One new sesquiterpene lactone, corialactone E （1）, one new neolignan, coriarianeolignan A （2）, together with three known apocarotenoids （3-5） and one known neolignan （6） have been isolated from a CHCI3 extract...One new sesquiterpene lactone, corialactone E （1）, one new neolignan, coriarianeolignan A （2）, together with three known apocarotenoids （3-5） and one known neolignan （6） have been isolated from a CHCI3 extract of the roots of Coriaria nepalensis. The structures including absolute configurations of 1-6 were elucidated through extensive NMR, HR-ESIMS, and CD data analysis. Structurally, compound I possessed novel variations in the structure, including the newly formed ether ring of C-3/O/C-9 and the lactone ring connecting C-13 and C-5. Compound 5 showed cytotoxic activity against SKOV3 （human ovarian cancer） cells with IC50 values of 4.67 μmol/L. In vivo system, compound 3 showed anti-convulsant activity by 34% at the dose of 5 mg/kg.展开更多
为了评价4,5-二氢-7-(4-氯苯氧基)-四唑[1,5-a]喹啉(S2011017)的抗癫痫活性,采用最大电惊厥(Maximum Electron Shock,MES)实验、多种化学致惊实验及急性神经毒性实验,测定了其作用时间和剂量关系。MES实验结果表明,腹腔给药5 min后,S201...为了评价4,5-二氢-7-(4-氯苯氧基)-四唑[1,5-a]喹啉(S2011017)的抗癫痫活性,采用最大电惊厥(Maximum Electron Shock,MES)实验、多种化学致惊实验及急性神经毒性实验,测定了其作用时间和剂量关系。MES实验结果表明,腹腔给药5 min后,S2011017表现出较好的抗癫痫活性(ED50=11.8 mg·kg-1)。在化学致惊实验中,S2011017对异烟肼(ISO),3-巯基丙酸(3-MP),荷包牡丹碱(BIC)和硫代氨基脲(THIO)引起的惊厥有效。因此,由于S2011017表现出广谱的抗惊厥活性,并且能够快速地达到抗惊厥活性的峰值,可以作为一种潜在抗癫痫药,进行深入的成药性评价。展开更多
基金Financial support from the National Natural Science Foundation of China(No.21132009)the National Science and Technology Project of China(No.2012ZX09301002-002)
文摘One new sesquiterpene lactone, corialactone E （1）, one new neolignan, coriarianeolignan A （2）, together with three known apocarotenoids （3-5） and one known neolignan （6） have been isolated from a CHCI3 extract of the roots of Coriaria nepalensis. The structures including absolute configurations of 1-6 were elucidated through extensive NMR, HR-ESIMS, and CD data analysis. Structurally, compound I possessed novel variations in the structure, including the newly formed ether ring of C-3/O/C-9 and the lactone ring connecting C-13 and C-5. Compound 5 showed cytotoxic activity against SKOV3 （human ovarian cancer） cells with IC50 values of 4.67 μmol/L. In vivo system, compound 3 showed anti-convulsant activity by 34% at the dose of 5 mg/kg.
文摘为了评价4,5-二氢-7-(4-氯苯氧基)-四唑[1,5-a]喹啉(S2011017)的抗癫痫活性,采用最大电惊厥(Maximum Electron Shock,MES)实验、多种化学致惊实验及急性神经毒性实验,测定了其作用时间和剂量关系。MES实验结果表明,腹腔给药5 min后,S2011017表现出较好的抗癫痫活性(ED50=11.8 mg·kg-1)。在化学致惊实验中,S2011017对异烟肼(ISO),3-巯基丙酸(3-MP),荷包牡丹碱(BIC)和硫代氨基脲(THIO)引起的惊厥有效。因此,由于S2011017表现出广谱的抗惊厥活性,并且能够快速地达到抗惊厥活性的峰值,可以作为一种潜在抗癫痫药,进行深入的成药性评价。
