Evaluating the consistency of herb injectable formulations could improve their product quality and clinical safety,particularly concerning the composition and content levels of trace ingredients.Panax notoginseng Sapo...Evaluating the consistency of herb injectable formulations could improve their product quality and clinical safety,particularly concerning the composition and content levels of trace ingredients.Panax notoginseng Saponins Injection(PNSI),widely used in China for treating acute cardiovascular diseases,contains low-abundance(10%-25%)and trace saponins in addition to its five main constituents(notoginsenoside R1,ginsenoside Rg1,ginsenoside Re,ginsenoside Rb1,and ginsenoside Rd).This study aimed to establish a robust analytical method and assess the variability in trace saponin levels within PNSI from different vendors and formulation types.To achieve this,a liquid chromatography-triple quadrupole mass spectrometry(LC-MS/MS)method employing multiple ions monitoring(MIM)was developed.A“post-column valve switching”strategy was implemented to eliminate highly abundant peaks(NR_(1),Rg_(1),and Re)at 26 min.A total of 51 saponins in PNSI were quantified or relatively quantified using 18 saponin standards,with digoxin as the internal standard.This study evaluated 119 batches of PNSI from seven vendors,revealing significant variability in trace saponin levels among different vendors and formulation types.These findings highlight the importance of consistent content in low-abundance and trace saponins to ensure product control and clinical safety.Standardization of these ingredients is crucial for maintaining the quality and effectiveness of PNSI in treating acute cardiovascular diseases.展开更多
Five new racemic N-acetyldopamine (NADA) trimers, asponchimides A−E ( 1 − 5 ), were isolated from Aspongopus chinensis, a prominent traditional Chinese medicinal insect employed for alleviating pain, treating indigest...Five new racemic N-acetyldopamine (NADA) trimers, asponchimides A−E ( 1 − 5 ), were isolated from Aspongopus chinensis, a prominent traditional Chinese medicinal insect employed for alleviating pain, treating indigestion, and addressing kidney ailments. Compounds 1 − 5 were successfully resolved by chiral high-performance liquid chromatography (HPLC), yielding five pairs of enantiomers: (+)- and (−)-asponchimides A−E ( 1a / 1b − 5a / 5b ). Their structural identities were discerned by extensive spectroscopic analyses, including high-resolution mass spectrometry (HRMS), ultraviolet-visible (UV-Vis) spectroscopy, infrared (IR) spectroscopy, and nuclear magnetic resonance (NMR), and their absolute configurations were determined by electronic circular dichroism (ECD) calculations. Compounds 1 − 5 are pioneering instances of NADA trimers featuring a Δ7 double bond. When subjected to a series of bioassays, a majority of the compounds exhibited weak inhibitory activity against nitric oxide (NO) production in LPS-induced RAW 264.7 cells.展开更多
The phytochemical investigation of the leaves and twigs of Croton yunnanensis resulted in the isolation of eight new clerodane furanoditerpenoids,named croyunfuranoids A-H(1-8),along with three known analogs(9-11).The...The phytochemical investigation of the leaves and twigs of Croton yunnanensis resulted in the isolation of eight new clerodane furanoditerpenoids,named croyunfuranoids A-H(1-8),along with three known analogs(9-11).The structures of these compounds were elucidated using spectroscopic analyses,and their absolute configurations were determined through a combination of electronic circular dichroism(ECD)calculations and single-crystal X-ray diffraction.Notably,Croyunfuranoid D(4)is identified as a rare 18,19-dinor-clerodane diterpenoid.Additionally,the structure of a previously reported diterpenoid,crotonyunnan B,was revised.All isolated compounds were evaluated for their inhibitory activities on nitric oxide(NO)production in LPS-induced RAW 264.7 macrophages.Among them,compounds 5 and 6 demonstrated significant inhibitory effects,with IC_(50)values of 20.33±2.31 and 22.80±1.31μmol·L^(-1),respectively.展开更多
基金supported by the Science and Technology Service Network Initiative of the Chinese Academy of Sciences(STS,No.KFJ-STS-QYZD-2021-03-003)the Construction Projects of the Research Center for Notoginseng Health Products by the Department of Science and Technology of Guangxi Province(No.AD20297068)the Sanming Project of Medicine in Shenzhen(No.SZZYSM202106004).
