Effect of Hydro Alcoholic Extracts of Boswellia serrata and Terminalia bellerica Against Cyclo-Oxygenase and Lipoxygenase Enzymes- An In Vitro Approach

Introduction: Inflammation is a key mediator in plenty of important physiological abnormalities like cancer, myocardial infarction and arthritis. Natural anti-inflammatory agents are of great demand owing to its decreased side effects and increased curative properties. Aim: To investigate the in vitro inhibitory effect of three different concentrations of hydroalcoholic extract of Boswellia serrata (BS) and Terminalia bellerica (TB) on COX-2 and LOX-2 enzymes. Materials and Methods: Three different concentrations of hydroalcoholic menstruum of BS and TB were prepared using the standard procedures. The in vitro inhibitory activities of COX-2 and LOX-2 were performed using previously mentioned methods with minor modifications. Results: Among the different concentrations used the 90:10 menstruum of BS at 12 mg/ml displayed maximum inhibitory potential against COX-2 enzyme when compared to the same concentration of TB extract. This is suggestive that the majority of bioactive compounds present in BS was alcohol soluble and hence elicited maximum inhibition potential at 90 % ethanol ratio. A similar pattern of results were observed against LOX-2 enzyme as well. Conclusion:From the results it is concluded that the 90:10 hydroalcoholic extract of Boswellia serrata and Terminalia bellerica exhibit appreciable percentage of COX-2 and LOX-2 inhibition, which could be attributed to the ethanol soluble bioactive components present in the extract.

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Lack of Small Intestinal Dysbiosis Following Long-Term Selective Inhibition of Cyclooxygenase-2 by Rofecoxib in the Rat

Cells ◽

10.3390/cells8030251 ◽

2019 ◽

Vol 8 (3) ◽

pp. 251 ◽

Cited By ~ 2

Author(s):

Bernadette Lázár ◽

Gábor Brenner ◽

András Makkos ◽

Mihály Balogh ◽

Szilvia László ◽

...

Keyword(s):

Selective Inhibition ◽

Mucosal Damage ◽

Inhibitory Effect ◽

Intestinal Dysbiosis ◽

Bowel Diseases ◽

Direct Inhibitory Effect ◽

Cox 2 ◽

Small Intestinal

Intestinal dysbiosis is linked to numerous gastrointestinal disorders, including inflammatory bowel diseases. It is a question of debate if coxibs, selective inhibitors of cyclooxygenase (COX)-2, cause dysbiosis. Therefore, in the present study, we aimed to determine the effect of long-term (four weeks) selective inhibition of COX-2 on the small intestinal microbiota in the rat. In order to avoid mucosal damage due to topical effects and inflammation-driven microbial alterations, rofecoxib, a nonacidic compound, was used. The direct inhibitory effect of rofecoxib on the growth of bacteria was ruled out in vitro. The mucosa-sparing effect of rofecoxib was confirmed by macroscopic and histological analysis, as well as by measuring the intestinal levels of cytokines and tight junction proteins. Deep sequencing of bacterial 16S rRNA revealed that chronic rofecoxib treatment had no significant influence on the composition and diversity of jejunal microbiota. In conclusion, this is the first demonstration that long-term selective inhibition of COX-2 by rofecoxib does not cause small intestinal dysbiosis in rats. Moreover, inhibition of COX-2 activity is not likely to be responsible per se for microbial alterations caused by some coxibs, but other drug-specific properties may contribute to it.

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α-Mangostin fromCratoxylum arborescens(Vahl) Blume Demonstrates Anti-Ulcerogenic Property: A Mechanistic Study

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2013/450840 ◽

2013 ◽

Vol 2013 ◽

pp. 1-10 ◽

Cited By ~ 10

Author(s):

Heyam M. A. Sidahmed ◽

Siddig Ibrahim Abdelwahab ◽

Syam Mohan ◽

Mahmood Ameen Abdulla ◽

Manal Mohamed Elhassan Taha ◽

...

