Progress on pharmacological activities and hepatotoxicity of bavachinin / 药学实践杂志

Bavachinin is a dihydroflavone isolated from dried ripe fruits of Psoralea corylifolia L.，which has various pharmacological activities, such as anti-tumor, anti-virus, anti-diabetes, anti-inflammatory and neuroprotective, and good potential in clinical applications. With the increasing concern about the safety of P. corylifolia applications in clinical, the bavachinin has been found to be one of the main components causing liver injury. In this paper, the pharmacological activities and hepatotoxicity of bavachinin in the recent 20 years were reviewed, in order to provide reference for the further study and clinical application.

Anti-diabetic effects of linarin from Chrysanthemi Indici Flos via AMPK activation / 中草药·英文版

Objective: The purpose of this study is to investigate the anti-diabetic effects of linarin, a flavonoid extracted from Chrysanthemi Indici Flos (CIF), and its potential mechanisms. Methods: The effects of linarin on cell viability and glucose consumption in HepG2 cells were measured. Meanwhile, monosodium glutamate (MSG) mouse model was constructed to monitor the changes of insulin tolerance, glucose tolerance, triglyceride and cholesterol. The protein expression levels of p-AMPK, p-ACC, PEPCK and p-GS were detected by Western blot. Results: Linarin could increase the relative glucose consumption of HepG2 cells, improve insulin tolerance and glucose tolerance, and decrease the levels of triglyceride and cholesterol of MSG mice. Simultaneously, the expression levels of p-AMPK and p-ACC in HepG2 cells and the liver tissue of MSG mice were increased, while the expression levels of PEPCK and p-GS were decreased after treatment with linarin. Conclusion: Insulin resistance could be ameliorated by linarin in type 2 diabetes, and its mechanism may be related to AMPK signaling pathway.

Research progress on chemical constituents of Citrullus colocynthis and their pharmacological effects / 中国中药杂志

Citrullus colocynthis is widely distributed in the desert regions of the world. C. colocynthis has shown to improve constipation, liver diseases, jaundice, typhoid fever, diabetes and asthma in traditional use. As a kind of exterritorialy medicinal material, C. colocynthis has been used in China and introduced successfully. The main active ingredients of C. colocynthis are cucurbitacin, flavonoids, alkaloids and phenolic acids, which have been proven to have antioxidant, anti-diabetic, anti-pathogenic microorganisms and anti-cancer activities in modern pharmacological research. This paper reviews the traditional application, chemical composition and pharmacological effects of C. colocynthis, and provides reference for the in-depth study for the efficacy and mechanism of different components of C. colocynthis.

Antidiabetic properties of Solanum villosum and Solanum nigrum var sarrachoides in a streptozotocin-induced diabetic mice model

Background: Diabetes mellitus (DM) poses immense challenge to the health of people worldwide. Current therapies are limited by cost and adverse effects. Solanum nigrum, a complex of many species in the family Solanaceae has been recorded to be used by many communities in the management of DM. The aim of this study was to evaluate the phytochemical, antidiabetic efficacy and safety of two species, namely; Solanum villosum and S. nigrum var sarrachoides using streptozotocin-induced diabetic mice model.Methods: Qualitative assessment for phytochemical constituents was carried out. Acute toxicity was conducted based on 慜rganisation of Economic Cooperation and Development� 2001 guidelines. Diabetes was induced by injection of streptozotocin at a dose of 200 mg/kg body weight intraperitoneal after the mice fasted for 8 hours. Aqueous extracts were administered orally using an oral gavage at doses of 150, and 300 mg/kg body weight for each plant daily and monitored weekly for 28 days.Results: Both plants contain vital phytochemicals. Flavonoids, alkaloids, tannins, saponins, phenols, and glycosides were present in both plants. However, phytosterols and coumarins were absent in S. villosum. Additionally, both plants did not show toxicity. Both plants showed efficacy with S. nigrum var sarrachoides being more potent at both doses.Conclusions: The study validates the use of these plants by herbalists and recommends further studies on them with the aim of elucidating the active compounds that can be used as novel therapies for diabetes. Additionally, the study recommends the evaluation of other species in this complex for antidiabetic properties.

