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Snake Venom Phospholipase A₂ and its Natural Inhibitors 蛇毒磷脂酶a2及其天然抑制剂
Q3 Chemistry Pub Date : 2020-12-31 DOI: 10.20307/nps.2020.26.3.259
Pushpendra Singh, Mohammad Yasir, Ruchir Khare, M. Tripathi, R. Shrivastava
Snakebite is a severe medical, economic, and social problem across the world, mostly in the tropical and subtropical area. These regions of the globe have typical of the world''s venomous snakes present where access to prompt treatment is limited or not available. Snake venom is a complex mixture of toxin proteins like neurotoxin and cardiotoxin, and other enzymes like phospholipase A2 (PLA2), haemorrhaging, transaminase, hyaluronidase, phosphodiesterase, acetylcholinesterase, cytolytic and necrotic toxins. Snake venom shows a wide range of biological effects like anticoagulation or platelet aggregation, hemolysis, hypotension and edema. Phospholipase A2 is the principal constituent of snake venom; it catalyzes the hydrolysis of the sn-2 position of membrane glycerophospholipids to liberate arachidonic acid, which is the precursor of eicosanoids including prostaglandins and leukotrienes. The information regarding the structure and function of the phospholipase A2 enzyme may help in treating the snakebite victims. This review article constitutes a brief description of the structure, types, mechanism occurrence, and tests of phospholipase A2 and role of components of medicinal plants used to inhibit phospholipase A2.
蛇咬伤是全球范围内严重的医疗、经济和社会问题,主要发生在热带和亚热带地区。这些地区是世界上典型的毒蛇聚集地,但获得及时治疗的机会有限或无法获得。蛇毒是一种复杂的毒素蛋白质混合物,如神经毒素和心脏毒素,以及其他酶,如磷脂酶A2 (PLA2)、出血酶、转氨酶、透明质酸酶、磷酸二酯酶、乙酰胆碱酯酶、细胞溶解和坏死毒素。蛇毒具有广泛的生物效应,如抗凝血或血小板聚集、溶血、低血压和水肿。磷脂酶A2是蛇毒的主要成分;它催化水解膜甘油磷脂的sn-2位置,释放花生四烯酸,花生四烯酸是包括前列腺素和白三烯在内的二十烷类化合物的前体。有关磷脂酶A2酶的结构和功能的信息可能有助于治疗蛇咬伤受害者。本文就磷脂酶A2的结构、类型、作用机制、检测方法以及药用植物中抑制磷脂酶A2的成分的作用作一综述。
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引用次数: 3
Chemicals Constituents from Leaves of Diospyros iturensis (Gürke) Letouzey & F. White and their Biological Activities 薯蓣(Diospyros iturensis, g<s:1> rke) Letouzey & F. White叶化学成分及其生物活性研究
Q3 Chemistry Pub Date : 2020-12-31 DOI: 10.20307/nps.2020.26.4.311
Marius Feumo Feusso Hermann, Catherine Vardamides Juliette, de dieu Dongmo Jean, Laure Maza Djomkam Hermine, Mvot Akak Carine, M. Lateef, A. Ayaz, Guy Blaise Azebaze Anatole, François Kamdem Waffo Alain, Shaiq Ali Muhammad
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引用次数: 2
Characterization and Potent Application of Pleurotus floridanus Trypsin Inhibitor (PfTI) 花菇胰蛋白酶抑制剂(PfTI)的特性及其应用
Q3 Chemistry Pub Date : 2020-09-30 DOI: 10.20307/NPS.2020.26.3.207
M. Pannippara, S. Kesav, R. Raghavan, Abraham Mathew, S. Bhat, Elyas Kothanan Kozhiyil
Characterization and in vitro inhibition studies of protease inhibitor from the mushroom Pleurotus floridanus (PfTI) towards the pest Papilio demoleus is studied. The addition of 1 mM Mn2+, Na2+, Ba2+ and Ni 2+ enhanced the PfTI activity. The ICP-atomic emission spectrum showed the presence of Ca2+, Mg2+ and Zn2+ in the PfTI. Surfactants SDS and CTAB at a concentration of 1% reduced the PfTI activity whereas, the nonionic detergents Triton X and Tween 80 increased the activity. The inhibitory activity gradually decreased with increase in concentration of DMSO and H2O2. The activity was increased by dithiothreitol up to a concentration of 80 μM and inactivated at 140 μM. The activity of PMSF modified PfTI was drastically reduced to 0.234 U/mL at 4 mM concentration and similar results were obtained for modification of cysteine by N-Ethylmaleimide at slightly higher concentrations. The complex of trypsin and PfTI showed complete loss in fluorescence intensity at 343 nm compared with control. In vitro inhibition studies of PfTI with midgut proteases isolated from citrus pest P. demoleus with protease activity of 1.236 U was decreased to 0.613 U by 50 μL (0.1 mg/mL) of the inhibitor. Inhibitor was stable up to 0.04 M concentration of HCl.
