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溶血血小板活化因子乙酰基转移酶(LPAFAT)活性检测方法的比较 被引量:3
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作者 胡傢椿 董继斌 +3 位作者 楼滨 李英霞 蒋宪成 丁庭波 《复旦学报(医学版)》 CAS CSCD 北大核心 2020年第4期488-495,共8页
目的通过3种方法检测溶血血小板活化因子(platelet activating factor,PAF)乙酰基转移酶(Lyso-PAF acetyl transferase,LPAFAT)的活性并测定抑制剂对酶活性的抑制作用,比较这些方法的优劣。方法分别采用LC/MS/MS检测产物PAF,巯基反应探... 目的通过3种方法检测溶血血小板活化因子(platelet activating factor,PAF)乙酰基转移酶(Lyso-PAF acetyl transferase,LPAFAT)的活性并测定抑制剂对酶活性的抑制作用,比较这些方法的优劣。方法分别采用LC/MS/MS检测产物PAF,巯基反应探针结合分光光度法检测产物CoA-SH,TLC检测荧光标记产物法鉴定阳性和假阳性两种不同化合物对LPAFAT酶活性的抑制作用。结果LC/MS/MS方法通过检测天然产物PAF的含量测定酶活性,抑制剂筛选结果准确可靠。巯基反应探针结合分光光度法虽然可以监测产物CoA-SH的含量,但反应体系中产生了大量干扰性的CoA-SH,因此并不能真实反映LPAFAT酶活性,亦不适于抑制剂活性筛选。TLC检测荧光标记产物法因底物NBD-Lyso PC结构已被修饰,不能代表天然底物的真实反应情况,可能存在错筛和漏筛。结论LC/MS/MS检测产物PAF测定LPAFAT活性以及筛选抑制剂,方法灵敏,数据结果可靠,但成本较高。监测产物CoA-SH的含量不适合于测定LPAFAT酶活性。TLC检测荧光标记产物,操作简便,灵敏度高,但筛选抑制剂时存在假阳性的可能,只适用于抑制剂活性的初筛。 展开更多
关键词 血小板活化因子(PAF) Lyso-PAF乙酰基转移酶(LPAFAT) 抑制活性测定 LC/MS/MS
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Polyprenylated acylphloroglucinols from the fruits of Hypericum henryi 被引量:3
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作者 Yang Liao Shu-Ya Yang +2 位作者 Xiao-Nian Li Xing-Wei Yang Gang Xu 《Science China Chemistry》 SCIE EI CAS CSCD 2016年第9期1216-1223,共8页
Hyphenrones R–X(1–7), seven new polyprenylated acylphloroglucinols derivatives, were isolated from the fruits of Hypericum henryi, together with eight know analogues. Compounds 1 and 2 were elucidated to possess com... Hyphenrones R–X(1–7), seven new polyprenylated acylphloroglucinols derivatives, were isolated from the fruits of Hypericum henryi, together with eight know analogues. Compounds 1 and 2 were elucidated to possess complex caged skeleton, while compounds 3–6 shared a common 3,9-epoxy moiety deriving from the normal polyprenylated acylphloroglucinols with a bicyclo[3.3.1]nonane-2,4,9-trione core. The new structures were elucidated on the basis of the interpretation of nuclear magnetic resonance(NMR) data, circular dichroism(CD) comparison, and single-crystal X-ray diffraction. In the bioassay, several compounds exhibited inhibitory activities against human tumor cell lines in vitro. 展开更多
关键词 polyprenylated acylphloroglucinols Hypericum henryi hyphenrones R-X ANTITUMOR
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