乳菇属蘑菇中N-苯甲酰基苯基异丝氨酸倍半萜酯的体外抗病毒活性

乳菇属(Lactarius)蘑菇中的某些倍半萜烯和倍半萜醇有昆虫拒食、细胞毒、抗微生物等多种活性,某些倍半萜烯及其化学合成的衍生物还显示抗病毒活性,并增强某些药物如紫杉醇的疗效。因此作者用乳菇属蘑菇中倍半萜醇类酯化紫杉醇的支链 N-苯甲酰基苯基异丝氨酸,合成了16个化合物,并研究     

海绵共附生真菌Purpureocillium lilacinum的化学成分及T细胞调节活性研究

目的 对海绵Hymeniacidon sp.共附生真菌Purpureocillium lilacinum的化学成分及T细胞调节活性进行研究。方法 运用硅胶柱色谱、凝胶柱色谱及高压液相色谱等色谱技术对真菌乙酸乙酯粗提物进行分离纯化得到单体化合物,通过现代波谱（核磁共振,质谱）及光谱（旋光）的综合运用并结合文献对照对化合物结构进行鉴定,运用流式实验对化合物T细胞调节活性进行测试。结果 共分离获得5个甾体化合物,鉴定为(24R)-豆甾-4-烯-6β-醇-3-酮（1）、(22E,24R)-麦角甾-7,22-二烯-3β,5α,9α-三醇-6-酮（2）、(22E,24R)-麦角甾-7,22-二烯-3β,5α-二醇-6-酮（3）、麦角甾-5,24-二烯-3β-醇-7,23-二酮（4）及(22E,24R)-麦角甾-5,8,22-三烯-3β-醇-7-酮（5）。体外活性筛选实验中,化合物2~5在2.5 μmol/L时对刀豆蛋白A（ConA）诱导的T细胞增殖显示抑制活性,化合物5在10 μmol/L时对CD3+T细胞的增殖显示显著抑制活性,所有受试化合物对CD4+/CD8+ T细胞分化活性均无影响。结论 化合物1~4为首次从P. lilacinum中分离获得。本文是对化合物1~5 T细胞调节活性的首次报道。     

中国南海软珊瑚Sinularia dissecta的化学成分研究

目的研究中国南海软珊瑚Sinularia dissecta的化学成分。方法运用色谱方法进行化学成分的分离和纯化,运用现代波谱技术鉴定各化学成分的结构,并用MTT法和SRB法测定部分化学成分对6种肿瘤细胞株的细胞毒活性。结果与结论共分离鉴定了11个化学成分,分别为:(1S,4R,2E,7E,11E)-西松烷-2,7,11-三烯-4-醇(1)(、1S,2E,4E,7E,11E)-西松烷-2,4,7,11-四烯(2)、(1R,3S,4S,7E,11E)-3,4-环氧西松烷-7,11,15-三烯(3)、4α-甲基-麦角甾-24-烯-3β-醇(4)、26-甲基-麦角甾-5-烯-3β-醇(5)、麦角甾-5,24-二烯-3β-醇(6)、胆甾-5-烯-3β-醇(7)、鲨肝醇(8)、对羟基苯甲醛(9)、尿嘧啶(10)、胸腺嘧啶脱氧核苷(11)。化合物1对PC-3MIE8人前列腺癌细胞的IC50为2.54μg.mL-1。所有化合物都是首次从该种软珊瑚中分离得到。通过2D-NMR首次对化合物1和4进行了全归属,并论证了其立体构型。     

中药大血藤中酚类化学成分及其抗肿瘤活性

目的阐明中药大血藤中抗癌活性成分.方法以细胞周期抑制、坏死性细胞毒活性为抗癌指标,采用硅胶、Sephadex LH-20、大孔树脂HP-20等色谱方法,跟踪分离活性成分,利用理化性质及波谱方法鉴定了化学结构,用SRB法及流式细胞术评价其抗癌活性.结果与结论从大血藤茎中分离得到7个酚酸类化合物:3,5-O-二甲基-没食子酸(1)、原儿茶酸(2)、绿原酸(3)、N-(对-羟基苯乙基)阿魏酸酰胺(4)、对-羟基苯乙醇(5)、(-)-表儿茶素(6)、缩合鞣质B2(7).化合物3对人慢性髓性白血病K562细胞的半数抑制浓度(IC50)为97.2 μg/mL,化合物4在100 μg/mL浓度下对K562细胞的增殖抑制率为46.6%.流式细胞术检测表明,化合物7对小鼠乳腺癌tsFT210细胞和K562细胞均显示G2/M期抑制作用,为一新的细胞周期抑制剂.除化合物2外,其余6个化合物均为首次从该属植物中分离得到.     

