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1.
Nat Prod Res ; : 1-9, 2019 May 28.
Artigo em Inglês | MEDLINE | ID: mdl-31135216

RESUMO

Two new compounds, including a diterpenoid glycoside (1) and a triterpenoid glycoside (6), along with six known compounds were isolated from Clinopodium chinense. The structures of the new compounds were determined on basis of extensive spectral analysis and chemical method. Compounds 1-8 were evaluated for their insulin resistance effect and cytotoxic activity against the A549 and HepG2 cancer cell lines. None of the compounds were cytotoxic (IC50 > 100 µM), while compounds 1-3 and 5 showed the activity of ameliorating insulin resistance in HepG2.

2.
Molecules ; 24(4)2019 Feb 22.
Artigo em Inglês | MEDLINE | ID: mdl-30813246

RESUMO

Stroke is one of the most common neurological disorders and seriously threatens human life. Gross saponins of Tribulus terrestris fruit (GSTTF) are used for neuroprotective treatment on convalescents of ischemic stroke. However, the therapeutic effects and mechanisms have not yet well understood, especially from the metabolic perspective. In this study, the protective effect of GSTTF on ischemic stroke in a middle cerebral artery occlusion (MCAO) rat model was investigated by the GC-MS-based metabolomics approach. 2,3,5-triphenyltetrazolium chloride (TTC) staining of brain tissues showed that GSTTF significantly reduced the infarct area after MCAO surgery. Metabolomic profiling showed a series of metabolic perturbation occurs in ischemic stroke compared with sham group. GSTTF can reverse the MCAO-induced serum metabolic deviations by regulating multiple metabolic pathways including fatty acids metabolism, amino acids metabolism, and carbohydrates metabolism. The current study provided a useful approach for understanding the mechanism of MCAO-induced ischemic stroke and a reliable basis for evaluating the efficacy of GSTTF in the treatment of ischemic stroke.


Assuntos
Metabolômica/métodos , Fármacos Neuroprotetores/administração & dosagem , Saponinas/administração & dosagem , Acidente Vascular Cerebral/prevenção & controle , Tribulus/química , Animais , Modelos Animais de Doenças , Cromatografia Gasosa-Espectrometria de Massas , Regulação da Expressão Gênica/efeitos dos fármacos , Masculino , Redes e Vias Metabólicas/efeitos dos fármacos , Metaboloma/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Ratos , Saponinas/farmacologia , Acidente Vascular Cerebral/etiologia , Acidente Vascular Cerebral/metabolismo , Acidente Vascular Cerebral/patologia , Sais de Tetrazólio/metabolismo
3.
Chin J Nat Med ; 16(7): 499-504, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30080648

RESUMO

Two previously undescribed steroidal compounds, 16, 23-epoxy-22, 26-epimino-cholest-22(N), 23, 25(26)-trien-3ß-ol-3-O-ß-D-glucopyranosyl-(1→2)-ß-D-glucopyranosyl-(1→4)-ß-D-galactopyranoside (1) and 26-O-ß-D-glucopyranosyl-(25R)-5α-furost-20(22)-en-3ß, 26-diol (2), together with 7 known ones including 26-O-ß-D-glucopyranosyl-(25R)-5, 20(22)-dien-furost-3ß, 26-diol (3), (25R)-5-en-spirost-3ß-ol-O-ß-D-glucopyranosyl-(1→4)-[α-L-rhmanopyranosyl-(1→2)]-ß-D-galactopyranoside (4), funkioside D (5), aspidistrin (6), tigogenin-3-O-ß-D-lucotrioside (7), desglucolanatigonin II (8), and degalactotigonin (9), were isolated from Solanum lyratum Thunb. Their cytotoxic activities were tested in two cancer cell lines by MTT method. One of the steroidal glycosides (6) showed significant cytotoxic activity against gastric cancer SGC7901 and liver cancer BEL-7402 cells.


