Anti-nociceptive activity of a few structurally related trimethoxy flavones and possible mechanisms involved

Nadipelly, Jagan; Sayeli, Vijaykumar; Kadhirvelu, Parimala; Shanmugasundaram, Jaikumar; Cheriyan, Binoy Varghese; Subramanian, Venkataraman

doi:10.1515/jbcpp-2015-0079

Cited by 7 publications

(10 citation statements)

References 39 publications

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“…Previous studies reported that mono and polymethoxyflavones (PMFs) exert opioid mediated antinociceptive effect (Thirugnanasambantham et al, 1993 ; Pandurangan et al, 2014 ; Nadipelly et al, 2016 ). Structure activity relationships study revealed that the presence of methoxy group (-OCH 3 ) at 5 or 7 positions on flavone moiety could induce opioid mediated analgesia (Thirugnanasambantham et al, 1993 ).…”

Section: Discussionmentioning

confidence: 99%

“…PMFs are termed as flavones which contain more than one methoxy (-O-CH 3 ) groups on their essential benzo-γ-pyrone skeleton, generally constituted by 15 carbons (C 6 -C 3 -C 6 ), including a carbonyl group (C = O) at C-4 position (Ververidis et al, 2007 ; Li et al, 2008 ). Scientific studies revealed that PMFs might exert prominent in vivo or in vitro anti-nociceptive (Nadipelly et al, 2016 ), anti-inflammatory, anticarcinogenic (Li et al, 2009 ), cancer chemopreventive (Walle, 2007 ), sedative (Jin et al, 2012 ), anti-depressant, anxiolytic as well as benzodiazepine binding effects (Paladini et al, 1999 ; Abdelhalim et al, 2015 ) and possess excellent absorption and oral bioavailability (Li et al, 2009 ).…”

Section: Introductionmentioning

confidence: 99%

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Polymethoxyflavones from Nicotiana plumbaginifolia (Solanaceae) Exert Antinociceptive and Neuropharmacological Effects in Mice

et al. 2018

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Polymethoxylavones (PMFs) are known to exhibit significant anti-inflammatory and neuroprotective properties. Nicotiana plumbaginifolia, an annual Bangladeshi herb, is rich in polymethoxyflavones that possess significant analgesic and anxiolytic activities. The present study aimed to determine the antinociceptive and neuropharmacological activities of polyoxygenated flavonoids namely- 3,3′,5,6,7,8-hexamethoxy-4′,5′-methylenedioxyflavone (1), 3,3′,4′,5′,5,6,7,8-octamethoxyflavone (exoticin) (2), 6,7,4′,5′-dimethylenedioxy-3,5,3′-trimethoxyflavone (3), and 3,3′,4′,5,5′,8-hexamethoxy-6,7-methylenedioxyflavone (4), isolated and identified from N. plumbaginifolia. Antinociceptive activity was assessed using the acetic-acid induced writhing, hot plate, tail immersion, formalin and carrageenan-induced paw edema tests, whereas neuropharmacological effects were evaluated in the hole cross, open field and elevated plus maze test. Oral treatment of compounds 1, 3, and 4 (12.5–25 mg/kg b.w.) exhibited dose-dependent and significant (p < 0.01) antinociceptive activity in the acetic-acid, formalin, carrageenan, and thermal (hot plate)-induced pain models. The association of ATP-sensitive K+ channel and opioid systems in their antinociceptive effect was obvious from the antagonist effect of glibenclamide and naloxone, respectively. These findings suggested central and peripheral antinociceptive activities of the compounds. Compound 1, 3, and 4 (12.5 mg/kg b.w.) demonstrated significant (p < 0.05) anxiolytic-like activity in the elevated plus-maze test, while the involvement of GABAA receptor in the action of compound 3 and 4 was evident from the reversal effects of flumazenil. In addition, compounds 1 and 4 (12.5–25 mg/kg b.w) exhibited anxiolytic activity without altering the locomotor responses. The present study suggested that the polymethoxyflavones (1–4) from N. Plumbaginifolia could be considered as suitable candidates for the development of analgesic and anxiolytic agents.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Polymethoxyflavones from Nicotiana plumbaginifolia (Solanaceae) Exert Antinociceptive and Neuropharmacological Effects in Mice

et al. 2018

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“…Based on the above few reports and earlier results on the effectiveness of trimethoxy flavones in attenuating visceral, neurogenic and inflammatory pain 7 , it was considered interesting to evaluate the possible role of trimethoxy flavones in ameliorating paclitaxel – induced peripheral neuropathy.…”