中国东海冈村凹顶藻的化学成分及其生物活性研究

目的: 对采自中国东海南麂岛海域的海洋红藻冈村凹顶藻(Laurencia okamurai)进行系统的化学成分研究,并对得到的单体化合物进行抗菌活性筛选。方法：采用正相硅胶柱色谱、凝胶Sephadex LH-20以及半制备高效液相色谱HPLC等层析手段对冈村凹顶藻的甲醇提取物进行了系统的分离纯化,同时运用1H NMR、13C NMR、EIMS等光谱技术手段对得到的化合物进行结构鉴定,并利用无乳链球菌、鳗弧菌、嗜水气单胞菌、塔氏弧菌、海豚链球菌、鮰爱德华和HN016对所得单体化合物进行抗菌活性测试。结果：从冈村凹顶藻中分离得到了11个化合物,包括7个倍半萜化合物、1个甾体化合物、1个不饱和脂肪酸、一个脂类化合物和一个醛类化合物,分别是aplysin (1),debromolaurinterol(2),aplysinol (3),debromoisolaurinterol (4),3β-hydroperoxyaplysin (5),laurinterol acetate (6),Laurokomurenene A (7),cholesterol (8),棕榈油酸(9),octadec-3(E)-en-2-one(10)和(2E)-2-tridecyl-2-heptadecenal (11)。其中化合物2对无乳链球菌和鳗弧菌HLPF表现出强的特异性抑制活性,其余化合物均无明显的抗菌活性。结论：本研究首次发现化合物2对无乳链球菌和鳗弧菌显示出很好的特异性抑制活性。     

水杨柳根的化学成分

本文的目的是对水杨柳的根部进行化学成分研究， 采用硅胶柱色谱的方法分离和纯化化合物， 根据理化性质和波谱方法鉴定化合物结构。从水杨柳的根部分离得到了13个化合物， 包括1-羰基-油桐酸(1)， 油桐酸(2)， 3-乙酰氧基-油桐酸(3)， 蒲公英赛酮(4)， 蒲公英赛醇(5)， 3-乙酰氧基-12-齐墩果烯-28-酸甲酯(6)， 3-乙酰氧基-12-齐墩果烯-28-醇(7)， 熊果酸(8)， 羽扇豆醇(9)， 乙酰氧羽扇豆醇酯(10)， 臭矢菜素A(11)， 大黄酚(12)和没食子酸(13)。化合物1为新的蒲公英赛烷三萜类化合物， 化合物2～12均为首次从该植物中分离得到。并用MTT法测定了化合物1～3对AGZY 83-a和SMMC-7721细胞的抑制作用。证明化合物2对AGZY 83-a细胞有弱抑制作用(IC50 33.055 μg·mL^-1)。     

三宝木枝条抗菌活性成分的分离与鉴定

目的研究三宝木(Trigonostemon chinensis Merr.)枝条的化学成分。方法采用多种柱色谱技术进行分离纯化,通过理化性质和波谱数据分析鉴定化合物的结构,采用滤纸片琼脂扩散法测定化合物抗菌活性。结果从三宝木枝条乙醇提取物的乙酸乙酯萃取物中分离得到了12个已知化合物,经波谱分析鉴定为松脂醇(1)、(+)-de-4″-O-methylmagnolin(2)、丁香脂素(3)、nitidanin(4)、臭矢菜素A(5)、6-deoxyjacareubin(6)、巴西红厚壳素(7)、豆甾-4,22-二烯-3-酮(8)、3β-羟基豆甾-5-烯-7-酮(9)、豆甾-4-烯-3-酮(10)、正十八酸(11)、β-谷甾醇(12)。结论 12个化合物均为首次从该植物中分离得到,其中,化合物2、4、5、8、9、10是首次从该属植物中分离得到。初步抗菌活性结果表明化合物7对金黄色葡萄球菌、烟草青枯菌具有抑制活性。     

