Toosendanin(TSN),a tetracyclic triterpenoid derived from Melia toosendan and M.azedarach,demonstrates broad application prospects in cancer treatment.Although previously employed as a pesticide,recent studies have rev...Toosendanin(TSN),a tetracyclic triterpenoid derived from Melia toosendan and M.azedarach,demonstrates broad application prospects in cancer treatment.Although previously employed as a pesticide,recent studies have revealed its potential therapeutic value in treating various types of cancer.TSN exerts an anticancer effect via mechanisms including proliferation inhibition,apoptosis induction,migration suppression,and angiogenesis inhibition.However,TSN's toxicity,particularly its hepatotoxicity,significantly limits its therapeutic application.This review explored the dual nature of TSN,evaluating both its anticancer potential and toxicological risks,emphasizing the importance of balancing these aspects in therapeutic applications.Furthermore,we investigated the incorporation of TSN into novel therapeutic strategies,such as Proteolysis-targeting chimeras(PROTAC)technology and nanotechnology-based drug delivery systems(DDS),which enhance treatment efficacy while mitigating toxicity in normal tissues.展开更多
To investigate the effect on central nervous transmission of toosendanin (TSN), a presynaptic blocker, rat striatum was perfused in vivo with a TSN-containing artificial cere-brospinal fluid (ACSF) and the level of do...To investigate the effect on central nervous transmission of toosendanin (TSN), a presynaptic blocker, rat striatum was perfused in vivo with a TSN-containing artificial cere-brospinal fluid (ACSF) and the level of dopamine (DA) as well as related metabolites in the collected dialysates has been determined by a microbore HPLC with electrochemical detection (mi-crobore HPLC-ECD). The results are as follows: ( i ) TSN induced a biphasic change of DA from its basal level;( ii ) the basal contents of two metabolites, 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) increased in turn and stayed at a higher level than basal control for a long period. The basal level of 5-hydroxyindoleacetic acid (5-HIAA), a metabolite of 5-hydroxytryptamine(5-HT), had a change similar to that of HVA; (iii) after per-fusion with TSN-containing ACSF, high K+-evoked DA release was inhibited. These results show that TSN does not selectively affect acetylcholine (ACh) release, but probably acts on a common展开更多
Toosendanin (TSN), a triterpenoid derivative extracted from the bark of Melia toosendan Seib et Zucc and used in Chinese traditional medicine as an anthelmintic against ascaris, is a presynaptic neuromuscular blocker....Toosendanin (TSN), a triterpenoid derivative extracted from the bark of Melia toosendan Seib et Zucc and used in Chinese traditional medicine as an anthelmintic against ascaris, is a presynaptic neuromuscular blocker. Without affecting the nerve conduction, the muscle resting potential as well as acetylcholine (ACh) sensitivity of the muscle membrane at the end-plate region, TSN blocks the neuromuscular transmission selectively by inhibiting ACh release from the motor nerve terminals. It was interesting to notice展开更多
A new method for the determination of toosendanin in the bark of Melia toosendan sieb.et zucc.by reversed-phase high performance liquid chromatography（RP-HPLC）with MeOH-H2O as the mobile phase at 215 nm of the uv-vi...A new method for the determination of toosendanin in the bark of Melia toosendan sieb.et zucc.by reversed-phase high performance liquid chromatography（RP-HPLC）with MeOH-H2O as the mobile phase at 215 nm of the uv-vis wavelength was investigated.A good seperatioin of toosendanin with matrix was obtained within 20 min by using Eclipse XDB-C8 column.The linear regression equation for peak area-toosendain concentration is A=20.818C-31,r=0.9997.展开更多
