Antioxidant, Phytotoxic and Antiurease Activities, and Total Phenolic and Flavonoid Contents of Conocarpus lancifolius (Combretaceae)

Purpose: To evaluate the antioxidant, phytotoxic and anti-urease properties of dichloromethane and methanol extracts of Conocarpus lancifolius in correlation with total phenolic and flavonoid contents.Methods: The whole plant (dried aerial parts and root) of Conocarpus lancifolius was extracted successively with dichloromethane, methanol and water at room temperature. Antioxidant activity was determined by DPPH, Nitric oxide scavenging and FRAP methods. Phytotoxicity was performed by Lemna minor assay and analyzed relative to control with effective dose (ED50) to determine FI50 values (concentration necessary to inhibit 50 % frond proliferation) and 65 % confidence intervals. Urease inhibitory activity was assessed at a concentration of 125 μg/mL by Berthelot reaction with slight modification. Total phenolic contents were calculated with reference to gallic acid equivalent and confirmed by Folin and Ciocalteau’s phenol method. Total flavonoid was determined with reference to quercetin.Results: The DPPH and hydroxyl radical scavenging activities of the methanol extract were 93.35 %. The phytotoxicity of the methanol extract was 90 % growth regulation while the anti-urease inhibitory activity was 91.1 % with half-maximal inhibitory concentration (IC50) of 49.1 ± 1.3 μg/mL. Total flavonoid contents of dichloromethane extract was 629.4 ± 1.57 μg/mL. The phenolic content of the extract calculated with reference to quercetin, gallic acid, chlorogenic acid, ferulic acid and 4-hydroxy 3-methoxy benzoic acid equivalent was 45.772, 9.779, 70.304, 74.93 and 57.80 ppm, respectively.Conclusion: The results confirm that Conocarpus lancifolius extracts possess some antioxidant, phytotoxicity and anti-urease potentials due to its phenolic and flavonoid contents.Keywords: Antioxidant, Phenolics, Falvonoids, Phytotoxicity, Anti- urease, Conocarpus lancifoliu

Determination of the anti-diabetic effect of methanolic extract of Sphaeranthus indicus L. on alloxan induced diabetic rabbits

The aim of present study was to determine the anti-diabetic effect of methanolic extract of Sphaeranthus indicus L. (SMe) in alloxan induced diabetic rabbits. It was further aimed to determine the effect of SMe on various biochemical parameters, namely blood glucose levels, total cholesterol, lipoproteins (HDL and LDL), liver functions (SGOT and SGPT), serum creatinine and urea level in alloxan induced diabetic rabbits. Rabbits were divided into five groups: one non-diabetic control, treated with vehicle and four experimental (diabetic) groups. The experimental groups can be described as diabetic negative control, treated with vehicle, diabetic positive control, treated with 80 mg/kg of diamicron, a reference drug; and diabetic treated with 150 or 300 mg/kg of SMe. Pre- and post-experimental lipid profile, liver function and kidney function of rabbits was determined. The SMe at the dose of 300 mg/Kg body weight significantly (p 0.05).Colegio de Farmacéuticos de la Provincia de Buenos Aire

Determination of the anti-diabetic effect of methanolic extract of Sphaeranthus indicus L. on alloxan induced diabetic rabbits

The aim of present study was to determine the anti-diabetic effect of methanolic extract of Sphaeranthus indicus L. (SMe) in alloxan induced diabetic rabbits. It was further aimed to determine the effect of SMe on various biochemical parameters, namely blood glucose levels, total cholesterol, lipoproteins (HDL and LDL), liver functions (SGOT and SGPT), serum creatinine and urea level in alloxan induced diabetic rabbits. Rabbits were divided into five groups: one non-diabetic control, treated with vehicle and four experimental (diabetic) groups. The experimental groups can be described as diabetic negative control, treated with vehicle, diabetic positive control, treated with 80 mg/kg of diamicron, a reference drug; and diabetic treated with 150 or 300 mg/kg of SMe. Pre- and post-experimental lipid profile, liver function and kidney function of rabbits was determined. The SMe at the dose of 300 mg/Kg body weight significantly (p 0.05).Colegio de Farmacéuticos de la Provincia de Buenos Aire

Antidiabetic activity of aqueous extract of Sigesbeckia orientalis (St. Paul’s Wort) in alloxan-induced diabetes model

The current study evaluated antidiabetic and antihyperlipidemic activities of aqueous extract of Sigesbeckia orientalis L. (St. Paul’s Wort) (AESO) in an alloxan-induced diabetic rat model. Following OECD guidelines safe doses of AESO were assessed in rats for the main study. Serum/bood glucose, α-amylase, and lipids levels and histopathological evaluations were conducted to assess antidiabetic and associated antihyperlipidemic efficacies of AESO. AESO was found to be safe up to the dose of 2000 mg/kg. Significant (p < 0.05) reduction in glucose and lipids (total cholesterol, triglycerides, low‑density lipoproteins) levels was observed in AESO treatment groups. Serum α-amylase, high‑density lipoproteins, and total body weight was increased significantly (p < 0.05) in diabetic rats treated with AESO. Histopathological data showed improvement in hepatocyte and pancreatic β-cells islets architecture. HPLC analysis identified quercetin, gallic acid, vanillic acid, p-coumaric acid, m-coumaric acid and cinnamic acid in AESO which are suggested to be responsible for observed antihyperglycemic and antihyperlipidemic attributes. Further studies to standardise the extract and evaluation of safety profile in long-term toxicity studies are recommended for safe and effective antidiabetic nutraceuticals development

