Standard Acetyl Salicylic Acid Research Articles

Evaluation of In-vitro Anti-Inflammatory, Anti-Fungal, Thrombolytic, Membrane Stabilizing and Cytotoxic Properties of (Camellia chrysantha Hu Tuyama)

The current study was set out to look into the anti-inflammatory, anti-fungal, cytotoxic, thrombolytic and membrane stabilizing activities of the methanolic extract from the leaf of Camellia chrysantha (Hu) Tuyama (MECCL). Primary evaluation of MECCL was performed via phytochemical screening. Phytochemical analysis of the leaf extract revealed the presence of reducing sugar, flavonoids, alkaloids, and steroids. Anti-inflammatory activity test was done using egg albumin denaturation assay. In the result of MECCL’s anti-inflammatory test showed 88.88% compared to the standard acetyl salicylic acid 98.56%. The anti-fungal activity test was performed by Disc Diffusion method using zone of inhibition against four fungi. MECCL showed moderate antifungal activity compared to standard Griseofulvin against Aspergillus niger, Saccharomyces cerevisiae (yeast), Penicillium notatum. Zones of inhibition of the fungi Aspergillus niger, Saccharomyces cerevisiae (yeast), Penicillium notatum is 11mm, 14mm and 14mm at the concentration of 700 µg/disc, which is close to the standard Griseofulvin 19mm, 20mm, and 21mm respectively at 50 µg/disc concentration. Mucor hiemalis showed mild zone of inhibition in 300, 500, and 700 µg/disc (7mm). Brine Shrimp lethality bioassay method was used to test the lethality of the methanolic leaf extract. The extract showed significant cytotoxic activity against brine shrimp nauplii with LC50 value of 0.843 µg/mL when compared with the standard Vincristine sulphate (LC50 value: 0.608 µg/mL). Comparison with positive control Vincristine sulphate signifies that cytotoxicity exhibited by MECCL and further bioactivity guided investigation can be done to find potent antitumor compounds. In thrombolytic activity test, MECCL demonstrated 95.69% thrombolysis which was significant compared to standard Streptokinase (SK) which demonstrated 91.304 % thrombolysis. While doing membrane stabilizing activity test, Heat induced hemolysis assay was performed and the percent of protection was 85.35 compared to the standard DS 73.63 which was very significant. The results highlight the potential of Camellia chrysantha (Hu) Tuyama as a valuable source of phytochemicals that possess notable anti-inflammatory, thrombolytic, and membrane-stabilizing properties. The methanolic leaf extract also shows moderate antifungal and cytotoxic effects, suggesting potential for future therapeutic advancements.

Antiinflammatory Activity of Syzygium Caryophy Llatum and Syzygium Nervosum (Myrtaceae)

In the present study examined, the anti-inflammatory potential of aqueous, hexane, ethyl acetate and ethanolic leaf extracts of Syzygium caryophyllatum and Syzygium nervosum (Family: Myrtaceae) was carried out according to method of Mizushima et al (1968) and Sakat et al (2010) with slight modifications. The absorbance was checked at 660nm against the blank. Acetyl Salicylic acid was used as positive control and water as negative control. The experiment was performed in triplicates for all the test samples. Percentage of inhibition was calculated. Our results indicate that the leaf extracts of Syzygium caryophyllatum and Syzygium nervosum were showed potent anti-inflammatory activity than the standard Acetyl Salicylic acid.

GC-MS and HPTLC bioautography-based phytochemical profiling and evaluation of biological activity Neptunia prostrata Linn whole plant and leaves

This work used experimental methods to evaluate the chemical composition of GC-MS, HPTLC-based bioautographaphy, antioxidant, anti-diabetic, and protein denaturation properties of the Neptunia prostrata Linn (family: Mimosaceae) whole plant and leaves. Three methods, namely DPPH, metal chelating, and reducing power assays, were used to estimate the antioxidant effects. In addition, α-amylase, a carbohydrate-hydrolyzing enzyme, was targeted to test the anti-diabetic activity. The protein denaturation assay was used to evaluate the anti-inflammatory activity of the plant. GC-MS, an important analytical tool, was performed to identify bioactive compounds of medicinal plants used in pharmaceutical industries. Biochemical derivatization HPTLC-based bioautography with DPPH was executed to identify antioxidant agents from N. prostrata. The validated HPTLC method was used to quantify identified antioxidant agents. The stability of compounds, preparation of calibration curves, linearity, range, precision, limit of detection, limit of quantification, robustness, and accuracy are examined to develop a robust method. Higher total phenolic content (TPC) content was observed in N. prostrata hydroalcoholic extract of the whole plant (81.12 ± 4.19 mg GAE/g) and methanolic extract of leaves (105.16 ± 3.11 mg GAE/g). Methanolic extract of N. prostrata leaves showed significantly high antioxidant potential for all DPPH (IC50:28.05 ± 1.78 µg/mL), metal chelating (IC50:1598 ± 23.51 µg/mL), and reducing power assay compared to standard ascorbic acid (DPPH assay: IC50:24.14 ± 2.34 µg/mL and metal chelating: IC50:1301.16 ± 6.14 µg/mL). N. prostrata aqueous extract of the whole plant (IC50:179.47 ± 10.59 µg/mL) and leaves (IC50:130.86 ± 3.58 µg/mL) showed significantly high α-amylase inhibitory activity as compared to standard acarbose (IC50:148.62 ± 7.84 µg/mL). Methanolic extract of whole plants (IC50:131.46 ± 11.81 µg/mL) and chloroform extract of leaves (IC50:122.61 ± 8.19 µg/mL) exhibited strong anti-inflammatory activity as compared to standard acetylsalicylic acid (IC50:117.77 ± 4.95 µg/mL). GC-MS analysis revealed the presence of several bioactive compounds, where 2-cyclopenten-1-one, 2-hydroxy showed the most abundant bioactive compounds in the plant with 17.01%. HPTLC-bioautography identified three phenolic acids (chlorogenic acid, gallic acid, and 4-hydroxybenzoic acid) and one flavonoid (naringenin), further quantified with the validated HPTLC method. These findings propose that N. prostrata has therapeutic potential for treating diseases related to oxidative damage, diabetes, and inflammation, which may be due to the presence of bioactive compounds.