Keyword(s):

Antioxidant Properties ◽

Inhibitory Effect ◽

Mechanistic Study ◽

Gastric Lesions ◽

Property A ◽

Hsp70 Protein ◽

Cox 2 ◽

H Pylori ◽

Asian Herbal Medicine

Cratoxylum arborescens(Vahl) Blume is an Asian herbal medicine with versatile ethnobiological properties including treatment of gastric ulcer. This study evaluated the antiulcerogenic mechanism(s) ofα-mangostin (AM) in a rat model of ulcer. AM is a prenylated xanthone derived through biologically guided fractionation ofC. arborescens. Rats were orally pretreated with AM and subsequently exposed to acute gastric lesions induced by ethanol. Following treatment, ulcer index, gastric juice acidity, mucus content, histological and immunohistochemical analyses, glutathione (GSH), malondialdehyde (MDA), nitric oxide (NO), and nonprotein sulfhydryl groups (NP-SH) were evaluated. The anti-Helicobacter pylori, cyclooxygenase-2 (COX-2) inhibitory effect, and antioxidant activity of AM were also investigatedin vitro. AM (10 and 30 mg/kg) inhibited significantly (P<0.05) ethanol-induced gastric lesions by 66.04% and 74.39 %, respectively. The compound induces the expression of Hsp70, restores GSH levels, decreases lipid peroxidation, and inhibits COX-2 activity. The minimum inhibitory concentration (MIC) of AM showed an effectivein vitroanti-H. pyloriactivity. The efficacy of the AM was accomplished safely without presenting any toxicological parameters. The results of the present study indicate that the antioxidant properties and the potent anti-H. pylori, in addition to activation of Hsp70 protein, may contribute to the gastroprotective activity ofα-mangostin.

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An in-vitro study to compare and evaluate the anti-diabetic effect of mixed fruit juice nanoemulsion with acarbose

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v12i1.3936 ◽

2021 ◽

Vol 12 (1) ◽

pp. 72-76

Author(s):

Gayathri K ◽

Karpagavel L ◽

Murugavel K ◽

Manikandan N

Keyword(s):

Fruit Juice ◽

In Vitro Study ◽

Punica Granatum ◽

Inhibitory Effect ◽

Health Concern ◽

Maximum Inhibition ◽

Nano Emulsion ◽

Alpha Glucosidase ◽

Relative Inhibition

Diabetes has become a global health concern, its management lies hugely on expensive medical care and monitoring; thus the need to investigate possible alternatives to reduce treatment cost and also to reduce the side effects of commonly used anti diabetic drugs. This study aims to assess the anti-diabetic effect of mixed fruit juice nanoemulsion of Coccinia grandis, Punica granatum and Phyllanthus emblica. Mixed fruit juice nanoemulsion were prepared in the ratio of VCO oil:water:surfactant- 32:36:32 (%w/w). characterization parameters of mixed fruit juice nanoemulsion including PH, zeta potential, size, morphology were within the standard limits and was used for the study. The anti diabetic effect of nano emulsified mixed fruit juice was compared with that of acarbose by measuring their inhibitory effect on the enzyme alpha glucosidase. Maximum Inhibitory effect of formulated Nano emulsion on enzyme alpha glucosidase was 83% at concentration 81μg/ml whereas that for the standard anti-diabetic drug Acarbose was 93% at concentration 540μg/ml. For acarbose, the maximum Inhibition was 92% at the concentration of 540μg/ml. The relative inhibition Percentage of Nano emulsion versus Control has been analyzed and the results found to be statistically significant (P<0.003).

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Chemical Characterization of Opuntia ficus-indica (L.) Mill. Hydroalcoholic Extract and Its Efficiency against Gastrointestinal Nematodes of Sheep

Veterinary Sciences ◽

10.3390/vetsci5030080 ◽

2018 ◽

Vol 5 (3) ◽

pp. 80 ◽

Cited By ~ 1

Author(s):

Carolina Santos ◽

Luciano Campestrini ◽

Douglas Vieira ◽

Izanara Pritsch ◽

Fábio Yamassaki ◽

...

