Design and oral hypoglycemic activity of novel oral hypoglycemic peptide ODA / 中国药科大学学报

@#Incretin promotes insulin secretion through a glucose-dependent mechanism, involving glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). Therefore, their correspondingly specific receptors GLP-1R and GIPR are suitable targets for the treatment of type 2 diabetes. Based on the oral hypoglycemic peptide OHP2 designed by our team, we further designed a new oral hypoglycemic peptide, ODA to reduce glucose. Compared with OHP2, ODA exhibited better lipophilicity as well as the enhanced endocytosis and transcytosis in Caco-2 cells. In addition, ODA remained the ability to activate GLP-1R and enhanced the binding ability to GIPR. The hypoglycemic efficacy of the low-dose ODA (0.53 mg/kg) is comparable to that of OHP2 (1.06 mg/kg). These results indicated that ODA could be a new oral drug with potential for the treatment of type 2 diabetes.

Alkaloids from fruit of Lycium chinense var. potaninii / 中国中药杂志

Ten alkaloids(1-10) were isolated from the ethyl acetate extract of the fruit of Lycium chinense var. potaninii by silica gel, ODS, and preparative high performance liquid chromatography(HPLC), and identified by NMR and MS as methyl(2S)-[2-formyl-5-(hydroxymethyl)-1H-pyrrol-1-yl]-3-(phenyl)propanoate(1), methyl(2R)-[2-formyl-5-(methoxymethyl)-1H-pyrrol-1-yl]-3-(phenyl)propanoate(2), 3-hydroxy-4-ethyl ketone pyridine(3), indolyl-3-carbaldehyde(4),(R)-4-isobutyl-3-oxo-3,4-dihydro-1H-pyrrolo[2,1-c][1,4]oxazine-6-carbaldehyde(5),(R)-4-isopropyl-3-oxo-3,4-dihydro-1H-pyrrolo[2,1-c][1,4]oxazine-6-car-baldehyde(6), methyl(2R)-[2-formyl-5-(methoxymethyl)-1H-pyrrol-1-yl]-3-(4-hydroxyphenyl)propanoate(7), dimethyl(2R)-[2-formyl-5-(methoxymethyl)-1H-pyrrol-1-yl]butanedioate(8), 4-[formyl-5-(methoxymethyl)-1H-pyrrol-1-yl]butanoate(9), 4-[2-formyl-5-(methoxymethyl)-1H-pyrrol-1-yl]butanoic acid(10). All the compounds were isolated from the plant for the first time. Among them, compounds 1-3 were new compounds. Compounds 1-9 were evaluated for hypoglycemic activity in vitro with the palmitic acid-induced insulin resistance in HepG2 cells. At 10 μmol·L~(-1), compounds 4, 6, 7, and 9 can promote the glucose consumption of HepG2 cells with insulin resistance.

A new bibenzyl derivative from stems of Dendrobium officinale / 中国中药杂志

Eleven compounds were isolated from the 95% ethanol extract of the stems of Dendrobium officinale after water extraction by various modern chromatographic techniques, such as silica gel column chromatography(CC), octadecyl-silica(ODS) CC, Sephadex LH-20 CC, preparative thin layer chromatography(PTLC) and preparative high performance liquid chromatography(PHPLC). According to spectroscopic analyses(MS, 1D-NMR, 2D-NMR) combined with optical rotation data and calculated electronic circular dichroism(ECD), their structures were identified as dendrocandin Y(1), 4,4'-dihydroxybibenzyl(2), 3-hydroxy-4',5-dimethoxybibenzyl(3), 3,3'-dihydroxy-5-methoxybibenzyl(4), 3-hydroxy-3',4',5-trimethoxybibenzyl(5), crepidatin(6), alternariol(7), 4-hydroxy-3-methoxypropiophenone(8), 3-hydroxy-4,5-dimethoxypropiophenone(9), auriculatum A(10) and hyperalcohol(11). Among them, compound 1 was a new bibenzyl derivative; compounds 2 and 7-11 have not been previously reported from Dendrobium plants; compound 6 was reported from D.officinale for the first time. Compounds 3-6 exhibited potent antioxidant activity with IC_(50) values of 3.11-9.05 μmol·L~(-1) in ABTS radical scavenging assay. Compound 4 showed significant inhibitory effect on α-glucosidase, with IC_(50) value of 17.42 μmol·L~(-1), indicating that it boasted hypoglycemic activity.

