Alamri Fatima B, Sobahi Tariq R, Althagbi Hanan I, Abdel-Lateff Ahmed, Alfaifi Mohammed Y, Mohammed Ayeda Y, Abdel-Latif Ehab, Alarif Walied M
Department of Chemistry, Faculty of Science, King Abdulaziz University, PO. Box 80203, Jeddah 21589, Saudi Arabia.
Department of Chemistry, College of Science, University of Jeddah, Jeddah 21589, Saudi Arabia.
Saudi Pharm J. 2023 Jun;31(6):773-782. doi: 10.1016/j.jsps.2023.04.017. Epub 2023 Apr 23.
Two cytotoxic sesquiterpene lactones, 17-epichlorohyssopifolin A () and chlorjanerin (), and a monoterpene lactone, loliolide () were isolated from . The cytotoxicity of the total extract and terpenoids - were evaluated against three human cancer cells (HepG2, PC-3, and HT-29), along with the human normal primary epidermal keratinocytes (HEKa) cells. With IC values ranging between 0.6 ± 0.04 and 5.0 ± 0.61 μg/mL against HepG2; 0.2 ± 0.01 and 11.9 ± 1.31 μg/mL against PC-3, and 0.04 ± 0.013 and 8.9 ± 0.97 μg/mL against HT-29, the total extract, and lactones - demonstrated cytotoxic effects. Compound displayed the strongest impact on all cancer cells and a slightly safe effect on the normal cells HEKa. Compound caused accumulation of HepG2 and HT-29 cells in G1 phase as displayed cell cycle analysis. On the other hand, the cell distributions were increased in the S phase in PC-3 cells. Furthermore, caused apoptosis in PC-3 and HePG2 cells with 91.50%, and 79.72 %, respectively. A higher fraction of necrotic cells was observed in HT-29 cells amounting to 23.60%. These results suggested that the promising cytotoxicity exhibited by is brought by the apoptosis induction in the cancer cells, which were evaluated. As the compounds showed antiproliferative effect against the HT-29 cells, the docking simulation was performed aiming at determining how they would interact with the EGFR enzyme, whose PDB: 4I23 is considered one of the two distinct wild types of EGFR enzymes. The antibacterial activity results revealed that showed the most remarkable antibacterial effects, especially against the examined Gram-positive bacteria. The total extract exhibited potent activity against all examined bacteria. The total extract showed a potent antifungal effect against two and two pathogens. The antioxidant activity revealed the potency of the total extract and as antioxidant candidates. The obtained results refer to the importance of as a source of potent antiproliferative agents and the whole plant as an antipathogenic and antioxidant agent.
从……中分离出两种具有细胞毒性的倍半萜内酯，17-表氯紫苏内酯A（）和氯紫苏内酯（），以及一种单萜内酯，洛里奥利德（）。对总提取物和萜类化合物 - 的细胞毒性针对三种人类癌细胞（HepG2、PC-3和HT-29）以及人类正常原代表皮角质形成细胞（HEKa）进行了评估。总提取物和内酯 - 对HepG2的IC值在0.6±0.04至5.0±0.61μg/mL之间；对PC-3的IC值在0.2±0.01至11.9±1.31μg/mL之间，对HT-29的IC值在0.04±0.013至8.9±0.97μg/mL之间，显示出细胞毒性作用。化合物 对所有癌细胞的影响最强，对正常细胞HEKa有轻微的安全作用。细胞周期分析显示，化合物 导致HepG2和HT-29细胞在G1期积累。另一方面，PC-3细胞中S期的细胞分布增加。此外， 分别导致PC-3和HePG2细胞凋亡，凋亡率分别为91.50%和79.72%。在HT-29细胞中观察到较高比例的坏死细胞，达23.60%。这些结果表明，所评估的 所表现出的有前景的细胞毒性是由癌细胞中的凋亡诱导引起的。由于这些化合物对HT-29细胞显示出抗增殖作用，进行了对接模拟，旨在确定它们与EGFR酶的相互作用方式，其PDB：4I23被认为是EGFR酶的两种不同野生型之一。抗菌活性结果表明， 显示出最显著的抗菌作用，尤其是对所检测的革兰氏阳性菌。总提取物对所有检测细菌均表现出强效活性。总提取物对两种……和两种……病原体显示出强效抗真菌作用。抗氧化活性表明总提取物和 作为抗氧化候选物的潜力。所得结果表明 作为强效抗增殖剂来源的重要性，以及整个植物作为抗病原体和抗氧化剂的重要性。
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