Keyword(s):

Chemical Characterization ◽

Inhibitory Effect ◽

Gastrointestinal Nematodes ◽

Gastrointestinal Parasites ◽

In Vitro Tests ◽

Cactus Pear ◽

Opuntia Ficus Indica ◽

Hydroalcoholic Extract ◽

Quercetin Derivatives

Opuntia ficus-indica (L.) Mill. is a xerophylous plant that originated in tropical and subtropical America. This plant is popularly known in Brazil as “palma forrageira” (cactus pear) and plays a fundamental role in animal nutrition, mainly in the Northeastern semi-arid region of the country. The plant has several uses since it presents bioactive compounds that confer biological and pharmacological properties. In this context, the cactus pear can also be considered a potential product to combat parasite infections. The objective of this study was to chemically characterize the O. ficus-indica hydroalcoholic extract (OFIEOH) and to determine its efficacy against gastrointestinal parasites using in vitro tests. Initially, the hydroalcoholic extract from cladode peels of O. ficus-indica was produced by maceration for 21 days. For the chemical characterization, colorimetric dosages were performed for carbohydrates, proteins, phenols and condensed tannins. Liquid chromatography coupled to mass spectrometry/electron spray ionization (LC-MS/ESI) was used to characterize the polyphenolic profile of the OFIEOH extract. Fifteen compounds were identified in the OFIEOH extract, such as methyl, glycosylated and aglycone quercetin derivatives and aglycone and glycosylated kaempferol derivatives. Tri-glycosylated methyl quercetin derivatives were the main compounds identified. In vitro egg hatch (EHT) and larval migration tests (LMT) were used in a range of concentrations of OFIEOH from 12.5 to 100 mg/mL for EHT and 12.5 to 200 mg/mL for LMT. In addition, the LMT was used to test ivermectin (IVM) (from 11.4 to 57.1 µM), associated with the inhibitory concentration of 50% (IC50) for OFIEOH. The combination of OFIEOH (12.5 to 200 mg/mL) plus the IC50 of IVM was also tested. The efficacy of OFIEOH alone varied from 19.33 to 90.0% using the EHT. The LMT revealed an efficacy of 5.78 to 77.26% for the extract. Both tests showed a concentration-dependence inhibitory effect. We found a drug-extract antagonistic neutralizing effect when doses of IVM were added to OFIEOH (maximum efficacy of 73.78%), while a positive additive effect was observed when OFIEOH was added to the IC50 of IVM (IC50 of 82.79 for OFIEOH alone against an IC50 of 55.08 of OFIEOH + IVM). The data from this work indicate that OFIEOH alone may be considered as a suitable ecofriendly product to control gastrointestinal parasites of sheep, offering a more holistic approach to improve animal farming and welfare. The drug-extract interaction is also a promising therapeutic alternative, reducing the final dose to the host, with an optimum combination effect.

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In-vitro Antivenom Potential of Solanum dasyphyllum Methanolic Leaf and Fruit Extracts against Naja nigricollis Venom

European Journal of Medicinal Plants ◽

10.9734/ejmp/2020/v31i930269 ◽

2020 ◽

pp. 38-45

Author(s):

Adewunmi Rofiat Funmilola ◽

Gidado Abubakar ◽

Zanna Hassan

Keyword(s):

Medicinal Plants ◽

Leaf Extract ◽

Inhibitory Effect ◽

Fruit Extract ◽

Southwestern Part ◽

Fruit Extracts ◽

Snake Envenomation ◽

The Family ◽

Inhibitory Potential

Solanum dasyphyllum belongs to the family of plants called Solanaceae, it is commonly called "Africa eggplant" and one of the medicinal plants used in the treatment of snake envenomation in the southwestern part of Nigeria, but investigation concerning its anti-venom activity has not been established. The present study evaluates the in-vitroenzyme inhibition potential of S.dasyphyllum leaf and fruit extracts against Naja nigricollis (Black-necked spitting cobra) venom. The inhibitory potential of S. dasyphyllum leaf and fruit on proteases, acetylcholinesterase, phospholipase A2 and hyaluronidase enzymes present in the snake venom was evaluated. The methanolic leaf and fruit extracts of S. dasyphyllum inhibited the activity of all enzymes evaluated, however, the leaf extract exhibited better enzyme inhibitory effect on N. nigricollis venom when compared with the fruit. This could be due to the presence of various phytochemicals in leaf and fruit extract. This result substantiates the ethnomedicinal usage of S. dasyphyllum and would help to develop potent antidote therapy against N. nigricollis envenomation.