研究了蘑菇花菇蛋白酶抑制剂(PfTI)的特性及其对粉蝶的体外抑制作用。1mM Mn2+、Na2+、Ba2+和Ni2+的加入增强了PfTI的活性。ICP原子发射光谱显示PfTI中存在Ca2+、Mg2+和Zn2+。表面活性剂SDS和CTAB在1%的浓度下降低了PfTI的活性,而非离子洗涤剂Triton X和Tween 80则提高了活性。随着DMSO和H2O2浓度的增加,其抑制活性逐渐降低。二硫代苏糖醇浓度达到80μM时活性增加,140μM时失活。PMSF修饰的PfTI的活性在4mM浓度下显著降低至0.234U/mL,并且在稍高浓度下通过N-乙基马来酰亚胺修饰半胱氨酸获得类似的结果。与对照相比,胰蛋白酶和PfTI的复合物在343nm处显示出荧光强度的完全损失。50μL(0.1mg/mL)的抑制剂可将蛋白酶活性为1.236U的柑橘害虫脱模霉中肠蛋白酶对PfTI的体外抑制作用降低至0.613U。抑制剂在高达0.04M浓度的HCl时是稳定的。
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引用次数: 2
Isolation and Identification of Bioactive Compounds from the Tuber of Brassica oleracea var. gongylodes 甘蓝块茎中生物活性物质的分离与鉴定
Q3 Chemistry Pub Date : 2020-09-30 DOI: 10.20307/NPS.2020.26.3.214
Ritu Prajapati, S. Seong, Hyeung‐Rak Kim, H. Jung, Jae Sue Choi
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引用次数: 4
Effects of Compounds from Physalis angulata on Fatty Acid Synthesis and Glucose Metabolism in HepG2 Cells via the AMP-activated Protein Kinase Pathway 角藻化合物通过AMP激活蛋白激酶途径对HepG2细胞脂肪酸合成和葡萄糖代谢的影响
Q3 Chemistry Pub Date : 2020-09-30 DOI: 10.20307/NPS.2020.26.3.200
Hoang Thai Hoa, N. Thu, N. Dong, T. Oanh, T. T. Hien, D. Ha
The ability of the total extract from Physalis angulata; three fractions after partitioning with n-hexane, ethyl acetate (TBE), and water; and four withanolides (compounds 1 – 4) to phosphorylate 5'-adenosine monophosphate-activated protein kinase (AMPK) and acetyl-CoA carboxylase (ACC) in HepG2 cells was evaluated. The TBE fraction (50 μg/mL) activated p-ACC and p-AMPK expression most strongly. Compounds 1 – 4 (10 μM) upregulated p-ACC expression at different levels. Compound 4 induced the most significant changes in p-AMPK expression, followed by 1 and 2. Sterol regulatory element-binding proteins (SREBPs) play a functional role in the transcriptional regulation of the lipogenic pathway, including fatty acid synthase (FAS) and ACC. The effects of compounds 2 and 4 (10 μM) on FAS and SREBP-1c expression under high glucose conditions (30 mM) in HepG2 cells were evaluated further. Both dose-dependently inhibited FAS and SREBP-1c expression as well as lipid accumulation (1 – 10 μM) were compared to high-concentration glucose control, which upregulated FAS and SREBP-1c. These results suggest that compounds 2 and 4 upregulate AMPK, suppress FAS and SREBP-1c, and have potential effects on glucose and lipid metabolism. (Less)
