Antidiabetic and antioxidant potential of Durio zibethinus Murr. leaves ethanolic extract

Durio zibethinus Murr., commonly called Durian, though well known for its rich medicinal uses, only fewer studies are available on the leaves of this plant. In this study, we investigated the antioxidant and antidiabetic potential of ethanol extract of D. zibethinus leaves (DZL) from Malaysian geographical origin. DZL was subjected to the preliminary phytochemical screening along with the quantitative analysis of phenols and flavonoids. The in vitro antioxidant properties were evaluated by DPPH and ABTS methods and in vitro antidiabetic properties were evaluated by α-amylase and α-glucosidase enzyme inhibition studies. The results of the above biological activities were expressed as inhibitory concentration 50% for DZL and standard drugs (acarbose and ascorbic acid). Based on the acute oral toxicity test, two test doses (100 and 200 mg/kg) of DZL were compared with glibenclamide (5 mg/kg) for their effect on fasting blood glucose at various time intervals (0 to12 h) in glucose-loaded normoglycemic rats. DZL (200 mg/kg) showed a better response in streptozotocin (STZ) induced diabetic rats. The antioxidant assay of DZL showed an appreciable extract inhibitory concentration 50% against the free radicals generated by DPPH (1.61±0.07 μg/ mL) and ABTS (1.47±0.07 μg/mL) assays. Similarly, the in vitro antidiabetic assay results demonstrated a dose-dependent inhibition of α-amylase (2.58±0.08 μg/mL) and α-glucosidase enzymes (2.41±0.08 μg/ mL) by DZL. Both glucose-loaded normoglycemic rats and STZ-induced diabetic rats treated with DZL (200 mg/kg) exhibited a significant post-dose reduction in blood glucose levels (P <0.01, 8 h and P <0.001, 12 h) when compared to normal and diabetic control rats, respectively. These findings suggest that the presence of polyphenols in DZL might be responsible for antioxidant and antidiabetic properties and DZL could be a natural source as an herbal remedy for diabetes

ANTICHOLINESTERASE ACTIVITY OF OCTA PEPTIDES RELATED TO HUMAN HISTATIN 8: IN-SILICO DRUG DESIGN AND IN-VITRO

Objective: To evaluate the octapeptides related to human histatin 8 by in-silico and in-vitro studies.Method: Schrodinger, LLC and Ellman's method.Results: The compound HH1 and HH2 was found to be potent docking score of −9.494 and −7.401 against acetylcholinesterase (AChE) enzyme. The IC50 value of HH1 and HH2 was found to be 0.39±0.28 and 0.78±0.15 μg/mL. However, these compounds are shown to be highly effective as compared with the control AChE inhibitor donepezil (0.065±0.0050 μg/mL).Conclusion: In-silico docking study was conducted for the designed octapeptides related to human histatin 8 against AChE enzyme shows significance binding affinity toward HH1 and HH2 peptides and the AChE inhibitory activity of octapeptides shown to be a highly potent inhibitor as compared with control donepezil

DIABETIC NEPHROPATHY AN OBVIOUS COMPLICATION IN LONG TERM TYPE 1 DIABETES MELLITUS: A CASE STUDY

  Most overwhelming complications of Type 1 diabetes mellitus patients are responsible for complications related to the microvascular system most likely with kidney. In the kidney, hyperglycemia induced microangiopathy resulting not only thickening of the glomerular capillary basement membrane but also to the proliferation of the mesangial matrix and solidifying of the tubular basement membrane. Several biochemical and pathological, factors are concerned for the development of diabetic renal microangiopathy. These include the glomerular hyperperfusion and hyperfiltration, transformed morphology of podocytes accompanies these basement membrane modifications, Type IV collagen augmented synthesis following the hyperglycemia, and increased expression of tissue matrix metalloproteinase. The aim of this case review is to highlight the recent advances in understanding the pathogenesis, diagnosis, the overview and the potential renoprotective therapeutic agents that would prevent the development or the progression of diabetic nephropathy

PRETREATMENT VARIATIONS IN HAEMATOLOGICAL PARAMETERS OF BREAST CANCER PATIENTS

Objective: The objective of the presented study was to analyze the haematological parameters in female breast cancer (BC) patients before the start of the treatment.Methods: The study was conducted among female BC patients, visited King Fahd Hospital (KFH), Al Ahsa, Kingdom of Saudi Arabia (KSA) from January 2013 to December 2016. A retrospective analytical study was conducted. We analyzed the relationship of haematological parameters with various stages of breast cancer before the start of any treatment. We used complete blood count (CBC) reports to analyze the haematological parameters. The mean age of the patients was 57 y (31-83 y). Most of the patients were postmenopausal (51-59 y old). We divided the patients into 4 groups according to the disease stage, i.e., stage 1 (S1) to stage 4 (S4).Results: Among altered blood parameters, decreased haemoglobin (Hb 4.5-11 g/dl) and increased erythrocyte sedimentation rate (ESR 37–49 mm/first hour) in S1 to S4, increased neutrophil count in S3 and S4 (8.3-9.6 x103/mm3), and increased lymphocyte count (4-7.2 x103/mm3) in S1 and S2 patients were found.Conclusion: We found significant variations in haematological parameters at different stages of breast cancer. CBC is indeed an efficient and cost-effective investigation. By managing these parameters, treatment efficacy and survival rate of BC patients may be augmented

