Opportunities and challenges of incretin-based hypoglycemic agents treating type 2 diabetes mellitus from the perspective of physiological disposition

The treatment of patients with diabetes mellitus, which is characterized by defective insulin secretion and/or the inability of tissues to respond to insulin, has been studied for decades. Many studies have focused on the use of incretin-based hypoglycemic agents in treating type 2 diabetes mellitus(T2DM). These drugs are classified as GLP-1 receptor agonists, which mimic the function of GLP-1,and DPP-4 inhibitors, which avoid GLP-1 degradation. Many incretin-based hypoglycemic agents have been approved and are widely used, and their physiological disposition and structural characteristics are crucial in the discovery of more effective drugs and provide guidance for clinical treatment of T2DM.Here, we summarize the functional mechanisms and other information of the drugs that are currently approved or under research for T2DM treatment. In addition, their physiological disposition, including metabolism, excretion, and potential drug drug interactions, is thoroughly reviewed. We also discuss similarities and differences in metabolism and excretion between GLP-1 receptor agonists and DPP-4 inhibitors. This review may facilitate clinical decision making based on patients' physical conditions and the avoidance of drug drug interactions. Moreover, the identification and development of novel drugs with appropriate physiological dispositions might be inspired.

Effect of Yanggyuksanhwa-Tang on Non-Insulin-Dependent Diabetes Mellitus Unresponsive to Oral Hypoglycemic Agents:A Case Report

Diabetes mellitus is the fourth leading cause of death worldwide, following cancer, cerebrovascular disease, and heart disease. It is triggered by hyperglycemia and other metabolic disorders. Diabetes is a complex endocrine disease that causes chronic vascular complications such as diabetic nephropathy, retinopathy, and polyneuropathy.

A Preliminary Investigation of the Possible Hypoglycemic Activity of Hibiscus rosa-sinensis

The hypoglycemic activity of an ethanol extract of Hibiscus rosa-sinsnsis was studied in glucose located rats. Afer a single dose of the extract, a slight but insignificant hypoglycemic effect was observed at 30 and 90 min. At 120 min it was mild but significant. After repeated administration of the extract (once a day for seven consecutive days) a statistically significant (P < 0 .001 ) reduction in blood glucose levels was observed at 30, 90 and 120 min after glucose loading. The average hypoglycemic activity, after repeated administration of 250 mg kg-1 leaf extract was 81 %, under similar conditions average activity of tolbutamide was 96%. At 250 mg·kg-1 the efficacy of the extract was found to be 84% of tolbutawhde (100mg·kg- 1 ). Repeated treatment of animals either with tolbutandde a sulphonylurea or H. rosa-sinensis caused a 2-3-fold improvement in glucose tolerance as compared to those receiving only once. These data suggest that the leaf extract acts like tolbutamide and the meehanism of action may be a stimulation of pancreatic hata cells to produce more insulin or an increase of the glycogen deposition in liver. It appeare that the active principle in the tested extract has the sulphonylurea Skeleton in which -SO2-NH-CO- group and the substituents (S1 and S2) may be the possible active sites responsible for its hypolycemic activity.

Hypoglycemic Therapy in Chronic Hepatic Disease Literature Review

Chronic liver disease (CLD) refers to a structural and functional change of the liver, which modifies the pharmacokinetics of multiple drugs, including hypoglycemic agents. This alteration depends on the severity degree of the liver disease, clinical characteristics of the patient, and comorbidities presence such as kidney disease and drug biochemistry. Insulin is considered a safe therapeutic strategy in patients with CLD, however, for many oral hypoglycemic agents, its use and dose adjustment will depend on the Child-Pugh score, based on the risk of hypoglycemia in this type of patient.

