艾纳香中的黄酮类化合物及其抗菌活性

为明确艾纳香抗菌药效物质基础,采用硅胶柱色谱, 凝胶色谱和反相色谱等技术从艾纳香乙酸乙酯部位中分离获得15个单体化合物,经波谱学鉴定分别为：3,3°,5-三羟基-4°,7-二甲氧基二氢黄酮 (1)、4°,5-二羟基-3,3°,7-三甲氧基黄酮 (2)、艾纳香素 (3)、3,5,3°,4°-四羟基-7-甲氧基黄酮 (4)、香叶木素 (5)、3°,4°,5-三羟基-3,7-二甲氧基黄酮 (6)、异鼠李素 (7)、chrysosplenol C (8)、金丝桃苷 (9)、异槲皮苷 (10)、3°,5,7-三羟基-4°-甲氧基二氢黄酮 (11)、sakuranetin (12)、pilloin (13)、5,7,3°,4°-四羟基-3-甲氧基黄酮 (14)、5-羟基-3,7,3°,4°-四甲氧基黄酮 (15),其中化合物7、11、12和13为首次从该植物中分得。抗菌活性评价结果显示：化合物1、3、6、8和12对3株细菌具有不同程度的抑制活性,其中化合物3对金黄色葡萄球菌抑制活性最强, 最低抑菌浓度MIC值为32 μg/mL。     

普洱茶E8组分的化学成分研究

采用HPLC制备色谱等分析了普洱茶乙酸乙酯提取物E8组分的化学成分,并通过LC/MS和NMR等对制备得到的化合物进行了结构鉴定。结果表明,从E8组分中分离鉴定出5个化合物,分别为3',4',5-三羟基-7-甲氧基黄酮、3',4',5,7-四羟基黄酮（木犀草素）、槲皮素-3-O-β-D-葡萄糖甙、3',4',7-三羟基-5-甲氧基黄酮-7-O-β-D-葡萄糖甙和3',4',7-三羟基-5-甲氧基黄酮。     

辣木叶黄酮苷的分离鉴定及抗氧化活性研究

为研究辣木（Moringa Obleifera Lam.）叶片中的黄酮苷成分及其抗氧化活性,利用MCI凝胶柱、羟丙基葡聚糖凝胶（Sephadex LH-20）柱层析、硅胶柱层析（CC）、半制备高效液相色谱等分离手段对石油醚组分进行分离和纯化,利用LC-MS、1H-NMR、13C-NMR等现代波谱技术对分离得到的化合物进行结构鉴定,采用SRB法和DPPH·清除率对分离得到的化合物进行体外抗肿瘤活性筛选和抗氧化活性的测定。结果表明,从辣木叶的石油醚部分分离得到4个化合物,已鉴定为β-谷甾醇（Ⅰ）、胡萝卜苷（Ⅱ）、槲皮素-3-O-β-D-葡萄糖苷（Ⅲ）、山柰酚-3-O-β-D-葡萄糖苷（Ⅳ）。4种化合物均具有抗氧化活性,但化合物Ⅲ的抗氧化活性极显著强于其他三种化合物;体外抗肿瘤活性表明,化合物Ⅰ和化合物Ⅱ对乳腺癌细胞株（MDA-MB-231）有一定的抑制作用。      

艾纳香中绿原酸类化学成分研究

为全面了解海南传统黎药艾纳香抗菌药效物质基础,本研究采用硅胶柱色谱、凝胶色谱以及高效液相色谱技术对艾纳香提取物进行系统化学成分研究。结果显示:共分离鉴定6个绿原酸类成分:3,5-O-二咖啡酰奎尼酸乙酯(1),3,5-O-二咖啡酰奎尼酸甲酯(2),3,4-O-二咖啡酰奎尼酸甲酯(3),3,4-O-二咖啡酰奎尼酸(4),3,5-O-二咖啡酰奎尼酸(5),1,3,5-O-三咖啡酰奎尼酸(6)。化合物1~6均为首次从该植物中分离得到,其中化合物1为新天然产物。抗细菌活性评价显示化合物3对枯草芽孢杆菌及化合物6对金黄色葡萄球菌均具有较强抑制活性,MIC值均为64μg/mL,推测绿原酸类为艾纳香的重要抗菌活性组成。     

牛大力根的化学成分研究

从牛大力(Millettia speciosa Champ.)根95%乙醇提取物的乙酸乙酯部分中分离得到了7个化合物,经波谱分析及与文献数据对照鉴定其结构为:2’,4,4’-三羟基查耳酮(1),紫檀素(2),3’,7-二羟基-2’,4’-二甲氧基异黄酮(3),高丽槐素(4),豆甾醇(5),β-谷甾醇(6),胡萝卜苷(7)。其中化合物(2)和化合物(3)为首次从该植物根中分离得到。     

