RESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Longdan zhike tablet (LDZK) is a Tibetan medicine formula commonly used in the highland region of Tibet, China, to ameliorate respiratory diseases, such as acute bronchitis and asthma. In Chinese traditional medicine, some herbal formulas with anti-inflammatory properties targeting the respiratory system are clinically adopted as supplementary therapies for chronic obstructive pulmonary disease (COPD). However, the specific anti-COPD effects of LDZK remain to be evaluated. AIM OF THE STUDY: The aim of this study is to identify the principal bioactive compounds in LDZK, and elucidate the effects and mechanisms of the LDZK on COPD. METHODS: High-resolution mass spectrometry was utilized for a comprehensive characterization of the chemical composition of LDZK. The therapeutic effects of LDZK were assessed on the LPS-papain-induced COPD mouse model, and LPS-induced activation model of A549 cells. The safety of LDZK was evaluated by orally administering a single dose of 30 g/kg to rats and monitoring physiological and biochemical indicators after a 14-day period. Network pharmacology and Western blot analysis were employed for mechanism prediction of LDZK. RESULTS: A comprehensive analysis identified a total of 45 compounds as the major constituents of LDZK. Oral administration of LDZK resulted in notable ameliorative effects in respiratory function, accompanied by reduced inflammatory cell counts and cytokine levels in the lungs of COPD mice. Acute toxicity tests demonstrated a favorable safety profile at a dose equivalent to 292 times the clinically prescribed dose. In vitro studies revealed that LDZK exhibited protective effects on A549 cells by mitigating LPS-induced cellular damage, reducing the release of NO, and downregulating the expression of iNOS, COX2, IL-1ß, IL-6, and TNF-α. Network pharmacology and Western blot analysis indicated that LDZK primarily modulated the MAPK signaling pathway and inhibited the phosphorylation of p38/ERK/JNK. CONCLUSIONS: LDZK exerts significant therapeutic effects on COPD through the regulation of the MAPK pathway, suggesting its potential as a promising adjunctive therapy for the treatment of chronic inflammation in COPD.
Asunto(s)
Medicina Tradicional Tibetana , Enfermedad Pulmonar Obstructiva Crónica , Ratas , Ratones , Animales , Lipopolisacáridos/farmacología , Enfermedad Pulmonar Obstructiva Crónica/tratamiento farmacológico , Enfermedad Pulmonar Obstructiva Crónica/metabolismo , Pulmón , Transducción de SeñalRESUMEN
Study the suitability of organic film for salvianolic acid in the ultrafiltration process of Danshen Dizhuye. UPLC was used to analyze the migration of nine phenolic active ingredients in Danshen Dizhuye during ultrafiltration of PES hollow fiber membrane and PS hollow fiber membrane. The structural composition of multi-components was analyzed by three different batches of Danshen Dizhuye before and after ultrafiltration of the two membranes. The results showed that 9 phenolic active ingredients in Danshen Dizhuye did not change significantly after ultrafiltration through PES membrane. However, after ultrafiltration through PS membrane, the content of sodium danshensu, protocatechualdehyde, caffeic acid, 3-hydroxy-4-methoxycinnamic acid and rosmarinic acid in Danshen Dizhuye did not change significantly, while salvianolic acid D, salvianolic acid B and lithospermic acid decreased by about 20%, and the content of salvianolic acid A decreased significantly. The final content in equilibrium was only about 20% of the original solution. Therefore, an in-depth study on the migration particularity of salvianolic acid A in ultrafiltration membrane was the focuse. The results showed that the loss of salvianolic acid A was caused by both membranes during ultrafiltration, and salvianolic acid A was lost more in PS membrane. When the membrane was washed and regenerated, it was found that salvianolic acid A was detected in the ethanol washing solution, but not in the washing liquid, indicating that the loss of salvianolic acid A during the ultrafiltration was mainly adsorptive action. The results suggested that the migration of phenolic active ingredients in Danshen Dizhuye during the membrane ultrafiltration process did not completely follow the molecular weight passing rule of the membrane pore size. At the same time, it may be affected by factors, such as the structure of the membrane material, and the interaction between the membrane structure and the structure of components, and exhibit different migration behaviors during the ultrafiltration of the membrane.
