Acaricidal activity of Uvaria versicolor and Uvaria Klaineana (Annonaceae)

Three Uvaria species, namely U. klaineana, U. mocoli and U. versicolor were tested in vitro against Dermatophagoides pteronyssinus, the European house dust mite. The most active extracts were the Uvaria versicolor stems crude methanol and hexane extracts with EC(50) values of 0.095 g/m(2 )and 0.12 g/m(2), respectively. The bioassay-guided fractionation of the hexane extract led to the isolation of benzyl benzoate (1). which exhibited an EC(50) value of 0.045 g/m(2). A new fl avanone, versuvanone (2). and the known oxoaporphine liriodenine (3). were also isolated from this species and showed EC(50) values > 1.5 g/m(2). A weak acaricidal activity (0.85 g/m(2)) was observed for the dichloromethane extract of Uvaria klaineana, due to the presence of benzyl benzoate. Uvaria mocoli was inactive. The structures of compounds were elucidated using 2D-NMR techniques.     

紫玉盘化学成分的研究

目的：从紫玉盘Uvaria macrophylla var. microcarpa中分离具有抗癌活性成分。方法：用色谱方法分离紫玉盘中化学成分,用波谱技术（IR,ESI-MS,1H-NMR,13C-NMR,HMQC,COSY,HMBC, NOESY)进行鉴定结构。结果：从紫玉盘中分离得到4个化合物, uvarimacrins A （1）, B（2）and C（4）和uvamalols D（3）。结论：化合物（1）,（2）,（4）均为新化合物,（3）首次从紫玉盘中分离得到。     

Anti-Inflammatory and Phytochemical Analysis of the Crude Leaves Extracts of Boscia Coriacea Graells and Uvaria Leptocladon Oliv

BackgroundThe objective of this study was to evaluate the anti-inflammatory activities and phytochemical composition of the leaves extracts of Boscia coriacea Graells and Uvaria leptocladon Oliv.MethodsThe powdered leaves of Boscia coriacea Graells and Uvaria leptocladon Oliv were extracted by maceration and soxhlet extraction methods. Anti-inflammatory activity of the leaves extracts of Boscia coriacea Graells and Uvaria leptocladon Oliv were evaluated using carrageenan-induced paw edema model. Standard methods were used for analysis of phytochemical composition of the leaves extracts of Boscia coriacea Graells and Uvaria leptocladon Oliv. Data analysis was done using one way analysis of variance.ResultsU. leptocladon Oliv (200 mg/kg) and B. coriacea Graells (200 mg/kg) showed percent inhibition on mice paw edema of 86% and 75% after six hours of carrageenan injection, respectively. The ethanol fraction (100 mg/kg) of U. leptocladon Oliv showed the highest anti-inflammatory effect after six hours of carrageenan injection. The phytochemical analysis of the leaves extracts of B. coriacea and U. leptocladon revealed the presence of tannins, alkaloids, cardiac glycoside, flavonoids, phenols, quinones, and saponins.ConclusionThe crude leaves extracts of B. coriacea Graells and U. leptocladon Oliv contain phytochemicals with anti-inflammatory activities.     

Zeylenone对急性淋巴细胞白血病细胞增殖及凋亡的影响

目的探讨Zeylenone体外抗急性淋巴细胞白血病(Acute Lymphoblastic Leukemia,ALL)效应及作用的可能机制。方法应用MTT法比较Zeylenone对肿瘤细胞、正常细胞增殖的影响;AO/EB染色观察其对ALL细胞(Reh、RS4;11)凋亡形态学的改变;流式细胞仪检测药物对细胞凋亡及细胞周期的影响。结果 Zeylenone对多种细胞呈现增殖抑制作用,且对ALL细胞株呈现更高的敏感性,而对外周血单个核细胞(Peripheral blood mononuclear cell,PBMC)抑制作用较小,抑制Reh、RS4;11细胞增殖呈时间依赖性和剂量依赖性;Zeylenone能够诱导ALL细胞凋亡,阻滞细胞周期于G0/G1期。结论 Zeylenone体外具有抗ALL细胞增殖的作用,其作用与诱导细胞凋亡、阻滞细胞周期相关。     

Three polyoxygenated cyclohexenes from Uvaria calamistrata

Three new polyoxygenated cyclohexenes, named uvacanols F, G, H (1–3), were isolated from the roots of Uvaria calamistrata (Annonaceae). Their structures were determined to be 2-acetoxyl-5-chlorine-benzoyloxymethylcyclohex-1 (6)-ene-4-ol-3-benzoate (1), benzoyloxy-methylcyclohex-1 (6)-ene-2,3,4-triols-5-benzoate (2), 3-acetoxyl-benzoyloxymethylcyclohex-1 (6)-ene-4,5-diols-2-benzoate (3) by spectroscopic methods and chemical derivatization.     