Assuntos
Alcaloides/toxicidade , Antineoplásicos/isolamento & purificação , Antineoplásicos/toxicidade , Glicosídeos/toxicidade , Extratos Vegetais/toxicidade , Solanum/química , Esteróis/toxicidade , Alcaloides/química , Alcaloides/isolamento & purificação , Antineoplásicos/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Glicosídeos/química , Glicosídeos/farmacologia , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Fitosteróis/química , Fitosteróis/isolamento & purificação , Fitosteróis/toxicidade , Extratos Vegetais/química , Plantas Medicinais/química , Esteróis/química , Esteróis/farmacologia
4.
Exp Ther Med ; 14(6): 6052-6058, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29285156

RESUMO

Renal tubular cell apoptosis and tubular dysfunction is an important process underlying diabetic nephropathy (DN). Understanding the mechanisms underlying renal tubular epithelial cell survival is important for the prevention of kidney damage associated with glucotoxicity. Curcumin has been demonstrated to possess potent anti-apoptotic properties. However, the roles of curcumin in renal epithelial cells are yet to be defined. The present study investigated advanced glycation or glycoxidation end-product (AGE)-induced toxicity in renal tubular epithelial cells via several complementary assays, including cell viability, cell apoptosis and cell autophagy in the NRK-52E rat kidney tubular epithelial cell line. The extent of apoptosis was significantly increased in the NRK-52E cells following treatment with AGEs. The results also indicated that curcumin reversed this effect by promoting autophagy through the phosphoinositide 3-kinase/AKT serine/threonine kinase signaling pathway. These conclusions suggested that curcumin exerts a renoprotective effect in the presence of AGEs, at least in part by activating autophagy in NRK-52E cells. Collectively, these findings indicate that curcumin not only exerts renoprotective effects, however may also act as a novel therapeutic strategy for the treatment of diabetic nephropathy.

5.
Artigo em Inglês | MEDLINE | ID: mdl-28684967

RESUMO

BACKGROUND: Antiobesity drugs may not be optimal for treating obesity. However novel antiobesity agents, especially those derived from natural products, may be suitable. Therefore, we investigated the effects and mechanisms of Cyclocarya paliurus (CP) aqueous extract (CPAE) on obesity. METHODS: SHR.Cg-Leprcp/NDmcr (SHR/cp) rats were used as a model of obesity and metabolic syndrome. Experimental animals were allocated into two groups-control and CPAE (0.5 g/kg)-for a 7-week treatment period. Examinations were performed, including general physiological characteristics, obesity-related biochemical parameters, and insulin-signaling pathway-related proteins in the hypothalamus. RESULTS: Treatment with CPAE reduced food intake, body weight, organ weight, fat mass, and body mass index (BMI) in SHR/cp rats. Meanwhile, CPAE also decreased the levels of fasting serum glucose, fasting serum insulin, HOMA-IR, serum free fatty acids, serum malondialdehyde, serum superoxide dismutase, and serum total-glutathione. The levels of phosphorylation of target proteins-including InsR, IRS1, PI3Kp85, Akt, and FoXO1 as well as protein expression of POMC-were significantly upregulated in the hypothalamus, but NPY expression remarkably decreased. CONCLUSIONS: CPAE has antiobesity, antihypoglycemic, antihypolipidemic, and antioxidant properties. The mechanism responsible for the antiobesity effect of CPAE may be related to suppression of energy intake via regulation of insulin-signaling pathway in the hypothalamus.

6.
Mol Med Rep ; 16(2): 1333-1339, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28586016

RESUMO

Asiatic acid (AA) has been demonstrated to exhibit anti-diabetic activity. However, the mechanisms and underlying signaling pathways remain to be elucidated. The present study was performed to confirm the protective effect of AA and demonstrate its ability to regulate the phosphatidylinositol 3­kinase (PI3K)/protein kinase B (AKT)/glycogen synthase kinase­3ß (GSK­3ß) signaling pathway in db/db mice. Db/db mice fed on a high­fat diet were used to model diabetes mellitus. Modeled mice were divided randomly into the model control, pioglitazone hydrochloride tablet (PH) and AA groups. Age­matched C57 BL/6J mice served as normal controls. Lipid and glucose levels, and glycogen synthesis rates were assessed following treatment. Pathological changes were detected using hematoxylin and eosin staining. Expression of the PI3K/AKT/GSK­3ß signaling pathway at the mRNA level was measured using quantitative polymerase chain reaction analysis. The model control group revealed typical characteristics of obesity and diabetes, including high glucose and lipid levels, and decreased glycogen synthesis. Four weeks of treatment with AA or PH ameliorated these abnormalities. AA and PH treatments mitigated the upregulation of PI3K, AKT, insulin receptor, and insulin receptor substrate­1 mRNA expression in modeled mice. Furthermore, AA and PH treatments decreased GSK­3ß and glucose­6­phosphatase mRNA expression compared with the normal control group. The results of the present study confirmed that AA possesses anti­diabetic activity in db/db mice. The PI3K/AKT/GSK­3ß signaling pathway may mediate this protective effect.