Cloning of cytochrome P-450 2C9 cDNA from human liver and its expression in CHL cells

AIM: Using bacterial, yeast, or mammalian cell expressing a human drug metabolism enzyme would seem good way to study drug metabolism-related problems. Human cytochrome P-450 2C9(CYP2C9) is a polymorphic enzyme responsible for the metabolism of a large number of clinically important drugs. It ranks among the most important drug metabolizing enzymes in humans. In order to provide a sufficient amount of the enzyme for drug metabolic research, the CYP2C9 cDNA was cloned and expressed stably in CHL cells. METHODS: After extraction of total RNA from human liver tissue, the human CYP2C9 cDNA was amplified with reverse transcription-polymerase chain reaction (RT-PCR), and cloned into cloning vector pGEM-T. The cDNA fragment was identified by DNA sequencing and subcloned into a mammalian expression vector pREP9. A transgenic cell line was established by transfecting the recombinant vector of pREP9-CYP2C9 into CHL cells. The enzyme activity of CYP2C9 catalyzing oxidation of tolbutamide to hydroxy tolbutamide in S9 fraction of the cell was determined by high performance liquid chromatography(HPLC). RESULTS: The amino acid sequence predicted from the cDNA segment was identical to that of CYP2C9*1, the wild type CYP2C9. However, there were two base differences, i.e. 21T】C, 1146C】T, but the encoding amino acid sequence was the same, L7, P382. The S9 fraction of the established cell line metabolizes tolbutamide to hydroxy tolbutamide; tolbutamide hydroxylase activity was found to be 0.465 +/- 0.109 micromol.min(-1).g(-1) S9 protein or 8.62 +/- 2.02mol.min(-1).mol(-1) CYP, but was undetectable in parental CHL cell. CONCLUSION: The cDNA of human CYP2C9 was successfully cloned and a cell line of CHL- CYP2C9, efficiently expressing the protein of CYP2C9, was established.

Alzheimer’s disease and type 2 diabetes mellitus:Pathophysiologic and pharmacotherapeutics links

At present,Alzheimer’s disease(AD)and type 2 diabetes mellitus(T2DM)are two highly prevalent disorders worldwide,especially among elderly individuals.T2DM appears to be associated with cognitive dysfunction,with a higher risk of developing neurocognitive disorders,including AD.These diseases have been observed to share various pathophysiological mechanisms,including alterations in insulin signaling,defects in glucose transporters(GLUTs),and mitochondrial dysfunctions in the brain.Therefore,the aim of this review is to summarize the current knowledge regarding the molecular mechanisms implicated in the association of these pathologies as well as recent therapeutic alternatives.In this context,the hyperphosphorylation of tau and the formation of neurofibrillary tangles have been associated with the dysfunction of the phosphatidylinositol 3-kinase and mitogen-activated protein kinase pathways in the nervous tissues as well as the decrease in the expression of GLUT-1 and GLUT-3 in the different areas of the brain,increase in reactive oxygen species,and production of mitochondrial alterations that occur in T2DM.These findings have contributed to the implementation of overlapping pharmacological interventions based on the use of insulin and antidiabetic drugs,or,more recently,azeliragon,amylin,among others,which have shown possible beneficial effects in diabetic patients diagnosed with AD.

Inhibitory effect and mechanism of acarbose combined with gymnemic acid on maltose absorption in rat intestine

AIM: To compare the combinative and individual effect of acarbose and gymnemic acid (GA) on maltose absorption and hydrolysis in small intestine to determine whether nutrient control in diabetic care can be improved by combination of them. METHODS: The absorption and hydrolysis of maltose were studied by cyclic perfusion of intestinal loops in situ and motility of the intestine was recorded with the intestinal ring in vitro using Wistar rats. RESULTS: The total inhibitory rate of maltose absorption was improved by the combination of GA (0.1g/L-1.0 g/L) and acarbose (0.1 mmol/L-2.0 mmol/L) throughout their effective duration (P 【0.05, U test of Mann-Whitney), although the improvement only could be seen at a low dosage during the first hour. With the combination, inhibitory duration of acarbose on maltose absorption was prolonged to 3h and the inhibitory effect onset of GA was fastened to 15 min. GA suppressed the intestinal mobility with a good correlation (r = 0.98) to the inhibitory effect of GA on maltose absorption and the inhibitory effect of 2 mmol/L (high dose) acarbose on maltose hydrolysis was dual modulated by 1g/L GA in vivo indicating that the combined effects involved the functional alteration of intestinal barriers. CONCLUSION: There are augmented effects of acarbose and GA,which involve pre-cellular and paracellular barriers. Diabetic care can be improved by employing the combination.

