[1]蓝燕,杨梓超,刘涵,等.PSB0739抑制精液来源的淀粉样纤维形成[J].南方医科大学学报,2018,(11):1338.[doi:10.12122/j.issn.1673-4254.2018.11.10]
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PSB0739抑制精液来源的淀粉样纤维形成()
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《南方医科大学学报》[ISSN:1673-4254/CN:44-1627/R]

卷:
期数:
2018年11期
页码:
1338
栏目:
出版日期:
2018-11-30

文章信息/Info

Title:
PSB0739 inhibits formation of semen-derived amyloid fibrils
作者:
蓝燕杨梓超刘涵程宏彦刘叔文谭穗懿
关键词:
PSB0739淀粉样纤维人类免疫缺陷病毒性传播精液
Keywords:
PSB0739 amyloid fiber HIV-1 sexual transmission semen
DOI:
10.12122/j.issn.1673-4254.2018.11.10
摘要:
目的探究PSB0739对精液来源的淀粉样纤维形成的抑制作用。方法440 μmol/L的PAP248-286多肽分别与不同浓度的 化合物孵育,在不同时间点分别取样,用刚果红染色法、透射电子显微镜法检测药物对淀粉样纤维形成的影响;通过病毒感染实 验分析在PSB0739作用下,精液淀粉样纤维促进病毒感染的能力;利用Zeta电势仪检测PSB0739对成熟的精液来源性淀粉样 纤维表面电荷的影响;MTT法检测PSB0739对Hela细胞的毒性作用,以评价磺酸类化合物PSB073的体外安全性;体外细胞病 毒感染实验检测PSB0739抗HIV-1的活性。结果PSB0739在体外能有效抑制精液淀粉样纤维的形成,在48 h内,220 μmol/L 的PSB0739能抑制440 μmol/L的PAP248-286形成淀粉样纤维SEVI;透射电子显微镜可以直接观察到220 μmol/L的PSB0739 就能有效抑制PAP248-286形成的淀粉样纤维;PSB0739能拮抗SEVI介导的增强病毒感染的作用;体外220 μmol/L的PSB0739 能逆转SEVI携带的正电荷,差异均有统计学意义(P<0.05)。浓度低于62.5 μmol/L时PSB0739对宫颈癌Hela细胞无明显毒性 作用,细胞存活率无统计学意义(P>0.05);PSB0739能直接抑制HIV的能力与浓度正相关,PSB0739具有抗HIV作用,其IC50为 21.77±5.15 μmol/L。结论PSB0739能抑制精液来源的淀粉样纤维的形成。
Abstract:
Objective To explore the inhibitory effect of PSB0739 on the formation of semen-derived amyloid fibrils. Methods PAP248-286 (440 μmol/L) was incubated with PSB0739 at different concentrations, and at different time points of incubation, aliquots were taken from each sample for Congo red staining to detect the formation of amyloid fibers. The morphology of amyloid fibrils incubated in the presence or absence of PSB0739 was visualized using transmission electron microscope. The effect of PSB0739 on amyloid fibril formation was determined using virus infection assays at different time points, and the surface charges of amyloid fibril incubated with PSB0739 were calculated using a Zeta potentiometer. The cytotoxicity of PSB0739 in Hela cells was determined using MTT assay. The antiviral effect of PSB0738 against HIV- 1 was evaluated by infection assay. Results PSB0739 inhibited SEVI fibril formation in a dose-dependent manner in vitro. At 48 h of incubation, 220 μmol/L of PSB0739 obviously inhibited the formation of amyloid fibrils in 440 μmol/L of SEVI. Transmission electron microscopy revealed that 220 μmol/L PSB0739 prevented PAP248- 286 (440 μmol/L) from forming amyloid fibrils. PSB0739 antagonized SEVI-mediated enhancement of HIV-1 infection, and 1760 μmol/L of PSB0739 completely reversed the positive charge of SEVI (P<0.05). PSB0739 below the concentration of 62.5 μmol/L showed no obvious cytotoxicity in Hela cells in vitro (P>0.05). PSB0739 showed a direct anti-HIV activity with an IC50 of 21.77 ± 5.15 μmol/L. Conclusion PSB0739 can inhibit the formation of semen-derived amyloid fibrils in vitro.

相似文献/References:

[1]李锦清,宋亚丽,寻添荣,等.乳酸抑制精液来源淀粉样纤维的形成[J].南方医科大学学报,2017,(07):907.

更新日期/Last Update: 1900-01-01