Phytochemical Studies on Medicinally Important Plants
药用植物的植物化学研究
基本信息
- 批准号:RGPIN-2015-04743
- 负责人:
- 金额:$ 2.04万
- 依托单位:
- 依托单位国家:加拿大
- 项目类别:Discovery Grants Program - Individual
- 财政年份:2017
- 资助国家:加拿大
- 起止时间:2017-01-01 至 2018-12-31
- 项目状态:已结题
- 来源:
- 关键词:
项目摘要
Natural product (NP) chemistry is one of the major contributors of lead compounds to the drug discovery process due to its enormous chemical diversity. One aspect of this process is the identification of NPs with enzyme-inhibiting activities. Enzymes, essential to human life, perform biochemical processes including metabolism, cellular signal transduction, cell cycling, and development. Malfunction in these biochemical systems often leads to disease that can be caused by the dysfunction/overexpression/hyperactivation of the enzymes involved. An understanding of diseases at the molecular level has provided several enzyme inhibitors in clinics. For instance, lovastatin, a cholesterol-lowering agent, works by inhibiting the activity of enzyme (3S)-hydroxymethylglutaryl- coenzyme A reductase, involved in its biosynthesis. The purpose of this research is to chemically investigate ethnomedicinal plants, a source of a wide array of valuable NPs, to identify bioactive NPs that make them active. We have collected several plants from the Prairie Provinces of Canada and South Africa based on their ethnomedical uses by traditional healers to treat various ailments and their crude extracts exhibited various enzyme inhibitory activities including anti-acetylcholinesterase (AChE), anti-glutathione S-transferase (GST), anti-alpha-glucosidase, anti-Plasmodium falciparum Enoyl-ACP reductase (PfENR), anti-Mycobacterium tuberculosis Enoyl-ACP reductase (MtENR) and anti-renin activities. All of these enzymes (AChE, alpha-glucosidase, GST, PfENR, MtENR and renin) are reported to be involved in the pathogenesis of Alzheimer's disease/Parkinson's disease, diabetes, improving anti-cancer chemotherapy, malaria, TB and hypertension, respectively. The proposed NP research will validate their ethnomedicinal use and help to identify novel NPs that inhibit the enzymes, involved in the pathogenesis of aforementioned diseases, as their molecular target. The major objectives of the proposed research are to identify: (i) lead bioactive NPs from aforementioned plants using a combination of bioactivity and metabolomics profiling approach; (ii) endophytic fungi as an alternative source of these NPs; (iii) and to study their structure-activity relationships. This interdisciplinary research integrates advanced chemical instrumentation methods (HPLC, NMR spectroscopic and LC-MS techniques for the purification and identification of NPs), microbial reactions, synthetic organic chemistry, computational chemistry, biochemistry and microbiology. In carrying out this research, students will be trained as future scientists for many Canadian institutions including biotechnological, food, chemical or pharmaceutical industries. The successful completion of this discovery grant will provide new NPs with therapeutic activities that will be of benefit to Canadian's health.
天然产物(NP)化学由于其巨大的化学多样性,是药物发现过程中先导化合物的主要贡献者之一。该方法的一个方面是鉴定具有酶抑制活性的NP。酶是人类生命中必不可少的,它执行包括新陈代谢、细胞信号转导、细胞周期和发育在内的生化过程。这些生化系统的功能障碍通常会导致疾病,这些疾病可能是由相关酶的功能障碍/过度表达/过度活化引起的。在分子水平上对疾病的理解为临床提供了几种酶抑制剂。例如,降胆固醇剂洛伐他汀通过抑制参与其生物合成的酶(3S)-羟甲基戊二酰-辅酶A还原酶的活性而起作用。本研究的目的是化学研究民族药用植物,一个广泛的有价值的纳米颗粒的来源,以确定生物活性的纳米颗粒,使他们活跃。我们从加拿大和南非的草原省收集了几种植物,基于它们被传统治疗者用于治疗各种疾病的民族医学用途,它们的粗提物表现出各种酶抑制活性,包括抗乙酰胆碱酯酶(AChE)、抗谷胱甘肽S-转移酶(GST)、抗α-葡糖苷酶、抗恶性疟原虫烯酰-ACP还原酶(PfENR)、抗结核分枝杆菌烯酰-ACP还原酶(MtENR)和抗肾素活性。据报道,所有这些酶(AChE、α-葡糖苷酶、GST、PfENR、MtENR和肾素)分别参与阿尔茨海默病/帕金森病、糖尿病、改善抗癌化疗、疟疾、TB和高血压的发病机制。拟议的NP研究将验证其民族医学用途,并有助于确定抑制酶的新型NP,参与上述疾病的发病机制,作为其分子靶点。拟议研究的主要目标是:(i)使用生物活性和代谢组学分析方法的组合从上述植物中鉴定出具有生物活性的NP;(ii)内生真菌作为这些NP的替代来源;(iii)并研究它们的结构-活性关系。这种跨学科的研究整合了先进的化学仪器方法(HPLC,NMR光谱和LC-MS技术用于NP的纯化和鉴定),微生物反应,合成有机化学,计算化学,生物化学和微生物学。在进行这项研究时,学生将被培养为许多加拿大机构的未来科学家,包括生物技术,食品,化学或制药行业。这项发现补助金的成功完成将提供新的NP与治疗活动,将有利于加拿大的健康。
项目成果
期刊论文数量(0)
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Ata, Athar其他文献
Novel microbial transformations of sclareolide
- DOI:
10.1248/cpb.55.118 - 发表时间:
2007-01-01 - 期刊:
- 影响因子:1.7
- 作者:
Ata, Athar;Conci, Leigha J.;Sener, Bilge - 通讯作者:
Sener, Bilge
Anti-acetylcholinesterase, anti-α-glucosidase, anti-leishmanial and anti-fungal activities of chemical constituents of Beilschmiedia species
- DOI:
10.1016/j.fitote.2011.11.009 - 发表时间:
2012-03-01 - 期刊:
- 影响因子:3.4
- 作者:
Mollataghi, Abbas;Coudiere, Emilie;Ata, Athar - 通讯作者:
Ata, Athar
Chemical constituents of Barleria prionitis and their enzyme inhibitory and free radical scavenging activities
- DOI:
10.1016/j.phytol.2008.11.005 - 发表时间:
2009-02-19 - 期刊:
- 影响因子:1.7
- 作者:
Ata, Athar;Kalhari, Kosmulalage S.;Samarasekera, Radhika - 通讯作者:
Samarasekera, Radhika
Buxus Steroidal Alkaloids: Chemistry and Biology
- DOI:
10.1016/s1099-4831(08)00203-4 - 发表时间:
2008-01-01 - 期刊:
- 影响因子:0
- 作者:
Ata, Athar;Andersh, Brad J. - 通讯作者:
Andersh, Brad J.