Chemical Profiling and Antioxidant, Anti-Inflammatory, Cytotoxic, Analgesic, and Antidiarrheal Activities from the Seeds of Commonly Available Red Grape (Vitis vinifera L.).

The current study aimed to conduct a phytochemical screening of commonly known fruit red grape (Vitis vinifera L.) seed methanolic extract through gas chromatography and mass spectrometry (GC-MS) to identify the bioactive compounds responsible for its health benefits and evaluate the pharmacological potentialities of the extract and its fractions against oxidation, inflammation, pain, and diarrhea. The in vitro antioxidant, anti-inflammatory, and cytotoxic characteristics of methanolic extracts and various solvent fractions of V. vinifera were evaluated using the DPPH free radical scavenging assay, membrane stabilizing, and brine shrimp lethality bioassay. Furthermore, the study assessed the effects of crude extracts (200, 400, and 600 mg/kg of body weight) on pain relief and reduction of diarrhea in animals using methods such as tail immersion, the acetic acid-induced writhing technique, and a diarrheal mouse model induced with castor oil. A total of 73 phytoconstituents were predominantly found in the seed extract based on the GC-MS analysis. Among the identified compounds, 9-octadecenamide (13.7%), and (9E,11E)-octadeca-9,11-dienoate (11.07%) are most abundant. Several notable constituents, such as gamma-sitosterol, stigmasterol, paromomycin, 4,6-cholestadienol, gamma-tocotrienol, 24-Propylidenecholest-5-en-3beta-ol, and alpha-tocopherol acetate, are also present. The methanolic extract of V. vinifera seed and its different solvent fractions showed promising antioxidant properties (IC50 = 1.19-17.42 µg/mL) compared to the standard antioxidant butylated hydroxytoluene (IC50 = 20.46 µg/mL). Aqueous soluble fraction exerted inhibition of nearly 50% heat-induced hemolysis compared to the standard acetylsalicylic acid (42%). Besides, all the tested doses (200, 400, and 600 mg/kg bw) of the crude extract showed significant (P < .05) analgesic and antidiarrheal effects. The current findings endorsed the health benefits of V. vinifera by revealing potent antioxidant, anti-inflammatory, analgesic, and antidiarrheal effects. Nevertheless, further in-depth analysis of the plant's chemical constituents and pharmacological effects on health is warranted for novel drug discovery from V. vinifera.

Unveiling the therapeutic potential: Evaluation of anti-inflammatory and antineoplastic activity of Magnolia champaca Linn’s stem bark isolate through molecular docking insights

