RESUMO
The occurrence of macrocyclic daphnane orthoesters (MDOs) with a 1-alkyl group originating from a C14 aliphatic chain is extremely limited in the plant kingdom and has only been isolated from Edgeworthia chrysantha. In the present study, LC-ESI-MS/MS analysis was performed on different parts of E. chrysantha, including flower buds, flowers, leaves, and stems, and resulted in the identification of seven MDOs in all the four plant parts, including two previously unreported compounds 1 and 7. Further LC-MS guided isolation was carried out to afford compounds 1 and 7, and their structures were determined by various spectroscopic analyses. These compounds were also evaluated for anti-HIV activity, thus expanding insights into the structure-activity relationships for MDOs.
Assuntos
Diterpenos , Thymelaeaceae , Cromatografia Líquida , Espectrometria de Massa com Cromatografia Líquida , Espectrometria de Massas em Tandem , Estrutura Molecular , Thymelaeaceae/químicaRESUMO
A total of 147 oral Kampo prescriptions, which are used clinically in Japan, were evaluated for their anti-glycation activity. Kakkonto demonstrated significant anti-glycation activity, prompting further analysis of its chemical constituents using LC-MS, which revealed the presence of two alkaloids, fourteen flavonoids, two but-2-enolides, five monoterpenoids, and four triterpenoid glycosides. To identify the components responsible for its anti-glycation activity, the Kakkonto extract was reacted with glyceraldehyde (GA) or methylglyoxal (MGO) and analyzed using LC-MS. In LC-MS analysis of Kakkonto reacted with GA, the peak intensity of ephedrine was attenuated, and three products from ephedrine-scavenging GA were detected. Similarly, LC-MS analysis of Kakkonto reacted with MGO revealed two products from ephedrine reacting with MGO. These results indicated that ephedrine was responsible for the observed anti-glycation activity of Kakkonto. Ephedrae herba extract, which contains ephedrine, also showed strong anti-glycation activity, further supporting ephedrine's contribution to Kakkonto's reactive carbonyl species' scavenging ability and anti-glycation activity.
Assuntos
Medicamentos de Ervas Chinesas , Efedrina , Efedrina/farmacologia , Efedrina/análise , Cromatografia Líquida , Óxido de Magnésio , Espectrometria de Massas em Tandem , Aldeído Pirúvico , Produtos Finais de Glicação Avançada/análiseRESUMO
Edgeworthianins A-E (1-5) were isolated from Edgeworthia chrysantha as a class of macrocyclic daphnane orthoesters with an unusual macrocyclic ring formed from a C14 aliphatic chain. Their structures were elucidated by extensive physicochemical and spectroscopic analyses. Compounds 2, 4, and 5 exhibited potent anti-HIV activity against HIV-1 infection of MT4 cells with EC50 values of 29.3, 8.4, and 2.9 nM, respectively. These compounds broaden the findings of the structure-activity relationship of macrocyclic daphnane orthoesters for further anti-HIV drug development.
Assuntos
Fármacos Anti-HIV , Diterpenos , Thymelaeaceae , Diterpenos/química , Thymelaeaceae/química , Fármacos Anti-HIV/farmacologia , Fármacos Anti-HIV/química , Relação Estrutura-Atividade , Estrutura MolecularRESUMO
Feruloylated acylglycerols (FAGs) have recently garnered a lot of interest as water-oil-miscible ferulic acid derivatives. A novel FAG derivate, 1-feruloyl-3-hexadecanoylglycerol (1), was isolated from Wikstroemia pilosa and its structure was elucidated from extensive physiochemical and spectroscopic analysis. Since the limited distribution of FAGs in plant species has been reported, a high-resolution accurate mass (HRAM) LC-MS quantitative analysis was carried out to determine the contents of 1 in ten plants of Wikstroemia species. As a result, compound 1 was detected in all species at contents of 1.29-50.96 mg/kg dry weight and W. dolichantha contained 1 at the highest content.
Assuntos
Wikstroemia , Cromatografia Líquida , GlicerídeosRESUMO
Twenty-five steroidal glycosides including eight undescribed compounds which were named as polygonatumosides H-O, were isolated from the 70 % EtOH extract of rhizomes of Polygonatum odoratum (Mill.) Druce (Asparagaceae). Their structures were elucidated by extensive spectroscopic analyses and chemical methods. The isolated compounds were evaluated cytotoxicity against three human cancer cell lines: human non-small cell lung cancer (A549), human epithelial colorectal adenocarcinoma (Caco2), and human hepatocellular carcinoma (HepG2) cells. Five compounds showed cytotoxicity against these cell lines with IC50 values in the range of 1.7-30.8 µM.
