scholarly journals Pharmacological Potential of Anti-Inflammatory and Anti Nociceptive Activity of Bioactive Fractions from Leaves of Maytenus emarginata

Author(s):  
Sunil Kumar ◽  
Mathew George ◽  
Lincy Joseph

The antinociceptive & anti-inflammatory activities of extract were compared to dose of Phenylbutazone. The phytochemical secondary metabolites tested for include alkaloids, cardiac glycosides, flavonoids, phenols, saponins, steroids and terpenoids. Maytenus emarginata leaves extract demonstrated significant antinociceptive and anti- inflammatory effects in a dose-dependent manner. The extract dose at 200mg/kg bw exhibited the highest antinociceptive and anti-inflammatory activities & its activities were comparable to those of the respective reference drugs. BFLME (suspended in 1% carboxy methyl cellulose) in doses of 50, 100 and 200 mg/kg caused a dose-dependent inhibition of swelling caused by carrageenin equivalent to 30.2–63.2% protection (P<0.05– P<0.001) and in cotton pellet granuloma, 47.2–45.4% protection (P<0.01-P<0.001) was observed from inflammation. There was a significant increase in analgesiometer force induced pain in rat equivalent to 98.1–146.5% protection (P<0.01-P<0.001) and 7.19–37.8 % (P<0.05–P<0.001) protection against Acetic acid induced writhing. Phytochemical screening of the extract indicated the presence of alkaloids, cardiac glycosides, flavonoids, phenols, saponins, steroids and terpenoids. The present study therefore demonstrated the antinociceptive and anti-inflammatory properties of bioactive fraction of ethyl acetate extract from leaves of M. emarginata (BFLME), hence providing a basis for further research that may result in pure compounds that can be advanced into drug discovery.

2016 ◽  
Vol 11 (9) ◽  
pp. 1934578X1601100
Author(s):  
Masuri Kama Kamaruddin Shah ◽  
Hasnah Mohd Sirat ◽  
Shajarahtunnur Jamil ◽  
Juriyati Jalil

A new pyranoflavone, methoxycyclocommunol (1) together with four known flavonoids, artonin F (2), heteroflavanone A (3), cudraflavone C (4) and cyclocommunol (5) were isolated from the bark of Artocarpus integer var. silvestris Corner. Their structures were elucidated through extensive spectroscopic techniques (UV, IR, MS, 1D-NMR and 2D-NMR) and by comparison with literature data. All the pure compounds were tested for their anti-inflammatory activities by using screening kit and radioimmunoassay methods. In a 15-lipoxygenase (15-LOX) inhibitory assay, compounds 1, 2, 4 and 5 gave weak percentages of inhibition, 16.5, 18.3, 17.6, 10.2%, respectively at the concentration of 100 μM. Compounds 1, 3 and 4, however, showed strong dose-dependent inhibition towards prostaglandin E2 (PGE2) production in lipopolysaccharide-induced human whole blood using a radioimmunoassay method with IC50 values of 4.3, 0.8, and 0.07 μM, respectively suggesting that they strongly exhibited cyclooxygenase-2 (COX-2) activity.


2013 ◽  
Vol 2013 ◽  
pp. 1-4 ◽  
Author(s):  
Gaurav Kaithwas ◽  
Dipak K. Majumdar

The present investigation summarizes the effect of Linum usitatissimum fixed oil against different phases of acute inflammatory reaction, namely, protein exudation, peritoneal capillary permeability, and leukocyte migration. The fixed oil exhibited dose-dependent inhibition of protein exudation vascular permeability, comparable to standard aspirin. The oil also inhibited the leukocyte migration in pleural exudates in a dose-dependent manner. Production of less vasodilatory (PGE3) and chemotactic (LTB5) eicosanoids through EPA (derived from linolenic acid) metabolism could account for the above observations.


1987 ◽  
Vol 253 (1) ◽  
pp. G7-G12 ◽  
Author(s):  
J. R. Grider ◽  
G. M. Makhlouf

The role of vasoactive intestinal peptide (VIP) and its homologue, peptide histidine isoleucine (PHI), as neurotransmitters of inhibitory motor nerves of the gut, were examined in strips of guinea pig taenia coli and gastric fundic muscle. The stoichiometry of VIP release and muscle relaxation was determined in the presence and absence of the bee venom peptide, apamin, and the existence of prejunctional VIP/PHI receptors capable of regulating VIP/PHI release was explored. In both types of muscle, relaxation induced by field stimulation was proportional to the amount of VIP released. Apamin inhibited relaxation and VIP release in a dose-dependent manner: maximal relaxation was inhibited by 85–96% at 10(-7)-10(-6) M apamin. Analysis of residual responses showed that apamin did not affect the stoichiometry of VIP release and muscle relaxation. Because apamin had no effect on basal tone or on relaxation induced by exogenous VIP, its effect on neurally induced relaxation was attributed to inhibition of VIP release. Both secretin and PHI inhibited neurally induced VIP release in the two types of muscle. At the optimal concentration of 10(-7) M, secretin inhibited VIP release by 52%, whereas the closer neural homologue, PHI, abolished VIP release. The dose-dependent inhibition of VIP release by PHI, which is cosynthesized and coreleased with VIP, indicates the existence of prejunctional inhibitory VIP/PHI autoreceptors capable of regulating VIP/PHI release.


Author(s):  
Jagan Nadipelly ◽  
Vijaykumar Sayeli ◽  
Parimala Kadhirvelu ◽  
Jaikumar Shanmugasundaram ◽  
Binoy Varghese Cheriyan ◽  
...  