文摘Evaluating the consistency of herb injectable formulations could improve their product quality and clinical safety,particularly concerning the composition and content levels of trace ingredients.Panax notoginseng Saponins Injection(PNSI),widely used in China for treating acute cardiovascular diseases,contains low-abundance(10%-25%)and trace saponins in addition to its five main constituents(notoginsenoside R1,ginsenoside Rg1,ginsenoside Re,ginsenoside Rb1,and ginsenoside Rd).This study aimed to establish a robust analytical method and assess the variability in trace saponin levels within PNSI from different vendors and formulation types.To achieve this,a liquid chromatography-triple quadrupole mass spectrometry(LC-MS/MS)method employing multiple ions monitoring(MIM)was developed.A“post-column valve switching”strategy was implemented to eliminate highly abundant peaks(NR_(1),Rg_(1),and Re)at 26 min.A total of 51 saponins in PNSI were quantified or relatively quantified using 18 saponin standards,with digoxin as the internal standard.This study evaluated 119 batches of PNSI from seven vendors,revealing significant variability in trace saponin levels among different vendors and formulation types.These findings highlight the importance of consistent content in low-abundance and trace saponins to ensure product control and clinical safety.Standardization of these ingredients is crucial for maintaining the quality and effectiveness of PNSI in treating acute cardiovascular diseases.
基金supported by the Key Program of National Natural Science Foundation of China(NO.82130111)High-level Innovative Research Institute of Department of Science and Technology of Guangdong Province(No.2021B0909050003)High-level New R&D Institute of Department of Science and Technology of Guangdong Province(No.2019B090904008)。
文摘Five new racemic N-acetyldopamine (NADA) trimers, asponchimides A−E ( 1 − 5 ), were isolated from Aspongopus chinensis, a prominent traditional Chinese medicinal insect employed for alleviating pain, treating indigestion, and addressing kidney ailments. Compounds 1 − 5 were successfully resolved by chiral high-performance liquid chromatography (HPLC), yielding five pairs of enantiomers: (+)- and (−)-asponchimides A−E ( 1a / 1b − 5a / 5b ). Their structural identities were discerned by extensive spectroscopic analyses, including high-resolution mass spectrometry (HRMS), ultraviolet-visible (UV-Vis) spectroscopy, infrared (IR) spectroscopy, and nuclear magnetic resonance (NMR), and their absolute configurations were determined by electronic circular dichroism (ECD) calculations. Compounds 1 − 5 are pioneering instances of NADA trimers featuring a Δ7 double bond. When subjected to a series of bioassays, a majority of the compounds exhibited weak inhibitory activity against nitric oxide (NO) production in LPS-induced RAW 264.7 cells.
基金supported by the National Natural Science Foundation of China(Nos.82104020 and 82130111)the High-level Innovative Research Institute of Department of Science and Technology of Guangdong Province(No.2021B0909050003)the High-level New R&D Institute of Department of Science and Technology of Guangdong Province(No.2019B090904008)。
文摘The phytochemical investigation of the leaves and twigs of Croton yunnanensis resulted in the isolation of eight new clerodane furanoditerpenoids,named croyunfuranoids A-H(1-8),along with three known analogs(9-11).The structures of these compounds were elucidated using spectroscopic analyses,and their absolute configurations were determined through a combination of electronic circular dichroism(ECD)calculations and single-crystal X-ray diffraction.Notably,Croyunfuranoid D(4)is identified as a rare 18,19-dinor-clerodane diterpenoid.Additionally,the structure of a previously reported diterpenoid,crotonyunnan B,was revised.All isolated compounds were evaluated for their inhibitory activities on nitric oxide(NO)production in LPS-induced RAW 264.7 macrophages.Among them,compounds 5 and 6 demonstrated significant inhibitory effects,with IC_(50)values of 20.33±2.31 and 22.80±1.31μmol·L^(-1),respectively.