Synthesis and Biological Activity of Trolox Amide Derivatives

Abstract A series of Trolox amide derivatives were synthesized by modifying the carboxyl groups of Trolox. Thirty target compounds were obtained and characterized through nuclear magnetic resonance and mass spectrometry. Trolox derivatives were employed to explore the potential structure-antioxidant activity relationships. The antioxidant activities of these compounds were evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP) and hydroxyl radical assays. DPPH scavenging activity test results illustrated that compounds exhibited scavenging activities similar to L-ascorbic acid and Trolox, with compounds 14a, 18a, 24a and 26a in particular exhibiting higher scavenging activities than L-ascorbic acid. The results demonstrated that compounds displayed ABTS scavenging activities similar to L-ascorbic acid and Trolox, with compounds 26a and 29a in particular having potency twofold higher. FRAP assay results indicated that compounds 11a, 19a, 25a, 29a and 30a had activity similar to Trolox. The results revealed that compounds 6a and 19a had similarly high hydroxyl radical-scavenging activities as Trolox. The results of α-glucosidase experiments uncovered that compounds 10a, 25a, 28a and 29a had excellent inhibitory activity, which was similar to that of acarbose and different from Trolox. The results of acetylcholinesterase and butyrylcholinesterase experiments demonstrated that some compounds had weak anticholinesterase activities. 26a and 29a are important Trolox derivatives with better biological activity profiles and deserve further study

ROLE OF NELUMBO NUCIFERA (LOTUS) STEM AS IMMUNITY BOOSTER AND ANTI-INFLAMMATORY FOOD

In China and India, Nelumbo nucifera, a perennial aquatic plant, has been used as a medicinal herb. The various sections of plants, such as leaves, seeds, flowers and rhizomes, have been reported to have beneficial effects in the treatment of pharyngopathy, pectoralgia, spermatorrhoea, leucoderma, smallpox, dysentery, cough, haematemesis, epistaxis, haemoptysis, haematuria, metrorrhagia, hyperlipidaemia, fever, cholera, hepatopathy and hyperdipsia in the traditional medicine system. Different pharmacological activities such as anti-ischaemic activity, antioxidant activity, hepato- protective activity, anti-inflammatory activity, anti-fertility activity, anti- arrhythmic activity, anti-fibrosis activity, antiviral activity, anti-proliferative activity, anti-diarrhoeal activity, psychopharmacological activity, antipyretic activity, immune-modulatory activity, hypoglycaemic activity, aldose reductase inhibitory activity, antibacterial, aphrodisiac activity, anti-platelet activity, cardiovascular activity, anti-obesity activity, lipolytic activity, hypo-cholesterolaemic activity, hepato-protective activity, anticancer activitydiuretic activity, antioxidant activity have been clinically evaluated for N.nucifera. Different pharmacological activities such as anti-ischaemic activity, antioxidant activity, hepato-protective activity, anti-inflammatory activity, anti-fertility activity, anti-arrhythmic activity, anti- fibrosis activity, antiviral activity, anti-proliferative activity, anti-diarrhoeal activity, psychopharmacological activity, diuretic activity, antioxidant activity have been clinically evaluated for N.nucifera. A wide number of phytoprinciples from the plant have been isolated. The present review seeks to consolidate the traditional, ethno-botanical, phytochemical and pharmacological data available on N.nucifera stem and to explore its role as an immunity booster and anti-inflammatory food.

Submerged fermentation improves bioactivity of mulberry fruits and leaves / 中草药·英文版