Insulin is necessary for the hypertrophic effect of cholecystokinin-octapeptide following acute necrotizing experimental pancreatitis

AIM:In previous experiments we have demonstrated that by administering low doses of cholecystokinin-octapeptide (CCK-8),the process of regeneration following L-arginine (Arg)-induced pancreatitis is accelerated.In rats that were also diabetic(induced by streptozotocin,STZ),pancreatic regeneration was not observed.The aim of this study was to deduce whether the administration of exogenous insulin could in fact restore the hypertrophic effect of CCK-8 in diabetic-pancreatitic rats. METHODS:Male Wistar rats were used for the experiments. Diabetes mellitus was induced by administering 60mg/kg body mass of STZ intraperitoneally(i.p.),then,on d 8, pancreatitis was induced by 200mg/100 g body mass Arg i.p.twice at an interval of 1 h.The animals were injected subcutaneously twice daily(at 7 a.m.and 7 p.m.)with 1 μg/kg of CCK-8 and/or 2 IU mixed insulin(300g/L short- action and 700g/L intermediate-action insulin) for 14 d after pancreatitis induction.Following this the animals were killed and the serum amylase,glucose and insulin levels as well as the plasma glucagon levels,the pancreatic mass/body mass ratio(pm/bm),the pancreatic contents of DNA,protein,amylase,lipase and trypsinogen were measured.Pancreatic tissue samples were examined by light microscopy on paraffin-embedded sections. RESULTS:In the diabetic-pancreatitic rats treatment with insulin and CCK-8 significantly elevated pw/bm and the pancreatic contents of protein,amylase and lipase vs the rats receiving only CCK-8 treatment.CCK-8 administered in combination with insulin also elevated the number of acinar cells with mitotic activities,whereas CCK-8 alone had no effect on laboratory parameters or the mitotic activities in diabetic-pancreatitic rats. CONCLUSION:Despite the hypertrophic effect of CCK-8 being absent following acute pancreatitis in diabetic-rats, the simultaneous administration of exogenous insulin restored this effect.Our results clearly demonstrate that insulin is necessary for the hypertrophic effect of low-doses of CCK-8 following acute pancreatitis.

Seventy-two Cases of Antidiabetic-Induced Hepatopathy Treated by Huatan Yigan Decoction

In order to observe the therapeutic effects of Huatan Yigan Decoction (化痰益肝汤 Decoction for resolving phlegm and replenishing the liver) on antidiabetic-induced hepatopathy, 129 cases were divided into two groups, 72 cases in the treatment group were administrated with Huatan Yigan Decoction and 57 cases in the control group with the liver-protecting drugs. Their liver function, plasma prothrombin time (PT), blood urea nitrogen and symptoms of the patients before and after treatment were observed during the three therapeutic courses. Results: The total effective rate and cured rate of the treatment group manifested an obvious difference in comparison with those of the control group (P＜0.05 or P＜0.01). Even though the liver function, blood urea nitrogen (BUN) and symptoms in both groups were improved markedly, these indicators in the treatment group were improved more markedly than those in control group (P＜0.01). No adverse effect was found during the treatment. Conclusion: Huatan Yigan Decoction shows a repair action on hepatic injury.

A Clinical Investigation on Garlicin Injectio for Treatment of Unstable Angina Pectoris and Its Actions on Plasma Endothelin and Blood Sugar Levels

To investigate the therapeutic effects and mechanisms of garlicin for treatment of unstable angina pectoris (UAP), garlicin injectio was intravenously dripped 60 mg/day in 34 cases for 10 days. Nitroglycerine was used in 21 cases of the control group. The results showed that the total effective rates in improving symptoms and electrocardiogram after garlicin treatment were respectively 82% and 62%, and that the plasma endothelin and blood sugar levels were markedly lowered in cases with hyperglycemia.

