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Thai pigmented rice bran extracts inhibit production of superoxide, nitric oxide radicals and inducible nitric oxide synthase in cellular models
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作者 Kedsara Junmarkho Pintusorn Hansakul 《亚太热带生物医学杂志:英文版》 CAS 2019年第7期291-298,共8页
Objective:To study the inhibitory effect of rice bran extracts of Thai black Kam Muang and red Hawm Dawk Mali Deang on oxidative stress factors including superoxide(O2·-),nitric oxide(NO·),and inducible nitr... Objective:To study the inhibitory effect of rice bran extracts of Thai black Kam Muang and red Hawm Dawk Mali Deang on oxidative stress factors including superoxide(O2·-),nitric oxide(NO·),and inducible nitric oxide synthase(iNOS).Methods:Bran extracts(40%ethanol)of Kam Muang and Hawm Dawk Mali Deang were obtained and evaluated for in vitro 2-2′-azino-di-(3-ethylbenzthiazoline sulfonate)(ABTS)and NO·scavenging activity.Their inhibitory effects on cellular O2·-and NO·were measured in phorbol 12-myristate 13-acetate-stimulated neutrophil-like HL-60 cells and lipopolysaccharidestimulated RAW264.7 macrophages,respectively,and their viability was monitored using the MTT assay.The effect on iNOS expression was also assessed by the Western blotting assay.Total contents of phenolics,flavonoids,and subtypes were also determined.Results:Hawm Dawk Mali Deang exhibited about 3.5-fold greater cellular O2·-inhibitory activity than Kam Muang[EC50 values of(23.57±4.54)and(81.98±1.45)μg/mL,respectively]in phorbol 12-myristate 13-acetate-stimulated HL-60 cells.Hawm Dawk Mali Deang exhibited about 2-fold higher in vitro ABTS·+and NO·scavenging activity than Kam Muang,but it exerted cellular NO·inhibitory activity of only about 26%(undetermined EC50 value)in lipopolysaccharide-stimulated RAW264.7 cells.Conversely,Kam Muang exerted potent cellular NO·inhibitory activity[EC50 value:(281.13±59.18)μg/mL]and dose-dependently decreased iNOS levels.No cytotoxicity of both extracts was detected in both cell types.As for corresponding contents,Hawm Dawk Mali Deang contained higher contents of phenolics and flavonoids than Kam Muang.Moreover,Kam Muang and Hawm Dawk Mali Deang had a high content of total anthocyanins[(14.73±0.52)mg C3GE/g of extract]and total proanthocyanidins[(115.13±1.47)mg CE/g of extract],respectively.Conclusions:Based on these data,bran extracts of Thai black Kam Muang and red rice Hawm Dawk Mali Deang can help lower oxidative stress and inflammation attributed partly to O2·-and NO·. 展开更多
关键词 PIGMENTED rice BRAN EXTRACTS Nitric oxide INHIBITORY ACTIVITY Superoxide radical INHIBITORY ACTIVITY iNOS
Vitellaria paradoxa nutshells from seven sub-Saharan countries as potential herbal medicines for treating diabetes based on chemical compositions, HPLC fingerprints and bioactivity evaluation
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作者 LI Da XIAO Jian-Qi +7 位作者 LIU Wen-Yuan ZHANG Chao-Feng AKIHISA Toshihiro ABE Masahiko MASTERS Eliot-T. ZHAI Wei-Wei FENG Feng ZHANG Jie 《中国天然药物:英文版》 SCIE CAS CSCD 2019年第6期446-460,共15页
The aim of the study was to determine the feasibility of the Vitellaria paradoxa nutshell as a new medicinal resource for treating diabetes. A total of forty-one compounds were identified by HPLC-DAD-Q-TOF-MS and phyt... The aim of the study was to determine the feasibility of the Vitellaria paradoxa nutshell as a new medicinal resource for treating diabetes. A total of forty-one compounds were identified by HPLC-DAD-Q-TOF-MS and phytochemical methods in V. paradoxa nutshell methanol extract. Based on HPLC fingerprints, four characteristic constituents were quantified and the origin of twenty-eight V. paradoxa nutshells from seven sub-Saharan countries was compared, which were classified into three groups with chemometric method. Twenty-eight samples contained high total phenolic content, and exhibited moderate-higher antioxidant activity and strong α-glucosidase inhibitory activity. Furthermore, all fractions and isolated compounds were evaluated for their antioxidant and α-glucosidase inhibitory activities, and α-glucosidase inhibitory action mechanism of four characteristic constituents including protocatechuic acid, 3, 5, 7-trihydroxycoumarin,(2 R, 3 R)-(+)-taxifolin and quercetin was investigated via molecular docking method, which were all stabilized by hydrogen bonds with α-glucosidase. The study provided an effective approach to waste utilization of V. paradoxa nutshell, which would help to resolve waste environmental pollution and provide a basis for developing potential herbal resource for treating diabetes. 展开更多
关键词 Vitellaria paradoxa HPLC FINGERPRINTS Antioxidant ACTIVITY Α-GLUCOSIDASE INHIBITORY ACTIVITY Molecular DOCKING
Bioactive phenazines from an earwig-associated Streptomyces sp.
