Anti-Allergic, Anti-Inflammatory and Anti-Hyperglycemic Activity of Chasmanthe aethiopica Leaf Extract and Its Profiling Using LC/MS and GLC/MS

This study aims to comprehensively explore the phytoconstituents as well as investigate the different biological activities of Chasmanthe aethiopica (Iridaceae) for the first time. Metabolic profiling of the leaf methanol extract of C. aethiopica (CAL) was carried out using HPLC-PDA-ESI-MS/MS. Twenty-nine compounds were annotated belonging to various phytochemical classes including organic acids, cinnamic acid derivatives, flavonoids, isoflavonoids, and fatty acids. Myricetin-3-O-rhamnoside was the major compound identified. GLC/MS analysis of the n-hexane fraction (CAL-A) resulted in the identification of 45 compounds with palmitic acid (16.08%) and methyl hexadecanoic acid ester (11.91%) representing the major constituents. CAL-A exhibited a potent anti-allergic activity as evidenced by its potent inhibition of β-hexosaminidase release triggered by A23187 and IgE by 72.7% and 48.7%, respectively. Results were comparable to that of dexamethasone (10 nM) in the A23187 degranulation assay showing 80.7% inhibition for β-hexosaminidase release. Both the n-hexane (CAL-A) and dichloromethane (CAL-B) fractions exhibited potent anti-inflammatory activity manifested by the significant inhibition of superoxide anion generation and prohibition of elastase release. CAL showed anti-hyperglycemic activity in vivo using streptozotocin-induced diabetic rat model by reducing fasting blood glucose levels (FBG) by 53.44% as compared with STZ-treated rats along with a substantial increase in serum insulin by 22.22%. Molecular modeling studies indicated that dicaffeoylquinic acid showed the highest fitting with free binding energies (∆G) of −47.24 and −60.50 Kcal/mol for human α-amylase and α-glucosidase, respectively confirming its anti-hyperglycemic activity. Thus, C. aethiopica leaf extract could serve as an effective antioxidant natural remedy combating inflammation, allergy, and hyperglycemia.

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Antidiabetic potential of the leaf extract of Centella asiatica in alloxaninduced diabetic rats

Jahangirnagar University Journal of Biological Sciences ◽

10.3329/jujbs.v4i1.27785 ◽

2016 ◽

Vol 4 (1) ◽

pp. 51-59 ◽

Cited By ~ 2

Author(s):

Talha Bin Emran ◽

Mycal Dutta ◽

Mir Muhammad Nasir Uddin ◽

Aninda Kumar Nath ◽

Md Zia Uddin

Keyword(s):

Body Weight ◽

Leaf Extract ◽

Total Cholesterol Level ◽

Serum Insulin ◽

Fasting Blood Glucose ◽

Centella Asiatica ◽

Liver Glycogen ◽

Diabetic Control ◽

Diabetic Rats ◽

Diabetic Rat

The study was designed to evaluate the glucose and cholesterol lowering effect of the aqueous extract of Centella asiatica leaf using the alloxan-induced diabetic rats and compared the activity with diabetic control and antidiabetic drug (Glibenclamide). Leaf extract (50 mg/kg) of C. asiatica and Glibenclamide were administered to normal and experimental diabetic rats for the duration of 10 days. In the alloxan-induced diabetic rat model, C. asiatica extract (50 mg/kg) significantly (p < 0.05) lowered the fasting blood glucose level as well as the total cholesterol level. Serum insulin levels were not stimulated in the animals treated with the extract. In addition, changes in body weight, serum lipid profiles and liver glycogen levels assessed in the extract treated diabetic rats were compared with diabetic control and normal animals. Significant results (p < 0.05) were observed in the estimated parameters. Surprisingly, body weight was increased significantly (p < 0.05) in the C. asiatica treated diabetic group. Phytochemical screening showed the presence of alkaloids, flavonoids, glycosides, steroids and tannins in significant amountsJahangirnagar University J. Biol. Sci. 4(1): 51-59, 2015 (June)

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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 ◽

10.3390/molecules24071367 ◽

2019 ◽

Vol 24 (7) ◽

pp. 1367 ◽

Cited By ~ 25

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.

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Puerarin Improves Diabetic Aorta Injury by Inhibiting NADPH Oxidase-Derived Oxidative Stress in STZ-Induced Diabetic Rats

Journal of Diabetes Research ◽

10.1155/2016/8541520 ◽

2016 ◽

Vol 2016 ◽

pp. 1-9 ◽

Cited By ~ 17

Author(s):

Wenping Li ◽

Wenwen Zhao ◽

Qin Wu ◽

Yuanfu Lu ◽

Jingshan Shi ◽

...