Magnolia champaca Linn. has traditionally been used for medicinal activity in Asia for treating various chronic diseases as well as a source of food, medicines, and other commodities. Due to the long-used history of this plant, the present study was designed to explore the in vitro, in vivo and in silico anti-inflammatory and antineoplastic properties of the methanolic extract and fractions and the pure compound isolated from the most active chloroform fraction (CHF) of the stem bark of the plant. The isolated compound from the most active CHF was characterized and identified as a glycoside, trans-syringin, through chromatographic and spectroscopic (1H-NMR and 13C-NMR) analyses. In the in vitro anti-inflammatory assay, CHF was most effective in inhibiting inflammation and hemolysis of RBCs by 73.91 ± 1.70% and 75.92 ± 0.14%, respectively, induced by heat and hypotonicity compared to standard acetylsalicylic acid. In the egg albumin denaturation assay, CME and CHF showed the highest inhibition by 56.25 ± 0.82% and 65.82 ± 3.52%, respectively, contrasted with acetylsalicylic acid by 80.14 ± 2.44%. In an in vivo anti-inflammatory assay, statistically significant (p < 0.05) decreases in the parameters of inflammation, such as paw edema, leukocyte migration and vascular permeability, were recorded in a dose-dependent manner in the treated groups. In the antineoplastic assay, 45.26 ± 2.24% and 68.31 ± 3.26% inhibition of tumor cell growth for pure compound were observed compared to 73.26 ± 3.41% for standard vincristine. Apoptotic morphologic alterations, such as membrane and nuclear condensation and fragmentation, were also found in EAC cells after treatment with the isolated bioactive pure compound. Such treatment also reversed the increased WBC count and decreased RBC count to normal values compared to the untreated EAC cell-bearing mice and the standard vincristine-treated mice. Subsequently, in silico molecular docking studies substantiated the current findings, and the isolated pure compound and standard vincristine exhibited −6.4 kcal/mol and −7.3 kcal/mol binding affinities with topoisomerase-II. Additionally, isolated pure compound and standard diclofenac showed −8.2 kcal/mol and −7.6 kcal/mol binding affinities with the COX-2 enzyme, respectively. The analysis of this research suggests that the isolated bioactive pure compound possesses moderate to potent anti-inflammatory and antineoplastic activity and justifies the traditional uses of the stem bark of M. champaca. However, further investigations are necessary to analyze its bioactivity, proper mechanism of action and clinical trials for the revelation of new drug formulations.

Chemico-pharmacological and computational studies of Ophiorrhiza fasciculata D. Don and Psychotria silhetensis Hook. f. focusing cytotoxic, thrombolytic, anti-inflammatory, antioxidant, and antibacterial properties

The current study sought to examine the pharmacological potentials of crude methanolic extracts of Ophiorrhiza fasciculata and Psychotria silhetensis, as well as their various solvent fractionates, with a focus on cytotoxic, thrombolytic, membrane stabilizing, antioxidant, and antibacterial activities via in vitro and in silico approaches. The extensive chromatographic and spectroscopic analyses confirmed and characterized two compounds as (±)-licarin B (1) and stigmasterol (2) from O. fasciculata and P. silhetensis, respectively. Petroleum ether soluble fraction of O. fasciculata and the aqueous soluble fraction of P. silhetensis showed the lowest 50% lethal concentrations (1.41 and 1.94 μg/mL, respectively) in brine shrimp bioassay. Likewise, petroleum ether soluble fraction of O. fasciculata and aqueous soluble fraction of P. silhetensis showed the highest thrombolytic activity with 46.66% and 50.10% lyses of the clot, respectively. The methanol and dichloromethane soluble fractions of O. fasciculata reduced erythrocyte hemolysis by 64.03% and 37.08%, respectively, under hypotonic and heat-induced conditions, compared to 81.97% and 42.12% for standard acetylsalicylic acid. In antioxidant activity test, aqueous soluble fraction O. fasciculata (IC50 = 7.22 μg/mL) revealed promising antioxidant potentialities in comparison to standard butylated hydroxytoluene (IC50 = 21.20 μg/mL). In antibacterial screening, chloroform, and dichloromethane soluble fractions of P. silhetensis showed a mild antibacterial activity compared with the standard drug ciprofloxacin. Additionally, the molecular docking study corroborated the current in vitro findings, and the isolated two constituents had higher binding affinities toward epidermal growth factor receptor, tissue plasminogen activator, vFLIP-IKK gamma stapled peptide dimer, glutathione reductase, and dihydrofolate reductase enzyme than their corresponding standard drugs. In addition, the both isolated compounds exerted favorable pharmacokinetics (absorption, distribution, metabolism, excretion) and toxicological profiles with drug-like qualities in computational-based ADMET and drug likeliness analyses. The current research suggests that both plants have potential as a natural treatment for treating thrombosis, inflammation, and oxidative stress. However, more thorough research is required to thoroughly screen for phytochemicals and pinpoint the precise mechanisms of action of the bioactive metabolites derived from these plants against a broad range of molecular targets.

Physalis peruviana L. fruit metabolome profiling via HR-UPLC/MS and its in vitro antiarthritic activity

Physalis peruviana is an edible fruit becoming of increasing economic interest for its nutritional and beneficial health effects that even several countries targeted its cultivation recently to fulfill export demands taking the advantage of its adaptable nature to different soil types. Despite previous reports on its chemical content, little or no studies used metabolomics to reveal its chemical reservoir. Herein, the first comprehensive metabolome profiling of P. peruviana fruits via HR-UPLC/MS in both ionization modes that enabled detection of 71 metabolites including first-time reported compounds belonging to flavonoids, coumarins and withanolides. Additionally, 43 lipoidal compounds were identified via GC/MS and quantification of fat-/water-soluble vitamins was performed via HPLC. New evidence on its crude extract antiarthritic activity is presented as well for the first time using bovine serum albumin as it significantly inhibited protein denaturation at 500µg/ml and 1000µg/ml by 86.5± 0.422 % and 99.49 ± 0.426 %, respectively compared to 78.72 ± 1.23% and 97.80 ± 0.393 % for the standard drug acetyl salicylic acid at the same concentration, respectively, with comparable IC 50 values of 246.35 µg/ml and 229.69 µg/ml for the extract and standard drug, respectively; supporting its folk use in treatment of arthritis. • First metabolome profiling of Physalis peruviana fruit primary and secondary metabolites. • 71 metabolites were detected via HR-UPLC/MS including several first reported compounds that belong to flavonoids, withanolides and coumarins. • Total ethanol fruit extract possesses significant antarthritic activity via inhibition of protein denaturation supporting its folk use in treatment of arthritis.