A PROSPECTIVE CLINICALTRIAL OF AMLODIPINE IN COMPARISON TO PERINDOPRIL

Objective: The objective of this research was to perform a prospective clinical trial to compare antihypertensive effects of amlodipine and perindopril in hypertensive patients.Methods: In our study, we compared antihypertensive effects of well tolerated and commonly used antihypertensive drugs, amlodipine and perindopril. There were 81 hypertensive patients of both sexes over 40 y of age without other diseases included in this prospective clinical trial. Forty (40) patients were treated with amlodipine (5 mg/day) and forty-one (41) patients were treated with perindopril (4 mg/day). After one month of taking both drugs, blood pressure was measured in the supine position with a standard mercury sphygmomanometer in the morning.Results: Amlodipine and perindopril groups were having almost similar characteristics at the beginning of the study. There was significantly decrease insystolic blood pressure (sBP) throughout the study period in the amlodipine group (p≤ 0.05) but not in the perindopril group. The efficacy of amlodipine over perindopril on systolic blood pressure and diastolic blood pressure (dBP) was significant (p≤ 0.001 for sBP and p≤ 0.05 for dBP).Conclusion: It may be concluded that the antihypertensive efficacy of amlodipine was superior when compared to perindopril

Therapeutic Significance of Polymeric Nano Particles as Carriers for Sustained Ocular Therapy: An Overview

ABSTRACT Effective delivery of drug to the eye poses many problems through conventional eye drops due to its poor ocular retention and bioavailability. The use of nanocarriers provides interesting opportunities for topical ocular drug delivery. The association of an active drug to nanocarriers allows the drug to closely interact with specific ocular structures, also to overcome ocular barriers and to prolong its residence in the target area. Hence delivery of a drug through nanoparticles can accomplish main benefits like enhancement of drug permeation, controlled release, and targeting. Though several non polymeric and colloidal drug delivery systems, such as Prodrugs, Polymeric micelles, liposomes, neosome, nanoemulsions, nanocrystals and nanoparticles have been largely investigated and reported to enhance ocular bioavailability of ocular drugs. Owing to the submicron size of polymeric nanoparticles they are well tolerated and have the tendency to deposit in the cul-de-sac for prolonged period. In the present review our objective is focused on the fundamental aspects of polymeric nanoparticles as carrier for ocular drugs and its therapeutic applications with special emphasis to research studies in ocular delivery of polymeric nanoparticles with anti-infectious and anti inflammatory drugs

Identification of Nephelium lappaceum leaves phenolic and flavonoid component with radical scavenging, antidiabetic and antibacterial potential

360-365Nephelium lappaceum Linn. (Rambutan) is traditionally claimed, as a source of natural antioxidants and for its use in the treatment of diabetes and bacterial infections. The present study investigates the in vitro effect of ethanolic Rambutan leaves extract (NL) for its antioxidant effect, α-glucosidase, α-amylase enzyme inhibition, and antibacterial potentials. The total phenolic, total flavonoid content of NL was quantified and were expressed in terms of gallic acid (19.6±0.04 mg GAE/g) and rutin equivalents (16.7±0.01 mg RUE/g) respectively. The antioxidant assay revealed that NL exhibited significant inhibition of DPPH (IC50±SEM: 1.52±0.03 μg/mL) and ABTS (IC50±SEM: 1.295±0.05 μg/mL) radicals. NL also inhibited both α-amylase (IC50±SEM: 2.624±0.07 μg/mL), α-glucosidase (IC50±SEM: 2.416±0.06 μg/mL) enzyme activities, supported by its antioxidant potential and its phenolic and flavonoid content. The antibacterial activity was screened against seven human pathogenic ATCC strains for which the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were recorded. The selected MIC dose was tested, confirmed by Kirby-Bauer agar well diffusion method. NL exhibited MIC and MBC of 62.5 μg/mL and 125 μg/mL against B.subtilis and E.coli respectively. The results support the scientific claim of NL for its antioxidant, antidiabetic and antibacterial potential

Identification of Nephelium lappaceum leaves phenolic and flavonoid component with radical scavenging, antidiabetic and antibacterial potential

