scholarly journals Unravelling the Biological Activities of the Byttneria pilosa Leaves Using Experimental and Computational Approaches

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4737
Author(s):  
Mifta Ahmed Jyoti ◽  
Niloy Barua ◽  
Mohammad Shafaet Hossain ◽  
Muminul Hoque ◽  
Tahmina Akter Bristy ◽  
...  
Keyword(s):  
Protein Denaturation ◽  
Biological Activities ◽  
Significant Inhibition ◽  
Biologically Active ◽  
Dependent Inhibition ◽  
Anti Inflammatory ◽  
Isolated Compound ◽  
Dose Dependent

Byttneria pilosa is locally known as Harijora, and used by the native hill-tract people of Bangladesh for the treatment of rheumatalgia, snake bite, syphilis, fractured bones, elephantiasis and an antidote for poisoning. The present study was carried out to determine the possible anti-inflammatory, analgesic, neuropharmacological and anti-diarrhoeal activity of the methanol extract of B. pilosa leaves (MEBPL) through in vitro, in vivo and in silico approaches. In the anti-inflammatory study, evaluated by membrane stabilizing and protein denaturation methods, MEBPL showed a significant and dose dependent inhibition. The analgesic effect of MEBPL tested by inducing acetic acid and formalin revealed significant inhibition of pain in both tests. During the anxiolytic evaluation, the extract exhibited a significant and dose-dependent reduction of anxiety-like behaviour in mice. Similarly, mice treated with MEBPL demonstrated dose-dependent reduction in locomotion effect in the open field test and increased sedative effect in the thiopental sodium induced sleeping test. MEBPL also showed good anti-diarrheal activity in both castor oil induced diarrheal and intestinal motility tests. Besides, a previously isolated compound (beta-sitosterol) exhibited good binding affinity in docking and drug-likeliness properties in ADME/T studies. Overall, B. pilosa is a biologically active plant and could be a potential source of drug leads, which warrants further advanced study.

Anti-Inflammatory Steroids, Lysosomal Stabilization and Parachor

1975 ◽  
Vol 53 (10) ◽  
pp. 1047-1053 ◽  
Author(s):  
Parvez Ahmad ◽  
Colin A. Fyfe ◽  
Alan Mellors
Keyword(s):  
Partition Coefficients ◽  
Biological Activities ◽  
Biologically Active ◽  
Structure Activity ◽  
Assay Methods ◽  
Anti Inflammatory ◽  
Direct Proportionality ◽  
In Vivo Administration

Parachor is an additive constitutive property of a molecule and is related to the molar volume and the surface tension. The parachor of a steroid can be calculated from its constituent atoms and bonds. The parachor of a biologically active molecule is related to the ability of that molecule to permeate hydrophobic regions of cells, especially cellular membranes. An examination of the parachor values of a large number of steroids shows that these values are correlated with a number of different biological activities, from independent sources. The ability of steroids to release lysosomal enzymes from isolated lysosomes in vitro is inversely related to the parachor of the steroid. A similar relationship holds for the release of lysosomal β-glucuronidase (EC 3.2.1.31) from isolated lysosomes of rat preputial gland following in vivo administration of steroids. The relative anti-inflammatory potencies of steroids by several assay methods are directly proportional to their parachors. The relative ability of corticosteroids to uncouple oxidative phosphorylation and to swell isolated mitochondria in vitro show a direct proportionality with the steroidal parachor. The percutaneous absorptions of steroids show good correlation with parachors, stratum corneum – water partition coefficients and amylcaproate–water partition coefficients; but not with hexadecane–water partition coefficients. The application of parachor as a structure–activity correlation parameter in drug design is likely to yield useful information. The advantages and limitations of the calculated parachor method are discussed.

scholarly journals Investigation of the Biological Activities and Characterization of Bioactive Constituents of Ophiorrhiza rugosa var. prostrata (D.Don) & Mondal Leaves through In Vivo, In Vitro, and In Silico Approaches

Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1367 ◽  
Author(s):  
Md. Adnan ◽  
Md. Nazim Uddin Chy ◽  
A.T.M. Mostafa Kamal ◽  
Md Azad ◽  
Arkajyoti Paul ◽  
...  
Keyword(s):  
Biological Activities ◽  
Gastrointestinal Transit ◽  
Ethanol Extract ◽  
Indigenous Communities ◽  
Antibacterial Activities ◽  
Significant Inhibition ◽  
Bioactive Constituents ◽  
Anti Inflammatory