Assuntos
Diabetes Mellitus Tipo 2/metabolismo , Hipoglicemiantes/farmacologia , Triterpenos Pentacíclicos/farmacologia , Animais , Biomarcadores , Diabetes Mellitus Tipo 2/tratamento farmacológico , Modelos Animais de Doenças , Glicogênio Sintase Quinase 3 beta/metabolismo , Metabolismo dos Lipídeos/efeitos dos fármacos , Lipídeos/sangue , Camundongos , Fosfatidilinositol 3-Quinases/metabolismo , Pioglitazona , Proteínas Proto-Oncogênicas c-akt/metabolismo , Transdução de Sinais/efeitos dos fármacos , Tiazolidinedionas/farmacologia
7.
Biomed Pharmacother ; 93: 352-358, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28651236

RESUMO

Tanshinone I from tanshen has been used in traditional Chinese medicine for treating cardiovascular diseases and inflammatory diseases. Given the link between inflammation and Type 2 diabetes mellitus (T2DM), we suspect that tanshinone I may have a beneficial effect on T2DM. This study was to investigate the potential effects of tanshinone I on T2DM and its underlying mechanism. T2DM was thus induced in Sprague-Dawley (SD) rats using streptozotocin (STZ) and high-fat diet. It was observed that T2DM rats had higher levels of total cholesterol (TC), nonesterified fatty acids (NEFAs), total triglyceride (TG) and total low density lipoprotein cholesterol (LDL-C) compared with normal, healthy SD rats. Treatment with tanshinone I decreased these levels and lowered blood glucose level in T2DM rats. In addition, enzyme-linked immunosorbent assay (ELISA) analysis showed that T2DM rats had elevated levels of tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6). Furthermore, Western blot analysis revealed that T2DM rats had enhanced nuclear translocation of NF-κB as well as elevated phosphorylation of Ser307 in IRS-1(insulin receptor substrate 1). Treatment by tanshinone I lowered the levels of IL-6 and TNF-α, decreased nuclear translocation of NF-κB as well as phosphorylation of Ser307 in IRS-1. These results demonstrated that tanshinone I could alleviate T2DM syndrome in rats.


Assuntos
/farmacologia , Diabetes Mellitus Tipo 2/tratamento farmacológico , Proteínas Substratos do Receptor de Insulina/metabolismo , Resistência à Insulina/fisiologia , Animais , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Tipo 2/induzido quimicamente , Diabetes Mellitus Tipo 2/metabolismo , Dieta Hiperlipídica/efeitos adversos , Interleucina-6/metabolismo , Medicina Tradicional Chinesa/métodos , NF-kappa B/metabolismo , Fosforilação/efeitos dos fármacos , Ratos , Ratos Sprague-Dawley , Estreptozocina/farmacologia , Fator de Necrose Tumoral alfa/metabolismo
8.
Artigo em Inglês | MEDLINE | ID: mdl-28421123

RESUMO

The chickpea, a food and medicine used by the people of Xinjiang, has a beneficial hypoglycemic effect. To better utilize this national resource and develop hypoglycemic agents from components of the chickpea, a series of new derivatives of isoflavone compounds from the chickpea were synthesized. An insulin-resistant (IR) HepG2 cell model was used to screen the hypoglycemic activities of these compounds. And the structure-activity relationships of these compounds were explored. Additionally, several combinations of these compound displayed higher hypoglycemic activity than any single compound, and they had similar hypoglycemic activity to that of the positive control group (p > 0.05). In addition, combination 3 and combination 6 exerted different effects on the insulin sensitivity of H4IIE cells stimulated with resistin. And the results indicated that combination 3 would have higher hypoglycemic activity. These findings demonstrate the characteristics of multiple components and targets of Chinese herbal medicine. This evidence may provide new ideas for the development of hypoglycemic drugs.

