Serum Total Sialic Acid and Highly Sensitive C-reactive Protein: Prognostic Markers for the Diabetic Nephropathy.

BACKGROUND: This study was undertaken to evaluate and establish the role of total sialic acid (TSA) and highly sensitive C-reactive protein (hs-CRP) in type 2 diabetes mellitus (T2DM) and its correlation with complications such as diabetic nephropathy. MATERIALS AND METHODS: One hundred fifty-seven patients with T2DM with nephropathy (DN) and 162 patients of T2DM without nephropathy (DM) along with 165 unrelated age and sex-matched healthy controls were included in the study. Serum glucose (fasting and postprandial) levels, renal profile, and lipid profile were done as per standard protocol. Serum TSA test levels and hs-CRP level were evaluated using thiobarbituric acid assay and immunoturbidimetric method respectively. RESULTS: We observed a higher concentration of serum TSA (82.67 ± 6.63 mg/dl) and hs-CRP (3.2 ± 1.44 mg/L) in diabetic nephropathy than the diabetes mellitus group (73.83 ± 6.90 mg/dl and 2.07 ± 1.32 mg/L, respectively). Both TSA and hs-CRP levels were found significantly correlated with fasting and postprandial blood sugar, hemoglobin A1c, and urine microalbumin levels in both DM and DN groups. Multinomial logistic regression analysis showed that both TSA and hs-CRP was independently associated with diabetic nephropathy. CONCLUSION: High serum TSA and hs-CRP levels may increase the microangiopathic (diabetic nephropathy) complications of T2DM.

Bio-enhancing Effect of Piperine with Metformin on Lowering Blood Glucose Level in Alloxan Induced Diabetic Mice.

BACKGROUND: Diabetes mellitus is the most rampant metabolic pandemic of the 21(st) century. Piperine, the chief alkaloid of Piper nigrum (black pepper) is widely used in alternative and complementary therapies has been extensively studied for its bio-enhancing property. OBJECTIVE: To evaluate the bio-enhancing effect of piperine with metformin in lowering blood glucose levels in alloxan-induced diabetic mice. MATERIALS AND METHODS: Piperine was isolated from an extract of fruits of P. nigrum. Alloxan-induced (150 mg/kg intraperitoneal) diabetic mice were divided into four groups. Group I (control 2% gum acacia 2 g/100 mL), Group II (metformin 250 mg/kg), Group III (metformin and piperine 250 mg/kg + 10 mg/kg), and Group IV (metformin and piperine 125 mg/kg + 10 mg/kg). All the drugs were administered orally once daily for 28 days. Blood glucose levels were estimated at day 0, day 14, and end of the study (day 28). RESULTS: The combination of piperine with therapeutic dose of metformin (10 mg/kg + 250 mg/kg) showed significantly more lowering of blood glucose level as compared to metformin alone on both 14(th) and 28(th) day (P < 0.05). Piperine in combination with sub-therapeutic dose of metformin (10 mg/kg + 125 mg/kg) showed significantly more lowering of blood glucose as compared to control group and also showed greater lowering of blood glucose as compared to metformin (250 mg/kg) alone. CONCLUSION: Piperine has the potential to be used as a bio-enhancing agent in combination with metformin which can help reduce the dose of metformin and its adverse effects. SUMMARY: Piperine is known for its bioenhancing property. This study evaluates the effect of piperine in combination with oral antidiabetic drug metformin. Drugs were administered for 28 days in alloxan induced diabetic mice and blood glucose lowering effect was seen. Results showed significantly better effect of combination of piperine with therapeutic dose of metformin in comparison to metformin alone. Piperine in combination with subtherapeutic dose of metformin also showed better effect than therapeutic dose of metformin. Piperine, thus shows potential to be used as bioenhancer in combination with metformin.

Management of drug induced sexual dysfunction in male rats by ethyl acetate fraction of onion.

The present study aimed to investigate the effect of ethyl acetate fraction of A. cepa bulb on mating behavior in paroxetine-induced sexually dysfunction male rats. Sexual dysfunctions such as decreased libido, delayed orgasm, difficulties in maintaining an erection, and inhibition of ejaculation are common side effects of paroxetine. A. cepa bulb ethyl acetate fraction (200 mg/kg) was administered orally in paroxetine-induced sexually impaired male rats for 7 days. At the end of 7th day, mount frequency (MF), intromission frequency (IF), ejaculatory frequency (EF), mount latency (ML), intromission latency (IL), ejaculatory latency (EL) and post-ejaculatory interval (PEI) were the parameters observed. Results showed that in relation to the paroxetine treated group, ethyl acetate fraction, significantly restored the normal sexual behavior as evident from increased MF, IF, EF and reduced ML, IL, EL and PEI.

