Evaluation of pancreatic regeneration activity of Tephrosia purpurea leaves in rats with streptozotocin-induced diabetes.

BACKGROUND AND AIM: Flavonoid rich plant Tephrosia purpurea (T. purpurea), commonly known as Sarpunkha has been used in traditional systems of medicine to treat diabetes mellitus. However, its effectiveness in promoting regeneration of pancreas in diabetes has not been investigated. Therefore, the present study was undertaken to evaluate pancreatic ß-cells regeneration, antioxidant and antihyperlipidemic potentials of T. purpurea leaves extract, its fractions and main constituent Rutin in diabetic rats. EXPERIMENTAL PROCEDURE: The leaves extract and its fractions were first screened for acute and sub-chronic antidiabetic activity in a dose range of 250-500 mg/kg orally. Further, fractions with potent antidiabetic activity were screened for pancreatic ß-cells regeneration activity using histopathological studies and morphometric analysis, which was followed by estimation of biochemical parameters. RESULTS AND CONCLUSION: The most significant antidiabetic, pancreatic regeneration and antihyperlipidemic activity was exhibited by n-butanol soluble fraction of ethanol extract at the dose level of 500 mg/kg. Histopathology revealed that treatment with this fraction improved the ß-cell granulation of islets and prevented the ß-cells damage which was further confirmed by morphometric analysis. Thus, the present study validated the traditional use of T. purpurea plant in the treatment of diabetes, which might be attributed to pancreatic ß-cells regeneration potential of its active constituent Rutin. TAXONOMY CLASSIFICATION BY EVISE: Traditional Medicine; Metabolic Disorder; Experimental Design; Cell Regeneration and Histopathology.

Systematic Tuning of Fluoro-galectin-3 Interactions Provides Thiodigalactoside Derivatives with Single-Digit nM Affinity and High Selectivity.

Symmetrical and asymmetrical fluorinated phenyltriazolyl-thiodigalactoside derivatives have been synthesized and evaluated as inhibitors of galectin-1 and galectin-3. Systematic tuning of the phenyltriazolyl-thiodigalactosides' fluoro-interactions with galectin-3 led to the discovery of inhibitors with exceptional affinities (Kd down to 1-2 nM) in symmetrically substituted thiodigalactosides as well as unsurpassed combination of high affinity (Kd 7.5 nM) and selectivity (46-fold) over galectin-1 for asymmetrical thiodigalactosides by carrying one trifluorphenyltriazole and one coumaryl moiety. Studies of the inhibitor-galectin complexes with isothermal titration calorimetry and X-ray crystallography revealed the importance of fluoro-amide interaction for affinity and for selectivity. Finally, the high affinity of the discovered inhibitors required two competitive titration assay tools to be developed: a new high affinity fluorescent probe for competitive fluorescent polarization and a competitive ligand optimal for analyzing high affinity galectin-3 inhibitors with competitive isothermal titration calorimetry.

Involvement of NFκB in the antirheumatic potential of Chenopodium album L., aerial parts extracts.

ETHNOPHARMACOLOGICAL RELEVANCE: Chenopodium album L. (C. album) is commonly known as Bathua in Hindi (Family: Chenopodiaceae). Traditionally, the plant is used as a laxative, diuretic, sedative and the infusion of the plant is used for the treatment of rheumatism. However, no scientific validation is available on the antirheumatic potential of the plant. In the present investigation, role of NF kappa B (NFκB) in the antiarthritic potential of extracts of aerial parts of Chenopodium album was explored and evaluated. METHODS: The defatted aerial parts of Chenopodium album were successively extracted with ethylacetate, acetone, methanol and 50% methanol to study their antioxidant capacity followed by antiarthritic potential using Complete Freund׳s adjuvant (CFA) induced arthritis model in rats. The polyphenol, flavonoid and flavanone contents of different extracts were quantified and correlated with their antioxidant capacity, antiarthritic activity and NFκB inhibition potential. RESULTS: The experimental data indicated that the acetone extract of Chenopodium album (ACCA) has shown significant reduction in rat paw edema (80.13%) at dose level of 200 mg/kg per oral in 21 days of this study. On 22nd day, hematological and biochemical parameters were estimated and it was observed that the altered hematological parameters (Hb, RBC, WBC and ESR), biochemical parameters (Serum creatinine, total proteins and acute phase proteins) and loss in body weight in the arthritic rats were significantly brought back to near normal level by the ACCA extract. ACCA extract significantly decreased the NFκB expression in paraventricular nucleus of hypothalamus and this effect is comparable with standard indomethacine in CFA treated rats. The polyphenolic and flavonoid content of different extracts were in the range of 14.56±0.21-42.00±0.2 mg (gallic acid equivalent/g extract) and 2.20±0.003-7.33±0.5 mg (rutin equivalent/g extract) respectively. CONCLUSION: The antiarthritic activity possessed by ACCA extract can be correlated directly to its antioxidant potential, high flavonoidal content achieved by successive extraction and its capacity to inhibit the NFκB protein, as proven by immunohistochemistry study.