9.
J Tradit Chin Med ; 37(3): 361-370, 2017 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31682379

RESUMO

OBJECTIVE: To investigate the effects of Tangnaikang (TNK), a mixture of five herbal plant extracts, on inflammation-mediated insulin resistance and B-cell apoptosis in SHR.Cg-Leprcp/NDmcr (SHR-cp) rats. METHODS: Seven-week-old SHR-cp rats were randomly divided into a control (CON) group and a TNK (3.24 g/kg) group. Wistar-Kyoto rats at the same age were used as the normal control group. After 7 weeks of continuous intragastric administration of TNK, the glucose metabolic status and insulin sensitivity of the rats were evaluated by assessing fasting serum glucose (FBG), the oral glucose tolerance test (OGTT), fasting serum insulin (FINS), and the insulin sensitivity index (ISI). Serum tumor necrosis factor-a (TNF-a), interleukin-6 (IL-6), C-reactive protein (CRP) and adiponectin were measured via enzyme-linked immunosorbent assays. Macrophage infiltration and apoptosis in adipose tissues were detected through F4/80 immunohistochemistry and the terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay. Islet morphology and B-cell apoptosis were investigated using double immunofluorescence staining and the TUNEL assay. The expression of cytokine genes in adipose tissue, the liver, and the pancreas was detected in real-time polymerase chain reaction assays. The expression and phosphorylation levels of insulin signaling-, inflammation-, and B-cell survival-related proteins in the liver and pancreas of SHR-cp rats were detected by western blotting. RESULTS: TNK (3.24 g/kg) treatment significantly decreased body weight, FBG and FINS; improved impaired glucose tolerance; increased the ISI; reduced serum levels of TNF-a, CRP and IL-6; and increased serum adiponectin. The mRNA expression of inflammatory markers was markedly reduced in the liver, pancreas, and adipose tissue. F4/80- and TUNEL-positive cells in adipose tissues were decreased, as was the number of TUNEL-positive B-cells. The phosphorylation of c-Jun N-terminal kinase and that of insulin receptor substrate-1 at serines 307 and 1101 was significantly decreased. In the pancreas, the expression of nuclear factor kappa-light chain-enhancer of activated B cells-p65 was significantly decreased, and phosphoinositide 3-kinase and IRS-2 were significantly increased. CONCLUSION: TNK was able to improve insulin resistance and B-cell apoptosis in SHR-cp rats, which might be associated with its ability to relieve the overall and local metabolic inflammatory responses observed in SHR-cp rats.

10.
Pharm Biol ; 54(11): 2685-2691, 2016 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-27158744

RESUMO

CONTEXT: Folium Mori, the leaf of Morus alba L. (Moraceae), has been used in traditional Chinese medicine (TCM) for treating diabetes. However, it is unclear which components in the mulberry leaf are effective for the treatment of type 2 diabetes mellitus (T2DM). OBJECTIVE: To investigate the flavonoids and polyphenols in mulberry leaves and their antihyperglycemic and antihyperlipidemic effects in T2DM rats. MATERIALS AND METHODS: Male Sprague-Dawley rats were divided into five groups: normal control (NC), diabetic control (DBC), diabetic group with 0.3 mg/kg b.w./day rosiglitazone (RSG), diabetic group with 7 g/kg b.w./day TCM formula and diabetic group with 2 g/kg b.w./day Folium Mori extract (FME). After 4 weeks, the rats were sacrificed; biochemical parameters, gene and protein expression were measured. RESULTS: The FBG level was significantly lower in the FME group than in the DBC group (p < 0.05). In oral glucose tolerance test, the AUC was significantly lower in the FME group (p < 0.05). The HOMA-IR level was significantly decreased in the FME group (p < 0.05). FME decreased the total cholesterol (TC), triglyceride (TG) and low density lipoprotein (LDL) levels (p < 0.05). FME increased the mRNA and protein expression of IRS-1, PI3K p85α and Glut-4 increased significantly (p < 0.05). Histological analysis revealed amelioration of lipid accumulation following FME treatment. Additionally, immunohistochemical analysis displayed stronger staining of Glut-4 in the FME group compared to the DBC group. DISCUSSION AND CONCLUSION: FME could decrease the body weight, blood glucose, TG, TC and LDL levels, and improve insulin resistance. FME possessed significant antihyperglycemic and antihyperlipidemic activities via the IRS-1/PI3K/Glut-4 signalling pathway.


Assuntos
Diabetes Mellitus Tipo 2/tratamento farmacológico , Transportador de Glucose Tipo 4/fisiologia , Proteínas Substratos do Receptor de Insulina/fisiologia , Resistência à Insulina , Morus , Fosfatidilinositol 3-Quinases/fisiologia , Extratos Vegetais/farmacologia , Transdução de Sinais/efeitos dos fármacos , Animais , Diabetes Mellitus Tipo 2/metabolismo , Glucose/metabolismo , Metabolismo dos Lipídeos/efeitos dos fármacos , Masculino , Músculo Esquelético/efeitos dos fármacos , Músculo Esquelético/metabolismo , Folhas de Planta , Ratos , Ratos Sprague-Dawley
11.
Molecules ; 20(9): 17016-40, 2015 Sep 17.
Artigo em Inglês | MEDLINE | ID: mdl-26393547