In Vitro Antibacterial and Antifungal Activities of Extracts and Compounds from Uvaria scheffleri

Petroleum ether, dichloromethane, and ethanolic extracts of the stem bark and leaves of Uvaria scheffleri Diels (Annonaceae) exhibited antifungal activity against Aspergillus niger (wild strain), Aspergillus fumigatus (wild strain), and a Penicillium species (wild strain). The ethanol extract of the stem bark was also active against Candida albicans (Strain H6392). The dichloromethane extract of the leaves showed the highest antifungal activity and in addition it showed antibacterial activity against Staphylococcus aureus (NCTC 6571). Fractionation of the dichloromethane extract of the leaves yielded nine known compounds. They included a 1 : 1 mixture of stigmasterol (1) and β-sitosterol (2), which showed antifungal activity against Candida albicans. Others were 3-farnesylindole (3), 2′,6′-dihydroxy-3′,4′-dimethoxy-chalcone (4), 2′-hydroxy-3′,4′,6′-trimethoxychalcone (5), 5-hydroxy-7,8-dimethoxyflavanone (6), 5,7,8-trimethoxyflavanone (7), and a 3 : 2 mixture of 2′,6′-dihydroxy-4′-methoxychalcone (8) and 5,7-dihydroxyflavone (9). Compound 7 and the mixture of compounds 8 and 9 showed antibacterial activity against Escherichia coli (NCTC 10418, MIC 125 µg/ml) and Staphylococcus aureus (MIC 125 µg/ml), respectively. The mixture of compounds 8 and 9 was also active against Candida albicans (MIC 31.25 µg/ml), Aspergillus niger, Aspergillus fumigatus, and the Penicillium species (MIC 1000 µg/ml). We conclude that Uvaria scheffleri extracts contain compounds with antifungal and antibacterial activity. The activities observed in this study are weak. Based on previous studies, it is being speculated that, possibly, the most active compounds were lost during fractionation. Further work to isolate more antifungal and antibacterial compounds is suggested.     

超临界CO2萃取紫玉盘茎挥发油化学成分的分析

目的:研究紫玉盘茎挥发油的化学成分。方法:采用超临界CO2萃取法提取紫玉盘茎挥发油,用气相色谱-质谱联用技术对其化学成分进行分离鉴定。结果:从紫玉盘茎挥发油中共分离出68个色谱峰,鉴定其中37个化合物,占总量的85.73%,主要成分有苯甲酸、8-氧代-9H-环异长叶烯、对甲氧基桂皮酸乙酯。结论:超临界CO2萃取法提取挥发油与水蒸气蒸馏法提取挥发油的化学成分有明显的差异。     

大花紫玉盘的化学成分

通过正相硅胶、反相硅胶、大孔吸附树脂、Sephadex LH-20和高效液相色谱等多种现代色谱技术对番荔枝科紫玉盘属植物大花紫玉盘(Uvaria grandiflora)干燥根的化学成分进行系统地分离纯化,得到12个化合物,用现代波谱技术确定化合物的结构分别为:epicatechin-(4β→1′,2→O→2′)-phloroglucinol(1),proanthocyanidin A-1(2),proanthocyanidin A-2(3),表儿茶素(epicatechin)(4),phlorizin(5),圣草酚(eriodictyol)(6),erythro-guaiacylglycerol-8-O-4′-(coniferyl alcohol)ether(7),threo-guaiacylglycerol-8-O-4′-(coniferyl alcohol)ether(8),erythro-guaiacylglycerol-8-O-4′-(sinapyl alcohol)ether(9),threo-syringylglycerol-8-O-4′-(sinapyl alcohol)ether(10),burselignan(11),icariol A₂(12)。化合物1~12均为首次从该植物中分离得到,其中化合物1为新天然化合物。     

Antibacterial, antifungal and anthelmintic activities of root barks of Uvaria hookeri and Uvaria narum

On a pharmacological screening, substantial antibacterial, antifungal and anthelmintic activities were observed for the hexane and ethyl acetate extracts of the root barks of Uvaria narum Wall. and Uvaria hookeri King. Chromatographic fractionation of these extracts led to the isolation of the triterpenes glutinol, glutinone, taraxerol, β-sitosterol and Annonaceous acetogenins uvariamicins-I, II and III mixture, isodesacetyluvaricin, squamocin-28-one, narumicins-I and II stereoisomeric mixture, squamocin and panalicin. The acetogenins exhibited antimicrobial and anthelmintic activities in their individual screening comparable with standard drugs and hence their presence could be attributed to a great extent for the biocidal properties of U. narum and U. hookeri extracts.     

New polyoxygenated cyclohexenes from Uvaria calamistrata

Five new polyoxygenated cyclohexenes, named uvacalol A (1), B (2), C (3), D (4) and E (5) were isolated from the roots of Uvaria calamistrata. On the basis of spectral analysis and chemical derivatization, including the preparation of Mosher esters, the structures of compound 1-5 were established as (2R,3S,4R,5S)-2-acetoxyl-5-ethoxyl-1-benzoyloxymethylcyclohex-1(6)-ene-3,4-diol-3-benzoate, (2R,3S,4R,5S)-2-acetoxyl-5-ethoxyl-1-benzoyloxymethylcyclohex-1(6)-ene-3,4-diol-4-benzoate, (2R,3S,4R,5S)-5-ethoxyl-1-benzoyloxymethylcyclohex-1(6)-ene-2,3,4-triol-3-benzoate, (2R,3S,4R,5S)-3-methoxyl-1-benzoyloxymethylcyclohex-1(6)-ene-2,3,5-triol and (2R,3S,4R,5S)-2-acetoxyl-1-benzoyloxymethylcyclohex-1(6)-ene-3,4,5-triol-5-benzoate, respectively.