Evaluation of the effect of piperine per se on blood glucose level in alloxan-induced diabetic mice.

Abstract: Diabetes mellitus is a metabolic disorder and emerging pandemic of the 21st century. Piperine, the chief alkaloid present in Piper nigrum (black pepper), has a wide array of uses in alternative and complementary therapies. The effect of piperine on blood glucose level was studied in alloxan-induced diabetic mice in acute and subacute study models. Piperine was isolated from the fruits of Piper nigrum crude extract. Diabetes was induced using alloxan in albino mice which were then randomly divided into 5 groups (n = 6). In acute study, drugs were administered orally as: control (2% gum acacia, 10 mL/kg), standard (metformin 150 mg/kg), P10 (piperine 10 mg/kg), P20 (piperine 20 mg/kg) and P40 (piperine 40 mg/kg). Drug intervention for subacute study consisted of once daily oral administration for 14 days of 2% gum acacia 10 mL/kg, metformin 250 mg/kg, and piperine 5, 10 and 20 mg/kg, respectively, in the control, standard and P5, P10, P20 groups. Blood glucose levels were estimated before and at 1, 2, 3 and 4 h post dosing, respectively, in the acute study and on day 7 and 14 in the subacute study. Results of acute study showed that at 2 h post-dosing piperine at high dose of 40 mg/kg showed significant rise in blood glucose level (p < 0.05) in comparison to control group. In contrast, a significant blood glucose lowering effect was seen with piperine at dose of 20 mg/kg on day 14 (p < 0.05) in the subacute study. In summary, we suggest that subacute administration of piperine has statistically significant antihyperglycemic activity while acutely it raises blood glucose at high doses. Further investigations are needed to consider it as prospective anti-diabetic agent at appropriate dosage.

Recent studies on aphrodisiac herbs for the management of male sexual dysfunction--a review.

An aphrodisiac is a type of food or drink that has the effect of making those who eat or drink it more aroused in a sexual way. Aphrodisiacs can be categorized according to their mode of action into three groups: substances that increase libido (i.e., sexual desire, arousal), substances that increase sexual potency (i.e., effectiveness of erection) and substances that increase sexual pleasure. Some well-known aphrodisiacs are Tribulus terrestrins, Withania somnifera, Eurycoma longifolia, Avena sativa, Ginko biloba, and Psoralea coryifolia. Ethnobotanical surveys have indicated a large number of plants as aphrodisiacs. The paper reviews the recent scientific validation on traditionally used herbal plants as aphrodisiac herbs for the management of sexual disorder erectile dysfunction.

Dextran-etodolac conjugates: synthesis, in vitro and in vivo evaluation.

Etodolac (E), is a non-narcotic analgesic and antiinflammatory drug. A biodegradable polymer dextran has been utilized as a carrier for synthesis of etodolac-dextran conjugates (ED) to improve its aqueous solubility and reduce gastrointestinal side effects. An activated moiety, i.e. N-acylimidazole derivative of etodolac (EAI), was condensed with the polysaccharide polymer dextran of different molecular weights (40000, 60000, 110000 and 200000). IR spectral data confirmed formation of ester bonding in the conjugates. Etodolac contents were evaluated by UV-spectrophotometric analysis. The molecular weights were determined by measuring viscosity using the Mark-Howink-Sakurada equation. In vitro hydrolysis of ED was done in aqueous buffers (pH 1.2, 7.4, 9) and in 80% (v/v) human plasma (pH 7.4). At pH 9, a higher rate of etodolac release from ED was observed as compared to aqueous buffer of pH 7.4 and 80% human plasma (pH 7.4), following first-order kinetics. In vivo investigations were performed in animals. Acute analgesic and antiinflammatory activities were ascertained using acetic acid induced writhing model (mice) and carrageenan-induced rat paw edema model, respectively. In comparison to control, E and ED1-ED4 showed highly significant analgesic and antiinflammatory activities (p <0.001). Biological evaluation suggested that conjugates (ED1-ED4) retained comparable analgesic and antiinflammatory activities with remarkably reduced ulcerogenicity as compared to their parent drug--etodolac.