一种国外沉香中2-(2-苯乙基)色酮类化合物研究

为了了解一种国外沉香中的2-(2-苯乙基)色酮类化合物,采用多种色谱分离技术从该沉香的乙醇提取物中分离得到6个化合物,通过波谱学方法分别鉴定为：6-羟基-8-氯-2-[2-(4°-羟基苯基)乙基]色酮（1）,6-羟基-2-[2-(3°-甲氧基-4°-羟基苯基)乙基]色酮（2）,6-羟基-7-甲氧基-2-[2-(4°-羟基苯基)乙基]色酮（3）,沉香四醇（4）,5α,6β,7β,8α-四羟基-2-[2-(4°-甲氧基苯基)乙基]-5,6,7,8-四氢色酮（5）和6-羟基-2-[2-(3°-甲氧基-4°-羟基苯基)乙烯基]色酮（6）。化合物1为新的2-(2-苯乙基)色酮。对化合物2~6的细胞毒活性测试结果表明,化合物6对5株人体肿瘤细胞均表现出一定活性,其中对人慢性髓原白血病细胞K562和人肝癌细胞BEL-7402具有显著抑制活性,半数抑制浓度（IC₅₀）为2.87和 4.75 μg/mL,化合物2、3、5对5株人体肿瘤细胞表现出中等活性,IC₅₀范围为9.91~45.38 μg/mL。     

沉香样品中曲霉属真菌菌株 HNWSW-20 的分离鉴定及其次生代谢产物的研究

本文采用平板分离法从沉香样品中分离得到一株真菌 HNWSW-20,从形态学和分子生物学上鉴定其为曲霉菌（Aspergillus sp.）,并利用多种色谱技术对其次生代谢产物进行分离纯化,根据波谱数据和理化性质鉴定其化合物结构为：2?,3?-dihydrosorbicillin（1）,sorbicillin（2）,2,3-二氢-2-(1-丙烯)-6,8-二甲基-7-羟基-色酮（3）,邻苯二甲酸二丁酯（4）,7-羟基-异苯并呋喃-1(3H)-酮（5）二十烷酸甲酯（6）;分别采用 Ellman 比色法和 pNPG 法测定化合物的乙酰胆碱酯酶抑制活性和 α-葡萄糖苷酶抑制活性,结果显示上述化合物 1、2、4 具有乙酰胆碱酯酶抑制活性,而化合物 1、3、5 具有 α-葡萄糖苷酶抑制活性。本文中化合物 1~2 为首次从曲霉属中分离得到,并首次报道具有乙酰胆碱酯酶和 α-葡萄糖苷酶抑制活性。     

麦冬须根正丁醇萃取物化学成分的分离与鉴定

为了研究麦冬须根中的化学成分,本研究采用大孔吸附树脂、ODS和Sephadex LH-20多种柱色谱技术对麦冬须根乙醇提取物的正丁醇萃取物进行分离纯化;通过波谱数据与理化性质分析并结合文献进行化合物结构鉴定。从麦冬须根的正丁醇萃取物中分离得到10个化合物,其结构分别鉴定为5-甲氧基-6-甲基-7-羟基-8-醛基-3S-(3', 4' -亚甲二氧基苯)-4-二氢色原酮（1）、甲基麦冬黄烷酮A（2）、甲基麦冬黄烷酮B（3）、大黄素（4）、肥牛木素（5）、E-对羟基桂皮酸（6）、Z-对羟基桂皮酸（7）、4-羟基苯甲酸（8）、25R-spirost-5-ene-1β, 3β-diol 1-O-[α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranoside]（9）和β-谷甾醇（10）。其中化合物1为新的高异黄酮类化合物,命名为麦冬黄烷酮D',化合物5和7为首次从百合科植物中分离得到,化合物9为首次从该植物中分离得到。     

艾纳香脱氢酶基因家族的生物信息学分析

采用RT-PCR和RACE（Rapid amplification of cDNA ends）技术,从艾纳香（Blumea balsamifera (L.) DC.）叶片中克隆到4条编码艾纳香脱氢酶（BbADH1、BbADH2、BbADH3、BbADH4）基因的cDNA序列,并对4条核苷酸及其编码的氨基酸序列进行生物信息学分析。结果显示:4条艾纳香脱氢酶序列开放阅读框均在900 bp左右,蛋白质等电点（pI）值在5.0~9.0之间,含量最多的氨基酸为亮氨酸（Leu）,最少的为色氨酸（Try）,具有明显的疏水区和亲水区,N端未发现信号肽,且无跨膜区;同源性比对结果显示,艾纳香BbADH蛋白与其他植物中ADH蛋白具有高度的相似性,且具有脱氢酶的特征功能域;系统发育分析表明,艾纳香（B. balsamifera (L.) DC.）BbADH1和BbADH3同处于一个分支,且与胡杨（Populus euphratica Oliv.）PeADH物种亲缘关系较近,而艾纳香BbADH4和BbADH2处于不同分支,且分别与葡萄（Vitis vinifera）VvADH和烟草（Nicotiana tabacum）NtADH物种亲缘关系较近。     

