Physiologic kinetic profile of glycemic response in a single dose of clonidine

Background: Clonidine activates peripheral α-2 adrenoreceptors and influences glycemic levels. Aim and Objective: The aim and objective of the study was to determine the physiologic kinetic profile of glycemic response in a single dose of clonidine. Materials and Methods: Experimental data on fasting glycemic levels of Sprague-Dawley rats in a single dose intraperitoneal administration of clonidine were used to describe the rate mechanisms behind the physiologic response. Parameters of the kinetic models including zero-order, first-order, and second-order were estimated and compared using nonlinear regression analysis. Results: Clonidine administration resulted to a dose-dependent fasting glycemic level with maximal cumulative dose effect at 4 µg/kg. The overall physiologic glycemic response behaved under zero-order and first-order kinetic models on the first 3 h, while second-order kinetic model captures the fasting glycemic levels on the 3rd-8th h after drug administration. Conclusion: A 4 µg/kg optimal dose accentuates glycemic response behaving under a zero-order or first-order rate mechanism with maximal effect on the first 3 h after clonidine administration. © 2017 Derick Erl P. Sumalapao MD

Elucidation on the Physicochemical Properties of Potential and Clinically Approved Antiviral Drugs: A Search for Effective Therapies against SARS-CoV-2 Infection

COVID-19 has been confirmed in millions of individuals worldwide, rendering it a global medical emergency. In the absence of vaccines and the unavailability of effective drugs for the SARS-CoV-2 infection, vaccine development is being continuously explored and several antiviral compounds and immunotherapies are currently being investigated. Given the high similarity in genetic identity between SARS-CoV and SARS-CoV-2, the present investigation identified the interaction between the physicochemical properties and the antiviral activity of different potential and clinically approved antiviral drugs against SARS-CoV using hierarchically weighted principal component analysis. Representative drugs from the classes of neuraminidase inhibitors, reverse transcriptase inhibitors, protease inhibitors, nucleoside analogues, and other compounds with potential antiviral activity were examined. The pharmacologic classification and the biological activity of the different antiviral drugs were described using indices, namely, rotatable bond count, molecular weight, heavy atom count, and molecular complexity (92.32% contribution rate). The physicochemical properties and inhibitory action against SARS-CoV-2 of lopinavir, chloroquine, ivermectin, and ciclesonide validated the adequacy of the current computational approach. The findings of the present study provide additional information, although further investigation is warranted to identify potential targets and establish exact mechanisms, in the emergent search and design of antiviral drug candidates and their subsequent synthesis as effective therapies for COVID-19

Hierarchically weighted principal component analysis evaluation of antifungal azoles inhibitory potency on lanosterol-14α-demethylase in Candida albicans

Hierarchically weighted principal component analysis method was employed to assess the inhibitory potency of different antifungal azoles to Candida albicans lanosterol-14α-demethylase. Information regarding the molecular properties and biological activity of the antifungal azoles was utilized for evaluation. The molecular weight, complexity, heavy atom count, and rotatable count were identified as the most significant variables describing the inhibitory potency of the antifungal drugs. Newer generation drugs including itraconazole and fluconazole were identified to have better inhibitory potency than bifonazole and clotrimazole. The present study illustrated a method providing an effective approach in classifying antifungal azoles based on molecular properties and biological activity for possible synthesis of newer generation antifungal drugs for a better and more effective treatment of fungal infections. © 2019, Current Research in Environmental & Applied Mycology

Hepatoprotective activity of aqueous and ethanolic bixa orellana L. leaf extracts against carbon tetrachloride-induced hepatotoxicity