Ophiorrhiza rugosa var. prostrata is one of the most frequently used ethnomedicinal plants by the indigenous communities of Bangladesh. This study was designed to investigate the antidiarrheal, anti-inflammatory, anthelmintic and antibacterial activities of the ethanol extract of O. rugosa leaves (EEOR). The leaves were extracted with ethanol and subjected to in vivo antidiarrheal screening using the castor oil-induced diarrhea, enteropooling, and gastrointestinal transit models. Anti-inflammatory efficacy was evaluated using the histamine-induced paw edema test. In parallel, in vitro anthelmintic and antibacterial activities were evaluated using the aquatic worm and disc diffusion assays respectively. In all three diarrheal models, EEOR (100, 200 and 400 mg/kg) showed obvious inhibition of diarrheal stool frequency, reduction of the volume and weight of the intestinal contents, and significant inhibition of intestinal motility. Also, EEOR manifested dose-dependent anti-inflammatory activity. Anthelmintic action was deemed significant (P < 0.001) with respect to the onset of paralysis and helminth death. EEOR also resulted in strong zones of inhibition when tested against both Gram-positive and Gram-negative bacteria. GC-MS analysis identified 30 compounds within EEOR, and of these, 13 compounds documented as bioactive showed good binding affinities to M3 muscarinic acetylcholine, 5-HT3, tubulin and GlcN-6-P synthase protein targets in molecular docking experiments. Additionally, ADME/T and PASS analyses revealed their drug-likeness, likely safety upon consumption and possible pharmacological activities. In conclusion, our findings scientifically support the ethnomedicinal use and value of this plant, which may provide a potential source for future development of medicines.

scholarly journals Scrutinizing pharmacological efficiency for Acacia auriculiformis by experimental and computational approach

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Shafinaz Nur ◽  
Md. Mohotasin Hossain ◽  
Nadia Islam ◽  
Abu Montakim Tareq ◽  
Nujhat Binte Hanif ◽  
...  
Keyword(s):  
Protein Denaturation ◽  
Acacia Auriculiformis ◽  
Dependent Manner ◽  
Binding Interaction ◽  
Standard Drug ◽  
Brine Shrimp Lethality Assay ◽  
Anti Inflammatory ◽  
Dose Dependent

Abstract Background The study sought to investigate the biological efficacy of methanol leave extract of Acacia auriculiformis (MEAA) via in vitro, in vivo, in silico approaches. The in vitro cytotoxicity was evaluated through brine shrimp lethality assay, and anti-inflammatory activity was determined by membrane stabilisation and protein denaturation methods (BSA and egg albumin). The in vivo antipyretic activity was examined via Brewer’s yeast induced pyrexia model. Results A. auriculiformis extract unveiled moderate cytotoxicity with significant anti-inflammatory efficacy (p < 0.001) compared to standard drug. This extract also exhibited dose-dependent time of paralysis and death for the worm (p < 0.001) in the anthelmintic test which was directly proportional to employed concentrations. A notable percentage of clot lysis effect (36.42 ± 1.95%, p < 0.001) was also observed for MEAA in human blood compared to control. However, this extract significantly (p < 0.05) reduced fever in a dose-dependent manner during the antipyretic experiment. Besides, in computer-aided investigations, two compounds (2,4-ditert-butylphenol and 3-hydroxy-β-damascone) revealed the best binding interaction with six proteins for cytotoxicity, inflammation, helminthic, thrombolytic and pyretic effect. Moreover, these two compounds satisfy Lipinski’s ‘Rule of Five’ and revealed drug-likeness profiles in the toxicological study. Conclusions These findings disclosed that methanol leaves extract of A. auriculiformis might be a potent source for anti-inflammatory, anti-helminthic, thrombolytic and antipyretic agents.

scholarly journals In-vitro anti-inflammatory activity and anti-arthritic activity of ethyl acetate extracts of Skimmia anquetilia leaves

2020 ◽  
pp. 42-44
Author(s):  
Poonam Verma ◽  
Baljinder Singh ◽  
Amarjit Kaur ◽  
Vijender Kumar
Keyword(s):  
Ethyl Acetate ◽  
Protein Denaturation ◽  
Diclofenac Sodium ◽  
Maximum Effect ◽  
Membrane Stabilization ◽  
Dependent Inhibition ◽  
Dose Dependent Inhibition ◽  
Anti Inflammatory ◽  
Dose Dependent