RP—HPLC法测定泽兰中木犀草素-7-0-β-D-葡萄糖苷的含量

目的建立反相高效液相色潜法测定泽兰中木犀草素-7-0-β-D-葡萄糖苷的含量。方法采用AlltimaTM—C18（250minx4．6mm,51．Lm）;以乙腈-0．2％磷酸水溶=20：80进行等度洗脱,流速为1．0ml／min,检测波长为350mm,柱温为35℃。结果木犀草素-7-0-β-D-葡萄糖苷的线性范围为0．412-10．30μg（r=0．9999）,平均回收率为100．25％。结论该方法结果准确、简便可行、重复性好,可为泽兰的质量控制提供依据。     

海洋共生菌Aspergillus sp.HDf2新活性次生代谢产物研究(英文)

对紫海胆共生真菌Aspergillus sp.HDf2的次生代谢产物进行分离和鉴定。采用摇瓶液体发酵,运用柱层析等方法对其发酵液成分进行分离纯化,经波谱解析和质谱分析进行结构鉴定,并运用滤纸片法对化合物进行体外抗金黄色葡萄球菌的活性测试。结果从该真菌发酵产物中鉴定出2个secospiculisporic acid新类似物,分别为secospiculisporic acid B(1)和secospiculisporic acid C(2),其中化合物1具有弱抗菌活性,抑菌直径为9.2 mm(20 mg/mL)。首次对化合物1的NMR数据进行了归属,化合物2为secospiculisporic acid类的新化合物。     

New Isocoumarin Analogues from the Marine-Derived Fungus Paraphoma sp. CUGBMF180003

Nine new secondary metabolites, including six isocoumarin analogues, 7-hydroxyoospolactone (1), 7-methoxyoospolactone (2), 7-methoxy-9-hydroxyoospolactone (3), 10-acetoxy-9-hydroxyoospolactone (4), 6-dehydroxysescandelin (5), parapholactone (6), and three compounds with a rare skeleton of isocoumarin coupled with phenylethylamine, namely paraphamide A (12), paraphamide B (13), and paraphamide C (14), together with five known compounds, oospolactone (7), 8-O-methyloospolactone (8), 10-hydroxyoospolactone (9), 9,10-dihydroxyoospolactone (10), and oospoglycol (11), were isolated and identified from the marine-derived fungus Paraphoma sp. CUGBMF180003. Their chemical structures were determined using spectroscopic data, including HRESIMS and 1D and 2D NMR techniques. Furthermore, the stereogenic carbons in 5 and 14 were determined by comparing the experimental and calculated electronic circular dichroism (ECD) spectra. The carbon skeleton of 12–14 was identified as the first example of isocoumarin coupled with phenylethylamine derivatives. All of these compounds were examined for antimicrobial activities against Candida albicans and Staphylococcus aureus. Both 1 and 6 showed antibacterial activity against S. aureus with MIC values of 12.5 μg/mL.     

New Secondary Metabolites from the Marine-Derived Fungus Talaromyces mangshanicus BTBU20211089

Seven new compounds, namely talaromanloid A (1), talaromydene (2), 10-hydroxy-8-demethyltalaromydine and 11-hydroxy-8-demethyltalaromydine (3 and 4), talaromylectone (5), and ditalaromylectones A and B (6 and 7), together with seven known compounds were identified from a marine-derived fungus, Talaromyces mangshanicus BTBU20211089, which was isolated from a sediment sample collected from the South China Sea. Their chemical structures were determined using spectroscopic data, including HRESIMS, 1D, and 2D NMR techniques. The absolute configurations of 1 and 2 were elucidated by comparing experimental and calculated ECD spectra. Compounds 1, 2, 6, and 7 are new compounds possessing a novel carbon skeleton. Compound 6 is a dimeric molecule of 3 and 9. Compound 7 shared a unique structure of the cyclized dimer of 3 and 4. All the compounds were tested for their bioactivities against Staphylococcus aureus, Escherichia coli, and Candida albicans.     