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作者 HAN Hao GUO Zhi-Kai +6 位作者 ZHANG Bo ZHANG Mei SHI Jing LI Wei JIAO Rui-Hua TAN Ren-Xiang GE Hui-Ming 《中国天然药物:英文版》 SCIE CAS CSCD 2019年第6期475-480,共6页
Three new phenazine-type compounds, named phenazines SA–SC(1–3), together with four new natural products(4–7), were isolated from the fermentation broth of an earwig-associated Streptomyces sp. NA04227. The structu... Three new phenazine-type compounds, named phenazines SA–SC(1–3), together with four new natural products(4–7), were isolated from the fermentation broth of an earwig-associated Streptomyces sp. NA04227. The structures of these compounds were determined by extensive analyses of NMR, high resolution mass spectroscopic data, as well as single-crystal X-ray diffraction measurement. Sequencing and analysis of the genome data allowed us to identify the gene cluster(spz) and propose a biosynthetic pathway for these phenazine-type compounds. Additionally, compounds 1–5 exhibited moderate inhibitory activity against acetylcholinesterase(AChE), and compound 3 showed antimicrobial activities against Micrococcus luteus. 展开更多
关键词 Earwig-associated ACTINOMYCETE PHENAZINE Biosynthetic pathway Antimicrobial ACTIVITY Acetylcholinesterase inhibitory ACTIVITY
Design, Synthesis, Biological Activity and Molecular Docking Study of Coumarin Derivatives Bearing 2-MethyIbiphenyl Moiety
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作者 MA Junjie HUANG Kun +3 位作者 NI Xin CHEN Roufen XU Boxuan WANG Cuifang 《高等学校化学研究:英文版》 SCIE CAS CSCD 2019年第3期410-417,共8页
A hybrid pharmacophore approach was used to design and synthesize a series of coumarin derivatives bearing 2-methylbiphenyl moiety, which were evaluated for their in vitro anticancer activities against four cancer cel... A hybrid pharmacophore approach was used to design and synthesize a series of coumarin derivatives bearing 2-methylbiphenyl moiety, which were evaluated for their in vitro anticancer activities against four cancer cell lines(MCF-75 A549, H460 and HT29) and PD-1/PD-L1 inhibitory activities. Moreover, several compounds with excellent anticancer activities were selected to evaluate the cytotoxicities against one normal cell line(HEK-293). The most promising compound llo showed the best anticancer activities against the four tested cancer cell lines with the IC50 values of 6.45, 