RESUMO
BACKGROUND: Hyperglycemia and dyslipidemia are classic features of patients with diabetes mellitus (DM). Cordyceps taii, a folk medicinal fungus native to southern China, possesses various pharmacological activities. This study aimed to assess the glucose-lowering and hypolipidemic effects of polysaccharides from C. taii (CTP) in streptozotocin (STZ)-induced diabetic mice. METHODS: Kunming mice were intraperitoneally injected with STZ at a dose of 100 mg/kg body weight. After induction of diabetes, diabetic mice were randomly divided into five groups: diabetic mellitus group (DM), metformin-treated group, low, medium, and high-dose CTP-treated group (CTP-L, CTP-M, and CTP-H). Normal mice served as the control group. After treatment for 28 days, body weight, fasting serum insulin (FSI), fasting blood glucose (FBG), homeostasis model assessment-insulin resistance (HOMA-IR), triglyceride (TG), total cholesterol (TC), low-density lipoprotein-cholesterol (LDL-C), high-density lipoprotein-cholesterol (HDL-C), tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and C-reactive protein (CRP) levels were measured. Histological analysis of pancreatic tissue and immune organ indices was also performed to evaluate the anti-diabetes effect of CTP. SPSS (version 21.0) software was used for statistical analysis, and statistical differences were considered significant at p < 0.05. RESULTS: Compared with the DM group, the body weight and FSI level of CTP-H group increased by 36.13 and 32.47%, whereas the FBG and HOMA-IR decreased by 56.79 and 42.78%, respectively (p < 0.05). Histopathological examination of the pancreas revealed that CTP improved and repaired the impaired islet ß-cells in pancreatic tissue. Compared with the DM group, the levels of TC, TG, and LDL-C decreased by 13.84, 31.87, and 36.61%, whereas that of HDL-C increased by 28.60% in CTP-H (p < 0.05). Further study showed that the thymus index in CTP-H was elevated by approximately 54.96%, and the secretion of pro-inflammatory cytokines TNF-α, IL-6, and CRP was inhibited by approximately 19.97, 34.46, and 35.41%, respectively (p < 0.05). CONCLUSION: The anti-diabetes effect of CTP is closely associated with immunoregulation and anti-inflammation, and CTP may be considered as a therapeutic drug or functional food for DM intervention.
Assuntos
Cordyceps/química , Diabetes Mellitus Experimental/metabolismo , Polissacarídeos Fúngicos/farmacologia , Hipoglicemiantes/farmacologia , Hipolipemiantes/farmacologia , Animais , Glicemia/efeitos dos fármacos , Peso Corporal/efeitos dos fármacos , Colesterol/sangue , Polissacarídeos Fúngicos/química , Hipoglicemiantes/química , Hipolipemiantes/química , Masculino , Medicina Tradicional Chinesa , Camundongos , EstreptozocinaRESUMO
Three new cytochalasins (1-3) together with two known cytochalasin analogues (4 and 5) were isolated from the chloroform fraction of ethanolic extract of a medicinal macrofungus Cordyceps taii. The structures of the new compounds were elucidated on the basis of spectroscopic analysis, including HRESIMS, 1D and 2D NMR experiments. The cytotoxicities of Compounds 1-5 were investigated by the sulforhodamine B (SRB) method in vitro against human highly metastatic lung cancer cell 95-D, human lung cancer cell line A-549 and normal hepatocyte HL-7702. The results revealed that Compounds 4 and 5 showed potent antitumor activities against human lung cancer cell 95-D with IC50 value of 3.67 and 4.04 µM, respectively. In comparison with cisplatin, the first-line chemotherapy drug, they had little or no cytotoxicity on normal cells, but showed stronger cytotoxic effects on cancer cells 95-D.
Assuntos
Antineoplásicos/farmacologia , Cordyceps/química , Citocalasinas/farmacologia , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Citocalasinas/química , Citocalasinas/isolamento & purificação , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Relação Estrutura-AtividadeRESUMO
The antibacterial agent helvolic acid, which was isolated from the active antitumor fraction of Cordyceps taii, showed potent cytotoxicity against different human cancer cells. In the present study, the in vivo antitumor effect of helvolic acid was investigated in murine sarcoma S180 tumor-bearing mice. Doses of 10 and 20 mg/kg/day helvolic acid did not exert significant antitumor activity. Interestingly, co-administration of 10 mg/kg/day helvolic acid and 20 mg/kg/day cyclophosphamide (CTX) - a well-known chemotherapy drug - showed promising antitumor activity with a growth inhibitory rate of 70.90%, which was much higher than that of CTX alone (19.5%). Furthermore, the combination markedly prolonged the survival of tumor-bearing mice. In addition, helvolic acid enhanced the immune organ index. The protein expression levels of ß-catenin, cyclin D1, and proliferating cell nuclear antigen were significantly suppressed in mice treated with 20 mg/kg/day helvolic acid and in those receiving combination therapy. Taken together, these results indicated that helvolic acid in combination with CTX showed potent in vivo synergistic antitumor efficacy, and its mechanism of action may involve the Wnt/ ß-catenin signaling pathway.