Influencing factors of rat small intestinal epithelial cell cultivation and effects of radiation on cell proliferation

INTRODUCTIONCrypt epithelial cells in normal small intestineproliferate at a high speed. But they are verydifficult to culture in vitro and passage stably. A lotof studies have been done[1-16]. Some domestic labsisolated and cultured crypt cells from embryonalintestines and aseptic animal intestine, but failed.We introduced normal rat epithelial cell line-IEC-6from the USA and its living condition for stablepassage was successfully established after trials. Thecell line was testified to be the small intestinalepithelial cell by electron microscopy,immunihistochemistry and enzymatic histoch-emistry. It has been applied to some relatedresearch work[17-21]. It was found that manyfactors were involved in the culture system. Ourpresent study focuses on the culture method and theinfluencing factors on IEC-6.

Clinical effects of antidiabetic drugs on psoriasis:The perspective of evidence-based medicine

Psoriasis and diabetes shared common underlying pathophysiological mechanisms.Emerging data suggested that antidiabetic medications may improve the psoriasis severity in patients with diabetes mellitus.Several hypoglycemic agents including thiazolidinediones,glucagon-like peptide-1 receptor agonists,dipeptidyl peptidase-4 inhibitors,and biguanides have been reported to make a remarkable reduction in the Psoriasis Area and Severity Index score from baseline.This antipsoriatic effect could be mediated not only by the glucoselowering action of these agents but also via inhibition of keratinocyte over proliferation,increase expression of differentiation markers,suppression the immune inflammatory pathway,and blocking the calcium channels and mitogen-activated protein kinase signaling pathways.On the other hand,there was no significant increase in adverse reactions associated with the treatment of pioglitazone or metformin.However,previous studies often had the relatively short duration of the trials,and did not have enough power to assess recurrence of psoriasis.Potential bias in the study and missing data could undermine the reliability of the results.Therefore,the appropriately randomized controlled studies with large sample sizes and long-term durations in various psoriasis patients are warranted for further support.

Effectiveness and safety of human umbilical cord-mesenchymal stem cells for treating type 2 diabetes mellitus

BACKGROUND Progressive pancreaticβ-cell dysfunction is a fundamental part of the pathology of type 2 diabetes mellitus(T2DM).Cellular therapies offer novel opportunities for the treatment of T2DM to improve the function of isletβ-cells.AIM To evaluate the effectiveness and safety of human umbilical cord-mesenchymal stem cell(hUC-MSC)infusion in T2DM treatment.METHODS Sixteen patients were enrolled and received 1×10^(6) cells/kg per week for 3 wk as intravenous hUC-MSC infusion.The effectiveness was evaluated by assessing fasting blood glucose,C-peptide,normal glycosylated hemoglobin A1c(HbA1c),insulin resistance index(homeostatic model assessment for insulin resistance),and isletβ-cell function(homeostasis model assessment ofβ-cell function).The dosage of hypoglycemic agents and safety were evaluated by monitoring the occurrence of any adverse events(AEs).RESULTS During the entire intervention period,the fasting plasma glucose level was significantly reduced[baseline:9.3400(8.3575,11.7725),day 14±3:6.5200(5.2200,8.6900);P<0.01].The HbA1c level was significantly reduced on day 84±3[baseline:7.8000(7.5250,8.6750),day 84±3:7.150(6.600,7.925);P<0.01].The patients’isletβ-cell function was significantly improved on day 28±3 of intervention[baseline:29.90(16.43,37.40),day 28±3:40.97(19.27,56.36);P<0.01].The dosage of hypoglycemic agents was reduced in all patients,of whom 6(50%)had a decrement of more than 50%and 1(6.25%)discontinued the hypoglycemic agents.Four patients had transient fever,which occurred within 24 h after the second or third infusion.One patient(2.08%)had asymptomatic nocturnal hypoglycemia after infusion on day 28±3.No liver damage or other side effects were reported.CONCLUSION The results of this study suggest that hUC-MSC infusion can improve glycemia,restore isletβ-cell function,and reduce the dosage of hypoglycemic agents without serious AEs.Thus,hUC-MSC infusion may be a novel option for the treatment of T2DM.