Assuntos
Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Polygonatum , Células CACO-2 , Glicosídeos/farmacologia , Humanos , Estrutura MolecularRESUMO
Structurally diverse tigliane diterpenoids have drawn significant research interest for drug discovery over many decades. Using LC-MS-guided fractionation and separation, the first phytochemical investigation on Wikstroemia lamatsoensis led to the isolation of eight tiglianes (1-8), including two new compounds, wikstrocin D (1) and wikstrocin E (2). The new structures were elucidated based on extensive physicochemical and spectroscopic analyses. The characteristic ESIMS/MS fragmentations of tiglianes 1-8 were also summarized. Among the isolated tiglianes, three compounds (8, 5, and 7) showed the most potent anti-HIV activity, with IC50 values of 0.18, 3.8, and 12.8 nM, respectively.
Assuntos
Fármacos Anti-HIV/química , Diterpenos/química , Forbóis/química , Wikstroemia/química , Fármacos Anti-HIV/farmacologia , Linhagem Celular , China , Diterpenos/farmacologia , HIV-1/efeitos dos fármacos , Humanos , Estrutura Molecular , Forbóis/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologiaRESUMO
Macrocyclic daphnane orthoesters (MDOs) have attracted significant research interest for the drug discovery to cure HIV infection based on the "Shock and Kill" strategy. In the present study, the first chemical study on Wikstroemia ligustrina (Thymelaeaceae) was carried out by LC-MS analysis and phytochemical investigation. Nine daphnane diterpenoids (1-9) including seven MDOs were detected by LC-MS analysis. Further phytochemical investigation resulted in the isolation and structural elucidation of five daphnanes (1, 2, 5, 8, and 9) with potent anti-HIV activity. Taking the isolated MDO (1) as a model compound, the MS/MS fragmentation pathway was also elucidated.
Assuntos
Diterpenos , Infecções por HIV , Wikstroemia , Cromatografia Líquida , Humanos , Compostos Fitoquímicos , Espectrometria de Massas em TandemRESUMO
Seven undescribed cembranoids, sacraoxides A-G (1, 3-8) were isolated from the gum resin of Boswellia sacra. Their structures were elucidated by extensive physicochemical and spectroscopic analysis, as well as ECD calculation, modified Mosher's method and X-ray diffraction crystallography. Compounds 6 and 7 exhibited inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide in RAW264.7 cells with IC50 values of 24.9 ± 1.7 and 36.4 ± 2.9 µM.
RESUMO
The stress response in the brain is not fully understood, although stress is one of the risk factors for developing mental disorders. On the other hand, the stimulation of the olfactory system can influence stress levels, and a certain smell has been empirically known to have a stress-suppressing effect, indeed. In this review, we first outline what stress is and previous studies on stress-responsive biomarkers (stress markers) in the brain. Subsequently, we confirm the olfactory system and review previous studies on the relationship between smell and stress response by species, such as humans, rats, and mice. Numerous studies demonstrated the stress-suppressing effects of aroma. There are also investigations showing the effects of odor that induce stress in experimental animals. In addition, we introduce recent studies on the effects of aroma of coffee beans and essential oils, such as lavender, cypress, α-pinene, and thyme linalool on the behavior and the expression of stress marker candidates in the brain. The transfer of volatile components into the brain is also discussed while using the results of thyme linalool as an example. These studies may provide a good opportunity to connect chemical research at the molecular level with neuropharmacological approaches in the future.
Assuntos
Encéfalo/fisiologia , Percepção Olfatória , Estresse Fisiológico , Estresse Psicológico , Animais , Biomarcadores , Encéfalo/efeitos dos fármacos , Conectoma , Humanos , Neurofarmacologia , OlfatoRESUMO
A phytochemical investigation of the barks of Eucommia ulmoides Oliv. resulted in the isolation of 18 flavonoids (1-18). The new compound, eucommiaflavone (1) was structurally elucidated by various spectroscopic analyses. In particular, Mo2(OAc)4-induced circular dichroism (ICD) analysis was applied to determine the absolute configuration of 1. Furthermore, five flavonoids (4, 9, 11, 13, and 15) revealed significant in vitro hepatoprotective activity against D-galactosamine-induced cytotoxicity in human hepatoma HepG2 cells.
