Protective effect of saponins from Argania spinosa against free radical-induced oxidative haemolysis

Saponins from Argania spinosa at a non-haemolytic concentration diminish by 53.2% erythrocyte haemolysis induced by free radicals. 2 mM aspirin and acetaminophen diminish by 75% and 68% , respectively, erythrocyte haemolysis induced by free radicals, while 0.3 muM vitamin E shows no significant antioxidant activity. Interestingly, a combination of 1 mg/l of A. spinosa saponins and vitamin E at 0.3 muM resulted in a 68% level of protection against free radical-induced erythrocyte haemolysis, which may suggest that A. spinosa saponins enhance the antioxidant effect of vitamin E. In contrast, no synergic effect was observed for acetaminophen (2 mM) when in combination with vitamin E (0.3 muM). These results demonstrate the antioxidant properties of saponins from A. spinosa and their ability to potentate the antioxidant effect of vitamin E.     

Cycloartane saponins from Astragalus peregrinus as modulators of lymphocyte proliferation

From Astragalus peregrinus, four cycloartane-type saponins have been isolated and their structures elucidated by spectral means as 20(R),24(S)-epoxy-9β,19-cyclolanostane-3β,6α,16β,25-tetrol 3-O-β- -glucopyranoside (1), 20(R),24(S)-epoxy-9β,19-cyclolanostane-3β,6α,16β,25-tetrol 3-O-α- -rhamnopyranosyl-(1→4)-β- -glucopyranoside (2), 20(R),24(S)-epoxy-9β,19-cyclolanostane-3β,6α,16β,25-tetrol 3-O-α- -rhamnopyranosyl-(1→2)-β- -glucopyranoside (3) and 20(R),25-epoxy-9β,19-cyclolanostane-3β,6α,16β,24(S)-tetrol (24-O-acetyl)- 3-O-α- -rhamnopyranosyl-(1→2)-(6′-O-acetyl)-β- -glucopyranoside (4). Compounds 2 and 3 showed to stimulate the proliferation of mouse splenocytes and were not significantly cytotoxic.     

Three new triterpenoid saponins from root of Gardenia jasminoides Ellis

Three new compounds (Gardeniside A–C), 11α,12α-epoxy-3β-[(O-β-D-glucuronopyranoside-6′-O-methly ester)oxy]olean-28,13-olide (1), siaresinolic acid 3-O-β-D-glucuronopyranoside-6′-O-methly ester (2), and 3-O-β-D- glucuronopyranoside-6′-O-methly ester-siaresinolic acid-28-O-β-D- glucopyranoside (3), with seven known compounds oleanolic acid 3-O-β-D- glucuronopyranoside-6′-O-methly ester (4), oleanolic acid 3-O-β-D- glucuropyranoside (5), hederagenin 3-O-β-D- glucuronopyranoside-6′-O- methly ester (6), chikusetsusaponin IVa methyl ester (7), chikusetsusaponin (8), chikusetsusaponin IVa butyl ester (9), siaresinolic acid 28-o-β-d-glucopyranosyl ester (10) were isolated from the root of Gardenia jasminoides Ellis. Six compounds (1, 4–7, and 9) showed cytotoxic activities against HeLa, A549, MCF-7 and A354-S2 cell lines.     

Studies on antidepressant and antinociceptive effects of ethyl acetate extract from Piper laetispicum and structure-activity relationship of its amide alkaloids

