6-Methoxyflavanone attenuates mechanical allodynia and vulvodynia in the streptozotocin-induced diabetic neuropathic pain

Akbar, Shehla; Subhan, Fazal; Karim, Nasiara; Shahid, Muhammad; Ahmad, Nisar; Ali, Gowhar; Mahmood, Wajahat; Fawad, Khwaja

doi:10.1016/j.biopha.2016.10.017

Cited by 40 publications

(20 citation statements)

References 57 publications

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“…Isolated bioactive moieties from the flavonoid class are recognized as promising in different neuropathic pain conditions [14,16,23]. In the present study, the flavonoid, 6-MF allayed cisplatin-induced expression of neuropathic allodynia and thermal hypoalgesia whilst being devoid of the motor impairment associated with gabapentin.…”

Section: Discussionmentioning

confidence: 59%

“…To avoid cisplatin-induced kidney damage, hyperhydration was induced by subcutaneous injection of 2.0 mL of sterile saline 5 min before administration of cisplatin. 6-MF was administered once daily in doses of 25, 50 and 75 mg/kg via the intraperitoneal route [23]. Gabapentin was used as a positive control and was administered intraperitoneally once daily at a dose of 75 mg/kg (i.p) [24][25].…”

Section: Induction Of Cisplatin-induced Neuropathic Nociception and Tmentioning

confidence: 99%

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The flavonoid 6-methoxyflavone allays cisplatin-induced neuropathic allodynia and hypoalgesia

Shahid

Subhan

Ahmad

et al. 2017

Biomedicine & Pharmacotherapy

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Chemotherapy-induced peripheral neuropathy (CIPN) is a major dose limiting side-effect of several commonly used chemotherapeutic agents (such as cisplatin) that profoundly impairs patient quality of life. Unfortunately, neither prophylactic strategies nor symptomatic treatments have proven useful in this condition. Flavonoids are found ubiquitously in fruits and vegetables and exert a multiplicity of beneficial effects. In this study, the antinociceptive activity of 6-methoxyflavone (6-MF) was investigated and evaluated in comparison with gabapentin in a rat model of CIPN. The effect on motor balance was also assessed using the rotarod and footprint analysis paradigms. 6-MF possessed both peripheral and central antinociceptive activities against tonic and phasic nociceptive stimuli. Cisplatin administration (3.0mg/kg/week, i.p.) for four consecutive weeks generated temporal mechanical allodynia (decreased paw withdrawal threshold; PWT) and thermal hypoalgesia (increased paw thermal threshold; PTT) in the bilateral hindpaws. Daily treatment with 6-MF (25, 50 and 75mg/kg/day, i.p) for four weeks attenuated the cisplatin-induced expression of nocifensive behaviors observed as a significant increase in PWT and alleviation of PTT during the third and fourth weeks of cisplatin administration. Accordingly, daily gabapentin (75mg/kg, i.p) suppressed the expression of CIPN by normalizing the PWT and hotplate response latency. However, these antinociceptive actions were associated with motor impairment exemplified by a significant decrease in rotarod endurance latency and a deficit in the uniformity of step alternation. In contrast, 6-MF was devoid of these adverse side-effects. These findings suggested that 6-MF afforded desirable neuropathic pain alleviating effects in CIPN and it was devoid of gabapentin-like unwanted motor side-effects.

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Section: Discussionmentioning

confidence: 59%

Section: Induction Of Cisplatin-induced Neuropathic Nociception and Tmentioning

confidence: 99%

The flavonoid 6-methoxyflavone allays cisplatin-induced neuropathic allodynia and hypoalgesia

Shahid

Subhan

Ahmad

et al. 2017

Biomedicine & Pharmacotherapy

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“…Akbar et al demonstrated that 6-methoxyflavanone ( 4 ) has the potential to easily cross the blood-brain barrier and possesses anti-allodynic and anti-vulvodynic activities in the rat model of streptozotocin-induced diabetes mellitus. Therefore, this compound could be used to treat neuropathic pain associated with diabetes mellitus [ 14 ]. In another study, Akbar et al showed that 6-methoxyflavanone ( 4 ) exerted an anxiolytic-like effect in several tests conducted with mice [ 15 ].…”

Section: Introductionmentioning

confidence: 99%

Glycosylation of Methoxylated Flavonoids in the Cultures of Isaria fumosorosea KCH J2

2018

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Flavonoids are widely described plant secondary metabolites with high and diverse pro-health properties. In nature, they occur mostly in the form of glycosides. Our research showed that an excellent way to obtain the sugar derivatives of flavonoids is through biotransformations with the use of entomopathogenic filamentous fungi as biocatalysts. In the current paper, we described the biotransformations of five methoxylated flavonoid compounds (2′-methoxyflavanone, 3′-methoxyflavanone, 4′-methoxyflavanone, 6-methoxyflavanone, and 6-methoxyflavone) in cultures of Isaria fumosorosea KCH J2. As a result, we obtained twelve new flavonoid 4-O-methylglucopyranosides. The products were purified with methods that enabled the reduction of the consumption of organic solvents (preparative TLC and flash chromatography). The structures of the products were confirmed with spectroscopic methods (NMR: 1H, 13C, HSQC, HMBC, COSY). The compounds obtained by us expand the library of available flavonoid derivatives and can be used in biological research.

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“…6-Hydroxyflavone depicted a significant effect at flumazenilsensitive BDZ site (Ren et al, 2010). Moreover, 6methoxyflavanone and 6-methoxyflavone have been recently reported to exhibit significant anti-allodynic effects in streptozotocin-and cisplatin-induced neuropathic pain models (Akbar et al, 2016;Shahid et al, 2017). These protective effects against neuropathic pain were attributed to the positive allosteric modulatory effects of these molecules on opioid and GABA A receptors respectively (Akbar et al, 2016).…”

Section: Flavonoids As Gaba a Receptor Modulatorsmentioning

confidence: 99%

Flavonoids in neuropathic pain management: A new player on an old target

Akbar¹

2019

Afr. J. Pharm. Pharmacol.

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Neuropathic pain is the consequence of abnormal processing in the peripheral or central nervous system (CNS) elicited by neuronal injury. Due to its heterogeneous nature and important unwanted adverse effects of the commonly prescribed psychoactive drugs like benzodiazepines (BDZ), the treatment of neuropathic pain has remained a challenge for the scientific community. Flavonoids initially isolated from plants and used as tranquilizers in Folkloric medicine, have been reported to possess selective affinity for BDZ binding site. These positive ionotropic modulators of γ-amino butyric acid-A (GABA A) receptors enhance the chloride ion flux and provide a strong inhibitory effect. Therefore, for the treatment of central nervous system-related disorders such as neuropathic pain, these selective GABA A receptor modulators stand amongst the strongest candidates. This review provides an update on research development that has confirmed the activity of different flavonoids on GABA A receptors.

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6-Methoxyflavanone attenuates mechanical allodynia and vulvodynia in the streptozotocin-induced diabetic neuropathic pain

Cited by 40 publications

References 57 publications

The flavonoid 6-methoxyflavone allays cisplatin-induced neuropathic allodynia and hypoalgesia

The flavonoid 6-methoxyflavone allays cisplatin-induced neuropathic allodynia and hypoalgesia

Glycosylation of Methoxylated Flavonoids in the Cultures of Isaria fumosorosea KCH J2

Flavonoids in neuropathic pain management: A new player on an old target

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