硅学方法:鳞翅目蝙蝠分离化合物的 ADME/T 性能预测和 ACE 抑制作用

Udaya Chandrika P
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摘要

本研究旨在通过体外抗高血压活性、in-silico 分子对接和 ADME/T 分析来研究鳞翅目蝶形花(A. indica 和 A.cordata)的分离植物化合物。之前的报告揭示了一种事实,即多酚和三萜类化合物能够通过抑制血管紧张素转换酶(ACE)来控制血压。对分离出的配体儿茶素、异连翘素、鱼腥草素和熊果酸(A、B、C 和 D)进行了抑制血管紧张素转换酶的测试,并利用 Autodock 4.2、药物亲和性、理化性质、瑞士 ADME 和 ProTox 工具预测毒性与目标人体血管紧张素转换酶进行了对接。所有植物成分都表现出乐观的剂量反应抑制作用,化合物的 IC50(15.38 ± 0.53)μg/ml、B(20.21± 0.34 μg/ml)、C(17.62± 0.78 μg/ml)、D(23.98± 0.65 μg/ml)、卡托普利(15.86±0.32 μg/ml)表现出极高的 IC50。与卡托普利(-6.7)和利辛普利(-7.38 K.cal/mol)相比,分子 A 与靶蛋白的结合能最高(-7.3 K.cal/mol),与靶蛋白的配位明显,相互作用良好。ADME/T和配体的预测结果表明,这些生物活性化合物具有良好的药代动力学特性,其特点是胃肠道吸收率高、口服生物利用度高、毒性小且结合能高,因此这些生物活性化合物可作为可能的抗高血压药物进行进一步研究。
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In-silico approach: predictive ADME/T properties and ACE inhibitory action of isolated compounds of Aspidopterys sps
The current research study aimed to study Isolated phytocompounds of Aspidopterys sps (A. indica and A.cordata) by invitro antihypertensive activity, in-silico molecular docking, and ADME/T analysis. The preceding reports had revealed a fact of polyphenols and triterpenoids have an ability to control blood pressure by inhibition of Angiotensin converting enzyme (ACE). The isolated ligands Catechin, Isoorientin, Fisetin, and Ursolic acid (A , B, C and D) tested for ACE inhibition, docked with target Human Angiotensin-converting enzyme employing Autodock 4.2, drug-likeliness, physicochemical nature, toxicity prediction by Swiss ADME, ProTox tools available online. All phytoconstituents showed optimistic dose-responsive inhibition, Compounds exhibited magnificent IC50 (15.38 ± 0.53) μg/ml, B (20.21± 0.34 μg/ml), C (17.62 ± 0.78 μg/ml), D (23.98 ± 0.65 μg/ml), Captopril (15.86±0.32 μg/ml). Molecule A showed utmost binding energy (-7.3 K.cal/mol) significant alignment with target protein and good interactions compared to Captopril (-6.7) and Lisinopril (-7.38 K.cal/mol). Prediction of ADME/T and ligands showed good pharmacokinetic properties characterized by high absorption in the gastrointestinal tract, oral bioavailability, and minimal toxicity and high binding energies, so these bioactive compounds could be further explored as possible antihypertensive drugs.
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