Investigation of Analgesic and Anti-inflammatory Activities and Dose Optimization of Quercetin and Its Few Novel Semisynthetic O-methylated Derivatives

محورهای موضوعی :

Abhijit Bose ¹ , Sankhadip Bose ² , Kunal Gupta ³ , Purnendu Kumar Roychoudhury ⁴ , Kamalika Mazumder ⁵ , Subhasis Maity ⁶ , Sabyasachi Banerjee ⁷ , Sujayaita Mazumder ⁸

1 - T. C. G. Life Sciences Pvt. Limited (Chembiotek), Plot No-7, Salt Lake Electronics Complex, BN Block, Sector V, Kolkata, West Bengal-700091, India
2 - School of Pharmacy, The Neotia University, Sarisa, Diamond Harbour Road, South 24 Parganas, West Bengal 743368, India
3 - Eminent college of Pharmaceutical Technology, Barasat, Kolkata, West Bengal-700126, India
4 - T. C. G. Life Sciences Pvt. Limited (Chembiotek), Plot No-7, Salt Lake Electronics Complex, BN Block, Sector V, Kolkata, West Bengal-700091, India
5 - NSHM Knowledge Campus, Kolkata – Group of Institutions, 124 B.L. Saha Road, Kolkata, West Bengal-700053, India
6 - NSHM Knowledge Campus, Kolkata – Group of Institutions, 124 B.L. Saha Road, Kolkata, West Bengal-700053, India.
7 - Department of Pharmaceutical Chemistry, Gupta College of Technological Sciences, Asansol 713 301, West Bengal, India
8 - School of Pharmacy, The Neotia University, Sarisa, Diamond Harbour Road, South 24 Parganas, West Bengal 743368, India

تاریخ دریافت : 1403/08/05 تاریخ پذیرش : 1403/10/10 تاریخ انتشار : 1403/10/30

کلید واژه: Quercetin, O-methylated quercetin derivatives, Pilot study, Analgesic, Anti-inflammation, Toxicity ,

چکیده مقاله :

Pain and inflammation are associated with numerous disorders, and many conventional treatments carry unwanted side effects. Plant-derived compounds like flavonoids play a significant role in alleviating such conditions by scavenging free radicals, chelating metal ions, or inhibiting radical-producing proteins. This study aimed to perform a preclinical pilot investigation of quercetin and its semisynthetic O-methylated derivatives to optimize their dose and establish their analgesic and anti-inflammatory efficacy using male Albino Wistar rats. For pilot study, the doses were selected according to OECD guideline 423. According to OECD guideline 423, doses of 0.025, 0.05, 0.1, and 0.2 g kg^-1 were selected. Analgesic activity was assessed using the tail-flick method, while anti-inflammatory activity was evaluated with the Carrageenan-induced paw edema test. Diclofenac sodium (0.01 g kg^-1) was used as the reference drug. Quercetin and its derivatives were tested at two optimized doses of 0.1 g kg^-1 and 0.2 g kg^-1. From the current pilot study, it was revealed that the selected standardized two doses (0.1 g per kilogram and 0.2 g per kilogram) of quercetin, its semisynthetic derivatives possessed significant activity in a dose-related pattern. The aforementioned approaches were conducted under a controlled and closely monitored environment, according to rigorous protocols for the ethical treatment of experimental animals, and with the explicit approval of the IAEC. The current investigation concluded that quercetin and its semisynthetic O-methylated derivatives had potent analgesic and anti-inflammatory effects when administered a dosage of 0.1 g per kilogram and 0.2 g per kilogram.

چکیده انگلیسی:

Pain and inflammation are associated with numerous disorders, and many conventional treatments carry unwanted side effects. Plant-derived compounds like flavonoids play a significant role in alleviating such conditions by scavenging free radicals, chelating metal ions, or inhibiting radical-producing proteins. This study aimed to perform a preclinical pilot investigation of quercetin and its semisynthetic O-methylated derivatives to optimize their dose and establish their analgesic and anti-inflammatory efficacy using male Albino Wistar rats. For pilot study, the doses were selected according to OECD guideline 423. According to OECD guideline 423, doses of 0.025, 0.05, 0.1, and 0.2 g kg^-1 were selected. Analgesic activity was assessed using the tail-flick method, while anti-inflammatory activity was evaluated with the Carrageenan-induced paw edema test. Diclofenac sodium (0.01 g kg^-1) was used as the reference drug. Quercetin and its derivatives were tested at two optimized doses of 0.1 g kg^-1 and 0.2 g kg^-1. From the current pilot study, it was revealed that the selected standardized two doses (0.1 g per kilogram and 0.2 g per kilogram) of quercetin, its semisynthetic derivatives possessed significant activity in a dose-related pattern. The aforementioned approaches were conducted under a controlled and closely monitored environment, according to rigorous protocols for the ethical treatment of experimental animals, and with the explicit approval of the IAEC. The current investigation concluded that quercetin and its semisynthetic O-methylated derivatives had potent analgesic and anti-inflammatory effects when administered a dosage of 0.1 g per kilogram and 0.2 g per kilogram.

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