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Inhibitory Effect of Ocimum gratissimum Leaf Extract on Postprandial Increase of Blood Glucose

Natural Product Communications ◽

10.1177/1934578x19883728 ◽

2019 ◽

Vol 14 (10) ◽

pp. 1934578X1988372

Author(s):

Hiroaki Shimada ◽

Chiaki Kuma ◽

Taichi Iseri ◽

Shin-ichi Matsumura ◽

Atsushi Kawase ◽

...

Keyword(s):

Blood Glucose ◽

Glucose Transporter ◽

Inhibitory Effect ◽

Glucose Absorption ◽

Dependent Manner ◽

Concentration Dependent Manner ◽

Ocimum Gratissimum ◽

Inhibitory Potential ◽

Hyperglycemic Effect

The tea of Ocimum gratissimum (OG) leaves has been commonly consumed by people living in Ishigaki Island, Okinawa prefecture, Japan, and is considered to be effective for improving diabetes mellitus. In this study, we aimed to clarify the inhibitory potential of OG leaves extract (OG-ext) on gastrointestinal glucose absorption and to provide theoretical evidence for the anti-hyperglycemic effect of OG-ext. The increase of blood glucose after oral administration of α-starch and glucose in mice was suppressed by co-administration of OG-ext. An in vitro enzymatic assay suggested that amylase and maltase were inhibited weakly by the addition of OG-ext. In Caco-2 cells, a human intestinal epithelial model, the sodium-dependent glucose transporter (SGLT) 1-mediated uptake of fluorescence glucose analog was inhibited significantly by the addition of OG-ext in a concentration-dependent manner. These results indicate that the inhibitory effect on SGLT1 is one of the mechanisms of the anti-hyperglycemic effect of the tea of OG leaves.

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EVALUATION OF α-GLUCOSIDASE INHIBITORY POTENTIAL OF METHANOLIC LEAF EXTRACT OF OCIMUM CANUM

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2018v10i1.22268 ◽

2018 ◽

Vol 10 (1) ◽

pp. 126

Author(s):

Kumari Smita

Keyword(s):

High Performance ◽

Leaf Extract ◽

Soxhlet Extraction ◽

Inhibitory Effect ◽

Polyphenolic Compounds ◽

Glucosidase Activity ◽

Glucosidase Inhibitors ◽

Vitro Model ◽

Inhibitory Potential

Objective: The present investigation was designed to study the inhibitory effects of methanolic leaf extract of Ocimum canum (O. canum) on α-glucosidase using in vitro model followed by an assessment of bioactive compounds.Methods: The methanolic leaf extract was prepared by Soxhlet extraction method and partially purified by thin layer chromatography (TLC). Each band was subjected to α-glucosidase inhibition study. The positive bands were further characterized by high-performance liquid chromatography (HPLC) and quadrupole time of flight (Q-TOF) micro mass spectrometer.Results: Out of the several combinations of solvent systems, toluene, ethyl acetate and formic acid combination in the ratio of 7:2:1 revealed 5 bands on the TLC sheet. Among all the TLC bands, 2 bands (band A and B) showed the significant inhibitory effect on α-glucosidase activity. HPLC analysis of band A and B revealed the presence of two important polyphenolic compounds, namely rosmarinic acid (RA) and ursolic acid (UA). Q-TOF micromass spectrometer analysis revealed the percentage availability of RA, caffeic acid, tartaric acid, quercetin and other polyphenolic components in the bioactive bands.Conclusion: The study revealed that methanolic leaf extract of O. canum exhibits potent inhibition of α-glucosidase activity. Inhibition of α-glucosidase activity might be attributed to the presence of the polyphenolic compounds like RA and UA. Therefore, this finding can lead to the development of natural α-glucosidase inhibitors by the O. canum leaf extract.