8.65, 6,57 and 8.13 gmol/L, respectively, and displayed weak cytotoxicity on the normal cell(HEK-293). Furthermore, screening of PD-1 /PD-L1 inhibitory activity revealed that compound llo could effectively inhibit the binding of PD-1/PD-L1, and the binding interactions of compound llo with PD-L1 protein were explored by molecular docking. All above evidences showed that compound llo might be worthy of further study as a valuable leading compound for the treatment of cancer. 展开更多
关键词 COUMARIN 2-Methylbiphenyl Anticancer ACTIVITY PD-1/PD-L1 inhibitory ACTIVITY MOLECULAR docking
龙眼叶提取物对α-葡萄糖苷酶抑制活性研究
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作者 黄春燕 梁洁 +3 位作者 黄团心 麦嘉妮 徐晖 杨川川 《亚太传统医药》 2019年第1期7-9,共3页
目的:研究龙眼叶不同提取物对α-葡萄糖苷酶的抑制活性。方法:通过建立体外α-葡萄糖苷酶抑制模型,对龙眼叶提取物进行活性筛选,并对提取物浓度与抑制活性关系进行研究。结果:龙眼叶乙酸乙酯提取物(IC50=0.105 2mg/mL)和正丁醇提取物(IC... 目的:研究龙眼叶不同提取物对α-葡萄糖苷酶的抑制活性。方法:通过建立体外α-葡萄糖苷酶抑制模型,对龙眼叶提取物进行活性筛选,并对提取物浓度与抑制活性关系进行研究。结果:龙眼叶乙酸乙酯提取物(IC50=0.105 2mg/mL)和正丁醇提取物(IC50=0.1261mg/mL)均有较好的α-葡萄糖苷酶抑制作用,抑制活性大于阳性对照药阿卡波糖(IC50=0.1960mg/mL),且抑制活性呈浓度依赖性。结论:龙眼叶乙酸乙酯和正丁醇提取物对α-葡萄糖苷酶活性有抑制作用,具有开发治疗糖尿病降血糖药物的价值。 展开更多
关键词 龙眼叶 Α-葡萄糖苷酶 抑制活性
New dammarane-type saponins from the leaves of Panax notoginseng
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作者 Jiwu Huang Chuangjun Li +5 位作者 Junzi Cao Jie Ma Yiqian Du Xinyi Liu Jingzhi Yang Dongming Zhang 《中国化学快报:英文版》 SCIE CAS CSCD 2019年第2期447-450,共4页
Two new triterpenoid saponins named notoginsenoside-Ng3(1) and notoginsenoside-Ng4(2) along with three known saponins (3-5), were isolated from a water extract of the leaves of Panax notoginseng. Their structures were... Two new triterpenoid saponins named notoginsenoside-Ng3(1) and notoginsenoside-Ng4(2) along with three known saponins (3-5), were isolated from a water extract of the leaves of Panax notoginseng. Their structures were elucidated by HRESIMS, NMR, X-ray techniques and acid hydrolysis. Moreover,compound 2 was characterized with the conjugated double bonds side-chain, which was rarely found in this plant. The absolute configuration of notoginsenoside Fa (3) with five sugars was confirmed by the single-crystal X-ray diffraction for the first time. Acetylcholinesterase inhibitory activity experiments were also conducted, all the isolated saponins showed weak inhibitory activities in the final concentration of 0.16 mmol/L. 展开更多
