This study was conducted in order to compare the biological activities of leaf and root water extracts of Smilax china L. (SC) by measuring the total polyphenol and flavonoid contents, anti-oxidant activity, inhibitory effect on alpha-glucosidase, and anti-inflammatory gene expression. The total polyphenol and flavonoid contents of SC leaf (SCLE) and root (SCRE) water extracts were 127.93 mg GAE/g and 39.50 mg GAE/g and 41.99 mg QE/g and 1.25 mg QE/g, respectively. The anti-oxidative activities of SCLE and SCRE were measured using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) radical scavenging activity assay and reducing power assay. Both SCLE and SCRE scavenged radicals in a concentration-dependent manner, and SCLE showed stronger radical scavenging activity and reducing power than SCRE; however, both SCLE and SCRE exhibited lower activities than ascorbic acid. Compared to the anti-diabetic drug acarbose, which was used as a positive control, SCLE and SCRE exhibited low alpha-glucosidase inhibition activities; nevertheless, the activity of SCLE was 3.7 fold higher than that of SCRE. Finally, SCLE caused significantly decreased expression of the LPS-induced cytokines, iNOS, and COX-2 mRNA in RAW264.7 cells, indicating anti-inflammatory activity. These results indicate that SCLE might be a potential candidate as an anti-oxidant, anti-diabetic, and anti-inflammatory agent.
Acarbose ; alpha-Glucosidases ; Ascorbic Acid ; Biphenyl Compounds ; China ; Cytokines ; Gene Expression ; Picrates ; RNA, Messenger ; Smilax ; Water

Acarbose is widely used as α-glucosidase inhibitor in the treatment of type Ⅱ diabetes. Actinoplanes sp. is used for industrial production of acarbose. As a secondary metabolite, the biosynthesis of acarbose is quite complex. In addition to acarbose, a few acarbose structural analogs are also accumulated in the culture broth of Actinoplanes sp., which are hard to remove. Due to lack of systemic understanding of the biosynthesis and regulation mechanisms of acarbose and its structural analogs, it is difficult to eliminate or reduce the biosynthesis of the structural analogs. Recently, the advances in omics technologies and molecular biology have facilitated the investigations of biosynthesis and regulatory mechanisms of acarbose and its structural analogs in Actinoplanes sp.. The genes involved in the biosynthesis of acarbose and its structural analogs and their regulatory mechanism have been extensively explored by using bioinformatics analysis, genetic manipulation and enzymatic characterization, which is summarized in this review.
Acarbose/metabolism* ; Diabetes Mellitus, Type 2/drug therapy* ; Genetic Techniques ; Humans

BACKGROUND: We evaluated the efficacy and safety of acarbose add-on therapy in Korean patients with type 2 diabetes mellitus (T2DM) who are inadequately controlled with metformin and sitagliptin. METHODS: A total of 165 subjects were randomized to metformin and sitagliptin (Met+Sita, n=65), metformin, sitagliptin, and acarbose (Met+Sita+Acarb, n=66) and sitagliptin and acarbose (Sita+Acarb, exploratory assessment, n=34) therapy in five institutions in Korea. After 16 weeks of acarbose add-on or metformin-switch therapy, a triple combination therapy was maintained from week 16 to 24. RESULTS: The add-on of acarbose (Met+Sita+Acarb group) demonstrated a 0.44%±0.08% (P<0.001 vs. baseline) decrease in glycosylated hemoglobin (HbA1c) at week 16, while changes in HbA1c were insignificant in the Met+Sita group (−0.09%±0.10%, P=0.113). After 8 weeks of triple combination therapy, HbA1c levels were comparable between Met+Sita and Met+Sita+Acarb group (7.66%±0.13% vs. 7.47%±0.12%, P=0.321). Acarbose add-on therapy demonstrated suppressed glucagon secretion (area under the curve of glucagon, 4,726.17±415.80 ng·min/L vs. 3,314.38±191.63 ng·min/L, P=0.004) in the absence of excess insulin secretion during the meal tolerance tests at week 16 versus baseline. The incidence of adverse or serious adverse events was similar between two groups. CONCLUSION: In conclusion, a 16-week acarbose add-on therapy to metformin and sitagliptin, effectively lowered HbA1c without significant adverse events. Acarbose might be a good choice as a third-line therapy in addition to metformin and sitagliptin in Korean subjects with T2DM who have predominant postprandial hyperglycemia and a high carbohydrate intake.
Acarbose ; Diabetes Mellitus, Type 2 ; Drug Therapy, Combination ; Glucagon ; Hemoglobin A, Glycosylated ; Humans ; Hyperglycemia ; Incidence ; Insulin ; Korea ; Meals ; Metformin ; Sitagliptin Phosphate