RESUMO

A set of novel isoflavone derivatives from chickpea were synthesized. The structures of derivatives were identified by proton nuclear magnetic resonance (¹H-NMR), carbon-13 ((13)C)-NMR and mass spectrometry (MS) spectral analyses. Their anti-diabetic activities were evaluated using an insulin-resistant (IR) HepG2 cell model. Additionally, the structure-activity relationships of these derivatives were briefly discussed. Compounds 1c, 2h, 3b, and 5 and genistein exhibited significant glucose consumption-enhancing effects in IR-HepG2 cells. In addition, the combinations of genistein, 2h, and 3b (combination 6) and of 3b, genistein, and 1c (combination 10) exhibited better anti-diabetic activity than the individual compounds. At the same dosage, there was no difference in effect between the combination 10 and the positive control (p > 0.05). Aditionally, we found the differences between the combination 10 and combination 6 for the protective effect of HUVEC (human umbilical vein endothelial cells) under high glucose concentration. The protective effects of combination 10 was stronger than combination 6, which suggested that combination 10 may have a better hypoglycemic activity in future studies. This study provides useful clues for the further design and discovery of anti-diabetic agents.


Assuntos
Cicer/química , Hipoglicemiantes/síntese química , Isoflavonas/síntese química , Isoflavonas/farmacologia , Extratos Vegetais/química , Genisteína/farmacologia , Células Hep G2 , Células Endoteliais da Veia Umbilical Humana , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Isoflavonas/química , Espectroscopia de Ressonância Magnética/métodos , Estrutura Molecular , Relação Estrutura-Atividade
12.
PLoS One ; 10(4): e0122024, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25874615

RESUMO

Increased energy intake and reduced physical activity can lead to obesity, diabetes and metabolic syndrome. Transcriptional modulation of metabolic networks has become a focus of current drug discovery research into the prevention and treatment of metabolic disorders associated with energy surplus and obesity. Tang-Nai-Kang (TNK), a mixture of five herbal plant extracts, has been shown to improve abnormal glucose metabolism in patients with pre-diabetes. Here, we report the metabolic phenotype of SHR.Cg-Leprcp/NDmcr (SHR/cp) rats treated with TNK. Pre-diabetic SHR/cp rats were randomly divided into control, TNK low-dose (1.67 g/kg) and TNK high-dose (3.24 g/kg) groups. After high-dose treatment for 2 weeks, the serum triglycerides and free fatty acids in SHR/cp rats were markedly reduced compared to controls. After 3 weeks of administration, the high dose of TNK significantly reduced the body weight and fat mass of SHR/cp rats without affecting food consumption. Serum fasting glucose and insulin levels in the TNK-treated groups decreased after 6 weeks of treatment. Furthermore, TNK-treated rats exhibited obvious improvements in glucose intolerance and insulin resistance. The improved glucose metabolism may be caused by the substantial reduction in serum lipids and body weight observed in SHR/cp rats starting at 3 weeks of TNK treatment. The mRNA expression of NAD+-dependent deacetylase sirtuin 1 (SIRT1) and genes related to fatty acid oxidation was markedly up-regulated in the muscle, liver and adipose tissue after TNK treatment. Furthermore, TNK promoted the deacetylation of two well-established SIRT1 targets, PPARγ coactivator 1α (PGC1α) and forkhead transcription factor 1 (FOXO1), and induced the phosphorylation of AMP-activated protein kinase (AMPK) and acetyl-CoA carboxylase (ACC) in different tissues. These observations suggested that TNK may be an alternative treatment for pre-diabetes and metabolic syndrome by inducing a gene expression switch toward fat oxidation through the activation of SIRT1 and AMPK signaling.


Assuntos
Diabetes Mellitus/tratamento farmacológico , Medicamentos de Ervas Chinesas/administração & dosagem , Ácidos Graxos não Esterificados/sangue , Síndrome Metabólica/tratamento farmacológico , Triglicerídeos/sangue , Proteínas Quinases Ativadas por AMP/sangue , Animais , Peso Corporal , Diabetes Mellitus/sangue , Diabetes Mellitus/patologia , Metabolismo Energético/efeitos dos fármacos , Regulação da Expressão Gênica/efeitos dos fármacos , Glucose/metabolismo , Humanos , Insulina/sangue , Síndrome Metabólica/sangue , Síndrome Metabólica/patologia , Ratos , Sirtuína 1/sangue
13.
BMC Complement Altern Med ; 15: 97, 2015 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-25887645