Objective: Mulberry (Morus spp.) fruits and leaves have been proven to possess nutraceutical properties. Due to its fast and easy growing characteristics, mulberry fruits (MF) and leaves (ML) potentially emerge as a great source of functional foods. This study aims to enhance bioactivities (antioxidant, anti-inflammation, and hypoglycemic activity) of MF and ML via submerged fermentation using bacteria (Lactobacillus plantarum TAR 4), yeast (Baker's yeast and red yeast) and fungi (Tempeh and Tapai starter). Methods: In this study, 25% (mass to volume ratio) of MF and ML were fermented (48 h) with 1% (mass to volume ratio) of different microbial cultures, respectively. Effects of different fermentations on MF and ML were determined based on the changes of total phenolics (TPC), flavonoids (TFC), anthocyanins, total sugar, DPPH activity, ferric reducing antioxidant power (FRAP), albumin denaturation inhibition activity (ADI), anti-lipoxygenase activity and α-amylase inhibition activity (AI). Results: Generally, ML had higher AI than MF. However, MF exhibited higher DPPH, FRAP and anti-lipoxygenase activity than ML. After all forms of fermentation, DPPH and AI activity of MF and ML were increased significantly (P < 0.05). However, the effects of fermentation on TPC, FRAP, ADI and anti-lipoxygenase activity of MF were in contrast with ML. TPC, FRAP and anti-lipoxygenase activity of ML were enhanced, but reduced in MF after fermentation. Although the effects exerted by different microorganisms in MF and ML fermentation were different, the bioactivities of MF and ML were generally improved after fermentation. Fermentation by Tempeh starter enhanced TPC (by 2-fold), FRAP (by 2.3-fold), AI (at 10% increment) and anti-lipoxygenase activity (by 5-fold) of ML, whereas Tapai fermentation effectively enhanced the DPPH (at 17% increment) and ADI (by 2-fold) activity of MF. Conclusion: Findings of this study provide an insight into the future process design of MF and ML processing into novel functional foods.

Research progress of biological activity of Ipomoea batatas and its main components in vivo / 中草药

Ipomoea batatas is a kind of both edible and medicinal plant, which provides a dietary source of vitamins, minerals, carbohydrates, proteins, anthocyanins, essential fatty acids, trace elements and other nutrients, and these active substances play a role in many pharmacological activities such as antitumor, immune regulation, hepatoprotective effect, hypoglycemic, hypolipidemic, anti-aging, intestinal regulation, anti-obesity, anti-radiation, anti-fatigue, etc, and promote health in many aspects. The Dictionary of Traditional Chinese Medicine and Chinese Materia Medica recorded that I. batatas have the characteristics of tonifying deficiency and replenishing qi, strengthening spleen and kidney. In recent years, it has become a research hotspot in multidisciplinary fields for its rich nutritional components and functional characteristics. In this paper, the research progress of biological activity of I. batatas in vivo was reviewed from aspects of basic and clinical researches, which may provide references for its further development, research and comprehensive utilization.

Chemical constituents and hypoglycemic activity of Phlomis tuberosa / 中草药

Objective: To study the chemical constituents and hypoglycemic activity of Phlomis tuberosa. Methods: The db/db diabetic mice was used to screen the hypoglycemic active site of P. tuberosa. The chemical constituents were isolated and purified by various separation and analysis techniques. The structures of these compounds were identified by spectroscopic analysis (1H-, 13C-NMR and MS). The hypoglycemic activities of these compounds were verified by the DPP-4 inhibitory activity in vitro. Results: Ethyl acetate extract of P. tuberosa showed significant hypoglycemic effect. Twenty-five compounds were isolated from the active site, containing β-stiosterol (1), stigmasterol (2), daucosterol (3), clerosterol-stigmast-4-ene-3,6-dione (4), 22-dehydro- stigmast-4-ene-3,6-dione (5), ellagic acid (6), ethyl gallate (7), gllagic acid (8), 4-hydroxybenzoic acid (9), 3,4-diohydroxybenzoic acid (10), cinnamic acid (11), p-hydroxy-cinnamic acid (12), caffeic acid (13), 5-hydromethylfuraldehyde (14), quinic acid (15), chlorogenic acid (16), ferulic (17), 2,3-dimethoxy-5-methyl-6-(3,7,11,15,19-pentamethyl-2,6,10,14,18-eicosapentaen-1- yl)-2,5-cyclohexadiene-1,4-dione (18), 1-O-caffeoyl- quinic acid (19), 3,5-dimethoxy-4-hydroxy-benzene carbonic-1-O-β-D-glucoside (20), 2-O-butyl-α-D-fructofuranoside (21), n-octadecanoic acid (22), stearic acid (23), methyl-5-(hydroxymethyl) furan-2-carboxylate (24) and 4-hydroxy-3-methoxy-benzaldehyde(25). Nine compounds were obtained from the genus Phlomis for the first time, in which ellagic acid (6), quinic acid (15), and 1-O- caffeoylquinic acid (19) showed strong DPP-4 inhibitory activity with IC50 of 72.3, 89.2, and 103.4 μmol/L, respectively. The IC50 of the positive drug diprotin A was 50 μmol/L. Conclusion: Compounds (3-7 and 18-21) are obtained from the genus Phlomis for the first time. Compound 6, 15, and 19 show DPP-4 inhibitory activities.

