OBJECTIVETo develop a HPLC assay for the determination of metformin hydrochloride-related substances.

METHODSThe separation was performed on SHIMADZU VP-ODS (250 4.6 mm, 5 microm) column. The mobile phase of dicyandiamide was composed of methyl alcohol-1 mmol x L(-1) sodium dodecylsulfate in 10 mmol x L(-1) phosphate salt solution (60:40) (pH=5.5). The mobile phase of other related substances was composed of methyl alcohol-1 mmol x L(-1) sodium dodecysulfate in 10 mmol x L(-1) phosphate salt solution (55:45)(pH=5.5). The detection wavelength was 232 nm, and the running speed was 0.8 ml min(-1) at room temperature.

RESULTGood resolution of dicyandiamide and main peak was obtained. The test results were reproducible.

CONCLUSIONThe method is simple, rapid and suitable for the determination of dicyandiamide and other metformin hydrochloride-related substances.

With the rise of incidence, fatality rate, and number of young cases, diabetes mellitus has been one of the seven major diseases threatening human health. Although many antidiabetic drugs(oral or for injection) are available, the majority have serious side effects during the long-term use. Thus, it is of particularly vital to develop new drugs with low risk and definite effect. Psoraleae Fructus, a traditional medicinal widely used in the folk, has hypoglycemic, anti-osteoporosis, antitumor, estrogen-like, and anti-inflammatory effects. Thus, it has great clinical application potential. Chinese medicine and the active ingredients, characterized by multiple targets, multiple pathways, and multiple effects in the treatment of diabetes mellitus, have distinct advantages in clinical application. However, the safety of Chinese medicine remains to be a challenge, and one of keys is to clarifying the mechanism of a single Chinese medicinal and its active ingredients. With the method of literature research, this study summarized and analyzed the hypoglycemic mechanisms of Psoraleae Fructus and its main active ingredients over the last decade: regulating glucose metabolism, improving insulin resistance, and directly acting on pancreatic β-cells. The result is expected to serve as a reference for further research on the effects of Psoraleae Fructus and its main chemical constituents in lowering blood glucose and preventing diabetes mellitus and the clinical application.
Drugs, Chinese Herbal/pharmacology* ; Fruit/chemistry* ; Humans ; Hypoglycemic Agents/pharmacology* ; Osteoporosis/drug therapy* ; Psoralea/chemistry*

In-vitro assay methods were established to evaluate transactivation and binding activity of compounds on peroxisome proliferator-activated receptor y (PPARγ). Firstly, plasmids were constructed for transactivation assay of PPARγ response element (PPRE) triggered reporter gene expression, and for cell-based binding activity assay of the chimeric receptor, which was fused with PPARγ ligand binding domain (LBD) and yeast transcriptional activator Gal4. Secondly, by using PPARy competitive binding assay based on time resolved-fluorescence resonance energy transfer (TR-FRET), affinities of compounds and drugs to PPARγ were evaluated. In application of these above methods, the PPARγ activating potency and characteristics of different compounds were evaluated, and a novel benzeneselfonamide derivative, ZLJ01, was found to have comparable binding activity and affinity with the well-known PPARy agonist, but lack of PPRE mediated transactivation activity. In preliminary study on in-vitro hypoglycemic activity, ZLJ1 was found to promote insulin-stimulated glucose uptake by liver cells. Therefore, we believe that combining transactivation and binding activity as well as affinity evaluation, the system could be used to screen non-agonist PPARγ ligand as anovel PPARγ modulator
Genes, Reporter ; Hepatocytes ; Hypoglycemic Agents ; chemistry ; Ligands ; PPAR gamma ; agonists ; chemistry ; Plasmids ; Response Elements ; Sulfonamides ; chemistry ; Transcriptional Activation

Eight compounds,(R)-2-[5-(methoxycarbonyl)-4-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl]acetic acid(1),(3S,4R)-3,4-dihydro-3,4-epoxy-5-hydroxynaphthalen-1(2H)-one(2),(-)-mitorubrinol(3),(-)-mitorubrin(4),(±)-asperlone A(5), terreusinone(6), verrucisidinol(7) and cerebroside C(8) were isolated from the endophytic fungus Talaromyces purpurogenus by using various column chromatographic techniques. Their structures were identified by NMR, MS, CD and optical rotation. Compounds 1 and 2 were new compounds. Their anti-diabetic activities in vitro were evaluated, and compound 1 showed moderate inhibitory activity toward XOD at 10 μmol·L~(-1) with the inhibition rate of 69.9%.
Endophytes/chemistry* ; Hypoglycemic Agents/chemistry* ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Secondary Metabolism ; Talaromyces/chemistry* ; Tylophora/microbiology* ; Xanthine Oxidase/antagonists & inhibitors*