RESUMO

BACKGROUND: Chinese medicine comprised of all natural herbs is widespread used in the treatment of diabetic nephropathy (DN). Podocyte contributes to the integrity of glomerular filtration barrier whose injury plays an important role in the initiation and progression of DN. Our study aimed to investigate the effect of Qiwei granules on podocyte lesion in diabetic KK-A(y) mice kidney and its underlying mechanism. METHODS: Twelve-week-old male KK-A(y) mice were randomly divided in vehicle group and Qiwei granules group, while C57BL/6J mice were used as normal control. The mice were gavage with 1.37 g/kg/day Qiwei granules or water for 10 weeks. We measured water, food intake and body weight (BW) and fasting blood glucose (FBG) every 2 weeks, and urine protein every 4 weeks. At the end of the experiment, all surviving mice were sacrificed. The kidney weight and serum renal parameters were measured, and the renal morphology was observed. To search the underlying mechanism, we examined the podocyte positive marker, slit diaphragm protein expression and some involved cell signal pathway. RESULTS: Qiwei granules treatment significantly improved the metabolic parameters, alleviated the urinary protein, and protected renal function in KK-A(y) mice. In addition, the glomerular injuries and podocyte lesions were mitigated with Qiwei granules treatment. Furthermore, Qiwei granules increased expression of nephrin, CD2AP, and integrin alpha3beta1 in the podocytes of KK-A(y) mice. Qiwei granules improved the phosphoration of Akt and inhibited cleaved caspase-3 protein expression. CONCLUSION: These finding suggest that Qiwei granules protects the podocyte from the development of DN via improving slit diaphragm (SD) molecules expression and likely activating Akt signaling pathway in KK-A(y) mice.


Assuntos
Nefropatias Diabéticas/tratamento farmacológico , Medicamentos de Ervas Chinesas/uso terapêutico , Rim/efeitos dos fármacos , Magnoliopsida , Fitoterapia , Podócitos/efeitos dos fármacos , Proteínas Adaptadoras de Transdução de Sinal/metabolismo , Animais , Biomarcadores/metabolismo , Peso Corporal , Caspase 3/metabolismo , Proteínas do Citoesqueleto/metabolismo , Nefropatias Diabéticas/metabolismo , Nefropatias Diabéticas/patologia , Medicamentos de Ervas Chinesas/farmacologia , Integrina alfa3beta1/metabolismo , Rim/metabolismo , Rim/patologia , Masculino , Proteínas de Membrana/metabolismo , Camundongos , Camundongos Endogâmicos C57BL , Podócitos/patologia , Substâncias Protetoras/farmacologia , Transdução de Sinais/efeitos dos fármacos
14.
J Asian Nat Prod Res ; 16(10): 982-90, 2014 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-25082464

RESUMO

Two new and six known steroidal glucosides were isolated from the tuber of Ophiopogon japonicus. The new steroidal glucosides were established as (20R,25R)-26-O-ß-d-glucopyranosyl-3ß,26-dihydroxycholest-5-en-16,22-dioxo-3-O-α-l-rhamnopyranosyl-(1 â†’ 2)-ß-d-glucopyranoside (1) and 26-O-ß-d-glucopyranosyl-(25R)-furost-5-en-3ß,14α,17α,22α,26-pentaol-3-O-α-l-rhamnopyranosyl-(1 â†’ 2)-ß-d-glucopyranoside (3) on the basis of spectroscopic data as well as chemical evidence.


Assuntos
Colestenos/isolamento & purificação , Colestenonas/isolamento & purificação , Glucosídeos/isolamento & purificação , Glicosídeos/isolamento & purificação , Ophiopogon/química , Esteroides/isolamento & purificação , Colestenos/química , Colestenonas/química , Glucosídeos/química , Glicosídeos/química , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Tubérculos/química , Estereoisomerismo , Esteroides/química
15.
Chin J Nat Med ; 12(4): 300-4, 2014 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-24863357

RESUMO

AIM: To study the chemical constituents of stems of Gymnema sylvestre (Retz.) Schult. METHODS: Chromatographic techniques using silica gel, C18 reversed phase silica gel, and prep-HPLC were used. The structures were elucidated on the basis of MS and spectroscopic analysis (1D and 2D NMR), as well as chemical methods. RESULTS: Seven compounds were isolated and their structures were elucidated as conduritol A (1), stigmasterol (2), lupeol (3), stigmasterol-3-O-ß-D-glucoside (4), the sodium salt of 22α-hydroxy-longispinogenin-3-O-ß-D-glucopyranosyl-(1→3)-ß-D-glu-curono-pyranosyl-28-O-α-L-rhamnopyranoside (5), oleanolic acid-3-O-ß-D-glucopyranosyl-(1→6)-ß-D-glucopyranoside (6), and the sodium salt of 22α-hydroxy-longispinogenin 3-O-ß-D-glucuronopyranosyl-28-O-α-L-rhamnopyranoside (7). The inhibition activities of compounds 1, 5-7 on non-enzymatic glycation of protein in vitro were evaluated. CONCLUSION: Compound 7 is a new triterpenoid saponin. It was shown that compounds 1, 5-7 have weak inhibition activities for non-enzymatic glycation of protein in vitro.