Piper laetispicum C.DC. (Piperaceae), is an endemic climbing, glabrous plant distributed in the southern part of China. A novel alkaloid amide, Laetispicine, from it has been proven to possess antidepressant activity. In this present study, antidepressant and antinociceptive effects of the ethyl acetate extract (EAE) of P. laetispicum have been studied in forced swimming, open field, acetic acid writhing and formalin tests in KM mice. A significantly antidepressant-like effect was showing at doses of higher than 60 mg/kg, which was not due to an increase in locomotive activity. The EAE also presented an analgesic effect, in our studies. At lower doses (30 mg/kg) the antinociceptive effect was likely mediated via peripheral inflammation and changes in central processing, and at higher doses (120 mg/kg) that was due to both central and peripheral pathways. We also quantitatively analyzed the major components of EAE by HPLC and approached the structure–activity relationship between structure of amide alkaloids and its antidepressant activities. The antidepressant effective components of EAE might be Leatispiamide A and Laetispicine. In their molecular structures, the isolated double bond from benzene ring and conjugated double bond located at 2–3 and 4–5 were necessary for its antidepressant activity.     

植物化感作用机理及其在园林植物配置中的应用

园林植物化感作用的研究对于园林植物配置的科学性和植物群落演替有着直接影响,同时也影响园林人工生态系统的稳定和功能发挥。通过分析园林植物的化感作用及其机理,阐述了植物化感作用在园林植物配置中的应用形式,指出了园林植物配置中利用植物化感作用,合理进行植物配置具有经济、生态等各方面的效益,能在一定程度上解决园林植物的可持续发展问题,为园林设计者提供了新的研究方向,有助于提高我国园林植物配置水平。     

Inhibitory effect of tanshinones on rat CYP3A2 and CYP2C11 activity and its structure-activity relationship

This study investigated the effect of tanshinones on rat liver microsomal CYP3A2 and 2C11 activity and explored the structure-activity relationship of tanshinones with CYP3A activity. Cryptotanshinone, tanshinone I and tanshinone IIA were competitive CYP3A2 inhibitors (K_i = 199-243 μM) and CYP2C11 inhibitors (K_i = 91-118 μM). Dihydrotanshinone was not only a noncompetitive inhibitor of CYP3A2 (K_i = 110 μM), but also a competitive CYP2C11 inhibitor (K_i = 55 μM). The structural difference between dihydrotanshinone and tanshinone I at C-15 position of furan ring resulted in the different modes of inhibition on CYP3A activity.     

土耳其棓子化学成分及抑菌活性的研究

对土耳其棓子的抑菌活性成分进行研究.采用硅胶柱色谱、SephadexLH-20凝胶柱色谱、制备薄层色谱、HPLC,对土耳其棓子中的化学成分进行分离,通过理化性质和光谱数据鉴定其结构,采用抑菌试验对土耳其棓子不同提取部位和单体化合物进行抑菌活性筛选.分离得到7个化合物,分别鉴定为:没食子酸(Ⅰ)、间-二没食子酸(Ⅱ)、对-二没食子酸(Ⅲ)、没食子酸甲酯(Ⅳ)、没食子酸乙酯(Ⅴ)、1,2,3,6-四-O-没食子酰基-β-D-葡萄糖(Ⅵ)和1,2,3,4,6-五-O-没食子酰基-β-D-葡萄糖(Ⅶ).土耳其棓子乙酸乙酯部位含主要抑菌活性成分,其中化合物Ⅲ和Ⅴ均为首次从该棓子中分离得到.     

柿叶化学成分及其抑菌活性研究

对柿叶的化学成分进行了定性分析和抗菌活性的研究.通过系统预试,初步确定柿叶中含有生物碱、皂苷、氨基酸、多肽、有机酸、酚类和鞣质、糖类、甾体、总黄酮、强心苷、蒽醌、挥发油等物质.抑制活性试验结果显示:乙醇提取物和乙酸乙酯萃取物对供试的6种细菌有较强的抑制作用;水相对供试的5种真菌有较强的抑制作用,而且对细菌有较小抑制作用;石油醚相对真菌和细菌几乎无抑制作用;正丁醇萃取物对细菌有不同程度的抑制作用,而对真菌无抑制作用.用不同质量浓度的乙酸乙酯提取物进行抑菌活性试验,结果显示:质量浓度越高,其抑菌能力越强,而且,在不同质量浓度下,对测试的6个细菌的抑制活性的大小顺序不一致.     