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Inhibition of Carrageenan-Induced Acute Inflammation in Mice by Oral Administration of Anthocyanin Mixture from Wild Mulberry and Cyanidin-3-Glucoside

BioMed Research International ◽

10.1155/2013/146716 ◽

2013 ◽

Vol 2013 ◽

pp. 1-10 ◽

Cited By ~ 22

Author(s):

Neuza Mariko Aymoto Hassimotto ◽

Vanessa Moreira ◽

Neide Galvão do Nascimento ◽

Pollyana Cristina Maggio de Castro Souto ◽

Catarina Teixeira ◽

...

Keyword(s):

Polymorphonuclear Leukocytes ◽

Acute Inflammation ◽

Biological Activities ◽

Inhibitory Effect ◽

Experimental Models ◽

Protein Levels ◽

Paw Oedema ◽

Cox 2

Anthocyanins are flavonoids which demonstrated biological activities inin vivoandin vitromodels. Here in the anti-inflammatory properties of an anthocyanin-enriched fraction (AF) extracted from wild mulberry and the cyanidin-3-glucoside (C3G), the most abundant anthocyanin in diet, were studied in two acute inflammation experimental models, in the peritonitis and in the paw oedema assays, both of which were induced by carrageenan (cg) in mice. In each trial, AF and C3G (4 mg/100 g/animal) were orally administered in two distinct protocols: 30 min before and 1 h after cg stimulus. The administration of both AF and C3G suppresses the paw oedema in both administration times (P<0.05). In the peritonitis, AF and C3G reduced the polymorphonuclear leukocytes (PMN) influx in the peritoneal exudates when administered 1 h after cg injection. AF was more efficient reducing the PMN when administered 30 min before cg. Both AF and C3G were found to suppress mRNA as well as protein levels of COX-2 upregulated by cg in both protocols, but the inhibitory effect on PGE2production in the peritoneal exudates was observed when administered 30 min before cg (P<0.05). Our findings suggest that AF and C3G minimize acute inflammation and they present positive contributions as dietary supplements.

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Steroidal ferrocenes as potential enzyme inhibitors of the estrogen biosynthesis

Biologia Futura ◽

10.1007/s42977-020-00023-7 ◽

2020 ◽

Vol 71 (3) ◽

pp. 249-264

Author(s):

Bianka Edina Herman ◽

János Gardi ◽

János Julesz ◽

Csaba Tömböly ◽

Eszter Szánti-Pintér ◽

...

Keyword(s):

Enzyme Inhibitors ◽

Inhibitory Effect ◽

Ferrocene Derivatives ◽

17Β Estradiol ◽

Inhibitory Potential ◽

Estrogen Biosynthesis

Abstract The potential inhibitory effect of diverse triazolyl-ferrocene steroids on key enzymes of the estrogen biosynthesis was investigated. Test compounds were synthesized via copper-catalyzed cycloaddition of steroidal azides and ferrocenyl-alkynes using our efficient methodology published previously. Inhibition of human aromatase, steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) activities was investigated with in vitro radiosubstrate incubations. Some of the test compounds were found to be potent inhibitors of the STS. A compound bearing ferrocenyl side chain on the C-2 displayed a reversible inhibition, whereas C-16 and C-17 derivatives displayed competitive irreversible binding mechanism toward the enzyme. 17α-Triazolyl-ferrocene derivatives of 17β-estradiol exerted outstanding inhibitory effect and experiments demonstrated a key role of the ferrocenyl moiety in the enhanced binding affinity. Submicromolar IC50 and Ki parameters enroll these compounds to the group of the most effective STS inhibitors published so far. STS inhibitory potential of the steroidal ferrocenes may lead to the development of novel compounds able to suppress in situ biosynthesis of 17β-estradiol in target tissues.

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