Assuntos
Medicamentos de Ervas Chinesas/química , Gymnema sylvestre/química , Caules de Planta/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Estrutura Molecular
16.
J Asian Nat Prod Res ; 16(2): 206-9, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24286491

RESUMO

A new dammarane triterpenoid glycoside named cyclocarioside J (1) and other three known triterpenoid glycosides were isolated from the leaves of Cyclocarya paliurus. Based on ESI-MS, HR-ESI-MS, (1)H NMR, (13)C NMR, and 2D NMR techniques including (1)H-(1)H COSY, HMBC, HMQC, and NOESY correlations, the structure of cyclocarioside J was elucidated as (20S,24R)-epoxydammarane 3ß,12ß,25-trihydroxy-12-O-ß-d-quinovopyranosyl-3-O-α-l-arabinopyranoside.


Assuntos
Medicamentos de Ervas Chinesas/isolamento & purificação , Glicosídeos/isolamento & purificação , Juglandaceae/química , Triterpenos/isolamento & purificação , Medicamentos de Ervas Chinesas/química , Glicosídeos/química , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Folhas de Planta/química , Triterpenos/química
17.
Molecules ; 18(12): 15648-61, 2013 Dec 16.
Artigo em Inglês | MEDLINE | ID: mdl-24352020

RESUMO

Psidium guajava leaves have a diverse phytochemical composition including flavonoids, phenolics, meroterpenoids and triterpenes, responsible for the biological activities of the medicinal parts. In particular, flavonol glycosides show beneficial effects on type II diabetes mellitus. A simple and efficient HSCCC method has been developed for the preparative separation of five flavonoid glycosides and one diphenylmethane glycoside from P. guajava. A solvent system composed of n-hexane-ethyl acetate-methanol-water (0.7:4:0.8:4, v/v/v/v) was optimized for the separation. The upper phase was used as the stationary phase, and the lower phase was used as the mobile phase. Under the optimized conditions, hyperoside (15.3 mg), isoquercitrin (21.1 mg), reynoutrin (65.2 mg), quercetin-3-O-ß-D-arabinopyranoside (71.7 mg), quercetin-3-O-α-L-arabinofuranoside (105.6 mg) and 2,4,6-trihydroxy-3,5-dimethylbenzophenone 4-O-(6''-O-galloyl)-ß-D-glucopyranoside (98.4 mg) were separated from crude sample (19.8 g). The structures of all the isolates were identified by ESI-MS, 1H- and 13C-NMR analyses and their purities (>95%) were determined using HPLC.


Assuntos
Benzofenonas/química , Distribuição Contracorrente , Flavonoides/química , Flavonoides/isolamento & purificação , Glicosídeos/química , Glicosídeos/isolamento & purificação , Psidium/química , Estrutura Molecular , Solventes/química
18.
BMC Complement Altern Med ; 13: 52, 2013 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-23452929

RESUMO

BACKGROUND: Metabolic syndrome (MS) and type 2 diabetes mellitus (T2DM) have been associated with insulin-resistance; however, the effective therapies in improving insulin sensitivity are limited. This study is aimed at investigating the effect of Guava Leaf (GL) extracts on glucose tolerance and insulin resistance in SHRSP.Z-Leprfa/Izm rats (SHRSP/ZF), a model of spontaneously metabolic syndrome. METHODS: Male rats at 7 weeks of age were administered with vehicle water or treated by gavage with 2 g/kg GL extracts daily for six weeks, and their body weights, water and food consumption, glucose tolerance, and insulin resistance were measured. RESULTS: Compared with the controls, treatment with GL extracts did not modulate the amounts of water and food consumption, but significantly reduced the body weights at six weeks post treatment. Treatment with GL extracts did not alter the levels of fasting plasma glucose and insulin, but significantly reduced the levels of plasma glucose at 60 and 120 min post glucose challenge, also reduced the values of AUC and quantitative insulin sensitivity check index (QUICKI) at 42 days post treatment. Furthermore, treatment with GL extracts promoted IRS-1, AKT, PI3Kp85 expression, then IRS-1, AMKP, and AKT308, but not AKT473, phosphorylation, accompanied by increasing the ratios of membrane to total Glut 4 expression and adiponectin receptor 1 transcription in the skeletal muscles. CONCLUSIONS: These data indicated that GL extracts improved glucose metabolism and insulin sensitivity in the skeletal muscles of rats by modulating the insulin-related signaling.