Chemical, Biological &amp; Pharmacological Investigations of Different Fractional Extracts of Passiflora edulis Sims. (Family: Passifloraceae)

In the evaluation of antimicrobial activity, antibacterial activity of ethanol, chloroform &amp; n-hexane extracts of P. edulis was tested against 10 bacteria at concentrations of 500µg/disc. Standard antibiotic disc of Azithromycin (30 µg/disc) was used for the comparison. The extracts showed no activity against gm (+ve) &amp; gm (-ve) bacteria at a concentration of 500 µg/disc. Antifungal activity of ethanol, chloroform &amp; n-hexane extracts of P. edulis was tested against 7 fungi at concentrations of 500µg/disc. Standard antifungal disc of Fluconazole (30 µg/disc) was used for the comparison. In antifungal screening the chloroform extract showed activity against A. fumigatus (15nm). In DPPH scavenging assay the ethanol extract of leaves showed maximum % inhibition of 73.41% at 100μg/ml while the standard ascorbic acid showed % inhibition of 82.14% at the same concentration. The DPPH radical scavenging activity was increased by increasing the concentration of the sample extract. The extract exhibited considerable DPPH free radical scavenging activity as indicated by their IC50 values which indicate the potency of scavenging activity. Standard ascorbic acid was found to have an IC50 of 1.66μg/ml. In comparison to standard ascorbic acid, ethanol extract of P. edulis showed of an IC50 of 2.57μg/ml. In the evaluation of anti-inflammatory activity by albumin denaturation assay method, the percent inhibition of protein denaturation in the experiment of ethanol extract of leaves of P. edulis was found to be 55.454% at 500μg/ml, 49.818% at 250μg/ml and 41.818% at 125μg/ml. The extract possesses significant activity comparable with that of the standard acetyl salicylic acid which showed percent inhibition of protein denaturation of 91.945%, 88.181% and 45.454% in the same concentration range. In this analgesic activity study using Eddy’s hot plate method in mice, the ethanol extract of P. edulis showed mild analgesic activity. After 30 minutes of administration of standard drug (Diclofenac 9 mg/kg), mean latency was found to be 17.34sec. While the extract at concentration of 400 mg/kg exposed mean latency of 6.67sec. Respectively. During antipyretic activity by Brewer’s yeast induced pyrexia method in mice, the ethanol extract of leaves of P. edulis produced moderate antipyretic activity. In this test, the extract reduced temperature from 102.4°F to 99.84°F (p=0.151188), 98.74°F (p=0.070485), 98.6℉ (p=0.056108), 98.37℉ (p=0.039072) and 98.27°F (p=0.110528) in 1st, 2nd, 3rd, 4th and 5th hour respectively and caused maximum reduction of temperature in 1st hour. During antidiarrhoeal activity by castor oil induced test in mice, the ethanol extract of P. edulis produced moderate antidiarrheal episode. The latent period and the total diarrheic faces were found to be 0.978 hr &amp; 8.34 at 500 mg/kg for P. edulis as compared to standard (Loperamide 3mg/kg) 2.845 hr &amp; 5.34. In the sedative and hypnotic activity by using open field box, hole cross box and swing Test method on swiss albino mice ethanol extract of P. edulis showed moderate sedative and hypnotic activity. During the open field test, squares crossed by the group receiving standard Diazepam and ethanol extract of leaves of P. edulis were 63 and 84.34 respectively. During the swing test, number of swings observed after administration of standard Diazepam and ethanol extract of leaves of P. edulis were 3.67 and 8.67 respectively. During diuretic activity by using the Lipschitz test in mice, ethanol, n-hexane and chloroform extracts of P. edulis (500mg/kg body wt.) showed no activity compared to standard drug Furosemide (20mg/kg body wt.)