Current investigations were carried out for the validation of in-vitro anti-inflammatory and anti-arthritic property of leaves of Skimmia anquetilia using red blood cells membrane stabilization and protein denaturation methods respectively. Defatted ethylacetate extracts at different concentration levels (50, 100, 200 and 400 mg/ml) were used in these studies. Dose dependent inhibition of protein denaturation was found 92.41% at 400 mg/ml of extracts and 96.21 % at 100 mg/ml of acetyl salicylic acid as standard in antiarthritic study. Similarly, in membrane stabilization methods, maximum effect found 90.70 % at 400 mg/ml of extracts and 94.88 % at 100 mg/ml of diclofenac sodium as standard for anti-inflammatory evaluation. The results concluded that, ethyl acetate extract of S. anquetilia leaves has shown significant (*aP<0.05) anti-inflammatory and anti-arthritic effects.

scholarly journals In vitro and in vivo biological activities of azulene derivatives with potential applications in medicine

2021 ◽  
Author(s):  
Paweł Bakun ◽  
Beata Czarczynska-Goslinska ◽  
Tomasz Goslinski ◽  
Sebastian Lijewski
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Biologically Active ◽  
Peptic Ulcers ◽  
Artemisia Absinthium ◽  
Potential Applications ◽  
Anti Inflammatory ◽  
Unique Chemical

AbstractAzulene is an aromatic hydrocarbon that possesses a unique chemical structure and interesting biological properties. Azulene derivatives, including guaiazulene or chamazulene, occur in nature as components of many plants and mushrooms, such as Matricaria chamomilla, Artemisia absinthium, Achillea millefolium, and Lactarius indigo. Due to physicochemical properties, azulene and its derivatives have found many potential applications in technology, especially in optoelectronic devices. In medicine, the ingredients of these plants have been widely used for hundreds of years in antiallergic, antibacterial, and anti-inflammatory therapies. Herein, the applications of azulene, its derivatives and their conjugates with biologically active compounds are presented. The potential use of these compounds concerns various areas of medicine, including anti-inflammatory with peptic ulcers, antineoplastic with leukemia, antidiabetes, antiretroviral with HIV-1, antimicrobial, including antimicrobial photodynamic therapy, and antifungal.

Metabolomics of Healthy Berry Fruits

2019 ◽  
Vol 25 (37) ◽  
pp. 4888-4902 ◽  
Author(s):  
Gilda D'Urso ◽  
Sonia Piacente ◽  
Cosimo Pizza ◽  
Paola Montoro
Keyword(s):  
Biological Activities ◽  
Biologically Active ◽  
In Vivo Studies ◽  
Bioactive Metabolites ◽  
Active Metabolites ◽  
Positive Effects ◽  
Cell Functions ◽  
Berry Fruits

The consumption of berry-type fruits has become very popular in recent years because of their positive effects on human health. Berries are in fact widely known for their health-promoting benefits, including prevention of chronic disease, cardiovascular disease and cancer. Berries are a rich source of bioactive metabolites, such as vitamins, minerals, and phenolic compounds, mainly anthocyanins. Numerous in vitro and in vivo studies recognized the health effects of berries and their function as bioactive modulators of various cell functions associated with oxidative stress. Plants have one of the largest metabolome databases, with over 1200 papers on plant metabolomics published only in the last decade. Mass spectrometry (MS) and NMR (Nuclear Magnetic Resonance) are the most important analytical technologies on which the emerging ''omics'' approaches are based. They may provide detection and quantization of thousands of biologically active metabolites from a tissue, working in a ''global'' or ''targeted'' manner, down to ultra-trace levels. In the present review, we highlighted the use of MS and NMR-based strategies and Multivariate Data Analysis for the valorization of berries known for their biological activities, important as food and often used in the preparation of nutraceutical formulations.

Fibrinolytic, Anti-Inflammatory and Cytotoxic Potentialities of Extracts and Chemical Constituents of Manglicolous Lichen, Graphis ajarekarii Patw. & C. R. Kulk

2020 ◽  
Vol 10 (1) ◽  
pp. 87-93 ◽  
Author(s):  
Vinay Bharadwaj Tatipamula ◽  
Girija Sastry Vedula
Keyword(s):  
Protein Denaturation ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Fibrin Clot ◽  
Hydroalcoholic Extract ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