Assuntos
Glicemia/metabolismo , Peso Corporal/efeitos dos fármacos , Resistência à Insulina , Síndrome Metabólica/tratamento farmacológico , Músculo Esquelético/efeitos dos fármacos , Extratos Vegetais/uso terapêutico , Psidium , Animais , Área Sob a Curva , Membrana Celular/efeitos dos fármacos , Membrana Celular/metabolismo , Modelos Animais de Doenças , Transportador de Glucose Tipo 4/metabolismo , Masculino , Síndrome Metabólica/metabolismo , Músculo Esquelético/metabolismo , Fosforilação , Extratos Vegetais/farmacologia , Folhas de Planta , Proteínas Proto-Oncogênicas c-akt/metabolismo , Ratos , Ratos Endogâmicos , Transdução de Sinais
19.
J Asian Nat Prod Res ; 14(12): 1186-90, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-23088362

RESUMO

Besides four known compounds, a new triterpenoid saponin was isolated from the stems of Gymnema sylvestre. The structure of the new triterpenoid saponin was established as 3ß,16ß,22α-trihydroxy-olean-12-ene 3-O-ß-D-xylopyranosyl-(1 → 6)-ß-D-glucopyranosyl-(1 → 6)-ß-D-glucopyranoside (1) on the basis of 1D and 2D NMR techniques, including COSY, HMBC, HMQC, and NOESY correlations. Four known compounds 2, 3, 4, and 5 were identified on the basis of spectroscopic data.


Assuntos
Medicamentos de Ervas Chinesas/isolamento & purificação , Gymnema sylvestre/química , Saponinas/isolamento & purificação , Triterpenos/isolamento & purificação , Medicamentos de Ervas Chinesas/química , Ressonância Magnética Nuclear Biomolecular , Saponinas/química , Triterpenos/química
20.
J Tradit Chin Med ; 32(3): 446-52, 2012 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23297571

RESUMO

OBJECTIVE: To investigate the effects of cinnamaldehyde (CA), an active and major compound in cinnamon, on glucose metabolism and insulin resistance in C57BLKS/J db/db mice. METHODS: Sixteen male C57BLKS db/db mice were randomly divided into control and CA treatment groups. CA was given (20 mg x kg(-1) x day(-1), p. o.) for 4 weeks. Pure water was given to control and db/+ mice. Subsequently, the levels of fasting blood glucose (FBG), fasting serum insulin, triglyeride, cholesterol, low-density lipoprotein-cholesterol (LDL-C), high-density lipoprotein-cholesterol (HDL-C), and free fatty acids (FFA), as well as the mRNA content of adiponectin and tumor necrosis factor (TNF)-alpha in adipose tissue, glucose transporter type 4 (GLUT-4) in skeletal muscle, and protein expressions of Akt, phospho-Akt (Thr308), AMPKalpha, phospho-AMPKalpha (Thr172) in skeletal muscle were measured. RESULTS: 1) CA decreased serum levels of FBG and insulin as well as body weight in db/db mice; 2) CA increased serum HDL-C levels; 3) CA significantly decreased the mRNA expression of TNF-alpha in adipose tissue and upregulated mRNA expression of GLUT-4 in skeletal muscle; 4) protein expression of p-Akt was increased in CA-treated mice, but Akt, AMPKalpha and p-AMPKalpha showed no change. CONCLUSION: CA has antihyperglycemic and antihyperlipidemic actions in db/db mice and could be useful in the treatment of type-2 diabetes.


Assuntos
Acroleína/análogos & derivados , Cinnamomum zeylanicum/química , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/administração & dosagem , Hipolipemiantes/administração & dosagem , Extratos Vegetais/administração & dosagem , Acroleína/administração & dosagem , Adiponectina/metabolismo , Animais , Diabetes Mellitus Tipo 2/genética , Diabetes Mellitus Tipo 2/metabolismo , Ácidos Graxos não Esterificados/metabolismo , Transportador de Glucose Tipo 4/genética , Transportador de Glucose Tipo 4/metabolismo , Humanos , Insulina/metabolismo , Masculino , Camundongos , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/metabolismo
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