Analysis on Changes of Chemical Composition Contents and Efficacy of Improving Insulin Resistance in Type 2 Diabetic Mice of Anemarrhenae Rhizoma Before and After Processing with Salt-water / 中国实验方剂学杂志

Objective:By comparing the changing of chemical composition contents and the effects of improving insulin resistance in type 2 diabetic KKAy mice， to explore the processing principle of Anemarrhenae Rhizoma processed with salt-water. Method:Ultra-performance liquid chromatography-tandem mass spectrometry （UPLC-MS） was established for determining the contents of seven saponins and mangiferin in raw and salt-processed products of Anemarrhenae Rhizoma. The mobile phase was 0.1% formic acid aqueous solution （A） and acetonitrile （B） for gradient elution （0-1 min， 90%-80%A； 1-2 min， 80%-78%A； 2-5.5 min， 78%-70%A； 5.5-10.5 min， 70%-40%A； 10.5-12 min， 40%-20%A； 12-12.1 min， 20%-90%A； 12.1-13 min， 90%A）. The flow rate was set at 0.3 mL·min-1. The mass spectrographic analysis employed electrospray ionization （ESI） and negative ion acquisition mode. The acquisition range was m/z 100-1 200. The experimental type 2 diabetic KKAy mice were divided into model group， Anemarrhenae Rhizoma group （7.2 g·kg-1·d-1） and Anemarrhenae Rhizoma processed with salt-water group （7.2 g·kg-1·d-1）. C57BL/6J mice were considered as normal group and were given the same volume of saline. There are nine mice in each group， once a day for 21 consecutive days. The fasting blood glucose （FBG） was measured once a week. Three hours after the last administration， the blood samples of mice were collected by drawing eyeballs and were centrifuged to separate serum for further experiment. The fasting insulin （FINS）， leptin （LEP）， glycated hemoglobin （HbA1c）， glycated albumin （GA）， glucagon-like peptide-1 （GLP-1） levels in serum were detected by enzyme-linked immunosorbent assay （ELISA）. The insulin sensitivity index （ISI） and the homeostasis model assessment insulin-resistance （HOMA-IR） were calculated. The expressions of phosphatidylinositol 3-kinase （PI3K）， phosphoenolpyruvate carboxylkinase （PEPCK） and peroxisome proliferator activated receptor gamma co-activator1 （PGC1） mRNA in hepatic and adipose tissue of mice from each group were detected by real-time fluorescence quantitative polymerase chain reaction method （Real-time PCR）. Result:After being processed with salt-water， the contents of 8 chemical components in Anemarrhenae Rhizoma were increased， among which the contents of timosaponin AⅢ， timosaponin BⅡ， timosaponin BⅢ， anemarrhenasaponin Ⅰ， anemarrhenasaponin Ⅰa， mangiferin were significantly increased， and increased by 43.78%， 38.77%， 25.84%， 28.21%， 22.51%， 24.04%， respectively. Compared with the model group， raw and salt-processed products of Anemarrhenae Rhizoma could significantly decrease the levels of FBG， FINS， HOMA-IR， HbA1c， LEP， GA （P<0.05， P<0.01）， increase the levels of ISI， GLP-1 （P<0.05， P<0.01） in serum of mice with type 2 diabetes， and significantly increase the expression of PI3K and PGC1 mRNA in hepatic and adipose tissue （P<0.05）. It is worth noting that salt-processed products is better than that of raw products. Conclusion:Raw and salt-processed products of Anemarrhenae Rhizoma have obvious hypoglycemic effect. And the hypoglycemic effect of Anemarrhenae Rhizoma can be promoted after being processed with salt-water by promoting insulin secretion and improving insulin resistance. Incremental components are the probably material basis for enhancement of hypoglycemic effect of Anemarrhenae Rhizoma after being processed with salt-water.