Evaluation of antidepressant like property of amisulpride per se and its comparison with fluoxetine and olanzapine using forced swimming test in albino mice.

Amisulpride, an atypical antipsychotic was evaluated for antidepressant like activity in forced swimming test in Swiss albino mice. The effect of amisulpride was compared with that of fluoxetine, the standard antidepressant and olanzapine, another atypical antipsychotic claimed to have antidepressant like activity. Both acute and chronic studies were carried out. In both the studies, animals were divided into four groups (n = 8 each) and subjected to oral drug interventions as follows -- Group 1- control (distilled water, 1 mL/kg); Group 2- fluoxetine in a dose of 10 mg/kg 23.5, 5 and 1 h before the test; Group 3-amisulpride in a dose of 70 mg/kg 23.5, 5 and 1 h before the test; Group 4- olanzapine in a dose of 2 mg/kg 23.5, 5 and 1 h before the study. In the chronic study, the treatment was given daily for 28 days with last dose being given 2 h prior to the test. A time sampling method was used to score the behavioral activity in each group. Results of both the studies indicated that animals given amisulpride displayed significant improvement in swimming behavior (p < 0.01), while markedly reducing immobility as compared to control group (p <0.01). Fluoxetine also showed significant difference in activity as compared to amisulpride and olanzapine (p < 0.01). There was no statistically significant difference between amisulpride and olanzapine in terms of effect on immobility and swimming phases in albino mice (p > 0.05). We conclude that amisulpride per se has an antidepressant like activity comparable to that of olanzapine though the activity was significantly less than that of fluoxetine.

Analgesic and anti-inflammatory activities of Trigonella foenum-graecum (seed) extract.

Analgesic and anti-inflammatory effects were examined in a partially purified fraction (MTH) of the Trigonella foenum-graecum seed extract. The analgesic effects of graded doses of fraction (MTH in 10-40 mg/kg p.o.) were evaluated in mice against acetic acid induced writhing (chemically induced pain) and hot-plate method (thermally induced pain). The analgesia produced by MTH was compared with the standard analgesics pentazocine (PTZ, 5 mg/kg p.o.) and diclofenac sodium (DIS, 5 mg/kg p.o.). Acute anti-inflammatory activity of fraction (MTH) was also evaluated in carrageenan-induced rat paw edema model at the doses 10 and 20 mg/kg i.p. and compared with diclofenac sodium (5 mg/kg i.p.). In comparison to control group MTH showed highly significant, dose dependent analgesic activity against thermally as well as chemically induced pain (p < 0.001). MTH at the dose of 40 mg/kg has shown significant analgesic activity (p < 0.001) as compared to diclofenac sodium and pentazocine at the doses employed. In comparison to control, MTH at the employed doses produced marked acute anti-inflammatory activity in rats (p <0.001). The results suggest that the water soluble fraction (MTH) of herbal origin has significant analgesic and anti-inflammatory potential as reflected by the parameters investigated. Further investigations are, however, necessary to explore mechanism(s) of action involved in these pharmacological activities.

Ketorolac-dextran conjugates: synthesis, in vitro and in vivo evaluation.

Ketorolac is a non-steroidal anti-inflammatory drug. Dextran conjugates of ketorolac (KD) were synthesized and characterized to improve ketorolac aqueous solubility and reduce gastrointestinal side effects. An N-acylimidazole derivative of ketorolac (KAI) was condensed with a model carrier polymer, dextran of different molecular masses (40000, 60000, 110000 and 200000). IR spectral data confirmed formation of ester bonding. Ketorolac contents were evaluated by UV-spectrophotometric analysis. The molecular mass was determined by measuring viscosity using the Mark-Howink-Sakurada equation. In vitro hydrolysis studies were performed in aqueous buffers (pH 1.2, 7.4, 9) and in 80% (V/V) human plasma (pH 7.4). At pH 9, a higher rate of ketorolac release from KD was observed as compared to aqueous buffer of pH 7.4 and 80% human plasma (pH 7.4), following first-order kinetics. In vivo biological screening in mice and rats indicated that conjugates retained analgesic and anti-inflammatory activities with significantly reduced ulcerogenicity compared to the parent drug.