Asunto(s)
Alquenos/química , Medicamentos Herbarios Chinos/química , Polifenoles/química , Salvia miltiorrhiza/química , Ultrafiltración , Cromatografía Líquida de Alta PresiónRESUMEN
To mine and discover the active components of " Coptidis Rhizome-Magnoliae Officinalis Cortex( C&M) " based on the network pharmacology,integrate and analyze the potential targets and mechanisms. The TCMSP database was used to screen active ingredients. TTD and Drug Bank databases were used to predict the potential targets by referring to relevant literature,and the pathway annotation technology was used to enrich and analyze the active ingredients and potential targets of " C&M". A total of 29 potential target active ingredients were screened from " C&M",including 12 alkaloids components such as( R)-canadine,berberine,coptisine,and palmatine; 3 lignans consisting of magnolol,honokiol and obovatol; 6 volatile oils consisting of α-eudesmol,ß-eudesmol,eucalyptol and so on,and flavonoids including quercetin and neohesperidin. Corresponding 199 predicted targets were screened out,mainly including PTGS2,PTGS1,NCOA2,Hsp90 AB1,and so on. 72 signaling pathways were involved,8 of which were related to cancer,such as prostate cancer,bladder cancer,and pancreatic cancer; 9 of which were related to endocrine,including oxytocin signaling pathway,insulin signaling pathway,thyroid hormone signaling pathway and so on,as well as inflammation-related pathway. This study has preliminarily mined and discovered the main active components and potential targets of " C&M",providing material source for the study on the preparation of structural components of traditional Chinese medicine.
Asunto(s)
Medicamentos Herbarios Chinos , Rizoma , Alcaloides , Humanos , Magnolia , MasculinoRESUMEN
UNLABELLED: Context Murraya paniculata (L.) Jack (Rutaceae), Qianlixiang in Chinese, is distributed in China. As an important traditional Chinese medicine (TCM), it demonstrates many bioactivities, such as febrifuge, astringent, anti-dysenteric, and tonic. OBJECTIVE: The objective of this study is to evaluate the anti-inflammatory effect of three flavonoids isolated from M. paniculata in lipopolysaccharide (LPS)-activated murine macrophage cell line and ethanol-induced gastric damage on gastric epithelial cell (GES-1). Materials and methods Three identified flavonoids were isolated from stems and leaves of M. paniculata using ultra performance liquid chromatography (UPLC). Cell viability was measured with MTT, mouse peritoneal macrophages and GES-1 cells were incubated with 0, 0.01, 0.1, 1, 10, and 100 µM P1, P3 and P8 for 24, 48, and 72 h. The inhibitory effect of pretreatment with various concentrations of 5,7,3',4',5'-pentamethoxyflavone (P1), 5,7,3',4'-tetramethoxyflavone (P3), or 5-desmethylnobiletin 5-hydroxy-6,7,8,3',4'-pentameth-oxyflavone (P8) ranging from 0.03 to 30 µM on nitric oxide (NO) secretion was quantified by the Griess assay for 24 and 48 h, while interleukin-6 (IL-6) was measured by ELISA for 24 and 48 h. Results The effects of P1, P3, and P8 on mouse peritoneal macrophages and GES-1 cells were not attributable to cytotoxic effects at the doses of 0-10 µM. The IC50 value of P1 is 53.40 µM, P3 is 120.98 µM, and P8 is 10.73 µM. The concentration of the three flavonoids had the best effects of anti-inflammation upon NO inhibition at the dose of 3 µM. P3 had the highest inhibition on IL-6 production. The GES-1 cells pretreated with three flavonoids showed a significant increase in the level of NO (P1: 7.94 ± 0.0635 µM, P3: 8.81 ± 0.0159 µM, and P8: 8.51 ± 0.0522 µM) at 24 h and a more significant increase at 48 h (P1: 9.34 ± 0.0975 µM, P3: 11.9 ± 0.0672 µM, and P8: 9.34 ± 0.0454 µM). Discussion and conclusion The current results suggested that the anti-inflammatory activity of three flavonoids was mainly manifested in the reduction of production of NO and IL-6 production. Analysis of the structure-activity relationship indicated that the double bond at C2-C3 and the position of the B ring at C2/C3 seemed to be indispensable for the anti-inflammatory activity.