海洋真菌zp6次级代谢产物及其抗真菌活性研究

目的对海洋真菌zp6发酵液的乙酸乙酯萃取部分及其抑菌活性进行研究。方法采用硅胶柱色谱及高效液相色谱进行分离纯化,根据理化性质及各种光谱技术进行结构鉴定,采用滤纸片法对分离到的化合物进行抑菌活性研究。结果从该菌中分离纯化得到8个化合物:(22E)-3β,5α,9α-三羟基-麦角甾-7,22-二烯-6-酮(1)、5α,8α-环二氧-24-甲基麦角甾-6,22-二烯-3β-醇(2)、赤藓糖醇(3)、腺嘌呤核苷(4)、(24R)-麦角甾-7,22-二烯-3β,5α,6β-三醇(5)、阿拉伯醇(6)、(7)、4-乙酰氧基苯甲酸(8)。结论化合物1和5具有抗真菌活性。     

北极真菌Nectria sp.B-13中酚醛倍半萜烯类化合物的研究

摘要：目的 对北极真菌 Nectria sp. B-13 中的酚醛倍半萜烯类化合物进行结构鉴定及生物学活性研究。方法 采用硅胶柱层析、Sephadex LH-20凝胶柱层析、高效液相色谱等分离手段对极地真菌Nectria sp. B-13发酵液的乙酸乙酯萃取部位进行了系统的分离,利用1H-和13C-NMR、LC-MS等现代波谱解析手段,结合文献对照,鉴定化合物结构;采用MTT法和微量稀释法测试了化合物的细胞毒活性和抗稻瘟霉作用。结果 从提取物中分离得到6个化合物,其中4个为酚醛倍半萜烯类化合物,分别为dechlorodeacetylchloronectrin（1）,LL-Z-1272 ε acid（2）,8''-hydroxyascochlorin（3）和LL-Z 1272 β（4）,以及邻苯二甲酸丁酯异丁酯（5）和邻苯二甲酸二丁酯（6）。活性测试的结果表明,化合物2对5种肿瘤细胞株均有一定程度的生长抑制作用,其IC50值的范围在48.67~92.18 μM之间;同时,化合物2还可抑制稻瘟霉的生长,MIC值为18.2 μg/mL。结论 化合物1和化合物2为首次从微生物次级代谢产物中获得的化合物,为新天然产物。化合物2有一定的细胞毒活性和抗稻瘟霉作用。     

浒苔来源真菌Aspergillus versicolor ZJOU-SKL-02次级代谢产物及其活性研究

目的 研究真菌Aspergillus versicolor ZJOU-SKL-02的次级代谢产物及其生物活性。方法 利用硅胶柱色谱、TLC、HPLC等方法对Aspergillus versicolor ZJOU-SKL-02发酵液进行分离纯化;通过ESI-MS、NMR、比旋光、化学合成等手段,并结合文献数据,确定了其产生的化合物结构及绝对构型。对分离得到的化合物进行了抑菌活性和α-葡萄糖苷酶抑制活性的测试。结果 分离得到6个二苯醚类化合物Diorcinol B(1)、Diorcinol C(2)、Diorcinol E(3)、Diorcinol J(4)、Diorcinol(5)和methyl diorcinol-4-carboxylate(6)。其中化合物5对铜绿假单胞菌有较强的抑菌活性,MIC值为4 μg/mL;化合物6显示出对铜绿假单胞菌和光滑念珠菌有较强的抑菌活性,MIC值分别为4和8 μg/mL。化合物3和化合物4具有强的α-葡萄糖苷酶抑制活性,IC50值分别为117.3和237.4 μM,优于阳性对照阿卡波糖的IC50 255.3 μM。结论 以上活性化合物可以为抗生素的发现和糖尿病的预防和治疗用药提供活性先导化合物资源。     

Hemorrhagic activity of the Duvernoy''s gland secretion of the xenodontine colubrid Philodryas patagoniensis from the north-east region of Argentina

Colubrid snakes belonging to Philodryas genus, widespread all over South America, bring about lesions (swelling, ecchymosis, transient bleeding from the bite site punctures), that are similar to those produced by Bothrops species (yarará). In the present work we began the characterization of Philodryas patagoniensis venom. We examined if this venom produces hemorrhagic lesions as those observed in victims bitten by Philodryas olfersii. Hemorrhagic, proteolytic and fibrinogenolytic activities were evaluated, and histological observations in samples of gastrocnemius muscle were carried out. Inhibition studies were carried out in metal chelator (ethylenediaminetetraacetic acid) presence. Our results show a small Minimum Hemorrhagic Dose (MHD=0.035 μg) and a high proteolytic activity (143 U/mg), and prove the capacity of this venom to degrade fibrinogen in vitro rendering it unclottable by thrombin, supporting the presence of proteases, principally metalloproteases, in P. patagoniensis venom that are able to alterate the vascular wall and degrade fibrinogen, being both activities responsible of a high hemorrhagic activity.     

