1.Screening of Anti-Streptococcus pneumoniae Active Ingredients from Pilea peltata
Zhiying WEI ; Yan HUANG ; Shenggao YIN ; Jie LIANG ; Chengsheng LU ; Fangchan LI ; Yuting XIE ; Yaohua LI ; Xiaojiao PAN
Herald of Medicine 2025;44(5):687-694
Objective To screen the anti-Streptococcus pneumoniae(Spn)active ingredients in vitro from different po-lar parts of Pilea peltata,and to examine the combined antibacterial effect of the active ingredient and amoxicillin(AMX).Methods A 96-well plate microdilution method was used to determine the minimum inhibitory concentration(MIC)of different polar parts;the most active polar part was separated by preparative high-performance liquid chromatography,and the active ingre-dients were identified using spectral technology.The fractional inhibitory concentration(FIC)of active ingredients and AMX was determined by the 96-well plate chessboard microdilution method.The crystal violet method was used to investigate the effect of ac-tive ingredients on Spn biofilm.The effect of active ingredients on the appearance and morphology of Spn was investigated under the electron microscope.Results The MICs of the petroleum ether part,chloroform part,ethyl acetate part,n-butanol part,and water part were 1.000,1.000,0.500,1.000,and 2.000 mg·mL-1 respectively,among which the ethyl acetate part had the stron-gest antibacterial activity.Three compounds were isolated from ethyl acetate,namely 5,7,3',4'-tetramethoxyflavone 1,8-O-(p-coumaroyl)-1(10)E,4(5)E-humuladien-8-ol 2 and 1-O-p-coumaroyl copaborneol 3.These compounds were all isolated for the first time from Pilea peltate,their MICs against Spn were 200.000,50.000,and 25.000 μg·mL-1 respectively,and the compound 3 had the strongest antibacterial activity;the FIC value of AMX and compound 3 was 0.50,which had a synergistic antibacterial effect on Spn.Both AMX and compound 3 had inhibitory effects on Spn biofilm,but the biofilm inhibition rate of compound 3(59.10±1.04%)was significantly lower than AMX(87.38±0.84)%(P<0.01);Moreover,there was no significant difference in biofilm inhibition rate between the combination of the two and AMX(P>0.05).The scanning electron microscope results showed that the bacterial cells in the compound 3 group had a smooth surface but varying degrees of depression.The surface of the bacteri-al cells in the AMX group and the AMX combined compound 3 group showed severe swelling and rupture.Conclusions Fla-vonoids and sesquiterpenoids are both the anti-Spn active components of Pilea peltate.Among them,sesquiterpenoids have more potent antibacterial activity,and their antibacterial action mechanism is related to inhibiting bacterial biofilms.Compound 3 and AMX have a synergistic antibacterial effect on Spn,but its mechanism of action is not by enhancing biofilm inhibition;although compound 3 cannot destroy the cell wall of Spn,it still has a negative impact on the appearance of the bacteria.