Background: Lichens which are betide to mangroves are termed as Manglicolous Lichens (ML). As these ML are habituated under stress conditions, they are screened for unique metabolites and biological activities. Objective: The study aimed to establish the chemical and biological profile of ML, Graphis ajarekarii. Methods: The Ethyl Acetate Extract of G. ajarekarii (EAE) was subjected to chromatographic techniques and the obtained isolates were characterized by spectroscopic analysis. The hydroalcoholic extract of G. ajarekarii (AE), EAE, isolates and Hydroalcoholic Extract of host (HE) were evaluated for fibrinolytic (fibrin clot method), in vitro (protein denaturation method) and in vivo (formalin-induced rat paw oedema assay), anti-inflammatory and cytotoxicity (MTT assay) activities. Results: Chemical investigation of the EAE led to the isolation of two known compounds namely atranorin (1) and ribenone (2), which were confirmed by spectral data. The AE and EAE gradually lysed the fibrin clot with 94.54 and 65.07%, respectively, at 24 h. The AE inhibited protein denaturation of about 88.06%, while the standard (Indomethacin) with 93.62%. Similarly, the in vivo antiinflammatory analysis of AE (200 mg/mL) showed potent reduction of rat paw oedema than the standard, whereas EAE and 1 depicted moderate depletion. In addition, the AE revealed prominence inhibition on MCF-7, DU145 and K-562 with IC50 values of 69.5, 42.5 and 38 µg/mL, respectively, whereas the HE exhibited mild inhibitory profile against fibrin clot, inflammation and cancer. Conclusion: From the results, it can be concluded that the G. ajarekarii has an aptitude to act against coagulation, inflammation and cancer cells.

scholarly journals Sesquiterpene Lactones: Promising Natural Compounds to Fight Inflammation

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 991
Author(s):  
Melanie S. Matos ◽  
José D. Anastácio ◽  
Cláudia Nunes dos Santos
Keyword(s):  
Biological Activities ◽  
Sesquiterpene Lactones ◽  
Physiological State ◽  
Plant Secondary Metabolites ◽  
Inflammatory Pathways ◽  
Inflammatory State ◽  
Anti Inflammatory ◽  
Inflammatory Molecules

Inflammation is a crucial and complex process that reestablishes the physiological state after a noxious stimulus. In pathological conditions the inflammatory state may persist, leading to chronic inflammation and causing tissue damage. Sesquiterpene lactones (SLs) are composed of a large and diverse group of highly bioactive plant secondary metabolites, characterized by a 15-carbon backbone structure. In recent years, the interest in SLs has risen due to their vast array of biological activities beneficial for human health. The anti-inflammatory potential of these compounds results from their ability to target and inhibit various key pro-inflammatory molecules enrolled in diverse inflammatory pathways, and prevent or reduce the inflammatory damage on tissues. Research on the anti-inflammatory mechanisms of SLs has thrived over the last years, and numerous compounds from diverse plants have been studied, using in silico, in vitro, and in vivo assays. Besides their anti-inflammatory potential, their cytotoxicity, structure–activity relationships, and pharmacokinetics have been investigated. This review aims to gather the most relevant results and insights concerning the anti-inflammatory potential of SL-rich extracts and pure SLs, focusing on their effects in different inflammatory pathways and on different molecular players.

scholarly journals ANTI-INFLAMMATORY ACTIVITY OF CURCUMIN AND CAPSAICIN AUGMENTED IN COMBINATION

2017 ◽  
Vol 9 (6) ◽  
pp. 145
Author(s):  
Thriveni Vasanth Kumar ◽  
Manjunatha H. ◽  
Rajesh Kp
Keyword(s):  
Acetic Acid ◽  
Protective Effect ◽  
Vascular Permeability ◽  
Diclofenac Sodium ◽  
Significant Inhibition ◽  
Inflammatory Activity ◽  
Anti Inflammatory ◽  
The Individual

Objective: Dietary curcumin and capsaicin are well known for their health beneficial potencies. The current study was done to assess the anti-inflammatory activity of curcumin, capsaicin and their combination by employing in vitro and in vivo models.Methods: We investigated the protective effect of curcumin, capsaicin and their combination using in vitro heat induced human red blood cell (HRBC) membrane stabilisation, in vivo 3% agar induced leukocyte mobilisation and acetic acid induced vascular permeability assay.Results: Curcumin, capsaicin and their combination exhibited concentration dependent protective effect against heat-induced HRBC membrane destabilisation, while combined curcumin and capsaicin restored 87.0±0.64 % membrane stability and it is found to be better than curcumin, capsaicin and diclofenac sodium (75.0±0.25. 72±0.9 and 80.0±0.31 %) protective effect. In agar suspension induced leukocyte mobilization assay, the combined curcumin and capsaicin had shown 39.5±1.58 % of inhibition compared to individual curcumin and capsaicin, which showed moderate inhibition of 16.0±3.14 and 21.6±2.17 % respectively. Besides, the combined curcumin and capsaicin had shown highly significant inhibition of acetic acid-induced vascular permeability in rats (62.0±3.14 %), whereas individual curcumin and capsaicin showed moderate inhibition of vascular permeability with 36.0±2.41 and 43.0±1.92 % respectively.Conclusion: This study demonstrates the significant anti-inflammatory property of combined curcumin and capsaicin at half of the individual concentration of curcumin and capsaicin.

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