Chemical investigation of the culture extract of an endophytic Penicillium citrinum from Dendrobium officinale,afforded nine citrinin derivatives(1–9)and one peptide-polyketide hybrid GKK1032B(10).The structures of t...Chemical investigation of the culture extract of an endophytic Penicillium citrinum from Dendrobium officinale,afforded nine citrinin derivatives(1–9)and one peptide-polyketide hybrid GKK1032B(10).The structures of these compounds were determined by spectroscopic methods.The absolute configurations of 1 and 2 were determined for the first time by calculation of electronic circular dichroism(ECD)data.Among them,GKK1032B(10)showed significant cytotoxicity against human osteosarcoma cell line MG63 with an IC50 value of 3.49μmol·L–1,and a primary mechanistic study revealed that it induced the apoptosis of MG63 cells via caspase pathway activation.展开更多
A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-lH-indole-3-carboxylates 8a--8j and 11e--11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus（HBV） acti...A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-lH-indole-3-carboxylates 8a--8j and 11e--11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus（HBV） activity and cytotoxicity. Among them, six compounds showed more potent inhibitory activity than lamivudine. Compound 8e exhibited the most significant anti-HBV activity with an IC50 value of 1.62 μmol/L, which was 33-times more potent than the reference drug lamivudine（IC50=54.78μmol/L）.展开更多
基金the National Natural Science Foundation of China(Nos.82073728 and 31501104)the Natural Science Foundation of Shandong Province(Nos.ZR2019QH006 and JQ201721)+3 种基金the Project of Shandong Province Higher Educational Science and Technology Program(No.J17KA228)the Innovation Team Project of Jinan Science&Technology Bureau(No.2018GXRC003)the Young Taishan Scholars Program(No.tsqn20161037)Shandong Talents Team Cultivation Plan of University Preponderant Discipline(No.10027).
文摘Chemical investigation of the culture extract of an endophytic Penicillium citrinum from Dendrobium officinale,afforded nine citrinin derivatives(1–9)and one peptide-polyketide hybrid GKK1032B(10).The structures of these compounds were determined by spectroscopic methods.The absolute configurations of 1 and 2 were determined for the first time by calculation of electronic circular dichroism(ECD)data.Among them,GKK1032B(10)showed significant cytotoxicity against human osteosarcoma cell line MG63 with an IC50 value of 3.49μmol·L–1,and a primary mechanistic study revealed that it induced the apoptosis of MG63 cells via caspase pathway activation.
基金Supported by the National Natural Science Foundation of China(No.30672519)
文摘A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-lH-indole-3-carboxylates 8a--8j and 11e--11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus（HBV） activity and cytotoxicity. Among them, six compounds showed more potent inhibitory activity than lamivudine. Compound 8e exhibited the most significant anti-HBV activity with an IC50 value of 1.62 μmol/L, which was 33-times more potent than the reference drug lamivudine（IC50=54.78μmol/L）.