关键词 PANAX notoginseng Notoginsenoside-Ng3 Notoginsenoside-Ng4 SINGLE-CRYSTAL X-ray diffraction ACETYLCHOLINESTERASE inhibitory activity
国产绿奇楠沉香的化学成分研究 预览
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作者 李薇 梅文莉 +3 位作者 董文化 蔡彩虹 盖翠娟 戴好富 《热带亚热带植物学报》 CAS CSCD 北大核心 2019年第2期196-202,共7页
为了解国产绿‘奇楠’沉香的化学成分,采用色谱和波谱方法从其乙醚和乙醇提取物中分离鉴定了7个化合物,分别鉴定为顺式-7-羟基菖蒲烯(1),(5R,6R,7S,8R)-2-(苯乙基)-6,7,8-三羟基-5,6,7,8-四氢-5-[2-(2-苯乙基)色酮基-6-氧代]色酮(2), 1... 为了解国产绿‘奇楠’沉香的化学成分,采用色谱和波谱方法从其乙醚和乙醇提取物中分离鉴定了7个化合物,分别鉴定为顺式-7-羟基菖蒲烯(1),(5R,6R,7S,8R)-2-(苯乙基)-6,7,8-三羟基-5,6,7,8-四氢-5-[2-(2-苯乙基)色酮基-6-氧代]色酮(2), 1-羟基-1,5-二苯基戊-3-酮(3),丁香树脂酚葡萄糖苷(4),(3β)-齐墩果-12-烯-3,23-二醇(5),β-谷甾醇(6)和棕榈酸-α-单甘油酯(7)。化合物1、3~5和7均为首次从沉香中分离得到,其中化合物1表现出非常甜的芳香气味。乙酰胆碱酯酶体外抑制活性测试结果表明,50μmol L–1的化合物1对乙酰胆碱酯酶抑制率为(49.9±1.4)%。 展开更多
关键词 奇楠 沉香 化学成分 乙酰胆碱酯酶 抑制活性
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沙葱水提液体外抗氧化及α-葡萄糖苷酶与胰脂肪酶抑制作用的研究 预览
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作者 王婉愉 李姣 +2 位作者 王霄凯 张晓峰 吕全军 《食品研究与开发》 CAS 北大核心 2019年第3期1-6,共6页
以新鲜沙葱为原料,用纯水对其进行提取,并且以该取提液为研究对象,测定其中的黄酮含量,通过测定1,1-二苯基-2-苦肼基自由基(DPPH·)清除能力来评价沙葱水提液的体外抗氧化活性,并分别采用α-葡萄糖苷酶与胰脂肪酶抑制模型研究其对α... 以新鲜沙葱为原料,用纯水对其进行提取,并且以该取提液为研究对象,测定其中的黄酮含量,通过测定1,1-二苯基-2-苦肼基自由基(DPPH·)清除能力来评价沙葱水提液的体外抗氧化活性,并分别采用α-葡萄糖苷酶与胰脂肪酶抑制模型研究其对α-葡萄糖苷酶和胰脂肪酶活性的抑制作用。结果显示:沙葱中总黄酮含量为4.02 mg QE/g DW,对DPPH自由基有显著的清除活性,测定得到的Trolox等价抗氧化能力为51.82 mg Trolox/g,半抑制浓度(half maximal inhibitory concentration,IC50)为0.867mg/mL,对α-葡萄糖苷酶和胰脂肪酶活性抑制的IC50值分别为326.29mg/mL和179.48 mg/mL,且都呈明显的质量浓度依赖关系。结果表明,沙葱中黄酮含量丰富,有显著的体外抗氧化活性,并且有良好的α-葡萄糖苷酶与胰脂肪酶抑制活性,有深入开发研究的价值。 展开更多
关键词 沙葱 抗氧化 DPPH自由基 Α-葡萄糖苷酶 胰脂肪酶 抑制活性
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Taraxastane-type triterpenoids from the medicinal and edible plant Cirsium setosum
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作者 LIN Peng-Cheng JI Lin-Lin +4 位作者 ZHONG Xiang-Jian LI Jin-Jie WANG Xin SHANG Xiao-Ya LIN Sheng 《中国天然药物:英文版》 SCIE CAS CSCD 2019年第1期22-26,共5页
Guided by TNF-α secretion inhibitory activity assay, four taraxastane-type triterpenoids, including two new ones, 22-oxo-20-taraxasten-3β, 30-diol(1) and 22α-hydroxy-20-taraxasten-30β, 30-triol(2), have been obtai... Guided by TNF-α secretion inhibitory activity assay, four taraxastane-type triterpenoids, including two new ones, 22-oxo-20-taraxasten-3β, 30-diol(1) and 22α-hydroxy-20-taraxasten-30β, 30-triol(2), have been obtained from an active fraction of the petroleum ether-soluble extract of the the medicinal and