A comprehensive review on pharmacognosy, phytochemistry and pharmacological activities of 8 potent Prunus species of southeast Asia

Genus Prunus comprising around 430 species is a vast important genus of family Rosaceae, subfamily amygdalaoidae. Among all 430 species, around 19 important species are commonly found in Indian subcontinent due to their broad nutritional and economic importance. Some most common species of genus Prunus are Prunus amygdalus, Prunus persica, Prunus armeniaca, Prunus avium, Prunus cerasus, Prunus cerasoides, Prunus domestica, Prunus mahaleb, etc. A newly introduced species of Prunus i.e Prunus sunhangii is recently discovered which is morphologically very similar to Prunus cerasoides. Plants of Prunus species are short to medium-sized deciduous trees mainly found in the northern hemisphere. In India and its subcontinent,it extends from the Himalayas to Sikkim, Meghalaya,Bhutan, Myanmar etc. Different Prunus species have been extensively studied for their morphological,microscopic, pharmacological and phytoconstituents characteristics. Total phenolic content of Prunus species explains the presence of phenols in high quantity and pharmacological activity due to phenols. Phytochemical screening of species of genus Prunus shows the presence of wide phytoconstituents which contributes in their pharmacological significance and reveals the therapeutic potential and traditional medicinal significance of this genus. Genus Prunus showed a potent antioxidant activity analyzed by 1,1-diphenyl-2-picryl-hydrazyl radical assay. Plant species belonging to the genus Prunus is widely used traditionally for the treatment of various disorders. Some specific Prunus species possess potent anticancer, anti-inflammatory,hypoglycemic etc. activity which makes the genus more interesting for further research and findings. This review is an attempt to summarize the comprehensive study of Prunus species from its distribution, morphological characters to phytoconstituents, and pharmacological activity.

Pipeline of New Drug Treatment for Non-alcoholic Fatty Liver Disease/Metabolic Dysfunction-associated Steatotic Liver Disease

Given the global prevalence and rising incidence of metabolic dysfunction-associated steatotic liver disease(MASLD),the absence of licensed medications is striking.A deeper understanding of the heterogeneous nature of MASLD has recently contributed to the discovery of novel groups of agents and the potential repurposing of currently available medications.MASLD therapies center on four major pathways.Considering the close relationship between MASLD and type 2 diabetes,the first approach involves antidiabetic medications,including incretins,thiazolidinedione insulin sensitizers,and sodium-glucose cotransporter 2 inhibitors.The second approach targets hepatic lipid accumulation and the resultant metabolic stress.Agents in this group include peroxisome proliferatoractivated receptor agonists(e.g.,pioglitazone,elafibranor,saroglitazar),bile acid-farnesoid X receptor axis regulators(obeticholic acid),de novo lipogenesis inhibitors(aramchol,NDI-010976),and fibroblast growth factor 21/19 analogs.The third approach focuses on targeting oxidative stress,inflammation,and fibrosis.Agents in this group include antioxi-dants(vitamin E),tumor necrosis factor a pathway regulators(emricasan,pentoxifylline,ZSP1601),and immune modulators(cenicriviroc,belapectin).The final group targets the gut(IMM-124e,solithromycin).Combination therapies targeting different pathogenetic pathways may provide an alternative to MASLD treatment with higher efficacy and fewer side effects.This review aimed to provide an update on these medications.