角Physalis angulata总提取物的提取能力用正己烷、乙酸乙酯(TBE)和水分馏后的三个馏分;并对HepG2细胞中磷酸化5′-腺苷单磷酸活化蛋白激酶(AMPK)和乙酰辅酶a羧化酶(ACC)的4种withanolides(化合物1 - 4)进行了评价。TBE组分(50 μg/mL)对p-ACC和p-AMPK表达的激活作用最强。化合物1 ~ 4 (10 μM)不同程度上调p-ACC的表达。化合物4诱导p-AMPK表达变化最显著,其次是化合物1和化合物2。甾醇调节元件结合蛋白(SREBPs)在脂肪生成途径的转录调控中发挥功能作用,包括脂肪酸合成酶(FAS)和ACC。进一步观察化合物2和4 (10 μM)对高糖条件下(30 mM) HepG2细胞FAS和SREBP-1c表达的影响。我们将剂量依赖性抑制FAS和SREBP-1c表达以及脂质积累(1 - 10 μM)与高浓度葡萄糖控制进行比较,高浓度葡萄糖控制上调FAS和SREBP-1c。这些结果表明,化合物2和4上调AMPK,抑制FAS和SREBP-1c,并对糖脂代谢有潜在影响。(少)
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引用次数: 3
Anti-adipogenic Pregnane Steroid from a Hydractinia-associated Fungus, Cladosporium sphaerospermum SW67 水螅相关真菌球孢枝孢SW67的抗脂肪妊娠类固醇
Q3 Chemistry Pub Date : 2020-09-30 DOI: 10.20307/NPS.2020.26.3.230
Lee Seoung-Rak, Kang, Hee-Sun, Yoo Min-Jeong, Yi Sang-Ah, B. Christine, Lee Jaecheol, Kim, Ki-Hyun
A pregnane steroid, 3α-hydroxy-pregn-7-ene-6,20-dione (1), was isolated from a Hydractiniaassociated Cladosporium sphaerospermum SW67 by repetitive column chromatographic separation and highperformance liquid chromatography (HPLC) purification. The planar structure of 1 was elucidated from the analysis of the spectroscopic data (1D and 2D NMR spectra) and LC-MS data. The absolute configuration of 1 was determined by interpretation of ROESY spectrum of 1, together with the comparison of reported spectroscopic values in previous studies. To the best of our knowledge, this is the first report of the identification of the pregnane scaffold from C. sphaerospermum, a natural source. Compound 1 was evaluated for its effects on lipid metabolism and adipogenesis during adipocyte maturation and showed that compound 1 substantially inhibited lipid accumulation compared to the control. Consistently, the expression of the adipocyte marker gene (Adipsin) was reduced upon incubation with 1. Further, we evaluated the effects of 1 on lipid metabolism by measuring the transcription of lipolytic and lipogenic genes. The expression of the lipolytic gene ATGL was significantly elevated upon exposure to 1 during adipogenesis, whereas the expression of lipogenic genes FASN and SREBP1 was significantly reduced upon treatment with 1. Thus, our findings provide experimental evidence that the steroid derived from Hydractinia-associated C. sphaerospermum SW67 is a potential therapeutic agent for obesity.