Assuntos
Eucommiaceae , Flavonoides/farmacologia , Humanos , Extratos VegetaisRESUMO
(1) Background: Sesame has been popular as a healthy food since ancient times, and effects of the aroma component of roasted sesame are also expected. However, little research has been reported on its scent; (2) Methods: Jcl:ICR male mice were housed under water immersion stress for 24 h. Then, the scent of saline or sesame oil was inhaled to stress groups for 90 min. We investigated the effects of sesame oil aroma on the behavior and brains of mice; (3) Results: In an elevated plus maze test, the rate of entering to open arm and the staying time were decreased by the stress. These decrements were significantly enhanced by sesame oil aroma. Stress had a tendency to increase the serum corticosterone concentration, which was slightly decreased by the aroma. Expression of Kruppel-like factor-4 (Klf-4) and Dual-specificity phosphatase-1 (Dusp-1) in the striatum were increased by water immersion stress, and the level of Klf-4 and Dusp-1 in the striatum and hippocampus were significantly attenuated by sesame oil aroma (4) Conclusions: The present results strongly suggest that the odor component of sesame oil may have stress suppressing effects. Moreover, Klf-4 and Dusp-1 may be sensitive stress-responsive biomarkers.
Assuntos
Ansiolíticos/farmacologia , Corpo Estriado/efeitos dos fármacos , Hipocampo/efeitos dos fármacos , Odorantes/análise , Óleo de Gergelim/farmacologia , Estresse Psicológico/tratamento farmacológico , Administração por Inalação , Animais , Ansiolíticos/química , Biomarcadores/metabolismo , Corpo Estriado/metabolismo , Corpo Estriado/fisiopatologia , Corticosterona/sangue , Fosfatase 1 de Especificidade Dupla/genética , Fosfatase 1 de Especificidade Dupla/metabolismo , Expressão Gênica/efeitos dos fármacos , Hipocampo/metabolismo , Hipocampo/fisiopatologia , Fator 4 Semelhante a Kruppel , Fatores de Transcrição Kruppel-Like/genética , Fatores de Transcrição Kruppel-Like/metabolismo , Masculino , Aprendizagem em Labirinto/efeitos dos fármacos , Aprendizagem em Labirinto/fisiologia , Camundongos , Camundongos Endogâmicos ICR , Óleo de Gergelim/química , Sesamum/química , Estresse Psicológico/metabolismo , Estresse Psicológico/fisiopatologia , Estresse Psicológico/psicologia , Natação/psicologiaRESUMO
During a chemical investigation of Wikstroemia scytophylla, three new [wikstrocins A-C (1-3)] and three known tigliane diterpenoids (4-6) were isolated. The structures of the new compounds were elucidated from extensive physiochemical and spectroscopic analysis. The correlations between the ECD Cotton effects and B ring structures of tiglianes were also evaluated. The isolated compounds were assessed for their anti-HIV activity against HIV-1 infection of MT4 cells, and two compounds (4 and 6) showed potent anti-HIV activity with IC50 values of 3.8 and 12.8 nM, respectively.
Assuntos
Fármacos Anti-HIV/farmacologia , Diterpenos/farmacologia , Forbóis/farmacologia , Wikstroemia/química , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Linhagem Celular , Diterpenos/isolamento & purificação , Humanos , Análise Espectral/métodosRESUMO
Five new [daphneodorins D-H (1, 5, and 10-12)] and seven known daphnane diterpenoids (2-4 and 6-9) were isolated from Daphne odora. The structures of the new compounds were elucidated by extensive physicochemical and spectroscopic analysis. The isolated compounds were evaluated for their anti-HIV activity against HIV-1 infection of MT4 cells. Nine daphnane diterpenoid orthoesters (1-9) showed potent anti-HIV activity with EC50 values of 1.5-7.7 nM.