Triterpenoidal alkaloids from Buxus hyrcana and their enzyme inhibitory, anti-fungal and anti-leishmanial activities
- DOI:
10.1016/j.phytochem.2010.06.017 - 发表时间:
2010-10-01 - 期刊:
- 影响因子:3.8
- 作者:
Ata, Athar;Iverson, Chad D.;Sener, Bilge - 通讯作者:
Sener, Bilge
Ata, Athar的其他文献
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{{ truncateString('Ata, Athar', 18)}}的其他基金
Phytochemical Studies on Medicinally Important Plants
药用植物的植物化学研究
- 批准号:
DDG-2020-00018 - 财政年份:2022
- 资助金额:
$ 2.04万 - 项目类别:
Discovery Development Grant
Phytochemical Studies on Medicinally Important Plants
药用植物的植物化学研究
- 批准号:
DDG-2020-00018 - 财政年份:2021
- 资助金额:
$ 2.04万 - 项目类别:
Discovery Development Grant
Phytochemical Studies on Medicinally Important Plants
药用植物的植物化学研究
- 批准号:
DDG-2020-00018 - 财政年份:2020
- 资助金额:
$ 2.04万 - 项目类别:
Discovery Development Grant
Phytochemical Studies on Medicinally Important Plants
药用植物的植物化学研究
- 批准号:
RGPIN-2015-04743 - 财政年份:2019
- 资助金额:
$ 2.04万 - 项目类别:
Discovery Grants Program - Individual
Phytochemical Studies on Medicinally Important Plants
药用植物的植物化学研究
- 批准号:
RGPIN-2015-04743 - 财政年份:2018
- 资助金额:
$ 2.04万 - 项目类别:
Discovery Grants Program - Individual
Mass spectrometer for use in chemistry research at the University of Winnipeg
温尼伯大学用于化学研究的质谱仪
- 批准号:
RTI-2019-00894 - 财政年份:2018
- 资助金额:
$ 2.04万 - 项目类别:
Research Tools and Instruments
Phytochemical Studies on Medicinally Important Plants
药用植物的植物化学研究
- 批准号:
RGPIN-2015-04743 - 财政年份:2016
- 资助金额:
$ 2.04万 - 项目类别:
Discovery Grants Program - Individual
Phytochemical Studies on Medicinally Important Plants
药用植物的植物化学研究
- 批准号:
RGPIN-2015-04743 - 财政年份:2015
- 资助金额:
$ 2.04万 - 项目类别:
Discovery Grants Program - Individual
Development of novel UV-Vis-NIR spectrophotometric technique for wine chemical analysis
开发用于葡萄酒化学分析的新型紫外-可见-近红外分光光度技术
- 批准号:
469452-2014 - 财政年份:2014
- 资助金额:
$ 2.04万 - 项目类别:
Engage Grants Program
Phytochemical Studies on Medicinally Important Plants
药用植物的植物化学研究
- 批准号:
RGPIN-2014-05169 - 财政年份:2014
- 资助金额:
$ 2.04万 - 项目类别:
Discovery Grants Program - Individual
相似海外基金
Phytochemical Studies on Medicinally Important Plants
药用植物的植物化学研究
- 批准号:
DDG-2020-00018 - 财政年份:2022
- 资助金额:
$ 2.04万 - 项目类别:
Discovery Development Grant
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- 资助金额:
$ 2.04万 - 项目类别:
Discovery Development Grant
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- 批准号:
DDG-2020-00018 - 财政年份:2020
- 资助金额:
$ 2.04万 - 项目类别:
Discovery Development Grant
Phytochemical Studies on Medicinally Important Plants
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- 批准号:
RGPIN-2015-04743 - 财政年份:2019
- 资助金额:
$ 2.04万 - 项目类别:
Discovery Grants Program - Individual
Phytochemical Studies on Medicinally Important Plants
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- 批准号:
RGPIN-2015-04743 - 财政年份:2018
- 资助金额:
$ 2.04万 - 项目类别:
Discovery Grants Program - Individual
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- 批准号:
RGPIN-2015-04743 - 财政年份:2016
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$ 2.04万 - 项目类别:
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- 批准号:
RGPIN-2015-04743 - 财政年份:2015
- 资助金额:
$ 2.04万 - 项目类别:
Discovery Grants Program - Individual
Phytochemical Studies on Medicinally Important Plants
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- 批准号:
RGPIN-2014-05169 - 财政年份:2014
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