Keyword(s):

Nadph Oxidase ◽

Colorimetric Assay ◽

Serum Insulin ◽

Fasting Blood Glucose ◽

Serum Levels ◽

Rat Aorta ◽

Diabetic Rats ◽

Diabetic Rat ◽

Positive Staining ◽

Glucose Levels

Objective.Puerarin is a natural flavonoid isolated from the TCM lobed kudzuvine root. This study investigated the effect and mechanisms of puerarin on diabetic aorta in rats.Methods.Streptozotocin- (STZ-) induced diabetic rats were administered with puerarin for 3 weeks. Levels of serum insulin (INS), PGE2, endothelin (ET), glycated hemoglobin (GHb), H2O2, and nitric oxide (NO) in rats were measured by ELISA and colorimetric assay kits. The aortas were stained with H&E. Moreover, the mRNA expression of ICAM-1, LOX-1, NADPH oxidase 2 (NOX2), and NOX4 and the protein expression of ICAM-1, LOX-1, NF-κB p65, E-selectin, NOX2, and NOX4 in aorta tissues were measured by real-time PCR and Western blot, respectively. The localization of ICAM-1, NF-κB p65, NOX2, and NOX4 in the aorta tissues was also determined through immunohistochemistry.Results.Puerarin treatment exerted no effect on fasting blood glucose levels but significantly reduced the serum levels of INS, GHb, PGE2, ET, H2O2, and NO. In addition, puerarin improved the pathological alterations and inhibited the expression of ICAM-1, LOX-1, NOX2, and NOX4 at both mRNA and protein levels. Puerarin also significantly reduced the number of cells showing positive staining for ICAM-1, NOX2, NOX4, and NF-κB p65.Conclusion.Puerarin demonstrated protective effect on the STZ-induced diabetic rat aorta. The protective mechanisms may include regulation of NF-κB and inhibition of NOX2 and NOX4 followed by inhibition of cell adhesion molecule expression.

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

Molecules ◽

10.3390/molecules25204737 ◽

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.

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Design, Synthesis, Characterization and in silico molecular docking studies and in vivo anti-inflammatory Activity of Pyrazoline clubbed Thiazolinone Derivatives

Letters in Organic Chemistry ◽

10.2174/1570178617999201106113114 ◽

2020 ◽

Vol 17 ◽

Author(s):

Deepak Kumar Singh ◽

Mayank Kulshreshtha ◽

Yogesh Kumar ◽

Pooja A Chawla ◽

Akash Ved ◽

...

Keyword(s):

Molecular Docking ◽

Biological Activities ◽

Inflammatory Activity ◽

Standard Drug ◽

Docking Score ◽

Chemical Structures ◽

Cox 2 ◽

Anti Inflammatory ◽

Cox 1

Background: The pyrazolines give the reactions of aliphatic derivatives, resembling unsaturated compounds in their behavior towards permanganate and nascent hydrogen. This nucleus has been associated with various biological activities including inflammatory. Thiazolinone is a heterocyclic compound that contains both sulfur and nitrogen atom with a carbonyl group in their structure.Thiazolinone and their derivatives have attracted continuing interest because of their various biological activities, such as anti-inflammatory, antimicrobial, anti-proliferative, antiviral, anticonvulsant etc. The aim of the research was to club pyrazoline nucleus with thiazolinone in order to have significantanti-inflammatory activity. The synthesized compounds were chemically characterized for the establishment of their chemical structures and to evaluate as anti-inflammatory agent. Method: In the present work, eight derivatives of substituted pyrazoline (PT1-PT8) were synthesized by a three step reaction.The compounds were subjected to spectral analysis by Infrared, Mass and Nuclear magnetic resonance spectroscopy and elemental analysis data. All the synthesized were evaluated for their in vivo anti-inflammatory activity. The synthesized derivatives were evaluated for their affinity towards target COX-1 and COX-2, using indomethacin as the reference compound molecular docking visualization through AutoDock Vina. Results: Compounds PT-1, PT-3, PT-4 and PT-8 exhibited significant anti-inflammatory activity at 3rd hour being 50.7%, 54.3%, 52.3% and 57% respectively closer to that of the standard drug indomethacin (61.9%).From selected anti-inflammatory targets, the synthesized derivatives exhibited better interaction with COX-1 and COX-2 receptor, where indomethacin showed docking score of -6.5 kJ/mol, compound PT-1 exhibited highest docking score of -9.1 kJ/mol for COX-1 and compound PT-8 having docking score of 9.4 kJ/mol for COX-2. Conclusion: It was concluded that synthesized derivatives have more interaction with COX-2 receptors in comparison to the COX-1 receptors because the docking score with COX-2 receptors were very good. It is concluded that the synthesized derivatives (PT-1 to PT-8) are potent COX-2 inhibitors.