Assuntos
Fármacos Anti-HIV/química , Fármacos Anti-HIV/farmacologia , Daphne/química , Diterpenos/química , Diterpenos/farmacologia , Fármacos Anti-HIV/isolamento & purificação , Linhagem Celular , Diterpenos/isolamento & purificação , HIV/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Análise Espectral/métodos , Relação Estrutura-AtividadeRESUMO
Globally, alcohol consumption contributes to more than 3 million deaths each year. While much of its ramifications is preventable, a coherent public health discourse on how to limit alcohol-related harm has been overdue. By synthesizing information from national and global databases, we show in this analysis that alcohol consumption level and alcohol-attributable burden of diseases, particularly alcoholic liver disease (ALD), are intimately linked to national income distribution, cultural norms, religion, sex, age, and health status. Prevalence and burden of ALD are positively associated with economic standing in most countries, which necessitate active governmental control via cost-effective policies, such as the best buys proposed by the World Health Organization. To date, a number of critical questions remain unanswered over the molecular mechanisms underlying ALD pathophysiology; the insights gained thereof should provide new opportunities for the advancement of novel diagnostic and management strategies. In comparison with other prevailing liver diseases (e.g., viral hepatitis and nonalcoholic fatty liver disease), governmental support to ALD investigation has been sluggish in most Western countries and China, resulting in a dearth of breakthroughs on both the basic and clinical research fronts in the past decades. Emerging foci of clinical trials for ALD therapy include empirical use of probiotics, antioxidants, growth factors, monoclonal antibodies against key inflammatory mediators, and technology-enhanced behavioral interventions. In this article, we seek to provide a comprehensive analysis on the progress and challenges in tackling ALD as a global health problem, with particular emphasis on global disease burden, socioeconomic influences, research trends, government roles, and future therapies.
Assuntos
Carga Global da Doença/estatística & dados numéricos , Hepatopatias Alcoólicas/epidemiologia , Alcoolismo/complicações , Alcoolismo/prevenção & controle , Humanos , Hepatopatias Alcoólicas/diagnóstico , Hepatopatias Alcoólicas/etiologia , Hepatopatias Alcoólicas/terapia , Fatores SocioeconômicosRESUMO
Paeonol is a major bioactive ingredient in Moutan Cortex (the root barks of Paeonia suffruticosa Andrews) and exhibited a wide range of bioactivities such as anti-inflammation, anti-oxidation, hypoglycemic effect, analgesic, and others. Even though paeonol has been proven to possess significant pharmacological and therapeutic effects, its pharmacokinetic properties are not satisfactory since it has been found to have a rapid clearance in vivo. In the present study, the pharmacokinetics, tissue distribution and excretion of paeonol and its major metabolites were investigated in rats by an efficient and specific UPLC-MS/MS method. The results indicated that paeonol was rapidly absorbed, extensively metabolized, and widely distributed in various tissues without long-term accumulation after oral administration to rats. The major distribution tissues of paeonol and its metabolites were kidney, liver, and heart. Paeonol was able to cross the blood-brain barrier but rapidly decreased after 10 min. The total excretion of four metabolites in urine, bile, and feces was approximately 35.0% within 24 h, and the metabolites were mainly excreted through the urine. In addition, the hypoglycemic activities of paeonol and its metabolites were investigated by a glucose uptake assay on TNF-α mediated insulin resistance in 3T3-L1 adipocytes. The results showed that paeonol and its major metabolites displayed hypoglycemic activities. This is the first comprehensive and systematic report on the pharmacokinetics of paeonol and its metabolites. This research provides an important basis for the clinical development and application of active metabolites.
RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Sauropus androgynus L. Merr is an underexploited perennial shrub traditionally used as a medicinal plant in South Asia and Southeast Asia. The plant is regarded as not just a green vegetable for diet, but as a traditional herb for certain aliments. For instance, it has traditionally been used to relieve fever, to treat ulcers and diabetes, to promote lactation and eyesight, and to reduce obesity. AIM OF THE STUDY: This paper aims to review the botany, phytochemistry, ethnopharmacology, and pharmacological activities of S. androgynus, and discuss the known chemical constituents at work in S. androgynus-induced bronchiolitis obliterans for providing new ideas to the mechanism of the disease and pharmacology research of the plant. MATERIALS AND METHODS: The data presented in this review were collected from published literatures as well as the electronic databases of PubMed, CNKI, Web of Science, SCI finder, ACS, Science Direct, Wiley, Springer, Taylor, Google Scholar, and a number of unpublished resources, (e.g. books, and Ph.D. and M.Sc. dissertations). RESULTS: The scientific literature indicates that S. androgynus is a valuable and popular herbal medicine whose nutritional value is also higher than that of other commonly used vegetables. Phytochemical analyses identified high content of fatty acids, flavonoids, and polyphenols as the major bioactive components in S. androgynus. Crude extracts and phytochemical compounds isolated from S. androgynus show a wide spectrum of in vitro and in vivo pharmacological activities such as antioxidant, anti-inflammatory, anti-ulcer, skin whitening, anti-diabetic, and immunoregulatory activities. The traditional use, such as increasing lactation, treating ulcers and diabetes, and reducing obesity, have been evaluated and studied with various methods. Numerous reports have revealed the unusual link between the consumption of S. androgynus and the induction of a chronic and irreversible obstructive disease (namely, bronchiolitis obliterans), indicating that the toxicity and side effects of this plant that is presently used in health care and medicine are a major area of concern. CONCLUSION: Though little importance was attached to this green plant, S. androgynus has notable phytochemical constituents and various pharmacological activities including antioxidant, anti-inflammatory, and anti-obesity activities. Studies have firmly established the association between excessive consumption of the uncooked S. androgynus juice over a period of time and the occurrence of bronchiolitis obliterans. It is inadvisable to ingest excessive amounts of S. androgynus before fully understanding the pathogenesis and induction mechanism of this fatal disease. The phytochemistry of S. androgynus, its pharmacology for traditional use, S. androgynus-induced bronchiolitis obliterans still need further investigation.
Assuntos
Etnofarmacologia , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/toxicidade , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , Animais , Ásia , Humanos , Medicina Tradicional Chinesa , Medicina Tradicional , Compostos Fitoquímicos/química , Fitoterapia , Extratos Vegetais/química , Plantas MedicinaisRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Gogi berry is a traditional food supplement and medical herbal which has been widely used in Eastern Asian countries. Lycium barbarum polysaccharides (LBP) are the major active components of Gogi berry and have been proved to possess a lot of biological activities. AIM OF THE STUDY: We aimed to delineate the protective effect and mechanism of LBP on hepatic encephalopathy (HE). MATERIALS AND METHODS: We investigated the protective mechanism of LBP in a thioacetamide (TAA, intraperitoneally injected, 400â¯mg/kg) induced acute HE mice model. Key phenotypes of clinical HE were phenocopied in the mice model, including high mortality, severe hepatic histology injury, increased hepatic oxidative stress, apoptosis, enhanced circulating levels of pro-inflammatory cytokines and ammonia, suppressed tryptophan hydroxylase activity, and deficits in locomotor activity. RESULTS: The pathological alterations were effectively ameliorated by the oral administration with LBP (5â¯mg/kg, oral gavage, everyday), which were mediated by regulating MAPK pathways in both the liver and brain. Knockout of pro-inflammatory cytokines TNF-α or IL-6 effectively ameliorated impaired mice locomotor activity and MAPK activation in the brain. In an in vitro TNF-α-, IL-6-, or ammonia-induced microglia damaged cell model, cell injuries were evidently protected by the co-administration with LBP (50⯵g/ml). CONCLUSION: LBP ameliorated the hepatic/brain injuries and impaired locomotor activities in a HE mice model. Pro-inflammatory cytokines may serve as communicating molecules linking the liver and brain for the HE pathogenesis, partly through MAPK regulation.
Assuntos
Encéfalo/efeitos dos fármacos , Citocinas/metabolismo , Encefalopatia Hepática/prevenção & controle , Mediadores da Inflamação/metabolismo , Fígado/efeitos dos fármacos , Lycium , Extratos Vegetais/farmacologia , Polissacarídeos/farmacologia , Animais , Encéfalo/metabolismo , Encéfalo/patologia , Linhagem Celular , Citocinas/deficiência , Citocinas/genética , Modelos Animais de Doenças , Frutas , Encefalopatia Hepática/induzido quimicamente , Encefalopatia Hepática/metabolismo , Encefalopatia Hepática/patologia , Interleucina-6/metabolismo , Fígado/metabolismo , Fígado/patologia , Locomoção/efeitos dos fármacos , Lycium/química , Masculino , Camundongos Endogâmicos C57BL , Camundongos Knockout , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Extratos Vegetais/isolamento & purificação , Polissacarídeos/isolamento & purificação , Transdução de Sinais , Tioacetamida , Fator de Necrose Tumoral alfa/metabolismoRESUMO
Three novel gnidimacrin related macrocyclic daphnanes (GMDs), daphneodorins A-C (2-4), were isolated from Daphne odora Thunb., together with gnidimacrin (1). Their structures were established by extensive physicochemical and spectroscopic analyses. Compounds 2 and 3 potently inhibited HIV-1 replication at subnanomolar concentrations (EC50 0.16 and 0.25 nM, respectively). Compounds 2-4 represent a novel type of GMDs that are highly oxygenated on the macrocyclic ring, suggesting good potential for anti-HIV drug development by further chemical modification.