Isolation of Sesquiterpenoids and Steroids from the Soft Coral Sinularia brassica and Determination of Their Absolute Configuration

Two undescribed rearranged cadinane-type sesquiterpenoids (1–2), named sinulaketol A-B, together with one new chlorinated steroid (3), one new gorgosterol (4), one known sesquiterpene (5), one known dibromoditerpene (6) and two known polyhydroxylated steroids (7–8) were isolated from the soft coral Sinularia brassica. The structures of these compounds were established by extensive spectroscopic analysis, including HRESIMS, 1D, and 2D NMR spectroscopy. Their absolute configurations were also determined by the ECD calculations and DP4+ probability analysis. Antileishmanial activity of compounds 1–8 was evaluated in vitro against the amastigote forms of Leishmania donovani, in which compounds 3, 6, and 7 inhibited the growth of L. donovani by 58.7, 74.3, 54.7%, respectively, at a concentration of 50 μM. Antimicrobial effect of the isolated compounds were also evaluated against Candida albicans, Staphylococcus aureus, and Escherichia coli. Compound 6, a brominated diterpene, exhibited antimicrobial effect against S. aureus.     

Four New Antibacterial Xanthones from the Marine-Derived Actinomycetes Streptomyces caelestis

Four new polycyclic antibiotics, citreamicin θ A (1), citreamicin θ B (2), citreaglycon A (3), and dehydrocitreaglycon A (4), were isolated from marine-derived Streptomyces caelestis. The structures of these compounds were elucidated by 1D and 2D NMR spectra. All four compounds displayed antibacterial activity against Staphylococcus haemolyticus, Staphylococcus aureus, and Bacillus subtillis. Citreamicin θ A (1), citreamicin θ B (2) and citreaglycon A (3) also exhibited low MIC values of 0.25, 0.25, and 8.0 μg/mL, respectively, against methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300.     

Anti-proliferative activity of meroditerpenoids isolated from the brown alga Stypopodium flabelliforme against several cancer cell lines

The sea constitutes one of the most promising sources of novel compounds with potential application in human therapeutics. In particular, algae have proved to be an interesting source of new bioactive compounds. In this work, six meroditerpenoids (epitaondiol, epitaondiol diacetate, epitaondiol monoacetate, stypotriol triacetate, 14-ketostypodiol diacetate and stypodiol) isolated from the brown alga Stypopodium flabelliforme were tested for their cell proliferation inhibitory activity in five cell lines. Cell lines tested included human colon adenocarcinoma (Caco-2), human neuroblastoma (SH-SY5Y), rat basophilic leukemia (RBL-2H3), murine macrophages (RAW.267) and Chinese hamster fibroblasts (V79). Antimicrobial activity of the compounds was also evaluated against Staphylococcus aureus, Salmonella typhimurium, Proteus mirabilis, Bacillus cereus, Enterococcus faecalis and Micrococcus luteus. Overall, the compounds showed good activity against all cell lines, with SH-SY5Y and RAW.267 being the most susceptible. Antimicrobial capacity was observed for epitaondiol monoacetate, stypotriol triacetate and stypodiol, with the first being the most active. The results suggest that these molecules deserve further studies in order to evaluate their potential as therapeutic agents.     

New Dimeric Members of the Phomoxanthone Family: Phomolactonexanthones A,B and Deacetylphomoxanthone C Isolated from the Fungus Phomopsis sp.

Three new phomoxanthone compounds, phomolactonexanthones A (1), B (2) and deacetylphomoxanthone C (3), along with five known phomoxanthones, including dicerandrol A (4), dicerandrol B (5), dicerandrol (6), deacetylphomoxanthone B (7) and penexanthone A (8), were isolated in the metabolites of the fungus Phomopsis sp. HNY29-2B, which was isolated from the mangrove plants. The structures of compounds 1–3 were established on the basis of spectroscopic analysis. All compounds were evaluated against four human cancer cell lines including human breast MDA-MB-435, human colon HCT-116, human lung Calu-3 and human liver Huh7 by MTT assay. The compounds 4, 5, 7 and 8 showed cyctotoxic activities against tested cancer cell lines (IC₅₀ < 10 μM).     

Antiparasitic bromotyrosine derivatives from the marine sponge Verongula rigida

Nine bromotyrosine-derived compounds were isolated from the Caribbean marine sponge Verongula rigida. Two of them, aeroplysinin-1 (1) and dihydroxyaerothionin (2), are known compounds for this species, and the other seven are unknown compounds for this species, namely: 3,5-dibromo-N,N,N-trimethyltyraminium (3), 3,5-dibromo-N,N,N, O-tetramethyltyraminium (4), purealidin R (5), 19-deoxyfistularin 3 (6), purealidin B (7), 11-hydroxyaerothionin (8) and fistularin-3 (9). Structural determination of the isolated compounds was performed using one- and two-dimensional NMR, MS and other spectroscopy data. All isolated compounds were screened for their in vitro activity against three parasitic protozoa: Leishmania panamensis, Plasmodium falciparum and Trypanosoma cruzi. Compounds 7 and 8 showed selective antiparasitic activity at 10 and 5 μM against Leishmania and Plasmodium parasites, respectively. Cytotoxicity of these compounds on a human promonocytic cell line was also assessed.