Role of semi-purified andrographolide from Andrographis paniculata extract as nano-phytovesicular carrier for enhancing oral absorption and hypoglycemic activity / 中草药·英文版

Objective: Andrographis paniculata is a well-known medicinal plant in Southeast Asia, India and China. The plant contains andrographolide (AN), a very important phytochemical used in various health problems. However, AN is low in oral absorption bioavailability of AN due to the rapid clearance and high protein binding capacity. Methods: The present study was aimed to develop a nano-phytovesicular formulation of semi-purified AN extracts from a naturally occurring phospholipid (soya phosphatidylcholine) in order to increase the oral absorption and antihyperglycemic activity in rats. Results: The nano-phyto vesicle of semi-purified AN extracts equivalent to 25 mg /kg AN significantly protected the hyperglycemic condition of rats. The in vitro and in vivo experiments results proved that the nano- phytovesicular system of plant extracts containing AN produced better oral absorption, bioavailability and improved antihyperglycemic activity compared with that of free AN at dose of 50 mg/kg. Conclusion: Hence, the prepared semi-purified extract nano-phytovesicular system is helpful in solving the problem of rapid clearance of AN.

Research progress on chemical substances in Juglans regia and current status and development approaches of industrial development / 中草药

JugLans regia is the main economic crop in China and an important medicinal plant, which have antibacterial, anti-oxidant, anti-tumor and hypoglycemic effects. It mainly contains a variety of active small molecule compounds such as polysaccharides, flavonoids, phenolic acids, esters, saponins and quinones.It can be used not only for the development of pharmaceuticals or functional foods, but also for its market demand in the food industry with good application base. It is a resource material with great development potential in walnuts. In this paper, the chemical composition and pharmacological effects of walnut were systematically combed, and on this basis, the industrial application and development path were analyzed to provide a basis for the development and utilization of walnut resources in China.

Research Progress on Effect of Hypoglycemic Mechanism of Berberine in Treatment of Type 2 Diabetes Mellitus / 中国实验方剂学杂志

In recent years, type 2 diabetes mellitus (T2DM) has an increasing incidence worldwide along with the improvement of people' s living standards, and emerged as a serious threat to human health. T2DM is a progressive metabolic disease characterized by hyperglycemia, and its routine therapies include diet control, the use of oral hypoglycemic drugs or subcutaneous injection with insulin. At present, in addition to chemical drugs, such as metformin and thiazolidinediones, researchers have also found that natural medicines and traditional Chinese medicine compounds have mild hypoglycemic and insulin sensitizing effects. Besides, these drugs also have effects in alleviating diabetes complications and maintaining glucose homeostasis. Berberine is an isoquinoline alkaloid mainly isolated from Coptis chinensis with multiple pharmacological activities. Currently, berberine is considered to be one of the most promising natural hypoglycemic agents for the treatment of type 2 diabetes mellitus. However, mechanisms of the hypoglycemic effect of berberine were complex. In this review, we summarized the pharmacological mechanisms of hypoglycemic effect of berberine, including improving insulin resistance, promoting insulin and glucagon-like peptide-1 (GLP-1) secretion, inhibiting hepatic gluconeogenesis, reducing glucose absorption in intestinal cells, suppressing oxidative stress and inflammation and modulating gut microbiota, clarified the mechanisms of hypoglycemic effect of berberine could help to understand the pharmacology of berberine in the treatment of diabetes mellitus and provided evidence for rational application of berberine in the treatment of type 2 diabetes.

Design，Synthesis and in vitro Hypoglycemic Activity Study of N-aroyl Substituted Indoline- 3-Acetic Acid Derivatives / 中国药房

OBJECTIVE： To design and synthesize N-aroyl substituted indoline-3-acetic acid derivatives and evaluate their in vitro hypoglycemic activity. METHODS： Using indoline derivative 2-[5-（benzyloxy）-1-（4-chlorobenzoyl）-2-methyl-1H-inclol-3-yl]acetic acid （GY3） as leading compound， 4-（benzyloxy）phenyl hydrazine hydrochloride and methyl 4-oxopentanoate as raw material， 8 kinds of N-aroyl （3-hydroxybenzoyl， 3-cyanobenzoyl， 4-nitrobenzoyl， 4-methylsulfonylbenzoyl， 4-acetamidobenzoyl， 3-acetylaminobenzoyl， isoniacyl and pyridine-2-formyl） substituted indoline-3-acetic acid derivatives were synthesized via 4 steps reactions： Fischer indole cyclization， reduction， amidation and hydrolyzation. The human hepatoma HepG2 cell lines were used to investigate the glucose consumption activity of the target compounds. RESULTS： Totally 8 various N-aroyl substituted indoline-3-acetic acids were synthesized and their structures were confirmed by mass spectrum（MS）， nuclear magnetic resonance 1H-NMR and 13C spectrum. Under the condition of 1.0 μmol/L， the percentage of glucose- promoting consumption of the synthesized compounds on HepG2 cells was 5.4％-9.1％. 2-[（2R， 3S）-5-benzyloxy-2-methyl-1-（4-methylsulfonyl benzoyl）-2，3-dihydro-indole-3-yl] acetic acid showed the best hypoglycemic activity. The percentage of glucose- promoting consumption was （9.1±1.81）％， which was close to that of positive control metformin [（10.58±1.68）％]， but less potent than that of leading compound GY3[（12.15±0.78）％]. CONCLUSIONS： Different electron-withdrawing substituents are introduced into N-aroyl aromatic rings of dihydroindole compounds， such as cyano， nitro， methyl sulfonyl； hypoglycemic activity decreases in varying degrees and is weaker than halogen substituents.