2.Screening of Anti-Streptococcus pneumoniae Active Ingredients from Pilea peltata
Zhiying WEI ; Yan HUANG ; Shenggao YIN ; Jie LIANG ; Chengsheng LU ; Fangchan LI ; Yuting XIE ; Yaohua LI ; Xiaojiao PAN
Herald of Medicine 2025;44(5):687-694
Objective To screen the anti-Streptococcus pneumoniae(Spn)active ingredients in vitro from different po-lar parts of Pilea peltata,and to examine the combined antibacterial effect of the active ingredient and amoxicillin(AMX).Methods A 96-well plate microdilution method was used to determine the minimum inhibitory concentration(MIC)of different polar parts;the most active polar part was separated by preparative high-performance liquid chromatography,and the active ingre-dients were identified using spectral technology.The fractional inhibitory concentration(FIC)of active ingredients and AMX was determined by the 96-well plate chessboard microdilution method.The crystal violet method was used to investigate the effect of ac-tive ingredients on Spn biofilm.The effect of active ingredients on the appearance and morphology of Spn was investigated under the electron microscope.Results The MICs of the petroleum ether part,chloroform part,ethyl acetate part,n-butanol part,and water part were 1.000,1.000,0.500,1.000,and 2.000 mg·mL-1 respectively,among which the ethyl acetate part had the stron-gest antibacterial activity.Three compounds were isolated from ethyl acetate,namely 5,7,3',4'-tetramethoxyflavone 1,8-O-(p-coumaroyl)-1(10)E,4(5)E-humuladien-8-ol 2 and 1-O-p-coumaroyl copaborneol 3.These compounds were all isolated for the first time from Pilea peltate,their MICs against Spn were 200.000,50.000,and 25.000 μg·mL-1 respectively,and the compound 3 had the strongest antibacterial activity;the FIC value of AMX and compound 3 was 0.50,which had a synergistic antibacterial effect on Spn.Both AMX and compound 3 had inhibitory effects on Spn biofilm,but the biofilm inhibition rate of compound 3(59.10±1.04%)was significantly lower than AMX(87.38±0.84)%(P<0.01);Moreover,there was no significant difference in biofilm inhibition rate between the combination of the two and AMX(P>0.05).The scanning electron microscope results showed that the bacterial cells in the compound 3 group had a smooth surface but varying degrees of depression.The surface of the bacteri-al cells in the AMX group and the AMX combined compound 3 group showed severe swelling and rupture.Conclusions Fla-vonoids and sesquiterpenoids are both the anti-Spn active components of Pilea peltate.Among them,sesquiterpenoids have more potent antibacterial activity,and their antibacterial action mechanism is related to inhibiting bacterial biofilms.Compound 3 and AMX have a synergistic antibacterial effect on Spn,but its mechanism of action is not by enhancing biofilm inhibition;although compound 3 cannot destroy the cell wall of Spn,it still has a negative impact on the appearance of the bacteria.
3.Visualization analysis on research literature about TCM formula granules based on CiteSpace
Xiaohong HUANG ; Haiyan CHEN ; Zijiu LIANG ; Fangchan LI ; Qinghua LIN ; Qing CHEN ; Lin JIANG
International Journal of Traditional Chinese Medicine 2024;46(5):657-664
Objective:To analyze the research hotspots and development trends of TCM formula granules.Methods:Literature about TCM formula granules was retrieved from CNKI from the establishment of the database to August 31, 2022. CiteSpace 5.7.R5 software was used to visually analyze the information such as literature volume, journals, research authors, research institutions, and keywords, and to draw the knowledge map.Results:Totally 1 135 articles were finally included. The number of articles published on TCM formula granules research showed a year-on-year increase. The main journals were the Chinese Journal of Experimental Traditional Medical Formulation and the Asia-Pacific Traditional Medicine. The research teams represented by Sun Dongmei and Li Junshan and the research institutions of Guangdong Yifang Pharmaceutical Co.,Ltd. and Shenwei Pharmaceutical Group Co., Ltd. were formed. The research contents mainly covered characteristic chromatogram, content determination, quality standards, standard decoction, extraction processes and so on. Conclusions:The determination of the active components of TCM formula granules, their consistency with the chemical composition of tonics and their equivalence with clinical efficacy remain hotspots for future research. At present, the research on TCM formula granules is at a developmental stage and should be further developed and cooperation between institutions and authors should be strengthened.
4.Optimization of Extraction Process for the Total Alkaloids of Longzuan Tongbi Fang by Central Composite Design and Response Surface Method
A'na MI ; Yudong LUO ; Yuqiang WU ; Fangchan LI ; Lin JIANG ;
China Pharmacist 2017;20(4):629-634
Objective:To optimize the extraction process for the total alkaloids of Longzuan Tongbi Fang by central composite design and response surface method.Methods:The independent variables were the ethanol contention,solvent consumption and extraction time,and the dependent variable was the weighted overall desirability of the content of total alkaloids and kukoline.The extraction process for the total alkaloids of Longzuan Tongbi Fang was optimized by central composite design and response surface method.Results:The optimum extraction conditions were as follows:9-fold amount of solvent was used,refluxed for 130 min,extracted twice,and the ethanol concentration was 75%.Conclusion:The central composite design and response surface method used for the extraction optimization for the total alkaloids of Longzuan Tongbi Fang is very simple and highly predictive.

Result Analysis
Print
Save
E-mail