Biological potential of Moluccella laevis L. aerial parts, family Lamiaceae (Labiatae)

The current study aimed to determine the various in vivo biological activities of Moluccella laevis L. aerial parts. The anti-inflammatory activity demonstrated after two h, for both the total ethanolic extract (TEE) and the petroleum ether (pet. ether) fraction, exhibited the same percentage of inhibition (26.24%) as that of the indomethacin, whereas the following hour showed results quite higher than that of the positive control. Additionally, the TEE showed higher antipyretic activity compared to the used standard acetylsalicylic acid with a rapid onset (30 min) and a longer duration exhibiting the maximum activity. After four h from the beginning of the experiment, the pet. ether, ethyl acetate (EtOAc) and aqueous fractions displayed nearly the same effect as that of acetylsalicylic acid, which lasted up to five h. Moreover, the aqueous fraction exhibited the maximum analgesic activity with a rapid onset and a longer duration followed by the pet. ether fraction, TEE and the EtOAc fraction. These activities could be explained by the presence of the highest amount of phenolic and flavonoidal contents, which are found in both EtOAc fraction and TEE. Due to the pronounced results of M. laevis L. aerial parts, it can be considered as a success of natural products in further drug discovery.

Anti-inflammatory potential of ethanol leaf extract of Sphenocentrum jollyanum in experimental mice

Anti-inflammatory potential of the ethanol leaf extract of Sphenocentrum jollyanum (ELESJ) was assessed in-vivo in mice by using carrageenan-induced paw oedema, egg albumin-induced paw oedema, and xylene-induced ear oedema model at doses of 474.34, 948.68, and 1423.03 mg/kgbw respectively. A total of seventy-five matured mice of both sexes weighing between 20 g and 24 g (divided into three groups of 25 mice each for the 3 different studies) were used for this study. Treatment was done intraperitoneally. Distilled water (10 mL/kgbw), acetylsalicylic acid (ASA) (100 mg/kgbw) or dexamethasone (4 mg/kgbw) served as the normal and standard drugs respectively. The results showed that ELESJ produced significant (p &lt; 0.05), dose-dependent and time-dependent reductions in mean paw thickness in groups III-V compared with control group. Similarly, the extract caused a dose-dependent increase in percentage inhibition of carrageenan-induced paw oedema and egg-albumin induced paw oedema (34.49%, 36.71%) at the highest dose (1423.03 mg/kg), comparable with the anti-inflammatory effects of the standard drug ASA (34.69%, 31.54%). The ELESJ also caused significant (p &lt; 0.05), dose-dependent decreases in xylene-induced ear oedema weight in all the test groups relative to control group and standard drug group. In addition, ELESJ showed a dose-dependent percentage inhibitory effect (44%) at the highest dose (1423.03 mg/kg) comparable with that of the standard drug, dexamethasone (48%). The results obtained from this study support the use of the leaf in folk medicine as it has significant anti-inflammatory properties and this may be attributed to the phytochemical constituents of the leaf.

Curcumin: Natural Antimicrobial and Anti Inflammatory Agent

The pursuance of novel antimicrobial and anti-inflammatory agents has been expanding due to a significant need for more efficient pharmacotherapy of various infections and chronic diseases. During the last decade, pharmacokinetics, pharmacodynamics and pharmacological properties of curcumin have been extensively studied. The aim of the present study was to evaluate the antibacterial activity of curcumin against both Gram-positive and Gram-negative bacteria as well as its antifungal activity by using in vitro agar well diffusion assay. Moreover, the anti-inflammatory activity of curcumin was determined with in vitro assay of inhibition of protein denaturation. Results demonstrated wide antimicrobial activity of curcumin upon all of the test bacteria and fungi. The strongest activity of curcumin was observed at a concentration of 0.50 mg/ml against S. aureus, L. monocytogenes, E. coli, P. aeruginosa and C. albicans, resulting in a maximum zone of inhibition of 14.7 mm, 14.3 mm, 13.7 mm, 10.7 mm and 10.7 mm, respectively. Findings suggested that the antimicrobial activity of curcuminis dependent upon the concentrations. Furthermore, results demonstrated high effectiveness of curcumin compared to standard acetylsalicylic acid in inhibiting heat-induced protein denaturation, which activity is also depended upon the concentrations. The present study emphasises the potential application of curcumin as a natural antimicrobial and anti-inflammatory agent. However, findings of this study are restricted to in vitro assays and consideration should be given to conducting a study involving wider dose range test substances as well as including further research on in vivo models.

Stem extract of Albizia richardiana exhibits potent antioxidant, cytotoxic, antimicrobial, anti-inflammatory and thrombolytic effects through in vitro approach

