| Artemisia argyi Levl.et Van.is one of the earliest medicinal plants used in traditional Chinese medicine."Bencao Gangmu" records that "ai" is a plant created by heaven,which can tonify qi,nourish blood,aid digestion,and promote blood circulation.Traditional Artemisiae Argyi Folium is believed to have the functions of warming the meridians and stopping bleeding,dispelling cold and relieving pain.It is regarded as a Chinese herbal medicine for expelling evil and eliminating diseases,and is widely used in moxibustion,Chinese patent medicine,food(such as green rice cakes),and herbal baths.In traditional Chinese medicine,Artemisiae Argyi Folium is aged for more than three years to achieve mild,dry,and dispersing properties.While literature has reported a decrease in the content of volatile components during the aging process,there are few studies on the changes in non-volatile components.Since pharmacological effects are closely related to chemical composition,further research is needed to investigate whether the chemical composition of Artemisiae Argyi Folium changes during the aging process.This study aims to systematically investigate the chemical composition of three-year-old aged Artemisiae Argyi Folium produced in Nanyang and discover lead compounds with novel structures and significant pharmacological activities.This will provide scientific evidence for the traditional use of Artemisiae Argyi Folium as a long-term aged herb.Chapter 1 reviews the chemical composition and biological activities of Artemisiae Argyi Folium.It summarizes the chemical components such as volatile oils,flavonoids,organic acids,terpenes,and others,and the activities of Artemisiae Argyi Folium,such as antioxidant,anti-tumor,immune regulation,anti-inflammatory,antibacterial,insecticidal,and neuroprotective effects.This provides a theoretical basis for further research on Artemisiae Argyi Folium.Chapter 2 investigates the chemical composition of three-year-old aged Artemisiae Argyi Folium produced in Nanyang.Various chromatographic separation techniques,such as preparative and semi-preparative HPLC,were used to systematically isolate and analyze the ethyl acetate layer of three-year-old aged Artemisiae Argyi Folium produced in Nanyang.Of the 63 components identified,22 were new compounds,such as oxidized or open-ring sesquiterpenes,named Artemisiol A~V;and 41 were known compounds,including triterpenes(11),sesquiterpenes(25),flavonoids,and organic acids,among others.Chapter 3 summarizes 32 major components in Artemisiae Argyi Folium through literature research,and constructs a network relationship of "active ingredient groupmajor component-target pathway-pharmacological action-traditional medicinal effect" using network pharmacology analysis.The phenylpropanoic acid and flavonoid groups in the active ingredient group of Artemisiae Argyi Folium mainly act on PPAR,IL-17,MAPK,JAK-STAT,and other signaling pathways through targets such as AKT1,CASP3,and STAT3,showing anti-inflammatory and antioxidant effects.Sesquiterpenes may regulate EGFR and play an anti-tumor role,and EGFR is involved in the infection of HBV in host cells,indicating a potential anti-HBV effect.Finally,the cytotoxicity and anti-HBV activity of sesquiterpenes in three-yearold aged Artemisiae Argyi Folium produced in Nanyang were verified.Using lamivudine as a positive control,the Hep G 2.2.15 cell model was used to evaluate the cytotoxicity by MTT assay and detect the content of HBe Ag and HBs Ag by ELISA.It was found that the sesquiterpenes in Artemisiae Argyi Folium generally have cytotoxicity,and for the first time,sesquiterpenes with α-methylene-γ-lactone ring and3,4-epoxy-labdane-type sesquiterpenes with low cytotoxicity and high HBs Ag inhibition rate were discovered.Research shows that the organic acid and flavonoid components in three-year dried Artemisiae Argyi Folium from Nanyang have hardly changed.However,sesquiterpenoids are prone to double bond oxidation or ring opening,while triterpenoids are prone to side chain degradation,generating degraded triterpenoids.It is speculated that during the aging process and under the influence of external factors and their own properties,sesquiterpenoid components gradually undergo oxidation to form corresponding alcohols,and other oxidation products.The study found that some sesquiterpenoid compounds in dried Artemisiae Argyi Folium have certain anti-tumor activity,and some compounds have good potential for anti-HBV activity.This may be the material basis for the traditional medicinal effect of Artemisiae Argyi Folium in dispelling cold evils,reducing swelling,and dispersing masses. |