Hypoglycemic and hypolipidemic effects of rutin on hyperglycemic rats

OBJECTIVE:To study the effects of rutin on serum glucose and lipid levels in hyperglycemic rats.METHODS:Male Wistar rats were subjected to intraperitoneal streptozotocin injections and a high-sugar,high-fat diet to establish a hyperglycemic and hyperlipidemic model.The model was considered to be successfully established in rats with fasting blood sugar(FBS)≥11.1 mmol/L.The study included 6 groups with 10 rats each:a blank control group,a model group,a metformin group,and groups on large,medium and small doses of rutin.The groups received intraperitoneal streptozotocin or normal saline for 21 d.FBS,serum lipids,serum insulin,insulin sensitivity index(ISI),and levels of catalase(CAT),glutathione peroxidase(GSH-Px),superoxide dismutase(SOD)and malondialdehyde(MDA)levels were evaluated in all rats.Pancreatic tissue samples were harvested to observe structural changes in islet cells.RESULTS:Large,medium,and small doses of rutin were associated with significantly reduced FBS(P<0.05),and increased levels of ISI,CAT,GSH-Px and SOD,as well as decreased MDA(P<0.05).Rutin administration was also related with reduced total cholesterol,triglycerides and low density lipoprotein chesterol,as well as increased high density lipoprotein chesterol(P<0.05).Histologic evaluation revealed rutin induced repair of damaged islet cells.CONCLUSION:In diabetic rat models,rutin can significantly reduce FBS and blood lipids,improve anti-oxidant activity,increase insulin sensitivity,and induce repair of damaged islet cells.

Ethnobotanical survey of medicinal plants used in the management of cancer and diabetes

OBJECTIVE:To conduct an ethnobotanical survey and document the traditional anticancer and antidiabetic plants used by the local tribes of Mizoram,Northeast India.METHODS:A systematic survey was conducted in rural and urban areas of Mizoram by interviewing traditional practitioners,and cancer and diabetes patients.A detailed literature search was carried out using MEDLINE and SCOPUS and available literatures were selected and included in the study.The use value(UV)of the selected plants was calculated based on the number of citations per species given by informants.RESULTS:Data was obtained for 201 traditional medicinal plants from Mizoram,Northeast India.These plants were from 72 different families and belonged to 140 genera.Of these,103 plants were reported for the first time as possessing either anticancer or antidiabetic potential,and 105 plants were identified that were used for the treatment of both diseases.Three plants(Phlogacanthus thysiformis,Solanum gilo and Lobelia angulata)with antidiabetic potential,and six plants(Dillenia scabrella,Circium sinesis,Eupatorium nodiflorum,Pratia begonifolia,Vernonia teres and Plantago erosa)with both as anticancer and antidiabetic potential were documented for the first time.CONCLUSION:In this study,we documented several explored and unexplored medicinal plants that may be useful for the management of cancer and diabetes.This study suggests that there is a broad scope fordeveloping potent anticancer and antidiabetic agent from the flora of Mizoram,Northeast India.

Efficacy and Safety of Berberine in Patients with Type 2 Diabetes Mellitus: A Meta-Analysis

Objective To assess the efficacy and safety of berberine（BBR） in patients with type 2 diabetes mellitus（T2DM） by performing a systematic review. Methods PubM ed, Cochrane Library, Embase, CNKI, and CBM were searched until May 2014. The randomized controlled trials（RCTs） of the effects of BBR on blood glucose in patients with T2 DM were included. The quality of RCTs was assessed by the Jadad scale, and the Review Manager 5.1 software was used for data syntheses and analyses. Results Seventeen RCTs involving 1198 patients were included. The methodological quality of these RCTs was generally low. Compared with the control groups（placebo or no intervention with medicine）, BBR suggested the statistically significant benefits in improving fasting blood glucose（FBG）, postprandial blood glucose（PBG）, glycosylated hemoglobin, and homeostasis model assessment of insulin resistance. Subgroups analysis of BBR compared with metformin（MET） showed that 1.5g/d MET was significantly better than BBR（0.9-1.5 g/d） in lowering FBG and PBG. However, there was no significant difference between 1.5g/d BBR and 0.75g/d MET groups in blood glucose profiles. In comparison with rosiglitazone, BBR suggested the statistically significant benefits in lowering FBG. And there was no significant difference between BBR and glipizide groups in blood glucose profiles. In addition, the combination therapy of BBR and oral hypoglycemic agents had the advantages over oral hypoglycemic agents alone. No serious adverse effects of BBR have been reported. Conclusion BBR may have the beneficial effects in the control of blood glucose levels, though the efficacy of BBR is not superior to MET. BBR appeares to have advantages over rosiglitazone in improving FBG levels. In addition, the combination therapy of BBR and oral hypoglycemic agents may be a new attempt. However, the efficacy of BBR in patients with T2 DM should be further evaluated by more RCTs in a larger population of patients.