BackgroundAlbizia richardiana belongs Fabaceae family which different parts like fruits, flowers, barks, and roots are used medicinally. The study reports the in vitro anti-inflammatory, thrombolytic, cytotoxicity and antimicrobial activity of methanolic extract of A. richardiana stem and its different fractions.MethodThe methanolic extract of A. richardiana stem (MEAR) extracted with n-hexane (HXFAR), carbon tetrachloride (CTFAR), chloroform (CFAR), and aqueous (AQFAR) and subjected for DPPH scavenging activity and total phenol content (TPC). The cytotoxic activity evaluated by brine shrimp lethality bioassay, while the disk diffusion method used for the antimicrobial study. The anti-inflammatory and thrombolytic activities of the extracts evaluated by the hypotonic solution induced hemolysis, heat-induced hemolysis and human blood clot lysis, respectively.ResultsAll the extracts exhibited excellent antioxidant activity in the DPPH scavenging assay and maximum total phenol content observed by HXFAR. Secondly, the extract showed a moderate LC50 value in brine shrimp lethality bioassay, where the CTFAR extract exhibited potential antimicrobial activities against sixteen different microorganisms. In anti-inflammatory, all the extract exhibited a significant (P < 0.0001) protection against lysis of human erythrocyte membrane induced by heat and hypotonic solution, as compared to the standard acetyl salicylic acid. An extremely significant (P < 0.0001) clot lysis was found in MEAR (16.66%) while the standard drug streptokinase (70.94%).ConclusionAll the fractions revealed the significant free radical scavenging activity. Moreover, CTFAR showed wide spectrum of antimicrobial activity. Thus, the results of the present study provided scientific evidence for the use of Albizia richardiana as traditional medicine.

Vachellia farnesiana (L.) Wight &amp; Arn. Growing in Bangladesh Exerts In-vitro Antioxidant and In-vivo Analgesic and Anti-diarrheal Activities

The present study was conducted to evaluate the antioxidant, antidiarrheal and analgesic activities of Vachellia farnesiana (L.) Wight &amp; Arn. The methanol extract of V. farnesiana and its different fractionates were subjected to in-vitro assay for the determination of total phenolic content and antioxidative potential. The ethyl acetate soluble fraction (EASF) exhibited the highest free radical scavenging capacity (IC50 value of 21.49 ± 1.04 μg/ml) as compared to that exhibited by the standard butylated hydroxyl toluene (BHT) (IC50 value of 20.41 ± 0.05 μg/ml). Such prominent antioxidative potential was further reinforced by a phenolic content of 39.26 ± 0.85 mg of gallic acid equivalent per gram of extract. The plant extract, at the dose of 400 mg/kg body weight, reduced castor oil-induced diarrhea in mice model by a statistically significant (p &lt; 0.05) margin of 47.62%, while the standard loperamide produced 66.67% reduction of diarrheal feces. The central and peripheral analgesic activities of the crude methanol extract of V. farnesiana (MEVF) was determined by tail flick- and acetic acidinduced writhing methods, respectively, in Swiss albino mice. In the tail flick method, oral administration of MEVF at doses of 200 and 400 mg/kg body weight exhibited 221.09 and 237.09% elongation of pain response time, respectively, after 90 minutes of administration whereas the standard morphine effectuated 518.34% elongation within the same time. Furthermore, the same doses of the extract illustrated 63.27 and 69.39% reductions, respectively, in the acetic acid-induced abdominal constrictions in mice. Compared to the standard acetylsalicylic acid with 75.51% inhibition, statistically significant (p &lt; 0.05) peripheral analgesic activity was established. The results of the present investigations suggest that methanol extract of V. farnesiana possesses antioxidant, antidiarrheal and analgesic activities which eventually indicates the presence of biologically important phytoconstituents within the plant that needs further exploration. Bangladesh Pharmaceutical Journal 23(2): 181-186, 2020

Antidiarrheal and Analgesic Activities of Bouea oppositifolia (Roxb.) Adelb. in Experimental Animal Model

The current study was designed to evaluate the antidiarrheal and analgesic activities of the methanol extract of Bouea oppositifolia (Roxb.) Adelb. leaves through iv vivo studies in Swiss Albino mice. Oral administration of the extract at doses of 200- and 400-mg/kg of body weight demonstrated statistically significant (p &lt; 0.05) antidiarrheal activities in castor oil-induced diarrheal mice. The extracts and standard loperamide alleviated diarrhea by margins of 31.82-, 45.45- and 68.17%, respectively. Potential of the plant extract to effectuate analgesia was ascertained both centrally and peripherally. In tail immersion method for the determination of central analgesic activity, the plant extract at both doses enhanced pain tolerance to maximum extents of 192.76% and 221.09%, respectively, compared to standard morphine (419.57%) after 90 minutes of sample administration. Comparable levels of central analgesia were also observed for both doses of the plant extracts at 30 and 60 minutes of pharmacological intervention and the p value of less than 0.05 illustrated statistical significance of the activity. On a similar note, potent peripheral analgesic activities were observed for both doses of the extract as evident by 45.45- and 54.55% inhibitions of acetic acid induced writhing responses, respectively. Compared to the standard acetylsalicylic acid characterized by 78.18% inhibition, the peripheral analgesic activity of the plant was found to be statistically significant (p &lt; 0.05). The results of the study are indicative of the presence of potentially bioactive phytoconstituents with antidiarrheal and analgesic properties which might lead to newer drug candidates in future. Bangladesh Pharmaceutical Journal 23(2): 167-171, 2020

Phytol anti-inflammatory activity: Pre-clinical assessment and possible mechanism of action elucidation