Postprandial hypotension (PPH) has not been described as a cause of hypotension after the return of spontaneous circulation (ROSC) in the intensive care unit (ICU). A 74 year old man underwent cardiopulmonary resuscitation (CPR) due to monomorphic ventricular tachycardia. After the ROSC, inotropic agents were not reduced but increased. PPH had occurred, according to the flow sheet, so a provocation test was performed. We noted hypotension but no serum hypoglycemia or tachycardia. The hypotension was diagnosed as PPH. We chose acarbose for treatment; thus, the inotropic agents were discontinued. This is the first case in which hypotension occurred in a patient recovering after CPR in the ICU and that the PPH was treated with acarbose. PPH should be considered and treated to manage hypotension in elderly patients in the ICU.
Acarbose ; Aged ; Cardiopulmonary Resuscitation ; Humans ; Hypoglycemia ; Hypotension ; Critical Care ; Intensive Care Units ; Postprandial Period ; Tachycardia ; Tachycardia, Ventricular

Two components of the neuroendocrine-hormonal response to long-term treatment of acarbose, adipose tissue-derived leptin and central neuropeptide Y (NPY), were investigated in the ICR mice on a high-carbohydrate diet. Acarbose, administered 5 or 50 mg per 100 g diet for four weeks, dose dependently suppressed body weight gain. The body weight gain was reduced along with the amount of daily food intake in 50 mg acarbose-treated group at 7th and 28th day 5 or 50 mg acarbose treatment administered for four weeks reduced leptin mRNA levels to 62% and 77% of the control group, demonstrating that the amount of leptin mRNA in adipocytes correlates with body weight. As dose of acarbose increased, leptin mRNA level also increased, suggesting that potent inhibition of alpha-glycosidase by a higher dose of acarbose furthers the enzyme activity and leptin gene consequently. On the other hand, central expression level of NPY gene was increased significantly compared with the control group at the same amount of acarbose administered, reflecting that leptin and NPY operate in a negative-feedback circuit to regulate body fat stores.
Acarbose* ; Adipocytes ; Adipose Tissue ; Animals ; Body Weight ; Diet* ; Eating ; Hand ; Leptin ; Mice* ; Mice, Inbred ICR ; Neuropeptide Y* ; Neuropeptides* ; RNA, Messenger

BACKGROUND/AIMS: Collagenous colitis (CC) and lymphocytic colitis (LC) are characterized by chronic diarrhea and normal radiologic and endoscopic findings. These are currently not uncommon entities whose incidence in increasing as more clinicians take biopsies from macroscopically normal colons. The purpose of this study was to examine the clinical features and characteristics in microscopic colitis. METHODS: From January 2003 to December 2006, medical records were reviewed from 80 patients with chronic diarrhea, who had normal colonoscopic findings but underwent biopsy. Patients with microscopic colitis were identified by reviewing the pathology databases and by reviewing biopsies. RESULTS: Microscopic colitis was diagnosed in 12 patients (15%). Six patients with CC (Male:Female=2:4, mean age 54+/-20.1 years) and 6 patients with LC (Male:Female=5:1, mean age 51.2+/-21.4 years) were identified. Autoimmune disease was diagnosed in 4 patients (33%). Drug-induced disease was suspected in 3 patients (25%). The inciting drugs were NSAIDs, ticlopidine, ranitidine, and acarbose. Complete or partial resolution of diarrhea was achieved in all patients, including spontaneous resolution in 2 patients. Antidiarrheal drugs, mesalazine, and cholestylamine were highly effective in both diseases. Recurrence of symptoms occurred in 2 patients (17%). They are taking medicine at present. CONCLUSIONS: Microscopic colitis is a relatively common cause of chronic diarrhea that appears to be increasing in incidence. We reported clinical features, characteristics, treatment, and response of microscopic colitis in our experience.
Acarbose ; Anti-Inflammatory Agents, Non-Steroidal ; Antidiarrheals ; Autoimmune Diseases ; Biopsy ; Colitis, Collagenous ; Colitis, Lymphocytic ; Colitis, Microscopic ; Colon ; Diarrhea ; Humans ; Incidence ; Medical Records ; Mesalamine ; Ranitidine ; Recurrence ; Ticlopidine

BACKGROUND/OBJECTIVES: We investigated total 26 ingredients of Saengshik which will be commercially produced as an anti-diabetic dietary supplement. SUBJECTS/METHODS: Thirteen vegetables, nine cereals, three legumes and one seed were extracted with aqueous ethanol for 2 h at 60degrees C, and evaluated for their inhibitory effects against alpha-amylase and alpha-glucosidase and for total phenolic and flavonoid contents. RESULTS: All ingredients inhibited alpha-amylase activity except cabbage. Strong inhibitory activity of alpha-amylase was observed in leek, black rice, angelica and barley compared with acarbose as a positive control. Stronger inhibition of alpha-glucosidase activity was found in small water dropwort, radish leaves, sorghum and cabbage than acarbose. All Saengshik ingredients suppressed alpha-glucosidase activity in the range of 0.3-60.5%. Most ingredients contained total phenols which were in the range of 1.2-229.4 mg gallic acid equivalent/g dried extract. But, total phenolic contents were not observed in carrot, pumpkin and radish. All ingredients contained flavonoid in the range of 11.6-380.7 mg catechin equivalent/g dried extract. CONCLUSIONS: Our results demonstrate that Saengshik containing these ingredients would be an effective dietary supplement for diabetes.
Acarbose ; alpha-Amylases* ; alpha-Glucosidases* ; Angelica ; Brassica ; Catechin ; Edible Grain ; Cucurbita ; Daucus carota ; Dietary Supplements ; Ethanol ; Fabaceae ; Gallic Acid ; Food, Organic* ; Hordeum ; Oenanthe ; Phenol ; Phenols ; Raphanus ; Sorghum ; Vegetables