采用重复柱色谱分离和高效液相色谱(HPLC)纯化的方法,从水凝相关球形枝孢菌SW67中分离得到孕甾体3α-羟基-孕甾-7-烯-6,20-二酮(1)。通过光谱数据(1D和2D NMR光谱)和LC-MS数据的分析阐明了1的平面结构。通过对1的ROESY光谱的解释,以及对先前研究中报道的光谱值的比较,确定了1的绝对构型。据我们所知,这是第一份从天然来源球藻中鉴定孕烷支架的报告。评估了化合物1在脂肪细胞成熟过程中对脂质代谢和脂肪生成的影响,并表明与对照相比,化合物1显著抑制了脂质积聚。一致地,脂肪细胞标记基因(Adipsin)的表达在与1。此外,我们通过测量脂肪分解和脂肪生成基因的转录来评估1对脂质代谢的影响。在脂肪生成过程中,当暴露于1时,脂肪分解基因ATGL的表达显著升高,而当用1处理时,脂肪生成基因FASN和SREBP1的表达显著降低。因此,我们的研究结果提供了实验证据,证明来自Hydractinia associated C.sphaerospermum SW67的类固醇是一种潜在的肥胖治疗剂。
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引用次数: 43
Liver Function Analyses and Spleen Histology Assessment Following the Co-administration of Cisplatin and Methanolic Extract of Portulaca Oleracea in Wistar Rats: An Experimental Study 顺铂与马齿苋醇提物联合给药对Wistar大鼠肝功能及脾脏组织学的影响
Q3 Chemistry Pub Date : 2020-09-30 DOI: 10.20307/nps.2020.26.3.252
Okafor Izuchukwu Azuka, Nnamah Uchenna Somtochukwu, N. Jude
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引用次数: 0
Phytochemical Constituents of Phyllanthus urinaria 叶下珠的植物化学成分
Q3 Chemistry Pub Date : 2020-06-30 DOI: 10.20307/NPS.2020.26.2.151
J. M. Cha, J. Park, Sang-Un Choi, K. Lee
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引用次数: 1
NMR Assignments of Rotameric Aporphine Alkaloids from Liriodendron tulipifera 郁金香鹅掌楸中旋美阿啡类生物碱的核磁共振分配
Q3 Chemistry Pub Date : 2020-06-30 DOI: 10.20307/NPS.2020.26.2.171
InWha Park, M. Na
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引用次数: 0
Butyrylcholinesterase Inhibitory Activity and GC-MS Analysis of Carica papaya Leaves 番木瓜叶的丁酰胆碱酯酶抑制活性及GC-MS分析
Q3 Chemistry Pub Date : 2020-06-30 DOI: 10.20307/nps.2020.26.2.165
Nelson Jeng Yeou Chear, Sathiya Maran, K. Y. Yeong, Y. Ong, B. Goh
Carica papaya is a medicinal and fruit plant owing biological activities including antioxidant, antiviral, antibacterial and anticancer. The present study aims to investigate the acetyl (AChE) and butyryl (BChE) cholinesterase inhibitory potentials of C. papaya extracts as well as their chemical compositions. The chemical composition of the active extract was identified using a gas chromatography-mass spectrometry (GCMS). Ellman enzyme inhibition assay showed that the alkaloid-enriched leaf extract of C. papaya possessed significant anti-BChE activity with an enzyme inhibition of 75.9%. GC-MS analysis showed that the alkaloid extract composed mainly the carpaine (64.9%) - a major papaya alkaloid, and some minor constituents such as aliphatic hydrocarbons, terpenes and phenolics. Molecular docking of carpaine revealed that this molecule formed hydrogen bond and hydrophobic interactions with choline binding site and acyl pocket. This study provides some preliminary findings on the potential use of C. papaya leaf as an herbal supplement for the prevention and treatment of Alzheimer’s disease.
番木瓜是一种药用和果树,具有抗氧化、抗病毒、抗菌和抗癌等生物学活性。本研究旨在研究木瓜提取物的乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)抑制潜力及其化学成分。使用气相色谱-质谱法(GCMS)鉴定活性提取物的化学成分。Ellman酶抑制试验表明,富含生物碱的木瓜叶提取物具有显著的抗BChE活性,酶抑制率为75.9%。GC-MS分析表明,该生物碱提取物主要由木瓜主要生物碱carpaine(64.9%)和一些次要成分如脂肪烃、萜类和酚类组成。分子对接显示,该分子与胆碱结合位点和酰基口袋形成氢键和疏水相互作用。这项研究提供了一些关于木瓜叶作为草药补充剂预防和治疗阿尔茨海默病的潜在用途的初步发现。
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引用次数: 4
期刊
Natural product sciences
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