Eight terpenoids were isolated from the fruits of Amomum villosum by silica gel, Sephadex LH-20, Rp-C_(18), MCI GEL CHP20 P column chromatography, preparative TLC, and HPLC. Their structures were identified by HR-ESI-MS, ~1H and ~(13)C-NMR, IR, UV, [α]_D, and ECD spectroscopic data as kravanhin A 3-O-β-D-glucopyranoside(1), kravanhin B(2), 6-eudesmene-1β,4β-diol(3), oplodiol(4), vicodiol(5),(1R,2S,4R,7S)-vicodiol 9-O-β-D-glucopyranoside(6),(1R,2S,4S,5R)-angelicoidenol 2-O-β-D-glucopyranoside(7), and(1S,2S,4R,6S)-bornane-2,6-diol 2-O-β-D-glucopyranoside(8). Compound 1 was a new compound, and compounds 2-5 were isolated from A. villosum for the first time. Their hypoglycemic activity was tested based on STC-1 cell model and two enzymatic models(GPa and PTP1 B). The results showed that compounds 1, 7, and 8 could stimulate GLP-1 with the secretion rates of 692.8%, 398.6%, and 483.3% at 25.0 μmol·L~(-1), and compound 6 showed inhibitory activity against GPa with an IC_(50) value of 78.6 μmol·L~(-1).
Fruit/chemistry* ; Terpenes/analysis* ; Amomum ; Hypoglycemic Agents/analysis* ; Chromatography, High Pressure Liquid

Diabetes mellitus (DM) is a metabolic disorder caused by insufficient or inefficient insulin secretary response and it is characterized by increased blood glucose levels (hyperglycemia). DM is a heterogonous group of syndromes. Glucose is the main energy source for the body, and in the case of DM, management of glucose becomes irregular. There are three key defects in the onset of hyperglycemia in DM, namely increased hepatic glucose production, diminished insulin secretion, and impaired insulin action. Conventional drugs treat diabetes by improving insulin sensitivity, increasing insulin production and/or decreasing the amount of glucose in blood. This article provides a comprehensive review of the mode of action of most popular hypoglycemic herbs, such as ginseng, bitter melon, fenugreek, banaba, Gymnema sylvestre and Coptis chinensis. The herbs act by increasing insulin secretion, enhancing glucose uptake by adipose and skeletal muscle tissues, inhibiting intestinal glucose absorption and inhibiting hepatic glucose production. Although evidence from animals and humans consistently supports the therapeutic effect of these phytomedicines, multicenter large-scale clinical trials have not been conducted to evaluate the safety and efficacy of these herbal medicines and their interaction with conventional drugs when administered simultaneously.
Animals ; Biological Products ; chemistry ; therapeutic use ; Diabetes Mellitus ; drug therapy ; Humans ; Hypoglycemic Agents ; chemistry ; therapeutic use ; Plants, Medicinal

Acremonium ; chemistry ; Adjuvants, Immunologic ; pharmacology ; Animals ; Antineoplastic Agents ; pharmacology ; Cordyceps ; chemistry ; classification ; Humans ; Hypoglycemic Agents ; pharmacology ; Polysaccharides ; chemistry ; isolation & purification ; pharmacology

The diabetes is mainly treated by the oral administration of western medicines at present. Despite their rapid curative effect, there have been still many reports for the western medicines about their clinical adverse reactions, failure of effective prevention and treatment of complications and drug resistance. Hence, they are not suitable for long-term administration. Traditional Chinese medicines have a long history in treating diabetes mellitus (DM) , which is commonly known as Xiaokezheng in the theory of traditional Chinese medicines. In recent years, many scholars have taken extracts from traditional Chinese medicines or separated active constituents as the study objects in the expectation of developing new-type drugs for treating and preventing diabetes. Therefore, a large number of study reports have been emerged in this field. Due to their significant glucose-reducing effect and specific effect in treating complications of diabetes, traditional Chinese medicine Gardeniae Fructus and its iridoid component geniposide shall be given full attention. This paper summarized the advance in studies on the curative effect and action mechanism of Gardeniae Fructus and geniposide in preventing and treating diabetes.
Animals ; Diabetes Mellitus ; drug therapy ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; Fruit ; chemistry ; Gardenia ; chemistry ; Humans ; Hypoglycemic Agents ; administration & dosage ; chemistry

Anticholesteremic Agents ; isolation & purification ; pharmacology ; Antineoplastic Agents, Phytogenic ; isolation & purification ; pharmacology ; Hypoglycemic Agents ; isolation & purification ; pharmacology ; Lactones ; chemistry ; isolation & purification ; Lettuce ; chemistry ; Molecular Structure ; Plants, Medicinal ; chemistry ; Sesquiterpenes ; chemistry ; isolation & purification ; Triterpenes ; chemistry ; isolation & purification

Catalpol is a active component in Rehmannia Root, and its pharmacological effects are extensive. In this paper its effects and chemical changes were summarized. This will offer the reference for further research work catalpol.
Animals ; Antineoplastic Agents, Phytogenic ; pharmacology ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Glucosides ; chemistry ; isolation & purification ; pharmacology ; Humans ; Hypoglycemic Agents ; pharmacology ; Iridoid Glucosides ; Iridoids ; chemistry ; isolation & purification ; pharmacology ; Neuroprotective Agents ; pharmacology ; Plants, Medicinal ; chemistry ; Rehmannia ; chemistry ; Technology, Pharmaceutical ; methods