不同温度段苹果枝木醋液化学组成、抑菌及抗氧化活性比较

以苹果枝为原料,采用干馏法分3个温度段收集苹果枝木醋液.用GC-MS法分析各温度段苹果枝木醋液的有机成分,并对木醋液的抑菌活性和抗氧化活性进行测定.结果表明:3个温度段苹果枝木醋液的化学组成不同,含量差别较大,低温度段(100～200 ℃,AP_1)中检出45种物质,占整个出峰面积的91.26%,其中酚类含量为51.33%,有机酸酸含量为18.50%,酮类含量为8.98%,呋喃类含量为7.23%;中间温度段(200～310 ℃,AP_2)检出47种物质,占整个出峰面积的95.35%,其中酚类含量为24.69%,有机酸酸含量为40.05%,酮类含量为7.52%,呋喃类含量为12.81%;高温度段(310～500 ℃,AP_3)检出47种物质,占整个出峰面积的93.00%,其上述物质含量依次为34.66%,28.37%,12.49%和6.93%.有机酸在中间温度段木醋液中含量最多,酚类在低温度段含量最多.3个温度段的苹果枝木醋液均有抑菌和抗氧化活性,其抑菌活性顺序为AP_2＞AP_3＞AP_1,AP_2的抑菌活性最强,且与AP_1和AP_3的差异显著,其中对植物病原菌的EC_(50)为2.43～5.27 Mg·mL~(-1);抗氧化活性大小顺序为AP_1＞AP_3＞AP_2,且存在显著的量效关系,AP_1的抗氧化活性最强,均高于抗坏血酸和BHT.初步分析AP_2较强的抑菌活性和AP_1较强的抗氧化活性分别与其中高含量的有机酸和酚类物质有关.     

Larvicidal activity of saponin containing extracts and fractions of fruit mesocarp of Balanites aegyptiaca

Chloroform, ethyl acetate, butanol and methanol extracts of fruit mesocarp of Balanites aegyptiaca and five fractions from the methanol extract were tested against the Aedes aegypti mosquito larvae. All extracts showed larvicidal effects however the highest larval mortality was found in methanol extract. One fraction obtained from the silica gel column chromatography of the latter was found most effective for larval mortality. This fraction also interfered with adult emergence. A concentration of 0.0014% (w/v) of this active fraction showed inhibition of the 50% of the test larval population from emerging adults (EC(50)). The analysis of total saponin content of these tested extracts and fractions revealed a strong correlation between saponin content and larval mortality.     

苦竹叶化学成分对细菌及3种肿瘤细胞的抑制活性

【目的】评价苦竹叶提取物及其化学成分对细菌和3种肿瘤细胞的离体抑制生长活性,为竹叶化学成分的开发利用奠定基础。【方法】采用95%乙醇提取和柱色谱分离,从苦竹叶中获得提取物流分及单体化合物;以大肠杆菌、金黄色葡萄球菌及枯草芽孢杆菌为研究对象,采用抑菌圈法评价苦竹叶提取物各流分及单体化合物的离体抑菌活性;采用 MTT法和小鼠 H22肝癌细胞腹水瘤模型,评价木犀草素－6－C －洋地黄毒糖苷－4'－O －葡萄糖苷的体内外抗肿瘤活性。【结果】苦竹叶乙醇提取物萃取流分中,乙酸乙酯相的离体抑菌作用整体强于石油醚相和正丁醇相,水相抑菌作用不明显。乙酸乙酯相8个流分中 Fr．3的离体抑菌作用最强,在25 mg·mL －1浓度下,对枯草芽孢杆菌的离体抑菌作用最强,24 h抑菌圈直径为21.05 mm。25 mg·mL －1浓度下,单体化合物中从组分 Fr．4中分得的反式香豆酸对大肠杆菌和金黄色葡萄球菌的离体抑菌作用最强,24 h 的抑菌圈直径分别为20.23 mm及18.35 mm。离体试验表明,木犀草素－6－C－洋地黄毒糖苷－4'－O －葡萄糖苷对子宫颈癌 HeLa 细胞、肝癌 HepG2细胞及结肠癌 HT-29细胞具有明显的抑制增殖作用,IC50值分别为592,2058,1712 mg·L －1。5 mg·kg －1和10 mg·kg －1的木犀草素－6－C－洋地黄毒糖苷－4'－O －葡萄糖苷对 H22荷瘤鼠肝肿瘤有体内抑制作用,抑制率分别为2.9%和20.0%。【结论】苦竹叶化学成分具有一定的抑菌及抑制肿瘤增殖活性,在植物源农药及药物的开发利用方面具有一定的潜力。本研究为推进苦竹叶化学成分基础研究和促进苦竹叶资源的综合利用提供了依据。     