Prokaryotic expression and hypoglycemic activity determination of insulin G1 from Conus geographus / 生物工程学报

Rapid reduction of postprandial blood glucose is very beneficial to diabetics. In order to shorten the onset time of recombinant insulin, the cone snail insulin G1 (cI G1) of Conus geographus was studied. First, the nucleotide sequence of recombinant cone snail proinsulin G1 (cPI G1) was designed and synthesized according to the genes of human proinsulin (hPI) and cPI G1. The codon was optimized according to Escherichia coli (E. coli) codon usage frequency. Then, the plasmid pET22b(+)-cPI G1 was constructed and the recombinant cPI G1 was expressed in E. coli BL21(DE3) host strain. The recombinant cPI G1 was then purified and cleaved specially by trypsin to generate the recombinant cI G1, and its potency is 25.9 IU/mg. Fasting blood glucose test (FBGT) and oral glucose tolerance test (OGTT) suggested that the recombinant cI G1 could rapidly reduce blood glucose in normal and streptozotocin (STZ)-induced diabetic mice, but only for a short duration. This study provides a technical reference for the development of recombinant fast-acting insulin.

Hypoglycemic and antioxidant activities of Clerodendrum inerme leaf extract on streptozotocin-induced diabetic models in mice / 中草药·英文版

Objective: Recently, much attention has been paid to natural product-derived compounds for antidiabetic drug discovery. More recent studies are being focused on clarifying the bioactivity of plants and derived products. The aim of the present study was to investigate the anti-oxidant and antidiabetic activities of Clerodendrum inerme leaf extract (CILE) in streptozotocin-induced diabetic mice. Methods: C. inerme leaves were analyzed for preliminary phytochemical properties and the content of total phenolic and flavonoid were determined. In vitro anti-oxidant activity was measured using DPPH assay. Streptozotocin-induced diabetic model in mice was applied for in vivo study by the effect of CILE at two dose levels (343 and 686 mg/kg b.w.). Results: The results showed that C. inerme leaves contained the major constituents of flavonoids, alkaloids, tannins, triterpenes, and saponins. CILE exhibited the total polyphenol and flavonoid content with 120.458 mg gallic acid equivalent/g dry weight and 4.494 mg hispidulin equivalent/g dry weight, respectively. The anti-oxidant activity of CILE was expressed with IC50 = 25.28 µg/mL. CILE at the doses of 343 mg/kg and 686 mg/kg after 7 d administration exerted a decrease in plasma glucose, protected the liver, kidneys against oxidation stress via increasing glutathione content in the liver, and reduced malondialdehyde content in the liver and kidneys. Pancreatic histological analysis in diabetic mice treated with CILE also showed the pancreatic β-cells regeneration via increasing the size and number of pancreatic islets. Conclusion: These findings suggested that C. inerme leaves had potent antidiabetic and anti-oxidant activities. The results provide reliable scientific base, which is the premise for further research and development of CILE as supplements.

Chemical structures of alkaloids with hypoglycemic activity and their hypoglycemic mechanisms / 中草药

Alkaloids are a class of secondary metabolites with many structural types and significant biological activities in natural organisms. As one of the most important active ingredients in medicinal plants, they are characterized by containing nitrogen atoms in chemical structures, most of them have complex cyclic structures, possessing antitumor, antibacterial, antiviral activities, and so on. This review summarizes the structural types of hypoglycemic alkaloids and their mechanisms, which will provide new insights and references for the research on alkaloid hypoglycemic agents discovery, pharmacology, and structure-activity relationship.