基金supported by the National Natural Science Foundation of China(Nos.82322073,82304790,and 82173846)China Postdoctoral Innovative Talent Support Program(BX20220213)+10 种基金Shanghai Rising-Star Program(No.22QA1409100)Oriental Scholars of Shanghai(No.TP2022081)Jiangxi Province Thousand Talents Program(No.jxsq2023102168)Young Talent Lifting Project of China Association of Chinese Medicine[No.CACM-(2021-QNRC2-A08)]Shanghai Science and Technology Innovation Action Plan(No.21S11902800)Three-year Action Plan for Shanghai TCM Development and Inheritance Program[Nos.ZY(2021-2023)-0401 and ZY(2021-2023)-0208]Innovation Team and Talents Cultivation Program of National Administration of Traditional Chinese Medicine(No.ZYYCXTD-D-202004)CAMS Innovation Fund for Medical Sciences(CIFMS)(No.2023-I2M-3-009)Shanghai Sailing Program(Nos.22YF1445000 and 23YF1442600)the National Key R&D Program of China(No.2022YFC3502000)High-level Key Discipline of National Administration of Traditional Chinese Medicine,Innovation team of high-level local universities in Shanghai:Strategic Innovation Team of TCM Chemical Biology,Organizational Key Research and Development Program of Shanghai University of Traditional Chinese Medicine(No.2023YZZ02)。
文摘Toosendanin(TSN),a tetracyclic triterpenoid derived from Melia toosendan and M.azedarach,demonstrates broad application prospects in cancer treatment.Although previously employed as a pesticide,recent studies have revealed its potential therapeutic value in treating various types of cancer.TSN exerts an anticancer effect via mechanisms including proliferation inhibition,apoptosis induction,migration suppression,and angiogenesis inhibition.However,TSN's toxicity,particularly its hepatotoxicity,significantly limits its therapeutic application.This review explored the dual nature of TSN,evaluating both its anticancer potential and toxicological risks,emphasizing the importance of balancing these aspects in therapeutic applications.Furthermore,we investigated the incorporation of TSN into novel therapeutic strategies,such as Proteolysis-targeting chimeras(PROTAC)technology and nanotechnology-based drug delivery systems(DDS),which enhance treatment efficacy while mitigating toxicity in normal tissues.
文摘To investigate the effect on central nervous transmission of toosendanin (TSN), a presynaptic blocker, rat striatum was perfused in vivo with a TSN-containing artificial cere-brospinal fluid (ACSF) and the level of dopamine (DA) as well as related metabolites in the collected dialysates has been determined by a microbore HPLC with electrochemical detection (mi-crobore HPLC-ECD). The results are as follows: ( i ) TSN induced a biphasic change of DA from its basal level;( ii ) the basal contents of two metabolites, 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) increased in turn and stayed at a higher level than basal control for a long period. The basal level of 5-hydroxyindoleacetic acid (5-HIAA), a metabolite of 5-hydroxytryptamine(5-HT), had a change similar to that of HVA; (iii) after per-fusion with TSN-containing ACSF, high K+-evoked DA release was inhibited. These results show that TSN does not selectively affect acetylcholine (ACh) release, but probably acts on a common
基金This work was supported by National Institute for Physiological Science, Japan and the National Natural Science Foundation of China. Partial experiments were performed in Okazaki, Japan
文摘Toosendanin (TSN), a triterpenoid derivative extracted from the bark of Melia toosendan Seib et Zucc and used in Chinese traditional medicine as an anthelmintic against ascaris, is a presynaptic neuromuscular blocker. Without affecting the nerve conduction, the muscle resting potential as well as acetylcholine (ACh) sensitivity of the muscle membrane at the end-plate region, TSN blocks the neuromuscular transmission selectively by inhibiting ACh release from the motor nerve terminals. It was interesting to notice
文摘A new method for the determination of toosendanin in the bark of Melia toosendan sieb.et zucc.by reversed-phase high performance liquid chromatography（RP-HPLC）with MeOH-H2O as the mobile phase at 215 nm of the uv-vis wavelength was investigated.A good seperatioin of toosendanin with matrix was obtained within 20 min by using Eclipse XDB-C8 column.The linear regression equation for peak area-toosendain concentration is A=20.818C-31,r=0.9997.