edible plant Cirsium setosum. Their structures were elucidated by spectroscopic data and CD data analysis. In the TNF-α secretion inhibitory activity assay, compounds 1 and 2 were active with the IC50 of 2.6 and 3.8 μmol·L-1, respectively. In addition, compounds 1 and 2 showed moderately selective cytotoxicity against the human ovarian cancer(A2780) and colon cancer(HCT-8) cell lines. 展开更多
关键词 CIRSIUM setosum Taraxastane-type TRITERPENOID TNF-α secretion INHIBITORY activity Cytotoxicity
柑橘类果皮提取物对荞麦立枯丝核菌的抑制作用 预览 被引量:1
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作者 江兰 赵江林 +4 位作者 汤焘 李兴 钟灵允 袁健 赵钢 《贵州农业科学》 CAS 2019年第3期59-63,共5页
为柑橘皮的综合利用及荞麦立枯病新型防治药剂的开发研制提供依据,采用菌丝生长速率法检测6种柑橘(蜜柚、脐橙、椪柑、柠檬、不知火和沙糖橘)果皮提取物对荞麦立枯丝核菌菌丝生长的抑制活性。结果表明:6种柑橘果皮提取物对荞麦立枯丝核... 为柑橘皮的综合利用及荞麦立枯病新型防治药剂的开发研制提供依据,采用菌丝生长速率法检测6种柑橘(蜜柚、脐橙、椪柑、柠檬、不知火和沙糖橘)果皮提取物对荞麦立枯丝核菌菌丝生长的抑制活性。结果表明:6种柑橘果皮提取物对荞麦立枯丝核菌菌丝生长均表现出一定的抑制作用,其活性大小与提取物种类和供试浓度相关;醇提物的抑制活性均较相应水提物高。其中,浓度为6.0mg/mL时,沙糖橘果皮醇提物对荞麦立枯丝核菌的抑制作用最强,抑制率为75.2%;其次为蜜柚、柠檬和椪柑的果皮醇提物,抑制率分别为66.0%、60.1%和57.3%;不知火和脐橙果皮提取物的抑制活性相对较弱。沙糖橘、蜜柚、柠檬和椪柑果皮醇提物对荞麦立枯丝核菌的抑制中浓度(IC50)分别为1.29mg/mL、2.07mg/mL、2.57mg/mL和3.80mg/mL。 展开更多
关键词 荞麦 立枯丝核菌 柑橘类果皮 提取物 抑制活性
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衍生合成七种氮杂糖成分及其抑制α-葡萄糖苷酶构效关系分析 预览
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作者 晏仁义 李琼娅 +1 位作者 徐冰 陈若芸 《天然产物研究与开发》 CAS CSCD 北大核心 2019年第7期1216-1219,1284共5页
以白树(Suregada glomerulata)中分离得到的五个氮杂糖成分为底物,在其N上衍生合成,分析N上衍生基团对α-葡萄糖苷酶抑制活性的影响。分别合成了N-甲基化、N,N-二甲基化、N-丁基化和N-氧化衍生物,体外测试化合物的α-葡萄糖苷酶抑制活... 以白树(Suregada glomerulata)中分离得到的五个氮杂糖成分为底物,在其N上衍生合成,分析N上衍生基团对α-葡萄糖苷酶抑制活性的影响。分别合成了N-甲基化、N,N-二甲基化、N-丁基化和N-氧化衍生物,体外测试化合物的α-葡萄糖苷酶抑制活性。合成了7个未见文献报道的目标化合物,结构经1HNMR、13CNMR和MS确证。初步药理结果显示,所有衍生物均未见增强α-葡萄糖苷酶抑制活性。N-取代基对活性的影响较大;化合物5属于N,N-二取代衍生物,仍具有一定的α-葡萄糖苷酶抑制活性,值得进一步研究。 展开更多
关键词 氮杂糖 白树 Α-葡萄糖苷酶 抑制活性
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对峙培养法在生防菌抑制效果研究中的应用 预览
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作者 田书鑫 刘南南 王桂清 《河南农业科学》 北大核心 2019年第8期1-6,共6页
对峙培养法是明确有益微生物或其次生代谢产物的抑(杀)菌效果和作用范围时必须采用的方法,是研制开发微生物农药的第一步。按操作方式的不同,对峙培养法具体分为四大类,包括菌饼法、菌液法、划线法和扩散法。详细概述了不同对峙培养法... 对峙培养法是明确有益微生物或其次生代谢产物的抑(杀)菌效果和作用范围时必须采用的方法,是研制开发微生物农药的第一步。按操作方式的不同,对峙培养法具体分为四大类,包括菌饼法、菌液法、划线法和扩散法。详细概述了不同对峙培养法的应用范围、特点和操作流程,比较了彼此间的异同,为在抑菌试验中正确选择合适的对峙培养方法提供了有力的依据。 展开更多
关键词 生物防治 对峙培养法 抑菌活性 应用
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Moving fast,thinking fast:The relations of physical activity levels and bouts to neuroelectric indices of inhibitory control in preadolescents