番石榴叶的化学成分与药理作用研究动态

简述国内外近年对番石榴叶化学成分与药理作用的研究动态,为该作物的应用研发提供有价值的参考。     

Chemical characteristics of saponins from Paris fargesii var. brevipetala and cytotoxic activity of its main ingredient, paris saponin H

More attention was paid to the anti-tumor activity of Rhizoma Paridis (RP) recently, of which the wild resource was decreased significantly. This study was aimed to elucidate the chemical characteristics of Paris fargesii var. brevipetala (PFB) that may be administrated as alternate resource of legal RP. A HPLC-ELSD method was established to characterize the steroid saponins in rhizomes of PFB and two legal Paris species [Paris polyphylla var. chinensis (PPC) and P. polyphylla var. yunnanensis (PPY)] in Chinese Pharmacopoeia (CP). Ten saponins (paris saponins I, II, V, VI, VII, H, gracillin and other three paris saponins) were involved as standards. The results indicated that PFB contained pennogenyl saponins as the main components with small amounts of diosgenin saponins. The total contents of the detected saponins in PFB ranged from 9.12mg/g to 85.33mg/g. Nine of the twelve PFB samples own a total content of paris saponins I, II, VI, and VII more than 6.0mg/g (meeting the standard of CP 2010 edition). Principal Component Analysis (PCA) and Partial Least Squares-Discriminate Analysis (PLS-DA) both confirmed the fact that saponin profiles of PFB, PPC and PPY were different from each other. In addition, paris saponin H (Ps H), the predominant saponin of PFB (>50%), was tested in vitro to evaluate its cytotoxic activities on HepG2, A549, RPE and L929 cells with a positive control of Cisplatin. Ps H showed a remarkable cytotoxic activity on A549 cells with an IC(50) value of 1.53±0.08μg/mL.     

香根鸢尾挥发油的化学成分分析及抗菌活性研究

采用GC-MS技术分析了新鲜的和自然陈化的鸢尾挥发油的化学组成,确定了各种成分的化学结构与GC含量,并采用滤纸片琼脂平板扩散法与微量肉汤稀释法针对3种真菌和12种细菌(包括7种临床致病菌)进行了挥发油的药敏实验。结果表明:新鲜鸢尾挥发油共鉴定出26种成分,占总峰面积的92.09%,由醛类、酮类、酸类、酯类等化合物组成,其中十四酸(31.77%)、己酸(15.33%)、3-甲基丁酸(12.20%)、戊酸(9.29%)、庚酸(7.91%)、3-甲基戊酸(7.25%)、辛酸(2.44%)、2,4′-二羟基-3′-甲基苯乙酮(1.04%)是主要成分;自然陈化3年鸢尾挥发油共鉴定出45种成分,占总峰面积的85.63%,主要由醛类、酮类、酸类、酯类、醇类、酚类等化合物组成,其中十四酸(28.02%)、十四酸乙酯(10.42%)、(Z,Z)-9,12-十八碳二烯酸(7.67%)、十二酸(6.41%)、己酸(5.14%)、十六酸(4.44%)、十二酸乙酯(4.09%)、亚油酸乙酯(3.87%)、十六酸乙酯(3.13%)、油酸乙酯(2.85%)、6-甲基-α-紫罗兰酮(1.39%)、n-癸酸(1.31%)是主要成分;新鲜鸢尾挥发油对大部分微生物均具有很好的抗菌作用,其最低抑菌浓度(MIC)为0.25g/L,最低杀菌浓度(MBC)为0.35g/L;自然陈化3年鸢尾挥发油对大部分微生物均具有很好的抗菌作用,其MIC为0.05g/L,MBC为0.08g/L。     