Research progress of polyacetylenes from Bidens genus plants and their biological activity / 中草药

The genus Bidens (Compositae) are annual or perennial herbs distributed in tropical and subtropical regions. Many species of this genus are used in various folk medicines such as blood-pressure lowering and antihyperglycemic agents. As the characteristic components of plants in Bidens genus, polyacetylenes have attracted broad attention because of their antimalarial, hypoglycemic, antitumor and anti-inflammatory activities. In order to fully utilize the species of these medicinal plants, this paper reviewed the plant sources, type of the structure, and biological activity with view to providing the reference for the further researches and developments of polyacetylenes.

Evaluation of the toxicity and hypoglycemic effect of the aqueous extracts of Cnidoscolus quercifolius Pohl

Diabetes mellitus is one of the most common chronic degenerative diseases, and it is estimated to increase worldwide to around 415 million and to impact 642 million in 2040. Research shows that some plants are sources of bioactive compounds against diabetes. Thus, the objective of this work was to evaluate the oral toxicity and the hypoglycemic effect of the aqueous extract of the leaves of Cnidoscolus quercifolius Pohl. Diabetes was induced in Swiss mice with streptozotocin and the mice were treated with an aqueous extract of C. quercifolius leaves for a period of 30 days. Phytochemical analysis showed that the extract was rich in flavonoids, catechins and triterpenoid, which did not show any mortality and behavioral alterations in mice treated with 200, 1000, and 2000 mg/kg body weight of the extract for 14 days. Histopathological analysis of organs (kidney, pancreas, liver) from mice treated with the 2000 mg/kg extract revealed no architectural change. In the present study, we found a 29% reduction in glucose levels in animals receiving 200 mg/kg body weight. These results are very promising because they showed that C. quercifolius had a hypoglycemic effect and did not present oral toxicity, thus being a new source of compounds for the control of diabetes.

Acute and Chronic anti-hyperglycemic effect of Prosopis ruscifolia extract in Normoglycemic and Alloxan-Induced Hyperglycemic Rats.

Prosopis ruscifolia, vinal, is used to treat diabetes. This work aims to study the influence of the hydro-alcoholic extract of this plant on alloxan induced diabetic rats. Hydroalcoholic extract from aerial parts of Prosopis ruscifolia Griseb. (Fabaceae) was prepared (Pr) and the safety was assessed to determine the acute toxicity in mice. The hypoglycemic activity of the extract was evaluated in normo- and hyperglycemic rats. Hyperglycemia was induced by intravenous administration of alloxan monohydrate (32 mg/Kg body weight). Rats with blood glucose level higher than 200 mg/dL were used for the experiment. The animals were assigned to different groups and treated with a single dose of solvent (water, p.o.), Pr (100 mg/Kg, p.o.), tolbutamide (100 mg/Kg, p.o.) or insulin (5 IU/kg, i.p.); Pr extract was also administered to normoglycemic rats (100 mg/kg, p.o.). Fasted blood glucose level was measured at times 0, 1, 2, 4 and 24 h after treatment, in the acute test, and at days 0, 14, 21 and 28, in the chronic study. No evidence of acute toxicity in mice was observed. The results show that Pr extract significantly reduces blood glucose level in hyperglycemic rats (p < 0.01) 24 h after administration of a single oral dose of 100 mg/Kg. Treatment with Pr during 28 days showed a reduction in blood glucose level in experimentally hyperglycemic rats. Additionally, rats treated with the extract showed a reduced body weight gain. Prosopis ruscifolia hydroalcoholic extract showed low toxicity. After acute and chronic oral treatment was effective to reduce fasted blood glucose level, and the body weight gain was less after 28 days in the treated group.

Research progress in chemical constituents and biological activities of Armillaria mellea / 中草药

Armillaria mellea is a kind of medicinal and edible fungus belonging to Tricholomataceae family. It possesses comprehensive biological activities, such as hypnotic, sedative, improving cardiocerebral blood circulation, hypoglycemic, antioxidant, and immune regulation. Besides, it can inhibit tumor. A. mellea contains characteristic chemical constituents, such as, protoilludane sesquiterpenoid aromatic esters, diterpenoids, triterpenoids, polysaccharides, adenosine, and various types of secondary metabolites. This paper summarizes the chemical composition and biological activity of A. mellea to provide the reference for developing and utilizing it.