Evaluation of the Antimicrobial Activity of Ammoniacum Gum from Dorema ammoniacum

Antimicrobial activity of the dichloromethane-methanol (1 : 1) extract of ammoniacum gum (from Dorema ammoniacum D. Don) was evaluated against 14 microorganisms which included seven Gram-positive bacteria (Bacillus cereus, Bacillus pumilus, Bacillus subtilis, Micrococcus luteus, Staphylococcus epidermidis, Staphylococcus aureus and Streptococcus faecalis), four Gram-negative bacteria (Escherichia coli, Pseudomonas aereuginosa, Klebsiella pneumoniae and Bordetella bronchiseptica), one yeast (Saccharomyces cereviseae) and two fungi (Aspergillus niger and Candida albicans). The extract of ammoniacum gum exhibited a of broad spectrum antimicrobial activity by inhibiting all the seven Gram-positive bacterium, one Gramnegative bacterium, one yeast and one fungus, with a minimum inhibitory concentration (MIC) of 40µg/ml. To overcome the solubility problem often faced when herbal extracts are added to aqueous medium, we employed a modified broth method where the broth cultures were agitated at 150 rpm in an orbital shaking incubator. This method reduced the MIC of the extract considerably, to 5-20µg/ml, against B. bronchiseptica, S. aureus and S. epidermidis.     

Antipyretic, analgesic and anti-inflammatory effects of delta 9-tetrahydrocannabinol in the rat

The effects on body temperature produced by graded doses of Δ⁹-tetrahydrocannabinol (Δ⁹-THC) and phenylbutazone were compared in both normal and pyretic rats. Dose related hypothermic responses were produced by the oral administration of Δ⁹-THC in normal animals. Moreover, Δ⁹-THC significantly reduced elevated temperatures in yeast-induced pyretic rats to near normal levels at doses which exhibited little hypothermic activity in normal rats. The oral antipyretic potency of Δ⁹-THC was approximately 2 times that of phenylbutazone. The comparative oral antinociceptive activity of Δ⁹-THC and selected narcotic and non-narcotic analgesics was determined by the increase in response latency to pressure applied to normal and yeast-inflamed paws. Δ⁹-THC administered orally was essentially inactive at dose levels below those producing pronounced central nervous system depression. The oral anti-inflammatory efficacy of Δ⁹-THC was compared to phenylbutazone and acetylsalicylic acid. Δ⁹-THC was ineffective in inhibiting carrageenin-induced edema of the rat paw following acute or chronic administration.     

Investigation of the antimicrobial and anticancer activity of aminonaphthoquinones

In this study, we report on the inhibitory activity of synthesized aminonaphthoquinones against two bacterial and one fungal species to determine their antimicrobial properties. A minimum inhibitory concentration (MIC) of 7.8 μg/mL was obtained against the fungus, Candida albicans, which was better than that of Amphotericin B (MIC = 31.25 μg/mL). Escherichia coli (Gram -), was inhibited at a MIC of 23.4 μg/mL and Staphylococcus aureus (Gram +) at a MIC of 31.3 μg/mL. The aminonaphthoquinones were also screened against HCT116 colon, PC3 prostate and HepG2 liver cancer cell lines to evaluate their cytostatic effects. They had potent activity (GI₅₀ = 5.87–9.90 μM) which was about three-6-fold better than that of parthenolide (GI₅₀ = 25.97 μM) against the prostate cancer cell line. These compounds were generally more selective for cancer cells than for normal human lung fetal fibroblasts (WI-38).     

Antimicrobial and antineoplastic activities of agelasine analogs modified in the purine 2-position

Agelasines are 7,9-dialkylpurinium salts found in marine sponges (Agelas sp.), which display a variety of antimicrobial and cytotoxic effects. We have synthesized simplified agelasine analogs modified in the purine 2-position and examined their antimicrobial and anticancer activities. The compounds were screened against Staphylococcus aureus, Escherichia coli, Mycobacterium tuberculosis, Candida krusei, and Candida albicans, protozoa causing tropical diseases (Plasmodium falciparum, Leishmania infantum, Trypanosoma cruzi, and Trypanosoma brucei), a panel of human cancer cell lines (U-937 GTB, RPMI 8226/s, CEM/s, and ACHN) as well as VERO and/or MRC-5 cells. The results indicate that the introduction of a methyl group in the purine 2-position is beneficial for antimycobacterial and antiprotozoal activity, and that amino groups may enhance activity against several cancer cell lines.     