Anti-diabetic Activity of Convallatoxin Isolated from the Root Bark of Parquetina nigrescens (Afzel.) Bullock (Asclepiadaceae)

This study investigated the anti-diabetic activity of the root bark extract of Parquetina nigrescens and the isolated compound, convallatoxin, from the root bark. A powdered sample of the plant was extracted with methanol, and the extract (A) was tested in glucose-loaded normal rats at 100, 200 and 400 mg/kg for the determination of the most active dose. The anti-diabetic activity of A at 200 mg/kg was carried out on streptozotocin-induced diabetic rats. A was further partitioned to obtain its n-hexane (B1), dichloromethane (B2), ethyl acetate (B3) and mother liquor (B4) fractions that were tested for blood glucose lowering activity using glucose-loaded normal rats model. The anti-diabetic activity of the isolated compound from B3 was carried out on streptozotocin-induced diabetic rats. The results were subjected to one way ANOVA followed by Bonferroni post hoc tests and p< 0.05 was considered significant. A showed dose-independent and time dependent blood glucose level reduction activity at 200 mg/kg with the highest percentage of 30% at 4 h that was comparable to the standard, glibenclamide at 5 mg/kg. A at 200 mg/kg showed a blood glucose level reduction of 49, 68 and 70% by Day 4, 7 and 10 respectively as against glibenclamide at 5 mg/kg of 18, 33 and 39% by Day 4, 7 and 10 respectively on streptozotocin-induced diabetic rats. B3 showed a time-dependent blood glucose level reduction activity up to the fourth hour similar to glibenclamide with 35% as against 38% of glibenclamide. B1, B2 and B4 were devoid of blood glucose level reduction activity. Convallatoxin isolated from B3 gave 83 % blood glucose levels reduction at day 10 as against 38% of glibenclamide. The anti-diabetic activity of convallatoxin was significantly (p<0.05) more than glibenclamide at all-time point. The structure of convallatoxin was determined using IR, 1D and 2D NMR spectroscopy and the spectroscopic data compared well with published data in the literature.

Role of brown adipose tissue in metabolic syndrome, aging, and cancer cachexia / 医学前沿

Brown adipose tissue (BAT) plays a fundamental role in maintaining body temperature by producing heat. BAT that had been know to exist only in mammals and the human neonate has received great attention for the treatment of obesity and diabetes due to its important function in energy metabolism, ever since it is recently reported that human adults have functional BAT. In addition, beige adipocytes, brown adipocytes in white adipose tissue (WAT), have also been shown to take part in whole body metabolism. Multiple lines of evidence demonstrated that transplantation or activation of BAT or/and beige adipocytes reversed obesity and improved insulin sensitivity. Furthermore, many genes involved in BATactivation and/or the recruitment of beige cells have been found, thereby providing new promising strategies for future clinical application of BAT activation to treat obesity and metabolic diseases. This review focuses on recent advances of BAT function in the metabolic aspect and the relationship between BAT and cancer cachexia, a pathological process accompanied with decreased body weight and increased energy expenditure in cancer patients. The underlying possible mechanisms to reduce BAT mass and its activity in the elderly are also discussed.

Synthesis and preliminary anti-diabetic activity evaluation of novel PEGylated GLP-1 receptor agonists / 中国药科大学学报

@#In order to obtain glucagon-like peptide-1(GLP-1)analogs which can sustainedly control the levels of glucose, 12 derivatives were designed and synthesized by coupling monomethoxy polyethylene glycol(mPEG, with average molecular weights of 350, 550 and 750)to GLP-1 analogs. Preliminary pharmacological activities showed that all compounds retained GLP-1 receptor agonist activities, and the hypoglycemic activity of compound I-12 was similar to those of Ex-4 and Liraglutide, suggesting I-12 could be a potential long-acting GLP-1 receptor agonist.

Progress in Research on Physiological Activity of 1-Deoxynojirimycin and Its Derivatives / 中国药学杂志

1-Deoxynojirimycin(DNJ), a polyhydroxylated alkaloid,has demonstrated numerous physiological activites, such as anti-diabetes, lipid-lowering, anti-cancer and anti-virus effects. As research continues, related activities have been explained even more clearly, and new physiological activities have been found. In this review, new discoveries of the physiological activities of DNJ and DNJ derivatives were summarized. This will provide pharmaceutical basis for future study and application of DNJ.