光叶拟单性木兰挥发油的化学成分及其生物活性的初步研究

采用水蒸气蒸馏法(SD)提取光叶拟单性木兰叶片中的挥发油,用气相色谱-质谱(GC-MS)联用技术分析挥发油的成分,鉴定出34个化合物。其主要成分为1R-α-蒎烯(7.432%)、香桧烯(13.516%)、β-松节烯(7.615%)、间-甲基异丙基苯(7.21%)、桉油醇(7.139%)、松油-4-醇(5.004%)、β-石竹烯(5.577%)、β-荜澄茄烯(4.435%)。体外抑菌和抗肿瘤实验表明,光叶拟单性木兰挥发物质对大肠杆菌、金黄色葡萄球菌、红酵母有一定的抑制作用;对人非小细胞肺癌(NCI-H460)、胃腺癌(SGC-7901)有较强的抑制作用,当挥发油质量浓度为50μg.mL-1时,抑制率分别达到83.24%、72.26%。     

杨树木醋液的化学成分分析及抑菌试验

对于馏法制取、不同温度段采集到的杨树木醋液的抑菌效果进行研究,并对高温度段的化学成分用GC-MS进行分析.结果表明:150～300 ℃温度段木醋液除对大肠杆菌抑制效果差于对照庆大霉素外,对其他细菌的抑制作用均强于抗菌素;300～510℃温度段木醋液抑菌效果均好于对照庆大霉素,说明高温度段的木醋液具有很强的抑菌作用.300～510℃收集的木醋液约含有41种化学成分,其中主要成分为酸类、酚类、酮类、醇类、醛类和酯类等.在所有化合物中,乙酸含量最高,占总量的17.10%,其次为苯酚,含量为11.36%.初步分析确定其抑菌活性成分为乙酸和酚类物质.     

核桃楸树皮提取物的化学成分及其抗氧化活性研究

研究了核桃楸树皮的化学成分及其抗氧化活性.采用Sephadex LH-20柱色谱及薄层色谱等方法进行分离,从其70%丙酮提取物乙酸乙酯及水溶性部分中分到11种化合物,经波谱分析及理化性质鉴定化合物分别为:短叶松素(1)、花旗松素(2)、蛇葡萄素(3)、山奈酚(4)、槲皮素(5)、杨梅素(6)、阿福豆苷(7)、紫云英苷(8)、槲皮苷(9)、异槲皮苷(10)、杨梅苷(11).化合物1、3、5、6、8、10为首次从该植物中分得.经DPPH试验,测定了正己烷溶性、二氯甲烷溶性、乙酸乙酯溶性和水溶性部分以及粗提物和分得化合物的抗氧化活性.其中乙酸乙酯和水溶性部分及化合物1～6与对照组相比具有很强的抗氧化活性.     