Background: There is an increasing incidence of liver failure and lack of effective drugs for liver diseases. Aim and Objective: This study identified the phytochemicals present in aqueous and ethanolic Bixa orellana L. leaf extracts and investigated the hepatoprotective activity against carbon tetrachloride (CCl4)-induced hepatotoxicity in mice. Specifically, the study compared serum levels of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) and examined liver tissues histopathology. Materials and Methods: Aqueous and ethanolic B. orellana L. leaf extracts were prepared and screened for phytochemical contents. An oral dose of 500 mg/kg body weight was identified from toxicity test and administered to albino mice. Microscopic examination of the liver tissues assessed the extent of hepatic injury. Serum AST and ALT levels were compared using one-way analysis of variance with Bonferroni post hoc analysis at 5% level of significance using Stata/SE V12.0 software. Results: B. orellana L. leaves contained alkaloids, anthraquinones, sugars, and tannins. Aqueous and ethanolic leaf extracts of B. orellana L. did not show any toxicity up to 2000 mg/kg body weight oral dose in mice. Pre-treatment for 7 days before CCl4 administration significantly prevented elevation of serum AST and ALT levels with histopathologic findings showing a protective effect on the hepatocytes. Conclusion: B. orellana L. leaves have potent hepatoprotective activity against oxidative damage. © 2017 Derick Erl P Sumalapao, et al

Therapeutic and prophylactic effect of Andrographis paniculata on aspirin-induced gastric ulcer

Background: Andrographis paniculata is extensively used in the Southeast Asia in treating different kinds of diseases. Aims and Objectives: The study aimed to determine the chemical constituents of A. paniculata extract and its therapeutic and prophylactic effects on aspirin-induced gastric ulcer in male albino mice using histopathological analysis. Materials and Methods: Lyophilized filtered leaf extract of A. paniculata was administered to the experimental subjects at varying doses of 25%, 50%, and 75% concentrations once a day for 3 consecutive days in the prophylactic group followed by aspirin administration for another 3 days. For the therapeutic group, aspirin was administered first and after 3 days, plant extract was administered for 3 consecutive days. On the 7th day, longitudinal sections of the gastric tissue from the fundus of the mice were excised for histopathologic analysis using light microscopy to assess gastric mucosal lesions, presence of necrosis, and degree of inflammation. Results: Phytochemical tests on A. paniculata extract revealed the presence of tannins, glycosides, reducing substances, terpenoidal compounds, and flavones. Administration of 25%,50%, and 75% A. paniculata extract remarkably decreased the severity of ulceration, hastened regeneration and repair, and produced normal gastric mucosa, respectively. The prophylactic group showed similar results regardless of A. paniculata extract concentration in delaying gastric ulcer progression. Conclusion: Crude extract of A. paniculata plant has an ulcer-healing and prophylactic potential. © 2017, Mr Bhawani Singh. All rights reserved

Synthesis and characterization of epichlorohydrin-crosslinked lumbang (Aleurites moluccana)-derived activated carbon chitosan composite as cr(VI) bioadsorbent

Lumbang (Aleurites moluccana) activated carbon chitosan composite crosslinked with epichlorohydrin was synthesized for batch adsorption of toxic Cr(VI) ion from an aqueous solution. The synthesized biosorbent was characterized by instrumental techniques such as FTIR and SEM. The surface morphology of the adsorbent had a porous texture with round-and elliptical-shaped voids as adsorption sites for the adsorbate. Some functionalities including -OH and -NH2 groups were identified on the surfaces. The synthesized activated lumbang-biocharcoal chitosan composite crosslinked with epichlorohydrin adsorbent at the optimized conditions adsorbed 93% of Cr(VI) ion. The investigated adsorption phenomenon described a chemisorption process due to the functional groups identified and the high porosity of the adsorbent surfaces. © 2017 Bautista et al

Removal of lead (α) by lumbang, aleurites moluccana activated carbon carboxymethylcellulose composite crosslinked with epichlorohydrin