Progress of bioactivities other than antibacterial of β-lactam derivatives / 中国生化药物杂志

β-lactam compounds exhibit good antibacterial activity, which aroused widespread attention.Recently, the researches on the biological activities of beta-lactam derivatives have made great development.In this paper, we will review the recent research progress of β-lactam derivatives in the field of anti-tumor, anti-HIV, anti-tuberculosis, anti-parasitic, anti-diabetes, antithrombotic, plasma lipids regulation and treatment on nervous system diseases.

Antidiabetic and Beta Cell-Protection Activities of Purple Corn Anthocyanins

Antidiabetic and beta cell-protection activities of purple corn anthocyanins (PCA) were examined in pancreatic beta cell culture and db/db mice. Only PCA among several plant anthocyanins and polyphenols showed insulin secretion activity in culture of HIT-T15 cells. PCA had excellent antihyperglycemic activity (in terms of blood glucose level and OGTT) and HbA1c-decreasing activity when compared with glimepiride, a sulfonylurea in db/db mice. In addition, PCA showed efficient protection activity of pancreatic beta cell from cell death in HIT-T15 cell culture and db/db mice. The result showed that PCA had antidiabetic and beta cell-protection activities in pancreatic beta cell culture and db/db mice.

Chemical constituents and pharmacologic actions of Cynomorium plants / 中国天然药物

The stem of Cynomorium songaricum is a traditional Chinese medicine reputed to have tonic effects. C. coccineum growing in northern Africa and the Mediterranean region is regarded in Arabian medical practice as the "treasure of drugs". The major constituents of Cynomorium plants have been revealed to be phenolic compounds, steroids, triterpenes, etc. Pharmacologic studies showed that the Cynomorium plants had antioxidant, immunity-improving, anti-diabetic, neuroprotective, and other bioactivities. Some chemical constituents in Cynomorium plants are unstable, implying that the chemical components of the herbal medicines produced under different conditions may be variable. This review covers the literature published until December, 2011 and describes the pharmacologic effects and secondary metabolites of Cynomorium species.

Bioactivities Evaluation of Indonesian Mistletoes (Dendrophthoe pentandra (L.) Miq.) Leaves Extracts.

Mistletoes or benalu in bahasa Indonesia is a semi-parasitic plant that also known as medicinal plant. It used in traditional/alternative medicine such as for for cough, diabetes, hypertension, cancer, diuretic, smallpox, ulcer, skin infection and after child-birth treatment. There are many species of mistletoes in Indonesia. Dendrophthoe pentandra (L.) Miq. is one of the Indonesian mistletoes species that commonly found grew on many different species of host plant. In this paper we reported in vitro toxicity, antioxidant and antidiabetes activities of MeOH and water extracts of D. pentandra grew on four different host plants (Stelechocarpus burahol, Spondias dulcis, Annona squamosa and Camellia sinensis). Toxicity was measured using brine shrimp lethality test (BSLT). Antioxidant activity was measured using DPPH free radical scavenging assay. Antidiabetes activity was measured using -glucosidase inhibitor assay. The results show that all mistletoes extracts tested (MeOH and water extracts) were non-toxic and show significant antidiabetes activity, whereas for antioxidant activity, only MeOH extracts show significant activity. Therefore, it is suggest that D. pentandra extracts are potential source for natural antioxidant and antidiabetes compounds.

Dipeptidyl peptidase IV inhibitors: A new class of oral agents for treatment of type 2 diabetes mellitus / 国际药学研究杂志

Glucagon-like peptide-1 (GLP-1), one kind of incretins, contributes to control blood glucose level with several routines. It can be degraded rapidly by the enzyme dipeptidyl peptidase IV (DPP-IV). DPP-IV inhibitors augment glucose homeostasis by preventing degradation of GLP-1, which can stimulate insulin secretion, inhibit glucagon secretion, increase satiety, and slow gastric emptying. They are weight neutral, and are associated with low risk of hypoglycemia. This review highlights the characteristics of GLP-1, clinical efficacy, pharmacokinetics and adverse reactions of DPP-IV inhibitors.