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作者 Dominika M.Pindus Eric S.Drollette +9 位作者 Lauren B.Raine Shih-Chun Kao Naiman Khan Daniel R.Westfall Morgan Hamill Rebecca Shorin Emily Calobrisi Dinesh John Arthur F.Kramer Charles H.Hillman 《运动与健康科学:英文版》 SCIE 2019年第4期301-314,共14页
Background:Structured vigorous physical activity(VPA)can improve cognitive control in children,but studies relating daily physical activity(PA)to cognitive control have yielded conflicting findings.While objectively m... Background:Structured vigorous physical activity(VPA)can improve cognitive control in children,but studies relating daily physical activity(PA)to cognitive control have yielded conflicting findings.While objectively measured daily PA summarizes all occurrences of PA within a registered period,a minimum duration of continuous PA is required for registration of a PA bout.Because brief bouts of high-intensity PA can account for a large proportion of children’s daily activity-related energy expenditure,this study assessed whether daily and bouted VPA were selectively related to cognitive control in preadolescents relative to other PA intensities.Methods:A total of 75 children between the ages of 8 and 10 years(49%girls)wore an ActiGraph wGT 3 X+on the hip for 7 days.The acceleration signal from the vertical axis was summarized over 1 s,5 s,and 15 s epochs.Daily and boutecd modercate PA,moderate-to-vigorous PA,and VPA were measured.PA bouts were expressed as the frequency and time spent in 2 different continuous PA bouts,one lasting≥10 s and the other lasting≥30 s at a given intensity.Inhibitory control was assessed using behavioral responses to a modified flanker task(mean reaction time(RTmean)and accuracy).Attentional resource allocation and co gnitive processing speed were measured using the amplitude and latency of the P3 component of event-related brain potentials,respectively.Associations between PA,behavioral indices of inhibitory control,P3 amplitude,and latency were assessed using hierarchical regression models.Results:Daily VPA was not related to RTmean or accuracy on either congruent or incongruent trials.In contrast,more time spent in VPA bouts lasting≥30 s predicted shorter P3 latency across epochs and flanker congruencies(allβ≤-0.24,all p≤0.04).The associations between shorter P3 latency and the time spent in moderate-to-vigorous PA bouts lasting≥30 s were less consistent and largely limited to congruent trials(congruent:β(-0.3 1,-0.34)).No significant associations were observed upon corr 展开更多