360-365Nephelium lappaceum Linn. (Rambutan) is traditionally claimed, as a source of natural antioxidants and for its use in the treatment of diabetes and bacterial infections. The present study investigates the in vitro effect of ethanolic Rambutan leaves extract (NL) for its antioxidant effect, α-glucosidase, α-amylase enzyme inhibition, and antibacterial potentials. The total phenolic, total flavonoid content of NL was quantified and were expressed in terms of gallic acid (19.6±0.04 mg GAE/g) and rutin equivalents (16.7±0.01 mg RUE/g) respectively. The antioxidant assay revealed that NL exhibited significant inhibition of DPPH (IC50±SEM: 1.52±0.03 μg/mL) and ABTS (IC50±SEM: 1.295±0.05 μg/mL) radicals. NL also inhibited both α-amylase (IC50±SEM: 2.624±0.07 μg/mL), α-glucosidase (IC50±SEM: 2.416±0.06 μg/mL) enzyme activities, supported by its antioxidant potential and its phenolic and flavonoid content. The antibacterial activity was screened against seven human pathogenic ATCC strains for which the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were recorded. The selected MIC dose was tested, confirmed by Kirby-Bauer agar well diffusion method. NL exhibited MIC and MBC of 62.5 μg/mL and 125 μg/mL against B.subtilis and E.coli respectively. The results support the scientific claim of NL for its antioxidant, antidiabetic and antibacterial potential

Synthesis and antibacterial profile of novel azomethine derivatives of β-phenylacrolein moiety

Purpose: To develop some novel molecules effective against antibiotic-resistant bacterial infections.Methods: A series of azomethines (SB-1 to SB-6) were synthesized from β-phenyl acrolein moiety. The structures of the synthesized compounds were confirmed on the basis of their UV ultra-violet (UV) spectroscopy (λmax: 200 - 400 nm), Fourier transform infra-red (FTIR, vibrational frequency: 500-4000 cm-1), 1H nuclear magnetic resonance (NMR, chemical shift: 0 - 10 ppm), 13C NMR (chemical shift: 0 - 200 ppm), mass spectrometry (m/z values: 0 - 500) and carbon hydrogen nitrogen (CHN) elemental analysis. The new compounds were screened for antibacterial activity by test-tube dilution and disc diffusion methods using gentamicin as reference standard.Results: The structures of azomethine were in full agreement with their spectral data. Among all the synthesized compounds, compounds SB-5 and SB-6 exhibited the highest minimum inhibitory concentration (MIC) of 62.5 μg/mL. At MIC of 250 μg/mL, all compounds SB-1 to SB-6 displayed significant antibacterial activity, compared to gentamycin (p < 0.05). SB-5 and SB-6 were active against S. aureus, P. aeruginosa and K. pneumoniae; SB-3 was active against B. subtilis and S. aureus. SB-4 was active against P. aeruginosa and S. aureus while SB-1 and SB-2 were active against S. aureus.Conclusion: The synthesized compounds possess antibacterial activities compared to those of gentamycin.Keywords: Acrolein, Imines, Azomethine, Antibacterial, Gentamycin, Minimum inhibitory concentratio

Antidiabetic, antioxidant and in silico studies of bacterial endosymbiont inhabiting Nephelium lappaceum L.

Endophytes, notably obtaining attention, have been abided by potential origins of bioactive metabolites. In the acquaint study, endophyte was isolated from the leaves of Nephelium lappaceum L. The chosen endosymbiont was identified by 16s rRNA partial genome sequencing and investigated for their antioxidant and antidiabetic activities. A preliminary phytochemical test was comported for the affirmation of phytoconstituents in endophytic crude extract (NLM). Antioxidant activities were conducted by using 2-diphenyl-1-picrylhydrazyl (DPPH) method and 2,2′-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS) method to screen the radical scavenging potential. The evaluation of antidiabetic activities was done by using α-amylase and α-glucosidase inhibition assay. Qualitative phytochemical test on NLM affirmed the presence of phenols, carbohydrates, alkaloids, flavonoids, steroids, mucilage and glycosides. In silico parameters were also specified for antidiabetic activities. The antioxidant assay of NLM expressed proficient antioxidant activity of IC50±SEM 1.35±0.03 µg/mL and IC50±SEM 1.47±0.03 µg/mL, for ABTS and DPPH respectively. Antidiabetic assay results evidenced dose dependent percentage inhibition of the enzyme. The results testified estimable inhibition of α-amylase (IC50±SEM 2.549±0.08 µg/mL) and α-glucosidase inhibition (IC50±SEM 2.29±0.03µg/mL) compared to the standard drug (Acarbose). In silico study divulged that the ellagic acid component present in the plant was responsible for antidiabetic activity. Thus, the study shows that NLM has a wellspring of natural source of antioxidants and antidiabetic agents and furtherance of studies on its mechanism is recommended to know detailed facts