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

The Natural Products Journal ◽

10.2174/2210315508666180604101813 ◽

2020 ◽

Vol 10 (1) ◽

pp. 87-93 ◽

Cited By ~ 1

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.

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Defatted Hydroethanolic Extract of Ammodaucus leucotrichus Cosson and Durieu Seeds: Antidiabetic and Anti-Inflammatory Activities

Applied Sciences ◽

10.3390/app10249147 ◽

2020 ◽

Vol 10 (24) ◽

pp. 9147

Author(s):

Imane Es-Safi ◽

Hamza Mechchate ◽

Amal Amaghnouje ◽

Anna Calarco ◽

Smahane Boukhira ◽

...

Keyword(s):

Wistar Rats ◽

Fasting Blood Glucose ◽

Diabetic Mice ◽

North African ◽

Glucose Levels ◽

The North ◽

Blood Glucose Levels ◽

Anti Inflammatory ◽

Hydroethanolic Extract ◽

Inflammatory Effect

The seeds of Ammodaucus leucotrichus Cosson and Durieu have been used in the North African Sahara as a traditional medicine to treat diabetes. The present study investigates the antidiabetic, antihyperglycemic, and anti-inflammatory properties of the defatted hydroethanolic extract of Ammodaucus leucotrichus (DHEAM). The antidiabetic and the antihyperglycemic studies were assessed on alloxan-induced diabetic with orally administered doses of DHEAM (100 and 200 mg/kg). At the same time, its anti-inflammatory propriety was evaluated by measuring edema development in the Wistar rats paw induced with carrageenan. Treatment of diabetic mice with DHEAM for four weeks managed their high fasting blood glucose levels, improved their overall health, and also revealed an excellent antihyperglycemic activity. Following the anti-inflammatory results, DHEAM exhibited a perfect activity. HPLC results revealed the presence of seven molecules (chlorogenic acid, 3-p-coumaroylquinic acid, gallic acid, ferulic acid, myricetin, quercetin, luteolin). This work indicates that the DHEAM has an important antidiabetic, antihyperglycemic, and anti-inflammatory effect that can be well established as a phytomedicine to treat diabetes.

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Sesquiterpene Lactones: Promising Natural Compounds to Fight Inflammation

Pharmaceutics ◽

10.3390/pharmaceutics13070991 ◽

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.

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ANTI-INFLAMMATORY ACTIVITY OF CURCUMIN AND CAPSAICIN AUGMENTED IN COMBINATION

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2017v9i6.18635 ◽

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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Sequoyitol ameliorates diabetic nephropathy in diabetic rats induced with a high-fat diet and a low dose of streptozotocin

Canadian Journal of Physiology and Pharmacology ◽

10.1139/cjpp-2013-0307 ◽

2014 ◽

Vol 92 (5) ◽

pp. 405-417 ◽

Cited By ~ 8

Author(s):

Xian-Wei Li ◽

Yan Liu ◽

Wei Hao ◽

Jie-Ren Yang

Keyword(s):

Diabetic Nephropathy ◽

Blood Glucose ◽

High Fat Diet ◽

Low Dose ◽

Serum Insulin ◽

Fasting Blood Glucose ◽

Diabetic Rats ◽

High Fat

Sequoyitol decreases blood glucose, improves glucose intolerance, and enhances insulin signaling in ob/ob mice. The aim of this study was to investigate the effects of sequoyitol on diabetic nephropathy in rats with type 2 diabetes mellitus and the mechanism of action. Diabetic rats, induced with a high-fat diet and a low dose of streptozotocin, and were administered sequoyitol (12.5, 25.0, and 50.0 mg·(kg body mass)−1·d−1) for 6 weeks. The levels of fasting blood glucose (FBG), serum insulin, blood urea nitrogen (BUN), and serum creatinine (SCr) were measured. The expression levels of p22phox, p47phox, NF-κB, and TGF-β1 were measured using immunohistochemisty, real-time PCR, and (or) Western blot. The total antioxidative capacity (T-AOC), as well as the levels of malondialdehyde (MDA) and reactive oxygen species (ROS) were also determined. The results showed that sequoyitol significantly decreased FBG, BUN, and SCr levels, and increased the insulin levels in diabetic rats. The level of T-AOC was significantly increased, while ROS and MDA levels and the expression of p22phox, p47phox, NF-κB, and TGF-β1 were decreased with sequoyitol treatment both in vivo and in vitro. These results suggested that sequoyitol ameliorates the progression of diabetic nephropathy in rats, as induced by a high-fat diet and a low dose of streptozotocin, through its glucose-lowering effects, antioxidant activity, and regulation of TGF-β1 expression.

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