RESUMEN
Rhizome of Anemarrhena asphodeloides Bunge (AA, family Liliaceae) has been widely used in China for thousands of years to treat febrile diseases and diabetes. Steroidal saponins from AA show good antidiabetes effects and ameliorate diabetic complications. This study was designed to investigate the effects of sarsasapogenin (Sar), a major sapogenin from AA, on diabetic nephropathy (DN) in rats, and to explore the possible mechanisms. Diabetic rats were divided into 3 groups treated orally with Sar (0, 20, or 60 mg/kg) and carboxymethylcellulose sodium, whereas normal rats for Sar (0 or 60 mg/kg) and carboxymethylcellulose sodium. We found that chronic treatment with Sar for 9 weeks significantly ameliorated renal dysfunction of diabetic rats, as evidenced by decreases in albuminuria, kidney weight index, serum uric acid, and morphologic changes such as extracellular matrix expansion and accumulation (fibronectin and collagen IV levels, etc.). Meanwhile, Sar treatment resulted in decreases in interleukin-18, NLRP3, and activated caspase 1 levels as well as advanced glycation endproducts (AGEs) and their receptor (RAGE) levels in the renal cortex of diabetic rats. However, Sar has no effects on the above indices in the normal rats. Therefore, Sar can markedly ameliorate diabetic nephropathy in rats via inhibition of NLRP3 inflammasome activation and AGEs-RAGE interaction.
Asunto(s)
Nefropatías Diabéticas/tratamiento farmacológico , Espirostanos/farmacología , Anemarrhena/química , Animales , China , Diabetes Mellitus Experimental/complicaciones , Medicamentos Herbarios Chinos/farmacología , Productos Finales de Glicación Avanzada , Interleucina-18/metabolismo , Riñón/efectos de los fármacos , Masculino , Proteína con Dominio Pirina 3 de la Familia NLR/metabolismo , Ratas , Ratas Sprague-Dawley , Rizoma/química , Saponinas/farmacología , Ácido Úrico/sangreRESUMEN
BACKGROUND: Green vegetable soya beans, known as Maodou in China, are supplied as vegetable-type fruits of the soybean plant. Previous study indicated that green vegetable soya beans exhibited antioxidative and anti-inflammatory activities. However, the material basis and pharmacological activities of green soybean plant were not unravelled clearly. In this study, we investigated the chemical ingredients and their pharmacological activities. RESULTS: Investigation of the chemical ingredients indicated that two new isoflavones, 2'-hydroxyerythrin A (1), and daidzein-7-O-ß-d-{6â³-[(E)-but-2-enoyl]}glycoside (2), together with seven known ones - 7,4'-dihydroxy-6-methoxyisoflavone (3), daidzein (4), daidzin (5), genistein (6), formononetin (7), ononin (8), and isoerythrinin A (9) - were obtained. The structures of compounds 1-9 were elucidated on the basis of spectroscopic and chemical analysis. We evaluated the antimicrobial efficacies and free-radical scavenging potential of the isolated compounds (1-9). Compounds 1 and 9 exhibited the most pronounced efficacy against the tested bacterial strains with IC50 values ranging from 10.6 to 22.6 µg mL-1 . The isolated compounds showed moderate radical scavenging properties with compound 6 being the most active, followed by compounds 3, 1 and 4. CONCLUSIONS: This study indicated that the isoflavones from soya beans could be considered as potential antioxidants or antimicrobials in the food, cosmetics and pharmaceutical industries. © 2017 Society of Chemical Industry.