AbstractThe present study was designed to investigate the anti-nociceptive activity of a few structurally related trimethoxy flavones (7,2′,3′-TMF, 7,2′,4′-TMF, 7,3′,4′-TMF and 7,5,4′-TMF) and the possible mechanisms involved.Anti-nociceptive activity was evaluated in mice by employing acetic acid-induced writhing, formalin-induced nociception and hot water tail immersion methods. The involvement of opioid, GABAergic, tryptaminergic, adrenergic and dopaminergic mechanisms and KTrimethoxy flavones exhibited a significant and dose-dependent inhibition of acetic acid writhing. The paw-licking response time was reduced both in the early and late phases of formalin nociception in a dose-dependent manner by trimethoxy flavones. A significant increase in tail withdrawal latency time was also observed after trimethoxy flavones treatment. These observations revealed the potential anti-nociceptive action of the investigated trimethoxy flavones. Pretreatment with naloxone and bicuculline significantly attenuated the reduction of abdominal constrictions produced by all the tested trimethoxy flavones indicating a definite role of opioid and GABAergic mechanisms in the anti-nociceptive effect of trimethoxy flavones. The anti-nociceptive action elicited by various trimethoxy flavones was differently modulated by glibenclamide, ondansetron, yohimbine and sulpiride.The investigated trimethoxy flavones exhibited promising anti-nociceptive activity in various nociceptive models, and multiple mechanisms are involved in the anti-nociceptive activity of these compounds.


Author(s):  
Cyril Ogbiko ◽  
Dickson Achimugu Musa ◽  
Musa Usman Dabai ◽  
Ibeabuchi Jude Ali ◽  
Abubakar Sani Yelwa ◽  
...  

Herbal medicine despite its increase usage globally is being plagued by inadequate research on their effectiveness. Stachytarpheta indica commonly known as snakeweed is used locally in the management of asthma, headache, alopecia, bronchitis, bruise, chest cold, constipation, itch, diarrhea, skin sore, vermifuge, dysentery, dysmenorrhea among others. This study investigated the phytochemical composition, quantitative proximate parameters and in vitro anti-inflammatory activity of the leaves of S. indica using established methods. Results confirmed the presence of alkaloids, saponins, carbohydrate, cardiac glycosides, terpenoid, tannin, anthraquinones, phenolics and flavonoid. Moisture content (9.16 ± 0.04%), total ash (19.42 ± 0.15%), water insoluble ash (7.17 ± 0.22%), acid insoluble ash (3.63 ± 0.26%), alcohol soluble extractive (0.99 ± 0.06%) and water-soluble extractive (0.36 ± 0.02%) values were obtained from the quantitative proximate analysis. An infusion of the methanol leaf extract of Stachytarpheta indica demonstrated significant anti-inflammatory activity in a dose dependent manner comparable to that of indomethacin standard.


1996 ◽  
Vol 151 (3) ◽  
pp. 449-457 ◽  
Author(s):  
M Imai ◽  
M Yamoto ◽  
H Otani ◽  
R Nakano

Abstract In the present study, we examined the effects of tumour necrosis factor α (TNFα) and interleukin-1β (IL-1β) on inhibin secretion by cultured rat granulosa cells using immunoblotting and two-site enzyme immunoassay for inhibin A (α-βA dimer). FSH stimulated the secretion of the inhibin α-βA dimer (32 kDa) by the cells in a dose-dependent manner. In addition to the predominant 32 kDa inhibin α-βA dimer staining, staining of minor immunoreactive bands was also enhanced by FSH. TNFα alone did not have any effect on inhibin secretion. Immunoblot analyses using an antiserum against α-subunit and an antiserum against βA-subunit revealed a dose-dependent inhibition by TNFα of FSH-stimulated secretion of inhibin by rat granulosa cells. Similarly, TNFα inhibited in a dose-dependent manner FSH-stimulated inhibin secretion when measured using a two-site enzyme immunoassay. IL-1β alone did not exert any effect on inhibin secretion but it inhibited FSH-stimulated inhibin release in a dose-dependent manner (using both immunoblotting and a two-site assay for inhibin A). The present observations suggest that TNFα and IL-1β inhibit gonadotrophin-stimulated inhibin production by cultured rat granulosa cells. Journal of Endocrinology (1996) 151, 449–457


2015 ◽  
Vol 21 (4) ◽  
pp. 233-237 ◽  
Author(s):  
Xinbin Yang ◽  
Xiaolin Qin ◽  
Qin Wang ◽  
Yu Huang

AbstractA series of piperazine- and cyclen-conjugated dehydroabietylamine derivatives were synthesized and characterized by 1H NMR, 13C NMR, and HRMS. The in vitro antitumor activities of conjugates 10–13 against MCF-7 and HepG-2 tumor cell lines were evaluated using CCK-8 assay. The results show that the synthesized compounds cause a dose-dependent inhibition of cell proliferation and display different antitumor activities with the IC50 values ranging from 23.56 to 78.92 μm. Moreover, the antitumor activity of conjugate 10 against the MCF-7 cell line is superior to that of the positive control 5-fluorouracil. In addition, flow cytometric assay revealed that the representative conjugate 10 could induce apoptosis in MCF-7 tumor cells in a dose-dependent manner.


Author(s):  
Poonam Verma ◽  
Baljinder Singh ◽  
Amarjit Kaur ◽  
Vijender Kumar

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.


Sign in / Sign up

Export Citation Format

Share Document