Section: Discussionmentioning

confidence: 99%

“…A few reports indicate that flavonoids such as myricitrin 4 , quercetin and rutin 5 , 6 were inhibit various types of neuropathy in animal models. In a recent study, four trimethoxy flavone derivatives (7, 2′, 3′ – trimethoxy flavone, 7, 2′, 4′ – trimethoxy flavone, 7, 3′, 4′ – trimethoxy flavone and 7, 5, 4′ – trimethoxy flavone) have been shown to possess antinociceptive property in mice 7 . Based on the aforementioned information, it was considered interesting to explore the potential effect of these trimethoxy flavones in peripheral neuropathy induced by a chemotherapeutic drug, paclitaxel in mice.…”

Section: Introductionmentioning

confidence: 99%

Effect of certain trimethoxy flavones on paclitaxel - induced peripheral neuropathy in mice

Nadipelly

Sayeli

Kadhirvelu

et al. 2018

Integrative Medicine Research

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BackgroundThe anti - nociceptive effect of 7, 2′, 3′ – trimethoxy flavone, 7, 2′, 4′ – trimethoxy flavone, 7, 3′, 4′ – trimethoxy flavone and 7, 5, 4′ – trimethoxy flavone against inflammatory, neurogenic and thermal pain in mice was reported earlier. The present study was designed to investigate the effect of the above trimethoxy flavones in amelioration of peripheral neuropathy induced by paclitaxel.MethodsPeripheral neuropathy was induced in mice by administration of a single i.p. dose (10 mg/kg) of paclitaxel. The manifestations of peripheral neuropathy such as tactile allodynia, cold allodynia and thermal hyperalgesia were assessed 24 h later by employing hair aesthesiometer test, acetone bubble test and hot water tail immersion test respectively. Further, the role of inflammatory cytokines like TNF – α, IL - 1β and free radicals in the action of trimethoxy flavones was investigated using in vitro assays.ResultsThe test compounds dose dependently attenuated paclitaxel - induced tactile allodynia, cold allodynia and thermal hyperalgesia in mice. The test compounds inhibited TNF – α, IL - 1β and free radicals in a concentration dependent manner.ConclusionThe investigated trimethoxy flavones attenuated paclitaxel – induced peripheral neuropathy in mice. The inhibition of cytokines and free radicals in addition to many neuronal mechanisms reported earlier may contribute to this beneficial effect.

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“…Recently it has been reported that antioxidants reduce pain of tonic (second) phase of formalin test 27 . D. spatulata contain several flavonoids 28 and it has been reported that flavonoids have antioxidant properties 8,29,30 .…”

Section: Discussionmentioning

confidence: 99%

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2017

IJPSR

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ABSTRACT:The aim of the present study is to investigate and evaluate analgesic and anti-inflammatory potential of aqueous and methanolic extracts of Drosera spatulata using different models in rats. The aqueous and methanolic extracts of D. spatulata (at the doses of 3, 4, 5, 8 and 10 mg/Kg body weight) investigated for anti-inflammatory and analgesic activities using various experimental models. Analgesic activity was evaluated using formalin induced paw licking models in rats. Antiinflammatory activity was evaluated using measurement of paw edema volume model in rats. Our results showed that both extracts caused a significant (P < 0.05) dose-dependent reduction of inflammation and pains induced by agent used. These results provide support for the use of aqueous and methanolic extracts of Drosera spatulata in relieving inflammatory, pain and insight into the development of new agents for treating inflammatory and pain diseases but further studies are needed to elucidate the mechanism (s) of action and phytochemical constituents of the plant.

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Anti-nociceptive activity of a few structurally related trimethoxy flavones and possible mechanisms involved

Abstract: 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.

Cited by 7 publications

References 39 publications

Polymethoxyflavones from Nicotiana plumbaginifolia (Solanaceae) Exert Antinociceptive and Neuropharmacological Effects in Mice

Polymethoxyflavones from Nicotiana plumbaginifolia (Solanaceae) Exert Antinociceptive and Neuropharmacological Effects in Mice

Effect of certain trimethoxy flavones on paclitaxel - induced peripheral neuropathy in mice

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