Assuntos
Fármacos Anti-HIV/farmacologia , Daphne/química , HIV-1/efeitos dos fármacos , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Relação Dose-Resposta a Droga , Compostos Macrocíclicos/química , Compostos Macrocíclicos/isolamento & purificação , Compostos Macrocíclicos/farmacologia , Testes de Sensibilidade Microbiana , Conformação Molecular , Relação Estrutura-Atividade , Replicação Viral/efeitos dos fármacosRESUMO
Three-dimension quantitative structure activity relationship (3D-QSAR) was one of the major statistical techniques to investigate the correlation of biological activity with structural properties of candidate molecules, and the accuracy of statistic greatly depended on molecular alignment methodology. Exhaustive conformational search and successful conformational superposition could extremely improve the predictive accuracy of QSAR modeling. In this work, we proposed a solution to optimize QSAR prediction by multiple-conformational alignment methods, with a set of 40 flexible PTP1B inhibitors as case study. Three different molecular alignment methods were used for the development of 3D-QSAR models listed as following: (1) docking-based alignment (DBA); (2) pharmacophore-based alignment (PBA) and (3) co-crystallized conformer-based alignment (CCBA). Among these three alignments, it was indicated that the CCBA was the best and the fastest strategy in 3D-QSAR development, with the square correlation coefficient (r2) and cross-validated squared correlation coefficient (q2) of comparative molecular field analysis (CoMFA) were 0.992 and 0.694; the r2 and q2 of comparative molecular similarity indices analysis (CoMSIA) were 0.972 and 0.603, respectively. The alignment methodologies used here not only generated a robust QSAR model with useful molecular field contour maps for designing novel PTP1B inhibitors, but also provided a solution for constructing accurate 3D-QSAR model for various disease targets. Undoubtedly, such attempt in QSAR analysis would greatly help us to understand essential structural features of inhibitors required by its target, and so as to discover more promising chemical derivatives.
Assuntos
Inibidores Enzimáticos/farmacologia , Proteína Tirosina Fosfatase não Receptora Tipo 1/antagonistas & inibidores , Relação Quantitativa Estrutura-Atividade , Inibidores Enzimáticos/química , Humanos , Modelos Moleculares , Estrutura Molecular , Proteína Tirosina Fosfatase não Receptora Tipo 1/metabolismoRESUMO
Diabetes is one of the metabolic disorders in the world. It is the prime reason of mortality and morbidity owing to hyperglycemia which is link with numerus obstacles. Artemisia argyi is commonly used as an ingredient in healthy foods as well as an herbal medicine in Asian countries. The present research aims to evaluate the hypoglycemic effects of A. argyi and reveal its the potentially active constituents. The chemical composition was identified by HPLC-DAD-Q-TOF-MS, and fractionation was performed by extraction. The fractions were assessed by the blood glucose level, oral glucose tolerance and small intestinal α-glucosidase inhibitory tests, and an analysis of the total phenolic content (TPC), antioxidant and α-glucosidase inhibitory activities. In our efforts to characterize the compounds responsible for hypoglycemic effect, bioactivity-guided fraction of the MeOH extract and chemical investigation of its active EtOAc fraction led to the successful identification of caffeoylquinic acids, which were elucidated by molecular docking, using the crystal structure of S. cerevisiae isomaltase (PD code: 3AXI). In summary, this bio-guided search revealed that caffeoylquinic acids from A. argyi as potential active constituents displayed with hypoglycemic activity, which provided a basis for further study of pharmacological activity.