Evaluation of antidiabetic antihyperlipidemic and pancreatic regeneration, potential of aerial parts of Clitoria ternatea

The aim of the present study was to investigate the pancreatic regeneration potential of of diferent fractions of the ethanol extract Clitoria ternatea L., Fabaceae. The antidiabetic and antihyperlipidemic potential was evaluated in streptozotocin-induced diabetic rats and correlated with its in vivo and in vitro antioxidant activity. The extract and its fractions were initially screened for acute and sub-chronic antidiabetic activity in the dose range of 100200 mg/kg. The most potent extract and fractions were further evaluated for pancreatic β-cells regeneration activity along with antioxidant and antihyperlipidemic activity. The polyphenolic, flavonoid and flavanone contents were assessed and correlated with its antidiabetic activity. The most significant pancreatic regeneration activity, antidiabetic and antihyperlipidemic activity and was shown by ethanol extract and butanol soluble fraction at a dose level of 200 mg/kg, while rutin was found to be least potent. In conclusion, pancreatic regeneration studies of ethanol extract treated rats show nesidioblastosis. It is also suggested that the factors causing regeneration are present within the pancreas. The newly generated islets may have formed from the ductal precursor cells and reduced oxidative stress helps in restoration of β-cell function.

Antidiabetic potential of unripe Carissa carandas Linn. fruit extract.

ETHNOPHARMACOLOGICAL RELEVANCE: Carissa carandas commonly known as Karanda have a long history of use in traditional system of medicine. It is used by tribal healers of Western Ghat region of Karnataka as hepatoprotective and antihyperglycemic. However, no scientific data is available to validate the folklore claim. The present study has been designed to evaluate its unripe fruit for the antidiabetic activity. AIM: In the present study, methanol extract of unripe fruits and its fractions were studied for its antidiabetic potential. MATERIALS AND METHODS: The methanol extract and its fractions were screened for antidiabetic activity in alloxan induced diabetic rats. The polyphenolic, flavonoid and flavanone contents of methanolic extract and its fractions were also determined and correlated with its antidiabetic activity. RESULTS: The experimental data indicated that the methanol extract and its ethyl acetate soluble fraction has significantly lowered the elevated blood glucose levels by 48% (p<0.001) and 64.5% (p<0.001) respectively at dose level of 400mg/kg per oral after 24h as compared to diabetic control. In order to assess the role of polyphenolic components in the relevant activity, polyphenolic and flavonoid contents were determined. The polyphenolic and flavonoid content of methanol extract and its ethyl acetate soluble fraction were found to be 15.8 ± 1.2mg and 18.55 ± 0.34 mg (gallic acid equivalent/g extract) and flavonoid content 2.92 ± 0.03 mg and 1.534 ± 0.30 mg (rutin equivalent/g extract) respectively. CONCLUSION: The increased antidiabetic potential of ethyl acetate fraction over methanol extract is due to its partial purification achieved by fractionation which resulted in increase in degree of polymerization and segregation of secondary metabolites.

Antinociceptive activity of aqueous extract of Pachyptera hymenaea (DC.) in mice.

The standardized aqueous extract of leaves of Pachyptera hymenaea (DC.) belonging to family Bignoniaceae was investigated for possible antinociceptive effect in mice. Three different models were used to study the effects of extract on nociception, namely acetic acid-induced writhing test, formalin test (paw licking test) and tail flick test in mice. The extract was administered 1h prior to pain induction in the dose range of 25, 50 and 75mg/kg orally. The extract at the given dose range reduced the acetic acid induced nociception by 44.03, 52.90 and 62.46% respectively. The extract reduced formalin effect in both the phases of experiment by 32.36, 41.94, 54.29% and 35.39, 50.17, 55.86% respectively. In the tail flick study, animals' reaction time were increased by 22.69, 38.24 and 40.26% at the above selected doses respectively at 120min after drug administration. Naloxone (2mg/kg; s.c.) significantly antagonized the effect of extract in formalin and tail flick method, while partially antagonized the effect in writhing test. However caffeine completely reverted the extract effect in both the phases of formalin test. Results of these studies revealed that the extract have significant antinociceptive activity in the used models with a possible involvement of central mechanism and adenosine system.

Antinociceptive activity of alcoholic extract of Hemidesmus indicus R.Br. in mice.

The ethanolic extract of roots of Hemidesmus indicus R.Br. (family: Asclepiadaceae) was investigated for possible antinociceptive effect in mice. Three models were used to study the effects of extracts on nociception, which was induced, by acetic acid (Writhing test), formalin (Paw licking test) and hot plate test in mice. Hemidesmus indicus R.Br. extract was administered in the dose range of 25, 50 and 100mg/kg orally 1h prior to pain induction. The preliminary phytochemical screening of the extract showed the presence of triterpenes, flavonoids, pregnane glycosides and steroids. Oral administration of Hemidesmus indicus extract revealed dose-dependent antinociceptive effect in all the models for antinociception and it blocked both the neurogenic and inflammatory pain and the nociceptive activity was comparable with the reference drug. The results indicate that alcoholic extract of Hemidesmus indicus R.Br. possesses a significant antinociceptive activity. The activity can be related with the significant phytochemicals such as triterpenes, flavonoids, and sterols reported in the root extract.