Detailed approach toward the anti-hyperglycemic potential of Sterculia diversifolia G.Don against alloxan-induced in vivo hyperglycemia model

OBJECTIVE:To investigate Sterculia diversifolia G.Don for potential anti-diabetic activity in the in vivo mouse model of alloxan-induced hyperglycemia.METHODS:Sterculia diversifolia(S.diversifolia)was subjected to extraction and isolation techniques and structural characterization of the isolated compounds were performed using spectroscopic methods.The acute toxicity test was performed by orally administering S.diversifolia in doses of 500-2000 mg/kg.For the assessment of anti-hyperglycemic activity,S.diversifolia bark and leaves extracts were administered orally in doses of 50,100,and 200 mg/kg,along with metformin(150 mg/kg,i.p)as positive control,after confirmation of alloxan(150 mg/kg,i.p.)induced hyperglycemia in BALB/c mice.Serum biochemical parameters were monitored for the period of study.RESULTS:The phytochemical studies showed the presence of quercetin and kaempferol in S.diversifolia.The IC50 values in the in vivo acute toxicity study revealed the safety margin of S.diversifolia bark(1166.66 mg/kg)and leaves(683.34 mg/kg)extracts.A significant attenuation of alloxan induced hyperglycemia was produced by S.diversifolia extracts at 50 mg/kg(P<0.05),100 mg/kg(P<0.05,<0.01),and 150 mg/kg(P<0.05,<0.01,<0.001)during 1-4 h,which was comparable to metformin(P<0.001).Significant(P<0.001)improvement appeared in blood hemoglobin,protein,cholesterol,triglycerides,urea,creatinine,HDL,and LDL of the stem bark and leaves extracts treated diabetic mice.CONCLUSION:These findings connote the usefulness of S.diversifolia as an anti-diabetic in traditional medicine and this might be attributed to the presence of quercetin and kaempferol,among other phytochemicals.

In-vitro and in-vivo pharmacological screening of Iris albicans

OBJECTIVE:To evaluate the anti-oxidant,enzyme inhibition,anti-pyretic,anti-inflammatory and anti-diabetic activities of Iris albicans.METHODS:Anti-oxidant assay was evaluated using DPPH(2,2-diphenyl-1-picrylhydrazyl)radical scavenging and ABTS(2,2'-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid)inhibitory protocol while enzyme inhibitory assay was evaluated by lipoxygenase and cyclooxygenase-2 inhibitory protocol respectively.Antipyretic,anti-inflammatory and anti-diabetic potential was evaluated using brewer's yeast induced pyrexia,carrageenan induced paw edema and streptozocin induced diabetes protocols respectively.Serum biochemical parameters were monitored for the period of study.RESULTS:The anti-oxidant activity of chloroform fraction of Iris albicans showed the highest scavenging potential against DPPH and ABTS while the maximum inhibitory action recorded against lipo-oxygenase and cyclooxygenase-2 enzymes was shown by n-hexane and chloroform fractions respectively.The anti-pyretic potential of the crude methanolic extract showed dose dependent activity in reducing pyrexia,thereby when the dose was increased the anti-pyretic effect was also enhanced.The anti-inflammatory action of the crude methanolic extract administered at the dose of 300 mg/kg was significant at 1 h after its administration,which was found maintained up to 5 h.Similarly the anti-diabetic effect of the crude methanolic extract administered at the dose of 200 and 300 mg/kg was noted highly significant at day 6 and was found well maintained throughout the study time period up to 10 days.Significant(P<0.001)improvement appeared in hemoglobin,protein,cholesterol,triglycerides,urea,creatinine,HDL and LDL of extract treated diabetic mice.CONCLUSION:From this data it could be concluded that Iris albicans have significant anti-oxidant,enzyme inhibition,ant-pyretic,anti-inflammatory and anti-diabetic potential.