Phytol (PHY) is an acyclic natural diterpene alcohol and a chlorophyll constituent that exhibits several pharmacological effects, such as anticancer, antioxidant, and antimicrobial. Here, we aimed to assess the PHY anti-inflammatory effect in vitro and in vivo, and to deepen knowledge on the possible mechanism of action. For this purpose, egg albumin (in vitro) test was performed by using acetyl salicylic acid (ASA) as a standard nonsteroidal anti-inflammatory drugs (NSAID). For in vivo test, male Wistar albino rats were treated (intraperitoneally) with 100 mg/kg of PHY and/or standard NSAIDs ASA (100 mg/kg) and diclofenac sodium (Diclo-Na, 10 mg/kg) to evaluate the combined effect of PHY in formalin-induced paw edema model. Furthermore, an in silico (CADD) study was accomplished to assess the effect of PHY against cyclooxygenase (COX)-1 and 2 enzymes, nuclear factor kappa B (NF-κB), and interleukin-1β (IL-1β). Results revealed that PHY exhibits dose-dependent anti-inflammatory effect using the egg albumin method. PHY (100 mg/kg) co-treated with ASA and/or Diclo-Na reduced paw edema better than PHY alone or NSAIDs individual groups. Computational study showed that PHY efficiently interacts with COX-1 and 2, NF-κB, and IL-1β. In conclusion, PHY exhibits anti-inflammatory activity, possibly via COX-1 and 2, NF-κB, and IL-1β dependent pathways.

Once- versus Twice-Daily Aspirin in Patients at High Risk of Thrombotic Events: Systematic Review and Meta-Analysis.

Acetylsalicylic acid (ASA) is a frequently used antiplatelet agent, although some individuals have reduced antiplatelet responses on ASA, with recurrent ischemic events. It has been proposed that shortening the ASA dosing interval may overcome the time-dependent renewal of the drug target, leading to a greater antiplatelet effect. We conducted a systematic review of randomized controlled trials (RCTs) to determine the efficacy of once- versus twice-daily ASA in conditions with increased platelet turnover. We conducted a systematic review and meta-analysis by searching the CENTRAL, MEDLINE, and Embase databases for RCTs assessing once- versus twice-daily ASA. Data were screened, extracted, and appraised by two independent reviewers, and were pooled using a random-effects model. The primary outcomes were major adverse cardiovascular events (MACEs) and serum thromboxane B2 (TxB2). Other pharmacodynamic measures were retrieved as secondary outcomes. Results were reported as mean differences with corresponding 95% confidence intervals (CIs). We followed the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) guidelines. Seven RCTs were included, enrolling 379 participants overall. None of the studies reported clinical outcomes. Pooled results showed that compared with once-daily ASA, twice-daily ASA was associated with a decrease in mean TxB2 of 1.42ng/mL (95% CI - 2.71 to - 0.13; I2=66%). We found no differences in subgroup analyses based on disease subtype, trial blinding, or trial design. A greater antiplatelet activity of the twice-daily regimen was also found when using PFA-100-ADP methods, although not when using the VerifyNow, LTA-AA, and multiplate methods. Twice-daily ASA was associated with a greater antiplatelet effect compared with standard once-daily ASA.

Total phenolic and flavonoid contents and antioxidant, anti-inflammatory, analgesic, antipyretic and antidiabetic activities of Cordia myxa L. leaves

BackgroundMany plants of genus Cordia are traditionally used as astringent, anti-inflammatory, anthelminthic, antimalarial, diuretic, febrifuge, appetite suppressant and cough suppressant and to treat urinary infections, lung diseases and leprosy. The aim of the study is to determine the total phenolic and flavonoid contents of total ethanol extract and different fractions of C. myxa L. leaves, in addition to evaluation of some pharmacological activities including antioxidant, anti-inflammatory, analgesic, antipyretic and antidiabetic effects.MethodsAir dried powder of C. myxa leaves were extracted using 95% ethanol and fractionated successively with petroleum ether, dichloromethane, ethyl acetate and finally with n-butanol. The fractions were concentrated and then investigated for their antioxidant, anti-inflammatory, analgesic, antipyretic and antidiabetic activities using phosphomolybidinum and DPPH assays, carrageenan-induced paw edema, hot plate, yeast -induced pyrexia and streptozotocin-induced hyperglycemia methods, respectively.ResultsThe ethyl acetate fraction showed the highest antioxidant activity with high phenolic and flavonoid contents (31.03 ± 0.15 mg gallic acid equivalent/g dried weight and 811.91 ± 0.07 mg rutin equivalent/g dried weight, respectively). Dichloromethane and ethyl acetate fractions exhibited higher anti-inflammatory activity with percentages of inhibition 45.16% and 40.26%, respectively, which were quite comparable to that of indomethacin (51.61%). The petroleum ether and dichloromethane fractions showed the highest analgesic activity with reaction time 289.00 ± 3.00 and 288.33 ± 20.82, respectively. Evaluation of antipyretic activity revealed that the total ethanol extract and different fractions showed high antipyretic activities after 2 h, which were very close to that of the standard acetyl salicylic acid with a rapid onset (30 min). The total ethanol extract and the petroleum ether fraction exhibited the most potent hypoglycemic effect with a significant reduction in blood glucose level especially after 3 h to 95.67 ± 5.77 mg/dl and 87.67 ± 10.26 mg/dl, respectively and percentages decrease in blood glucose level were 68.22% and 70.78%, respectively.ConclusionCordia myxa L. extract and fractions exhibited antioxidant, anti-inflammatory analgesic, antipyretic and antidiabetic activities which may be attributed by the presence of active phytoconstituents.

