We have recently designed and synthesized several novel iminoquinone anticancer agents that have entered preclinical development for the treatment of human cancers.Herein we developed and validated a quantitative HPLC...We have recently designed and synthesized several novel iminoquinone anticancer agents that have entered preclinical development for the treatment of human cancers.Herein we developed and validated a quantitative HPLC-MS/MS analytical method for one of the lead novel anticancer makaluvamine analog,TCBA-TPQ,and conducted a pharmacokinetic study in laboratory rats.Our results indicated that the HPLC-MS/MS method was precise,accurate,and specific.Using this method,we carried out in vitro and in vivo evaluations of the pharmacological properties of TCBA-TPQ and plasma pharmacokinetics in rats.Our results provide a basis for future preclinical and clinical development of this promising anticancer marine analog.展开更多
TCBA是一种人工合成的植物生长谢节剂,学名是三氯苯甲酸,应用的多为2,3,5——三氯苯氯甲酸,亦有2,4,5——三氯苯甲酸异构物.据国外报道,花生应用TCBA可增产荚果21.4～23.5%,国内有关试验则不多,且对其作用、增产机理、喷洒时间、浓度等...TCBA是一种人工合成的植物生长谢节剂,学名是三氯苯甲酸,应用的多为2,3,5——三氯苯氯甲酸,亦有2,4,5——三氯苯甲酸异构物.据国外报道,花生应用TCBA可增产荚果21.4～23.5%,国内有关试验则不多,且对其作用、增产机理、喷洒时间、浓度等看法也不尽一致.原铁岭农学院试验,100～300 P Pm不同浓度,于始花或盛花不同时期喷洒皆宜,可增产22.1—62.8%;广东省湛江黄曼容报道,始花期喷洒TCBA,可使开花高峰提前,有效花量和总花量增加,产量提高5.6～18.7%.展开更多
基金supported by the National Institutes of Health(NIH)grants R01 CA112029,R01 CA121211,and R01 CA186662(to R.Z.)and 1UL1RR025777(to S.V.)
文摘We have recently designed and synthesized several novel iminoquinone anticancer agents that have entered preclinical development for the treatment of human cancers.Herein we developed and validated a quantitative HPLC-MS/MS analytical method for one of the lead novel anticancer makaluvamine analog,TCBA-TPQ,and conducted a pharmacokinetic study in laboratory rats.Our results indicated that the HPLC-MS/MS method was precise,accurate,and specific.Using this method,we carried out in vitro and in vivo evaluations of the pharmacological properties of TCBA-TPQ and plasma pharmacokinetics in rats.Our results provide a basis for future preclinical and clinical development of this promising anticancer marine analog.
文摘TCBA是一种人工合成的植物生长谢节剂,学名是三氯苯甲酸,应用的多为2,3,5——三氯苯氯甲酸,亦有2,4,5——三氯苯甲酸异构物.据国外报道,花生应用TCBA可增产荚果21.4～23.5%,国内有关试验则不多,且对其作用、增产机理、喷洒时间、浓度等看法也不尽一致.原铁岭农学院试验,100～300 P Pm不同浓度,于始花或盛花不同时期喷洒皆宜,可增产22.1—62.8%;广东省湛江黄曼容报道,始花期喷洒TCBA,可使开花高峰提前,有效花量和总花量增加,产量提高5.6～18.7%.