关键词 ACCELEROMETRY Bouts Children ERPS INHIBITORY control P3 Physical activity
白鲜皮化学成分及其α-葡萄糖苷酶抑制活性 预览
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作者 杨晓军 艾凤凤 +1 位作者 蔺军兵 汤江江 《中国药科大学学报》 CAS CSCD 北大核心 2019年第1期41-45,共5页
采用硅胶、凝胶柱色谱方法对白鲜皮( Dictamnus dasycarpu s)的化学成分进行分离纯化。从其石油醚部位分离得到了5个化合物,利用IR、MS和NMR等技术对分离得到的化合物进行了结构鉴定。5个化合物的结构分别为:二十二烷醇( 1 )、2,2-二二... 采用硅胶、凝胶柱色谱方法对白鲜皮( Dictamnus dasycarpu s)的化学成分进行分离纯化。从其石油醚部位分离得到了5个化合物,利用IR、MS和NMR等技术对分离得到的化合物进行了结构鉴定。5个化合物的结构分别为:二十二烷醇( 1 )、2,2-二二苯甲基-3,3-二苯基丙酸乙酯( 2 )、柠檬苦素( 3 )、黄柏酮( 4 )和白鲜碱( 5 )。其中化合物 2 为新化合物,化合物 1 首次从该植物中分离得到。采用PNPG 法筛选化合物的α-葡萄糖苷酶抑制活性。结果表明化合物 3 ~ 5 表现出较好的α-葡萄糖苷酶的抑制活性。该结果为白鲜皮的深度开发利用提供了理论依据。 展开更多
关键词 白鲜皮 化学成分 Α-葡萄糖苷酶 抑制活性 糖尿病
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酸荔枝核提取物对α-葡萄糖苷酶的抑制作用
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作者 陈华妮 李容 +2 位作者 陆海峰 黄敬文 钱力 《食品工业》 CAS 北大核心 2019年第5期59-61,共3页
探讨酸荔枝提取物对α-葡萄糖苷酶的抑制活性。将酸荔枝干燥核粉碎,用乙醇超声波法提取,对提取物用石油醚、乙酸乙酯、正丁醇进行萃取。采用α-葡萄糖苷酶体外活性抑制模型,测定酸荔枝的4种提取物对α-葡萄糖苷酶的抑制活性。结果表明,... 探讨酸荔枝提取物对α-葡萄糖苷酶的抑制活性。将酸荔枝干燥核粉碎,用乙醇超声波法提取,对提取物用石油醚、乙酸乙酯、正丁醇进行萃取。采用α-葡萄糖苷酶体外活性抑制模型,测定酸荔枝的4种提取物对α-葡萄糖苷酶的抑制活性。结果表明,这4种提取物对α-葡萄苷酶活性有较强的抑制作用,抑制活性均高于阿卡波糖,其中水部位的抑制作用最强,提示酸荔枝在抗糖尿病产品开发方面具有很好的应用前景。试验揭示酸荔枝核提取物对α-葡萄糖苷酶具有一定抑制作用。 展开更多
关键词 酸荔枝核 Α-葡萄糖苷酶 抑制活性
中药有效成分抗宫颈癌作用机制的研究进展
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作者 苏敏 龚小见 周欣 《中国中药杂志》 CAS CSCD 北大核心 2019年第4期675-684,共10页
宫颈癌是威胁女性健康的第二大癌症,因其极高的死亡率而备受国内外研究者的关注。目前,大多采用放射性治疗及化学药物治疗癌症的副作用较大,而中药有效成分在抗肿瘤方面有着多途径、多环节、多靶点、毒副作用小等优势,已成为抗癌药物的... 宫颈癌是威胁女性健康的第二大癌症,因其极高的死亡率而备受国内外研究者的关注。目前,大多采用放射性治疗及化学药物治疗癌症的副作用较大,而中药有效成分在抗肿瘤方面有着多途径、多环节、多靶点、毒副作用小等优势,已成为抗癌药物的重点研发对象。近年来,相关科研人员对中药有效成分作用于人宫颈癌细胞的体外抑制活性及作用机制研究尤为活跃。文章拟从中药提取物、多糖、生物碱、皂苷、黄酮类、萜类、醌类、挥发油、酯类、酚类、砷剂类、蛋白组分等中药有效成分为出发点,以抗宫颈癌作用机制即抑制细胞增殖,诱导癌细胞凋亡;抑制细胞侵袭、迁移及黏着斑激酶(FAK)磷酸化;抑制血管内皮生长因子(VEGF)过表达;干扰细胞有丝分裂;抑制端粒酶活性;调节细胞信号通路;下调HPV E6基因表达;调节机体免疫能力为主要内容,对宫颈癌细胞的体外抑制活性与作用机制进行综述,以期为抗宫颈癌药物的研发与利用提供理论参考。 展开更多
关键词 宫颈癌 中药 有效成分 抑制活性 作用机制
苄基哌嗪类衍生物的合成与蛋白酪氨酸激酶抑制活性的研究 预览
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作者 韩生华 刘红艳 +1 位作者 张海荣 马鹏飞 《西北药学杂志》 CAS 2019年第5期652-656,共5页