竹叶主要化学成分分析及其生物活性研究现状

就竹叶中黄酮类、活性多糖、氨基酸等主要化学成分及其生物活性研究现状进行了综述。     

Anti-thrombotic activity and chemical characterization of steroidal saponins from Dioscorea zingiberensis C.H. Wright

Steroidal saponins have long attracted scientific attention, due to their structural diversity and significant biological activities. Total steroidal saponins (TSS) extracted from the rhizomes of Dioscorea zingiberensis C.H. Wright (DZW) constitute an effective treatment for cardiovascular disease. However, the active constituents contained in DZW rhizomes and their pharmacological properties are not fully understood. The aim of this work is to determine and quantify the active constituents in DZW rhizomes using fingerprint technique, and evaluate its anti-thrombotic activity using inferior vena cava ligation thrombosis rat model and pulmonary thrombosis mice model after being gavaged with TSS for 1 or 2 weeks. In the study, a chemical fingerprint method was firstly established and validated to quantify and standardize TSS from DZW rhizomes including parvifloside, protodeltonin, protodioscin, protogracillin, zingiberensis saponin, deltonin, dioscin and trillin. TSS extracted from DZW rhizomes were showed to have the inhibitions on platelet aggregation (PAG) and thrombosis, and prolong activated partial thromboplastin time (APTT), thrombin time (TT), and prothrombin time (PT) in a dose-dependent manner in rats. TSS also prolonged the bleeding time and clotting time in a dose-dependent manner in mice. The results indicate that TSS could inhibit thrombosis by both improving the anticoagulation activity and inhibiting PAG action, suggesting that TSS from DZW rhizomes have the potential to reduce the risk of cardiovascular diseases by anti-thrombotic action.     

不同提取方法山苍子油的化学成分与抗氧化活性分析

【目的】比较不同提取方法对山苍子油提取效率与抗氧化活性的影响,通过 GC-MS分析,研究山苍子油成分构成与抗氧化活性的内在关联,分析山苍子油抗氧化活性的主要物质基础。【方法】采用液液萃取(分别加以超声波与磁化辅助处理)、二氧化碳超临界萃取以及水蒸气蒸馏法提取山苍子油,DPPH 法比较不同提取方式对山苍子油抗氧化活力的影响,GC-MS分析山苍子油的主要成分,并以1,4－二溴苯为内标,采用面积归化法解析主要成分的相对含量。【结果】山苍子油具有显著的抗氧化活性。液液萃取法的提取效率与山苍子油抗氧化活性最高,超声波辅助处理油得率最高,为26.3%,磁化辅助处理抗氧化活性最优,达到31.22 mg·mL －1( IC50),二氧化碳超临界萃取法次之,抗氧化活性为56.95 mg·mL －1( IC50),水蒸气蒸馏法抗氧化活性最弱,为64.95 mg·mL －1( IC50); GC-MS分析检测出122种以上的化合物,包括12种脂肪酸,16种萜烯,18种含氧萜烯以及其他微量化合物包括烯烃、醇、酮类与烷烃等。GC-MS分析结果表明：山苍子干果主要成分为饱和脂肪酸(月桂酸等)、不饱和脂肪酸(9,12－十八碳二烯酸、9－十八碳烯酸等)以及α蒎烯、β蒎烯、柠檬烯等萜烯、氧化萜烯类物质。液液萃取法得到的山苍子油脂肪酸含量(53.51%～66.61%)明显高于二氧化碳超临界萃取(17.64%)与水蒸气蒸馏法(8.1%),而二氧化碳超临界萃取与水蒸气蒸馏法得到的萜烯、氧化萜烯类含量分别达到29.37%和17.69%,明显高于液液萃取法(6.49%～9.75%)。【结论】磁化辅助处理有利于抗氧化活性物质的提取,且不饱和脂肪酸的含量最高;超声波辅助处理可以提升油的得率;水蒸气蒸馏法和超临界流体萃取法更有利于萜烯类化合物的获取;联系到水蒸气蒸馏法得到的山苍子油富含萜烯化合物却显示较低的抗氧化活性(64.95 mg·mL －1 ),色谱级的柠檬醛抗氧化活性最低(74.33 mg·mL －1),因此推测脂肪酸成分(特别是不饱和脂肪酸)是山苍子油抗氧化活性的主要物质基础。