关键词: Conocarpus lancifolius anti-Alzheimer’s anti-proliferative anti-viral antibiotic-resistant bacteria combretaceae cytotoxic infection lancifolamide

Mesh : Acetylcholinesterase / metabolism Animals Cholinesterase Inhibitors / chemistry Combretaceae / chemistry Herpes Simplex Herpesvirus 1, Human / drug effects Humans Methanol Mice Molecular Docking Simulation Plant Extracts / chemistry Rats

来  源:   DOI:10.3390/molecules27175480

Abstract:
Combretaceae, an immense family involving species (500) or genera (20), originates in tropical and subtropical regions. This family has evinced medicinal values such as anti-leishmanial, cytotoxic, antibacterial, antidiabetic, antiprotozoal, and antifungal properties. Conocarpus lancifolius (C. lancifolius) methanol extract (CLM) was prepared, then compound isolation performed by open column chromatography, and compound structure was determined by spectroscopic techniques (13C NMR, IR spectroscopy, 1H-NMR, mass spectrometry UV-visible, and 2D correlation techniques). Molecular docking studies of ligand were performed on transcriptional regulators 4EY7 and 2GV9 to observe possible interactions. Phytochemical screening revealed the presence of secondary metabolites including steroids, cardiac glycosides, saponins, anthraquinones, and flavonoids. The isolated compound was distinguished as lancifolamide (LFD). It showed cytotoxic activity against human breast cancer, murine lymphocytic leukemia, and normal cells, human embryonic kidney cells, and rat glioma cells with IC50 values of 0.72 µg/mL, 2.01 µg/mL, 1.55 µg/mL, and 2.40 µg/mL, respectively. Although no cytotoxic activity was noticed against human colon cancer and human lung cancer, LFD showed 24.04% inhibition against BChE and 60.30% inhibition against AChE and is therefore beneficial for Alzheimer\'s disease (AD). AChE and LFD interact mechanistically in a way that is optimum for neurodegenerative disorders, according to molecular docking studies. Methanol and dichloromethane extract of C. lancifolius and LFD shows antibacterial and antifungal activity against antibiotic resistance Bacillus subtilis, Streptococcus mutans, Brevibacillus laterosporus, Salmonella Typhi, Candida albicans, and Cryptococcus neoformans, respectively. LFD shows antiviral activity against HSV-1 with 26% inhibition IP. The outcomes of this study support the use of LFD for cognitive disorders and highlight its underlying mechanism, targeting AChE, DNA-POL, NF-KB, and TNF-α, etc., for the first time.
摘要:
梳子科,涉及物种(500)或属(20)的巨大家族,起源于热带和亚热带地区。这个家庭已经证明了药用价值,如抗利什曼原虫,细胞毒性,抗菌,抗糖尿病药,抗原生动物,和抗真菌特性。红果(C.lancifolius)甲醇提取物(CLM)的制备,然后通过开放柱色谱进行化合物分离,并通过光谱技术(13CNMR,红外光谱,1H-NMR,质谱紫外可见,和2D相关技术)。在转录调节因子4EY7和2GV9上进行配体的分子对接研究以观察可能的相互作用。植物化学筛选显示存在次级代谢产物,包括类固醇,强心苷,皂苷,蒽醌,和类黄酮.分离的化合物被区分为lancifolamide(LFD)。它显示出对人类乳腺癌的细胞毒活性,小鼠淋巴细胞白血病,正常细胞,人胚胎肾细胞,和大鼠神经胶质瘤细胞的IC50值为0.72µg/mL,2.01微克/毫升,1.55微克/毫升,和2.40µg/mL,分别。尽管没有发现对人结肠癌和人肺癌的细胞毒活性,LFD显示对BChE的24.04%抑制和对AChE的60.30%抑制,因此对阿尔茨海默病(AD)有益。AChE和LFD以最适合神经退行性疾病的方式进行机械相互作用,根据分子对接研究。lancifolius和LFD的甲醇和二氯甲烷提取物对抗生素抗性枯草芽孢杆菌具有抗菌和抗真菌活性,变形链球菌,侧孢短芽孢杆菌,伤寒沙门氏菌,白色念珠菌,和新生隐球菌,分别。LFD显示针对HSV-1的抗病毒活性,IP抑制26%。这项研究的结果支持LFD用于认知障碍,并强调其潜在机制,靶向AChE,DNA-POL,NF-KB,和TNF-α,等。,第一次。
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