌清澜港红树林采集78份植物组织和土壤样品。对样品进行真菌分离, 共分离得到真菌608株, 采用目测法对其体外抗肿瘤细胞活性进行检测, 发现81株红树林真菌对小鼠黑色素瘤B16细胞有不同程度的抑制作用, 占总分离菌株的13.32%。结果表明, 从红树植物杯萼海桑中分离得到真菌菌株的数量最多, 而从红树植物银叶树分离得到的抗肿瘤细胞活性菌株数量最多。     

Direct semi-synthesis of the anticancer lead-drug protoapigenone from apigenin, and synthesis of further new cytotoxic protoflavone derivatives

Protoapigenone, a natural flavonoid possessing an unusual p-quinol moiety on its B-ring, is a novel prospective anticancer agent with low toxicity that is currently in development. The first economical, one-step synthesis of protoapigenone from apigenin is described on up to gram scale. 13 new 1'-O-alkylflavone analogs were also synthesized, either from apigenin or β-naphthoflavone. The in vitro cytotoxic activity of each compound was tested on six human cancer cell lines (HepG2, Hep3B, Ca9-22, A549, MCF-7 and MDA-MB-231). In the case of 1'-O-alkyl-protoapigenone derivatives, structure-activity relationships were found depending on the side-chain, and protoapigenone 1'-O-butyl ether was found to exert significantly stronger activity against three of the cell lines (Hep3B, MCF-7 and MDA-MB-231) than its non-substituted analog, protoapigenone itself. In contrast to this, all β-naphthoflavone derivatives bearing the same pharmacophore on their B-ring showed decreased cytotoxic activities when substituted with an O-alkyl side-chain at position 1', comparing to that of the non-substituted compound.