Removal of Pb(II) using lumbang activated carbon carboxymethylcellulose composite crosslinked with epichlorohydrin was investigated. Batch adsorption studies were performed to evaluate the effects of pH, contact time, temperature, adsorbent dose, and metal concentration. To characterize the adsorbent, proximate analysis, bulk density, DSC, FT-IR, and SEM analysis were performed. Results of FT-IR revealed that crosslinking did not alter the structure of carboxymethylcellulose due to the presence of the-COO functional groups, while the presence of the C-O signal indicates that the adsorbent was successfully crosslinked by epichlorohydrin. Furthermore, SEM results showed highly porous nature of the prepared adsorbent. The optimized parameters of the adsorbent were pH 3, contact time of 15 min. 30 oC temperature, adsorbent dose of 4 g/L at 5 ppm Pb (II) solution. With these optimized parameters, 73% removal of Pb (II) was attained in aqueous solutions, while 37% removal was observed in the wastewater sample. Moreover, the adsorption process was best described by Dubinin-Radushkevich isotherm and obeyed the pseudo-second order kinetic model. © 2018 Oriental Scientific Publishing Company. All rights reserved

Biosorption of methylene blue from aqueous solution by coconut (Cocos nucifera) shell-derived activated carbon-chitosan composite

Charcoal produced from coconut shells through the retort method was consequently activated using CaCl2. The activated carbon-chitosan composite was prepared by coating the activated carbon with chitosan. Batch experiments with methylene blue as adsorbate were conducted under varying pH, contact time, initial dye concentration, adsorbent dosage, and temperature. The effects of these factors were investigated using batch adsorption studies with optimal conditions identified at pH 5, 30 min. contact time, 10 mg L-1 initial dye concentration, 9 g L-1 adsorbent dosage, and 25 °C adsorption temperature. Results of adsorption experiments showed that the composite had better removal efficiency compared to activated carbon. © 2018 Oriental Scientific Publishing Company. All Rights Reserved

Batch adsorption study and kinetic profile of Cr(VI) using lumbang (Aleurites moluccana)-derived activated carbon-chitosan composite crosslinked with epichlorohydrin

Batch adsorption of toxic Cr(VI) ion from an aqueous solution using lumbang (Aleurites moluccana) activated carbon-chitosan composite crosslinked with epichlorohydrin as an adsorbent was investigated. The adsorption experiments were performed at varying pH, agitation time, initial Cr(VI) ion concentration, temperature, and adsorbent dose. At an initial concentration of 60 ppm Cr(VI), the maximum adsorption was observed at pH 3, adsorbent dose of 3 g/L, contact time of 75 min, and temperature of 30°C. Analysis of the experimental data using different kinetic models revealed that the biosorption phenomenon behaved under a pseudo second-order rate mechanism. © 2017, Oriental Scientific Publishing Company. All rights reserved

Synergistic immune response to leptospira infection among smokers

As a result of the continuous heavy rain, poor road construction and poor sewage system, oods have been occuring in many areas of the Philippines. As a consequence, leptospirosis becomes one of the major health poblems in the Philippines. Exposure of an individual to leptospiral infection activates the immune system which includes macrophages and T-cells. Macrophages serve as the rst line of defense and these are phagocytic cells responsible in detecting, engul ng, and destroying pathogens and apoptotic cells. T-cells, on the other hand, are the second line of defense responsible for recognition and elimination of pathogens. Exposure to smoking impairs multiple organ systems including the human immune system resulting in numerous smoking-induced diseases. In this paper, a system of ordinary di erential equations was constructed in describing the synergy of leptospiral infection and smoking in the impairment of human immune system. We calculated di erent rate capacities of macrophages and T-cells in response to leptospiral infection based on the parameters collected. In the disease-free model, using the rates taken from the literature, the result had shown the population of macrophages are greater compared to T-cells. In the results of the study, the predominance of macrophages over T-cells were observed as well in the synergistic immune response to smoking and leptospiral infection. Since the e ect of leptospiral infection in human immune cells is dose-dependent, the leptospiral infection rate in smoking-impaired cells is more rapid compared in normal cells