Determination of the anti-diabetic effect of methanolic extract of Sphaeranthus indicus L. on alloxan induced diabetic rabbits

The aim of present study was to determine the anti-diabetic effect of methanolic extract of Sphaeranthus indicus L. (SMe) in alloxan induced diabetic rabbits. It was further aimed to determine the effect of SMe on various biochemical parameters, namely blood glucose levels, total cholesterol, lipoproteins (HDL and LDL), liver functions (SGOT and SGPT), serum creatinine and urea level in alloxan induced diabetic rabbits. Rabbits were divided into five groups: one non-diabetic control, treated with vehicle and four experimental (diabetic) groups. The experimental groups can be described as diabetic negative control, treated with vehicle, diabetic positive control, treated with 80 mg/kg of diamicron, a reference drug; and diabetic treated with 150 or 300 mg/kg of SMe. Pre- and post-experimental lipid profile, liver function and kidney function of rabbits was determined. The SMe at the dose of 300 mg/Kg body weight significantly (p 0.05).Colegio de Farmacéuticos de la Provincia de Buenos Aire

Immunomodulatory, antiglycation and anti-ulcerative properties of Ruellia squarrosa Fenzl Acanthaceae

Purpose: To evaluate the immunomodulatory, antiglycation and anti-ulcerative properties of Ruellia squarrosa Fenzl. Acanthaceae.Methods: Aerial parts and roots of Ruellia squarrosa were collected and extracted by maceration using dichloromethane and methanol as solvents. Luminol-enhanced chemiluminescence assay was used to evaluate immunomodulatory activity while antiglycation assay was performed by fluorescence method with rutin as standard. Anti-ulcerative activity was evaluated by enzymatic methods, namely, urease inhibition and carbonic anhydrase inhibition assays.Results: Dichloromethane extract showed immunomodulatory activity with half-maximal inhibitory concentration (IC50) of 39.48 ± 8.06 % using ibuprofen as standard and antiglycation effect (IC50 = 382.21 ± 3.43) using rutin as standard. The methanol extract of the aerial parts of the plant showed urease inhibition activity (IC50 = 130.2 ± 0.57) using thiourea as standard. The methanol extract of the aerial parts of the plant also showed carbonic anhydrase inhibition activity (IC50 = 1656.7 ± 0.08) using acetazolamide as standard.Conclusion: It was concluded from the present study that aerial and root extracts of the Ruellia squarrosa have significant immunomodulatory, antiglycation and anti-ulcerative properties.Keywords: Ruellia squarrosa, Immunomodulatory, Antiglycation, Anti-ulcerative activity, Carbonic anhydrase inhibition, Ureas

Pharmacological evaluation of the hypoglycemic and anti- Alzheimer’s activities of aerial parts of Breynia distachia (Phyllanthaceae)

Purpose: To determine the cytotoxic, bronchorelaxant, spasmolytic, antidiabetic, α-glucosidase, acetylcholinesterase, butyrylcholinesterase, α-chymotrypsin and lipoxygenase inhibitory attributes of methanol and dichloromethane extracts of the aerial parts of Breynia distachia.Methods: The dichloromethane and methanol extracts of the aerial parts of the plant were prepared by maceration. Various ex vivo assays were employed, such as the brine shrimp lethality assay, lipoxygenase inhibitory activity assay, α-glucosidase inhibitory assay and α-chymotrypsin assay, as well as assays to assess the spasmolytic and bronchorelaxant activity. Meanwhile, the hypoglycaemic effect were analysed using an alloxan-induced diabetic model in Wistar albino rats.Results: The methanol extract (aerial) showed significant (p ≤ 0.05) cytotoxicity towards brine shrimp larvae at concentrations of 10, 100 and 1,000 μg/mL, respectively, whereas the dichloromethane extract (aerial) of the plant showed non-significant (p ≥ 0.05) results. The methanol extract (aerial parts) also demonstrated significant (p ≤ 0.05) α-glucosidase inhibitory activity and lipoxygenase inhibitory activity, with IC50 (half-maximal inhibitory concentration) values of 40.37 ± 5.29 μg/mL and 132.9 ± 0.33 μg/mL, respectively, while the dichloromethane extract exhibited significant (p ≤ 0.05) α-glucosidase inhibitory activity, with an IC50 value of 135.43 ± 8.29 μg/mL. An in vivo antidiabetic model showed that the administration of 150 and 300 mg/kg methanol extract of the aerial parts significantly (p ≤ 0.05) lowered the blood glucose level in alloxan-induced diabetic rats compared to control (treated with water).Conclusion: Data from different in vitro and in vivo models suggest that the methanol extract (aerial parts) of B. distachia shows significant cytotoxic, bronchorelaxant, spasmolytic, antidiabetic and anti-Alzheimer’s activity Hence, these findings validate the folkloric use of B. distachia and highlight the need to further explore its medicinal potential and the phytoconstituents responsible for its pharmacological actions