目的合成苄基哌嗪类衍生物,考察目标化合物对蛋白酪氨酸激酶(PTK)的抑制活性。方法用呋喃甲醛和丙二酸合成呋喃丙烯酸,以15种取代苄基哌嗪为原料,分别与呋喃丙烯酸反应得到目标化合物。采用酶联免疫吸附法(Elisa)测定所得化合物对PTK的... 目的合成苄基哌嗪类衍生物,考察目标化合物对蛋白酪氨酸激酶(PTK)的抑制活性。方法用呋喃甲醛和丙二酸合成呋喃丙烯酸,以15种取代苄基哌嗪为原料,分别与呋喃丙烯酸反应得到目标化合物。采用酶联免疫吸附法(Elisa)测定所得化合物对PTK的抑制活性,并计算抑制率,筛选出具有抑制PTK活性的化合物。结果所得化合物均对PTK有一定的抑制活性。结论通过优化反应条件,成功合成15种苄基哌嗪类化合物,原料廉价易得,合成方法简单,反应温和。化合物结构经IR、1HNMR、EA和MS确证。经初步活性筛选发现化合物2h和2k的抑制活性较强。 展开更多
关键词 苄基哌嗪 合成 蛋白酪氨酸激酶 抑制活性
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烟草赤星病防治药剂的筛选 预览
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作者 朱宇航 黄思洋 +4 位作者 陈华保 常小丽 闫芳芳 张宗锦 龚国淑 《烟草科技》 EI CAS CSCD 北大核心 2019年第5期14-19,共6页
为筛选防治烟草赤星病的高效杀菌剂,测定了5种常用药剂(氟啶胺、啶氧菌酯、啶酰菌胺、嘧菌环胺、噁唑菌酮)对烟草赤星病菌(Alternaria alternata)的室内毒力及田间防效。结果表明,98%氟啶胺对病菌菌丝生长的抑制活性最强,EC50为0.1382mg... 为筛选防治烟草赤星病的高效杀菌剂,测定了5种常用药剂(氟啶胺、啶氧菌酯、啶酰菌胺、嘧菌环胺、噁唑菌酮)对烟草赤星病菌(Alternaria alternata)的室内毒力及田间防效。结果表明,98%氟啶胺对病菌菌丝生长的抑制活性最强,EC50为0.1382mg/L,其次为95%嘧菌环胺,EC50为3.5689mg/L,而95%噁唑菌酮最弱,EC50为30.0983mg/L。田间防效试验表明,5种杀菌剂中以50%氟啶胺SC和62%嘧菌环胺WG的防治效果较好,防效分别为70.44%和63.09%;以50%啶酰菌胺WG防治效果最差,为39.53%。综合室内毒力和田间防治试验结果,在烟草赤星病防治中推荐氟啶胺和嘧菌环胺。 展开更多
关键词 烟草赤星病 链格孢菌 抑制活性 防效 氟啶胺 嘧菌环胺
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贵州引种瓜蒌子乙酸乙酯提取物的α-葡萄糖苷酶抑制活性及成分分析
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作者 梁光平 杨俊 +4 位作者 刘亮 陈荣华 丁丽娜 万路平 陈东林 《华西药学杂志》 CAS CSCD 2019年第2期109-114,共6页
目的研究贵州引种瓜蒌子乙酸乙酯提取物的α-葡萄糖苷酶抑制活性及化学成分。方法以α-葡萄糖苷酶为酶源,检测不同浓度下的瓜蒌子乙酸乙酯提取物对α-葡萄糖苷酶的抑制活性。同时,采用超高效液相色谱串联三重四级杆飞行时间质谱法(UPLC-... 目的研究贵州引种瓜蒌子乙酸乙酯提取物的α-葡萄糖苷酶抑制活性及化学成分。方法以α-葡萄糖苷酶为酶源,检测不同浓度下的瓜蒌子乙酸乙酯提取物对α-葡萄糖苷酶的抑制活性。同时,采用超高效液相色谱串联三重四级杆飞行时间质谱法(UPLC-Triple-TOF/MS)进行成分检测,根据负离子质谱裂解规律以及相关文献的数据对照,分析瓜蒌子乙酸乙酯提取物的化学组成。结果在2.0 mg·mL^-1浓度下,贵州引种瓜蒌子乙酸乙酯提取物对α-葡萄糖苷酶抑制活性的抑制率为88.9%±1.67%。同时,从引种瓜蒌子乙酸乙酯提取物中共鉴定了14种化学成分,包括7种黄酮(含1个二聚体黄酮和1个橙酮)、5种酚酸衍生物、1种单萜糖苷、1种鞣花酸,所有化合物均为首次从瓜蒌子中发现。结论瓜蒌子乙酸乙酯提取物具有α-葡萄糖苷酶抑制活性,PLC-Triple-TOF/MS方法可用于快速分析瓜蒌子乙酸乙酯提取物的化学成分,为建立贵州引种瓜蒌子快速、准确的质量评价方法提供了参考。 展开更多
关键词 瓜蒌子 黄酮 Α-葡萄糖苷酶 抑制活性 负离子质谱裂解 液相色谱-质谱联用技术 成分分析 贵州省
水生植物对藻类的化感作用研究进展 预览
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作者 钱燕萍 赵楚 田如男 《生物学杂志》 CAS CSCD 北大核心 2018年第6期95-97,共3页
随着经济和社会快速发展,水体富营养化是面临的主要生态环境问题之一,会引起蓝藻水华等生态系统的异常响应。利用化感物质抑藻是较为生态高效的抑藻措施之一。总结了具有抑藻作用的沉水植物、挺水植物和浮水植物的种类及其能抑制的藻类... 随着经济和社会快速发展,水体富营养化是面临的主要生态环境问题之一,会引起蓝藻水华等生态系统的异常响应。利用化感物质抑藻是较为生态高效的抑藻措施之一。总结了具有抑藻作用的沉水植物、挺水植物和浮水植物的种类及其能抑制的藻类。并从水生植物抑制藻类生长的作用方式出发,总结出抑藻方式主要有水生植物与藻类共培养、水生植物种植水作用于藻类、水生植物提取物或纯化后的化感物质作用于藻类这3种。并对今后水生植物抑藻效应及机理等方向的研究进行了展望。 展开更多
关键词 水生植物 化感作用 抑藻活性 抑藻作用方式
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