Postprandial hypotension is an important minor clinical problem. It is a common disorder that causes unexplained dizziness, falls, lightheadedness, syncope, angina pectoris, and even transient ischemic attacks of the brain. It is often defined as a decrease in systolic blood pressure by more than 20 mmHg within 2 hours after a meal. The mechanism of postprandial hypotension is splanchnic blood pooling via the loading of glucose in the intestine and decompensation of the autonomic nervous system. The best tool for detecting a fall in systolic blood pressure is 24-hour ambulatory blood pressure monitoring. Acarbose, an alpha-glucosidase inhibitor, is very useful for preventing postprandial hypotension. We experienced a case of postprandial hypotension that presented with postprandial dizziness. The patient was treated successfully with acarbose before each meal.
Acarbose ; alpha-Glucosidases ; Angina Pectoris ; Autonomic Nervous System ; Blood Pressure ; Blood Pressure Monitoring, Ambulatory ; Brain ; Dizziness ; Glucose ; Humans ; Hypotension ; Intestines ; Ischemic Attack, Transient ; Meals ; Syncope

The objective of this study was to investigate the hypoglycemic effects of quercetin (QE) in animal models of diabetes mellitus (DM). A starch solution (1 g/kg) with and without QE (100 mg/kg) or acarbose (40 mg/kg) was orally administered to streptozotocin (STZ)-induced diabetic rats after an overnight fast. Postprandial plasma glucose levels were measured and incremental areas under the response curve were calculated. To study the effects of chronic feeding of QE, five-week-old db/db mice were fed an AIN-93G diet, a diet containing QE at 0.08%, or a diet containing acarbose at 0.03% for 7 weeks after 1 week of adaptation. Plasma glucose and insulin, blood glycated hemoglobin, and maltase activity of the small intestine were measured. Oral administration of QE (100 mg/kg) or acarbose (40 mg/kg) to STZ-treated rats significantly decreased incremental plasma glucose levels 30-180 min after a single oral dose of starch and the area under the postprandial glucose response, compared with the control group. QE (0.08% of diet) or acarbose (0.03% of diet) offered to db/db mice significantly reduced both plasma glucose and blood glycated hemoglobin compared to controls without significant influence on plasma insulin. Small intestine maltase activities were significantly reduced by consumption of QE or acarbose. Thus, QE could be effective in controlling fasting and postprandial blood glucose levels in animal models of DM.
Acarbose ; Administration, Oral ; Animals ; Blood Glucose ; Diabetes Mellitus ; Diet ; Fasting ; Glucose ; Hemoglobins ; Hyperglycemia ; Hypoglycemic Agents ; Insulin ; Intestine, Small ; Mice ; Models, Animal ; Plasma ; Quercetin ; Rats ; Starch ; Streptozocin

To elucidate antidiabetic effect and mechanism(s) of acarbose in a polygenic spontaneous hyperglycemic and hyperinsulinemic diabetic animal model, KKAy mice, acarbose was administered orally for 4 weeks and effects on body weight, plasma glucose and insulin levels, genetic expressions of intestinal sucrase-isomaltase (SI), sodium-glucose cotransporter (sGLT1) and glucose transporter in quadriceps muscle (GLUT4) were examined in this study. Although no differences in body weight were detected between control and acarbose-treated groups, plasma glucose level in acarbose-treated group was markedly reduced as compared to the control. In the mechanism study, acarbose downregulated the SI and SGLT1 gene expressions, and upregulated the GLUT4 mRNA and protein expressions when compared to the control group. In conclusion, the data obtained strongly implicate that acarbose can prevent the hyperglycemia in KKAy mice possibly through blocking intestinal glucose absorption by downregulations of SI and sGLT1 mRNA expressions, and upregulation of skeletal muscle GLUT4 mRNA and protein expressions.
Absorption ; Acarbose* ; Animals ; Blood Glucose ; Body Weight ; Gene Expression ; Glucose ; Glucose Transport Proteins, Facilitative ; Hyperglycemia ; Insulin ; Mice* ; Models, Animal ; Muscle, Skeletal ; Quadriceps Muscle ; RNA, Messenger ; Up-Regulation