Asunto(s)
Antiinflamatorios/farmacología , Flavonoides/farmacología , Mucosa Gástrica/efectos de los fármacos , Macrófagos/efectos de los fármacos , Murraya , Extractos Vegetales/farmacología , Animales , Antiinflamatorios/aislamiento & purificación , Línea Celular , Supervivencia Celular/efectos de los fármacos , Supervivencia Celular/fisiología , Relación Dosis-Respuesta a Droga , Células Epiteliales , Flavonoides/aislamiento & purificación , Mucosa Gástrica/metabolismo , Macrófagos/metabolismo , Ratones , Extractos Vegetales/aislamiento & purificaciónRESUMEN
Two new coumarin glycosides (1 and 2), along with six known compounds (3-8), were isolated from the roots of Euphorbia soongarica. The structures of two new compounds were elucidated as aesculetin-6-O-(6'-O-galloyl)-beta-D-galactopyranoside (1) and fraxetin-8-O-(6'-O-galloyl)-beta-D-galactopyranoside (2) by spectral methods and chemical evidences.
Asunto(s)
Cumarinas/aislamiento & purificación , Medicamentos Herbarios Chinos/aislamiento & purificación , Euphorbia/química , Galactósidos/aislamiento & purificación , Glicósidos/aislamiento & purificación , Umbeliferonas/aislamiento & purificación , Cumarinas/química , Medicamentos Herbarios Chinos/química , Galactósidos/química , Glicósidos/química , Estructura Molecular , Raíces de Plantas/química , Estereoisomerismo , Umbeliferonas/químicaRESUMEN
OBJECTIVE: To study the chemical constituents of the roots of Euphorbia soongarica (Xinjiang origin). METHOD: Compounds were isolated and purified by repeated normal column chromatography, preparative thin layer chromatography and Sephadex LH - 20 chromatography. The chemical structures were elucidated by NMR and MS spectra. RESULTS: Ten chemical constituents were isolated from the n-BuOH fraction and identified as ellagic acid (1) , 3, 3'-di-O-methylellagic acid (2) , 3, 3'-di-O-methylellagic acid-4'-O-alpha-D-arabinfuranoside (3), 3, 3'-di-O-methylellagic acid-4'-O-beta-D-xylopyranoside (4), 3, 3'-di-O-methylellagic acid-4-O-beta-D-glucopyranoside (5), 3, 3', 4'-tri-O-methylellagic acid (6), 3-O-methylellagic acid-4'-O-beta-D-xylopyranoside (7), 3, 3', 4-tri-O-methylellagic acid-4'-O-beta-D-glucopyranoside (8), brevifolin (9) and ethyl brevifolin carboxylate (10). CONCLUSION: All of above compounds were obtained from this plant for the first time.
Asunto(s)
Benzopiranos/aislamiento & purificación , Ácido Elágico/análogos & derivados , Ácido Elágico/aislamiento & purificación , Euphorbia/química , Plantas Medicinales/química , Benzopiranos/química , Ácido Elágico/química , Raíces de Plantas/químicaRESUMEN
OBJECTIVE: To study the flavone constituents in Chrozophora sabulosa (Xinjiang origin). METHOD: The compounds were extracted with 95% ethyl alcohol, isolated by various column chromatography and identified by spectroscopic methods. RESULT: Seven flavanoids were isolated and identified as quercetin (I), kaempferol (II), apigenin (III), chrysoerid (IV), isoquercitrin (V), chrysoerin-7-O-beta-D-glucoside (VI) and quercetin-3-O-alpha-D-arabinfuranoside (VII). CONCLUSION: All of these seven compounds were obtained from this genus for the first time.