SV预防血栓药理学作用及其机制研究探讨

血栓栓塞性疾病是人类首要致死病因,临床预防血栓药物均存在出血危险。选择性的内源性凝血途径抑制剂已成为低出血倾向预防血栓药物研发的重点方向。SV是以天然岩藻糖化糖胺聚糖(FG)为先导化合物经结构优化获得的选择性内源性凝血因子Xase抑制剂(IC50=30 nm),其抑制内源性凝血活性与依诺肝素相当,在等效抗凝血剂量的倍数剂量下出血倾向显著降低。本文探讨低出血倾向的SV预防血栓药理学作用及其机制,为选择性Xase抑制剂及其新药发现研究提供参考依据。     

Antioxidant and vasorelaxant activities of the Turraeanthus africanus methanol extract

The present studies evaluate the antioxidant and vasorelaxant activities of the methanol stem bark extract of Turraeanthus africanus (Welw.) Pellegr. (Meliaceae). The antioxidant property investigated through the DPPH scavenging activity showed that the methanol extract from the stem bark of T. africanus was active with an inhibition rate of 72.47% at 500 μg/mL and IC₅₀ of 29.2 μg/mL. This extract (0.1–700 μg/mL) induced a concentration-dependent relaxation of guinea-pig aortic rings precontracted with noradrenaline or KCl, with a maximum relaxation reaching 87.55 and 97.42%, respectively, at a concentration of 700 μg/mL. The extract showed no significant effect on the electrically induced contraction of the guinea-pig papillary muscle. The results of this study indicate that the extract from the stem bark has interesting antioxidant and vasorelaxant properties and represents a potential source of medicine for the treatment of cardiovascular diseases.     

Resveratrol isoforms and conjugates: A review from biosynthesis in plants to elimination from the human body

The natural isomers of resveratrol, cis- and trans-resveratrol, are natural phenolic substances synthetized via the shikimate pathway and found in many sources, including grapes, peanuts, blackberries, pistachios, cacao, cranberries, and jackfruits. They have functional and pharmacological properties such as anticarcinogenic, antidiabetic, anti-inflammatory, and cardioprotective activities. The aim of this article is to review the data published on resveratrol and its isomers, and their biosynthesis in plants, food sources, health and toxic effects, and the excretion of their metabolites. Due to its contribution to the promotion of human health, it is convenient to gather more knowledge about its functional properties, food sources, and the interactions with the human body during the processes of eating, digestion, absorption, biotransformation, and excretion, to combine this information to improve the understanding of these substances.     

Chemical constituents and bioactivities of the liposoluble fraction from different medicinal parts of Crocus sativus

Context: Crocus sativus Linn. (Iridaceae), commonly known as saffron, becomes more and more popular due to its versatile biological and medicinal properties. At present, studies mainly focus on the traditional medicinal part, the saffron stigma, with less attention to the other parts of saffron, such as the perianth, the stamen, and the corm, which are high yield compared to the stigma and also possess various pharmacological effects.

Objective: To determine the chemical compositions, antifungal, cytotoxic, and antioxidant activities of the ether fractions from the stamen, perianth, and stigma of saffron.

Materials and methods: The chemical constituents of the ether fractions from different parts of saffron were investigated by gas chromatography/mass spectrometry. Several pathogenic fungi isolates and tumor cell lines were employed to evaluate the antifungal and cytotoxic activities of these three ether fractions. 1,1-Diphenyl-2-picrylhydrazyl assay was used to determine the free radical-scavenging activity.

Results: The ether fractions composition of the three C. sativus parts are different from each other, but lauric acid, hexadecanoic acid, 4-hydroxydihydro-2(3H)-furanone, and stigmasterol were the common constituents shared by all the three fractions. The stamen ether fraction displayed the strongest antifungal and cytotoxic activities, whereas both of the saffron stamen and perianth ether fractions exhibited significant antioxidant activities.

Discussion and conclusion: These findings demonstrate that the saffron stamen and perianth possess significant antifungal, cytotoxic, and antioxidant activities as well as the stigma, though not to the same extent, prompting us to expand the medicinal resource and make best use of this valuable plant.