Asunto(s)
Antibacterianos/farmacología , Antioxidantes/farmacología , Glycine max/química , Isoflavonas/farmacología , Extractos Vegetales/farmacología , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Bacterias/efectos de los fármacos , Isoflavonas/química , Isoflavonas/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Verduras/químicaRESUMEN
Ten compounds were isolated and identified from green vegetable soya beans, of which five are new triterpenoid saponins (1-5) and five are known compounds (6-10). The chemical structures of the five triterpenoid saponins (1-5) were elucidated to be 3ß,24-dihydroxy-22ß,30-epoxy-30-oxoolean-12-en 3-O-α-l-rhamnopyranosyl-(1 â 2)-ß-d-xylopyranosyl-(1 â 2)-ß-d-glucuronopyranoside, 1; 3ß,24-dihydroxy-22ß,30-epoxy-30-oxoolean-12-en 3-O-α-l-rhamnopyranosyl-(1 â 2)-ß-d-(3â³-O-formyl)-galactopyranosyl-(1 â 2)-ß-d-glucuronopyranoside, 2; 22-keto-3ß,24-dihydroxy oleanane-12-ene 3-O-α-l-rhamnopyranosyl-(1 â 2)-ß-d-(3â³-O-formyl)-galactopyranosyl-(1 â 2)-ß-d-glucuronopyranoside, 3; 3ß,22ß,24-trihydroxy oxyolean-18(19)-ene-29-acid 3-O-α-l-rhamnopyranosyl-(1 â 2)-ß-d-galactopyranosyl-(1 â 2)-ß-d-glucuronopyranoside, 4; and punicanolic acid 3-O-α-l-rhamnopyranosyl-(1 â 2)-ß-d-galactopyranosyl-(1 â 2)-ß-d-glucuronopyranoside, 5 from the spectroscopic data (IR, GTC/FID, HR-ESI-MS, and 1D and 2D NMR). The nitric oxide release inhibitions of compounds 1-10 in LPS-stimulated RAW264.7 cells were evaluated, and the data suggested that compounds 1, 2, and 5 might possess moderate anti-inflammatory activities, with IC50 values of 18.8, 16.1, and 13.2 µM, respectively.
Asunto(s)
Antiinflamatorios/química , Antiinflamatorios/farmacología , Glycine max/química , Extractos Vegetales/química , Saponinas/química , Triterpenos/química , Verduras/química , Animales , Antiinflamatorios/aislamiento & purificación , Macrófagos/efectos de los fármacos , Macrófagos/inmunología , Ratones , Estructura Molecular , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Células RAW 264.7 , Saponinas/aislamiento & purificación , Saponinas/farmacología , Triterpenos/aislamiento & purificación , Triterpenos/farmacologíaRESUMEN
A comprehensive phytochemical study of the chemical constituents of green vegetable soybeans resulted in the isolation of two new alkaloids, soyalkaloid A, 1, and isoginsenine, 2, together with four known ones, ginsenine, 3, (1S,3S)-1-methyl-1,2,3,4-tetrahydro-ß-carboline-3-carboxylic acid, 4, (1R,3S)-1-methyl-1,2,3,4-tetrahydro-ß-carboline-3-carboxylic acid, 5, and indole-3-carboxylic acid, 6. The structures of compounds 1-6 were elucidated on the basis of spectroscopic and chemical analyses. All of the alkaloids were isolated from soybeans for the first time, and compound 1 was a new indole-type alkaloid with a novel carbocyclic skeleton. Their inhibitory activities on the proliferation of concanalin A-activated lymphocytes were assessed by CCK8 assay.
Asunto(s)
Alcaloides/farmacología , Proliferación Celular/efectos de los fármacos , Concanavalina A/metabolismo , Glycine max/química , Linfocitos/efectos de los fármacos , Extractos Vegetales/farmacología , Verduras/química , Alcaloides/química , Animales , Células Cultivadas , Linfocitos/citología , Ratones , Ratones Endogámicos ICR , Estructura Molecular , Extractos Vegetales/químicaRESUMEN
Atractylis lancea (Thunb.) DC. (AL), an important medicinal herb in Asia, has been shown to have anti-tumor effects on cancer cells, but the involved mechanisms are poorly understood. This study focused on potential effects and molecular mechanisms of AL on the proliferation of the Hep-G2 liver cancer cell line in vitro. Cell viability was assessed by MTT test in Hep-G2 cells incubated with an ethanol extract of AL. Then, the effects of AL on apoptosis and cell cycle progression were determined by flow cytometry. Telomeric repeat amplification protocol (TRAP) assays was performed to investigate telomerase activity. The mRNA and protein expression of human telomerase reverse transcriptase (hTERT) and c-myc were determined by real-time RT-PCR and Western blotting. Our results show that AL effectively inhibits proliferation in Hep-G2 cells in a concentration- and time-dependent manner. When Hep-G2 cells were treated with AL after 48h,the IC50 was about 72.1 µg/ mL. Apoptosis was induced by AL via arresting the cells in the G1 phase. Furthermore, AL effectively reduced telomerase activity through inhibition of mRNA and protein expression of hTERT and c-myc. Hence, these data demonstrate that AL exerts anti-proliferative effects in Hep-G2 cells via down-regulation of the c-myc/hTERT/ telomerase pathway.