Department of Pharmaceutical Chemistry, Government College University Faisalabad, Faisalabad 38000, Pakistan.
Gomal Center of Biochemistry and Biotechnology, Gomal University, Dera Ismail Khan 29050, Pakistan.
Molecules. 2022 Aug 26;27(17):5480. doi: 10.3390/molecules27175480.
, 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. methanol extract (CLM) was prepared, then compound isolation performed by open column chromatography, and compound structure was determined by spectroscopic techniques (C NMR, IR spectroscopy, H-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 IC 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 and LFD shows antibacterial and antifungal activity against antibiotic resistance and , 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.
, 一个巨大的科，涉及 500 种或 20 属，起源于热带和亚热带地区。这个科具有抗利什曼原虫、细胞毒性、抗菌、抗糖尿病、抗原生动物和抗真菌等药用价值。制备了甲醇提取物（CLM），然后通过开放柱色谱进行化合物分离，并通过光谱技术（C NMR、IR 光谱、H-NMR、质谱 UV-可见和 2D 相关技术）确定化合物结构。对转录调节剂 4EY7 和 2GV9 进行配体的分子对接研究，观察可能的相互作用。植物化学筛选显示存在包括甾体、强心苷、皂苷、蒽醌和黄酮类在内的次生代谢物。分离得到的化合物被鉴定为山萮酰胺（LFD）。它对人乳腺癌、鼠淋巴细胞白血病和正常细胞、人胚肾细胞和大鼠神经胶质瘤细胞具有细胞毒性活性，IC 值分别为 0.72 µg/mL、2.01 µg/mL、1.55 µg/mL 和 2.40 µg/mL。虽然对人结肠癌和人肺癌没有观察到细胞毒性活性，但 LFD 对 BChE 的抑制率为 24.04%，对 AChE 的抑制率为 60.30%，因此对阿尔茨海默病（AD）有益。分子对接研究表明，LFD 与 AChE 相互作用的机制有利于神经退行性疾病。甲醇和二氯甲烷提取物对 和 LFD 分别显示出对耐抗生素的 和 的抗菌和抗真菌活性。LFD 对 HSV-1 具有抗病毒活性，IP 抑制率为 26%。这项研究的结果支持将 LFD 用于认知障碍，并首次强调其针对 AChE、DNA-POL、NF-KB 和 TNF-α 等的潜在机制。
