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Novel peptides with HIV-1 reverse transcriptase inhibitory activity derived from the fruits of Quercus infectoria.
Chemical Biology & Drug Design ( IF 3 ) Pub Date : 2020-08-05 , DOI: 10.1111/cbdd.13770
Supaphorn Seetaha 1 , Supa Hannongbua 2 , Jatuporn Rattanasrisomporn 1, 3 , Kiattawee Choowongkomon 4, 5
Affiliation  

The HIV‐1 reverse transcriptase (HIV‐1 RT), which is responsible for transcription of viral RNA genomes into DNA genomes, has become an important target for the treatment of patients with HIV infection. Hydrolyzed peptides from plants are considered a new source of potential drugs. In order to develop new effective inhibitors, peptides extracted from 111 Asian medicinal plants were screened against the HIV‐1 RT. The crude hydrolyzed peptides from the fruit peel of Quercus infectoria were selected for purification and peptide sequence determination by HPLC and LC‐MS. Two peptides of interest were synthesized, and an IC50 test was performed to determine their ability to inhibit the HIV‐1 RT. The IC50 values of the peptides AIHIILI and LIAVSTNIIFIVV were determined to be 274 ± 5.10 nm and 236.4 ± 7.07 nm, respectively. This indicated that these peptides could be further developed as potential HIV‐1 RT inhibitors.

中文翻译:

来自 Quercus infectoria 果实的具有 HIV-1 逆转录酶抑制活性的新型肽。

HIV-1逆转录酶(HIV-1 RT)负责将病毒RNA基因组转录为DNA基因组,已成为治疗HIV感染患者的重要靶点。来自植物的水解肽被认为是潜在药物的新来源。为了开发新的有效抑制剂,针对 HIV-1 RT 筛选了从 111 种亚洲药用植物中提取的肽。选择从栎属果皮中提取的粗水解肽进行纯化,并通过 HPLC 和 LC-MS 进行肽序列测定。合成了两种感兴趣的肽,并进行了 IC 50测试以确定它们抑制 HIV-1 RT 的能力。IC 50测定肽AIHIILI和LIAVSTNIIFIVV的值是274±5.10Ñ和236.4±7.07Ñ分别。这表明这些肽可以进一步开发为潜在的 HIV-1 RT 抑制剂。
更新日期:2020-08-05
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