Cytotoxic and antioxidant potentials of ellagic acid derivatives from Conocarpus lancifolius (Combretaceae)

Purpose: Isolation, characterisation and structure elucidation of compounds obtained from Conocarpus lancifolius and screening of their pharmacological effects in vitro.Methods: After collection, authentication and extraction from whole C. lancifolius plants, screening for secondary metabolites, thin-layer  chromatography and subsequent open column chromatography were performed for phytochemical analysis and subsequent purification of the compounds. The chemical structures of the isolated compounds were elucidated using spectroscopic (UV-visible, infrared and mass) spectroscopy, and nuclear magnetic resonance (1H-NMR, 13C-NMR including BB, DEPT-135, 90 and two-dimensional correlation techniques, including HMBC and HSQC). The cytotoxic and antioxidant potentials of extracts and compounds obtained from C. lancifolius were evaluated using in vitro models.Results: Two ellagic acid derivatives, 2,3,8-tri-o-methylellagic acid (A) and 3-O-methylellagic acid 4-O-β-D-glucopyranoside (B), were isolated. Both compounds (A and B) were cytotoxic in a variety of cancer cell lines, including murine lymphocytic leukaemia (P-388, half-maximal inhibitory concentration (IC50) =3.60 and 2.40 μg/mL, respectively), human colon cancer (Col-2, IC50 = 0.76 and 0.92 μg/mL, respectively) and human breast cancer (MCF-7, IC50 = 0.65 and 0.54 μg/mL, respectively). Moreover, both compounds showed significant antioxidant potential in vitro.Conclusion: C. lancifolius extract and isolated ellagic acid derivatives (compounds A and B) possess cytotoxic and antioxidant properties. These findings suggest that C. lancifolius contains bioactive compounds that can be potentially developed as natural cytotoxic and antioxidant compounds. Keywords: Conocarpus lancifolius, Ellagic acid, Combretaceae, Cytotoxic activity, Antioxidan

A pH-responsive bi-MIL-88B MOF coated with folic acid-conjugated chitosan as a promising nanocarrier for targeted drug delivery of 5-Fluorouracil

Cancer has remained one of the leading causes of death worldwide, with a lack of effective treatment. The intrinsic shortcomings of conventional therapeutics regarding tumor specificity and non-specific toxicity prompt us to look for alternative therapeutics to mitigate these limitations. In this regard, we developed multifunctional bimetallic (FeCo) bi-MIL-88B-FC MOFs modified with folic acid—conjugated chitosan (FC) as drug delivery systems (DDS) for targeted delivery of 5-Fluorouracil (5-FU). The bi-MIL-88B nanocarriers were characterized through various techniques, including powder X-ray diffraction, scanning electron microscopy, energy-dispersive X-ray, thermogravimetric analysis, and Fourier transform infrared spectroscopy. Interestingly, 5-FU@bi-MIL-88B-FC showed slower release of 5-FU due to a gated effect phenomenon endowed by FC surface coating compared to un-modified 5-FU@bi-MIL-88B. The pH-responsive drug release was observed, with 58% of the loaded 5-FU released in cancer cells mimicking pH (5.2) compared to only 24.9% released under physiological pH (5.4). The in vitro cytotoxicity and cellular internalization experiments revealed the superiority of 5-FU@bi-MIL-88B-FC as a highly potent targeted DDS against folate receptor (FR) positive SW480 cancer cells. Moreover, due to the presence of Fe and Co in the structure, bi-MIL-88B exhibited peroxidase-like activity for chemodynamic therapy. Based on the results, 5-FU@bi-MIL-88B-FC could serve as promising candidate for smart DDS by sustained drug release and selective targeting

Revamping of Chronic Respiratory Diseases in Low- and Middle-Income Countries

Low- and middle-income countries (LMICs) endure an asymmetrically high burden of worldwide disease and death caused by chronic respiratory diseases (CRDs), i.e., asthma, emphysema, bronchiectasis, and post-tuberculosis lung disease (PTLD). CRDs are firmly related with indigence, infectious diseases, and other non-communicable diseases (NCDs) and add to complex multi-disease with great impact on the lives and livelihood of those affected. The pertinence of CRDs to health and demographic wellbeing is relied upon to increment in the long time ahead, as expectations of life rise and the contending dangers of right on time youth mortality and irresistible infections level. The WHO has distinguished the counteraction and control of NCDs as an earnest improvement issue and crucial for the sustainable development goals (SDSs) by 2030. In this review, we center on CRDs in LMICs. We examine the early life roots of CRDs, challenges in their avoidance, identification and administration in LMICs, and the pathways to resolve for accomplish valid widespread wellbeing inclusion