Analgesic, Anti-diarrheal, CNS-depressant, Membrane Stabilizing and Cytotoxic Activities of Canavalia virosa (Roxb.) W&amp;A

The methanol extract of the leaves of Canavalia virosa (Roxb.) W&amp;A was investigated for the evaluation of analgesic, anti-diarrheal and CNS-depressant activities in Swiss albino mice. The analgesic activity was assessed by formalin-induced paw licking method, where the crude extract of C. virosa (400 mg/kg, b.w.) exhibited 41.46% reduction of licking response in mice as compared to 73.17% reduction exhibited by standard acetylsalicylic acid. In the castor oil-induced diarrhea in mice, the plant extract at the dose of 200 mg/kg, b.w., demonstrated 56% reduction of diarrheal feces in mice, while the standard loperamide revealed 76% reduction of diarrheal feces. The CNS-depressant activity of the plant extract was assessed through phenobarbitone-Na induced sleeping time test. The methanol extract of C. virosa and its different Kupchan fractions were also subjected to screen membrane stabilizing and cytotoxic activities using acetylsalicylic acid and vincristine sulphate as standard, respectively. Bangladesh Pharmaceutical Journal 22(2): 214-218, 2019

Analgesic, Anti-diarrheal, Anti-depressant, Membrane Stabilizing and Cytotoxic Activities of Bridelia verrucosa Haines

The present study was aimed for the evaluation of analgesic, anti-diarrheal and anti-depressant activities of methanol crude extract of Bridelia verrucosa leaves in Swiss albino mice. The analgesic activity was assessed by formalin-induced paw licking method, where the crude extract of B. verrucosa (400 mg/kg, b.w.) exhibited 54.55% reduction of licking response in mice as compared to 69.09% reduction exhibited by standard acetylsalicylic acid. In the castor oil-induced diarrhea in mice, the plant extract at the dose of 400 mg/kg, b.w., demonstrated 57.67% reduction of diarrheal feces in mice. The antidepressant activity of the plant extract was evaluated through phenobarbitone-Na induced sleeping time test. The methanol extract of B. verrucosa and its different Kupchan fractions were also subjected to screenings for membrane stabilizing and cytotoxic activities using acetylsalicylic acid and vincristine sulphate as standard, respectively. Bangladesh Pharmaceutical Journal 22(1): 50-55, 2019

Stereospermum suaveolens (Roxb.) DC. Shows Potential in vivo and in vitro Bioactivities

The methanol extract of Stereospermum suaveolens (Roxb.) DC was investigated for antidiabetic, antidiarrheal and analgesic activities in Swiss Albino mice. Antidiabetic activity was evaluated by oral glucose tolerance test where the crude extract of S. suaveolens (400 mg/kg b.w.) exhibited 56.10% reduction of blood glucose level as compared to 58.53% by standard glibenclamide (0.1 mg/kg b.w.). In the castor oil-induced diarrhea in mice, the plant extract, at the dose of 400 mg/kg b.w. demonstrated 42.11% reduction of diarrheal feces, while the standard loperamide revealed 57.89% reduction of diarrheal feces. The analgesic activity of S. suaveolens was assessed by both radiant heat tail-flick and acetic acid-induced writhing test. The methanolic extract and different Kupchan fractions of S. suaveolens were also subjected to screening for total phenolic content, DPPH free radical scavenging assay, membrane stabilizing, thrombolytic and antimicrobial activities. In the DPPH assay, the aqueous soluble fraction of methanolic extract revealed highest antioxidant properties with IC50 value of 18.99 μg/ml. The membrane stabilizing activity was assessed by hypotonic solution- and heat-induced methods and was compared with standard acetyl salicylic acid. In hypotonic solution-induced haemolysis, the hexane and carbon tetrachloride soluble fraction inhibited 54.42% and 52.67% haemolysis of RBCs, respectively. On the other hand, in heat-induced haemolysis, the chloroform soluble fraction inhibited the haemolysis of RBC by 57.10% as compared to 72.09% produced by acetyl salicylic acid. In antimicrobial assay by disc diffusion method, only the hexane and carbon tetrachloride soluble fractions demonstrated moderate antimicrobial activity (zone of inhibition = 7.0-15.0 mm) against the test organisms.&#x0D; Dhaka Univ. J. Pharm. Sci. 17(2): 257-263, 2018 (December)