chlorogenic-acid and Diabetes-Mellitus--Type-2

Type II-diabetes mellitus (TII-DM) has been regarded as one of the most important public health problems in all nations in the 21st century. Although allopathic therapies remain the most important for the initial management of TII-DM, herbal remedies have gained wide acceptance for treating this condition. These alternative therapies are particularly valued in countries such as Mexico, rich in medicinal plants strongly attached to the cultural values of the population. Medicinal plants are prized sources of α-glucosidase inhibitors, which delay the liberation of glucose from complex carbohydrates, retarding glucose absorption, and thus controlling the characteristic hyperglycemia of TII-DM. Among the plant species used for treating diabetes in Mexico only 38 have been analyzed for their inhibitory activity of α-glucosidases. Most of these studies, reviewed in the present work, have focused on the evaluation of different types of extracts on the activity of α-glucosidases from diverse sources. Four species have been thoroughly analyzed in order to discover novel α-glucosidase inhibitors, namely, Hintonia latiflora and Hintonia standleyana (Rubiaceae), Ligusticum porteri (Apiaceae), and Brickellia cavanillesii (Asteraceae). Their ethnomedical uses, pharmacological and toxicological studies, chemical composition, and antihyperglycemic principles with α-glucosidase inhibitory activity are summarized.

Topics: Diabetes Mellitus, Type 2; Glycoside Hydrolase Inhibitors; Hypoglycemic Agents; Mexico; Molecular Structure; Plants, Medicinal

The study was performed to assess, for the first time, the in vitro anti-diabetic potential of ten Asteraceae plant extracts to inhibit the activity of digestive enzymes (α-amylase, α-, β-glucosidases and lipase) responsible for hydrolysis/digestion of sugar and lipids. Prevention of advanced glycation end-products (AGEs) formation was evaluated in bovine serum albumin/ribose glycation reaction model. The phytochemical profiles and caffeoylquinic acids (CQAs) contents were determined for the methanolic extract of each plant. Analyzed plant extracts exhibited significant inhibitory activity against key digestive enzymes linked to type II diabetes and obesity. A strong inhibition was observed for glucosidases and mild activity towards amylase and lipase (compared to reference compounds). Moreover, some extracts exhibited potent ability to prevent formation of AGEs, implicated in some diabetic complications. Caffeoylquinic acids were dominant in all plant extracts and findings demonstrate that these compounds are the most relevant hypoglycemic and anti-glycation agents. From the obtained results, Argyranthemum pinnatifidum, Helichrysum melaleucum, and Phagnalon lowei are good candidates for further development of phyto-pharmaceutical preparations as complementary therapy for diabetes and obesity control.

Topics: alpha-Amylases; Antioxidants; Asteraceae; Diabetes Mellitus, Type 2; Glycation End Products, Advanced; Hypoglycemic Agents; Obesity; Phytotherapy; Plant Extracts; Quinic Acid

Diet and exercise intervention can delay or prevent development of type-2-diabetes (T2D), and high habitual coffee consumption is associated with reduced risk of developing T2D. This study aimed to test whether selected bioactive substances in coffee acutely and/or chronically increase insulin secretion from β-cells and improve insulin sensitivity in skeletal muscle cells. Insulin secretion from INS-1E rat insulinoma cells was measured after acute (1-h) and long-term (72-h) incubation with bioactive substances from coffee. Additionally, we measured uptake of radioactive glucose in human skeletal muscle cells (SkMC) after incubation with cafestol. Cafestol at 10(-8) and 10(-6) M acutely increased insulin secretion by 12% (p < 0.05) and 16% (p < 0.001), respectively. Long-term exposure to 10(-10) and 10(-8) M cafestol increased insulin secretion by 34% (p < 0.001) and 68% (p < 0.001), respectively. Caffeic acid also increased insulin secretion acutely and chronically. Chlorogenic acid, trigonelline, oxokahweol, and secoisolariciresinol did not significantly alter insulin secretion acutely. Glucose uptake in SkMC was significantly enhanced by 8% (p < 0.001) in the presence of 10(-8) M cafestol. This newly demonstrated dual action of cafestol suggests that cafestol may contribute to the preventive effects on T2D in coffee drinkers and be of therapeutic interest.

Topics: Alkaloids; Animals; Butylene Glycols; Caffeic Acids; Chlorogenic Acid; Coffee; Diabetes Mellitus, Type 2; Diterpenes; Glucose; Guinea Pigs; Humans; Insulin; Insulin Secretion; Insulin-Secreting Cells; Lignans; Muscle, Skeletal

Obesity, considered as a consequence of overnutrition, sustains a low-degree inflammatory state and results in insulin-resistance and type 2 diabetes. Here, we investigated the anti-inflammatory effects of 5-caffeoylquinic acid (5-CQA) in high-fat diet-induced obese rats. Serum interleukin (IL)-6, monocyte chemotactic protein 1 (MCP-1), tumor necrosis factor-alpha (TNF-α), total cholesterol (TC), triglyceride (TG), and free fatty acid (FFA) levels were determined. Expression of genes related to TG metabolism, macrophage biomarkers, and inflammation was assessed by real-time PCR. Protein expression of NF-κB, PPARγ2, and phosphorylated IκBα was evaluated by western blotting, and the histology of adipose tissue was examined. Supplementation of the rat diet with 5-CQA reduced obesity development, macrophage infiltration, and steatosis. Additionally, 5-CQA decreased the expression of NF-κB and downstream inflammatory cytokines, but increased the expression of PPARγ2, in a dose-dependent manner. Thus, 5-CQA improved obesity and obesity-related metabolic disturbances via PPARγ2 and the NF-κB signaling pathway.

Topics: Adipose Tissue; Animals; Chemokine CCL2; Cholesterol; Diabetes Mellitus, Type 2; Humans; Macrophages; Male; NF-kappa B; PPAR gamma; Quinic Acid; Rats; Rats, Sprague-Dawley; Signal Transduction; Triglycerides; Tumor Necrosis Factor-alpha