Abstract
Purpose: To carry out computational and pharmacological evaluation of two stevioside derivatives in order to develop more effective candidates for analgesia and inflammation.Methods: Primarily, compounds were docked against targets of nociception and inflammation such as cyclooxygenase-1, cyclooxygenase-2, 5-lypooxygenase 12-lypooxygenase, 15-lypooxygenase, prostaglandin synthase, leukotrienes C4 synthase, mu, kappa, and delta receptors to obtain their possible binding modes. Test compounds were then screened in animal model of nociception and inflammation.Results: The results of docking show that IO possesses good affinity when compared to ID. IO showed two hydrogen bonds against COX-1 and COX-2. IO also demonstrated good binding against 5-LOX, 12- LOX and 15-LOX, exhibited four, one and two hydrogen bonds respectively. Against PG synthase and LTC4, both IO and ID produced moderate binding. IO also showed significant binding against opoid receptors (p < 0.05). IO and ID significantly decrease the number of writhes to 21.20 ± 2.1 and 27.0 ± 2.12 at 10 mg/kg in acetic acid mediated pain test respectively. In hot plate method, IO and ID increase the latency period of mice to 14.14 ± 0.40 and 10.50 ± 0.34 s, respectively. IO and ID significantly reduced the paw edema to 1.69 ± 0.14 and 1.94 ± 0.14 mL, respectively, in acute inflammation (p < 0.05). In chronic inflammatory model, IO and ID decreased paw volume to 3.26 ± 0.38 and 4.20 ± 0.38 mL, respectively.Conclusion: The results show that IO is a promising candidate for further development as analgesic and anti-inflammatory agents. However, their pharmacokinetic and pharmacodynamic profiles need to be investigated.
 Keywords: Computational, Stevioside, Docking, Analgesic, Anti-inflammatory
Highlights
Stevioside was first isolated from leaves of Stevia rebaudiana Bertoni, a perennial herb belongs to family asteraecea [1]
Stevioside are effective in controlling obesity, atherosclerosis [3], hypertension, diabetes mellitus [4], cancer, inflammation [5], and free radical scavenging activities [6]
After in-silico screening, isosteviol 16-Oxime (IO) and ID were evaluated for in-vivo experimentation in determining their analgesic and antiinflammatory potential in different animal models as acetic acid induced pain, thermal nociception, carrageenan and formalin mediated paw inflammation
Summary
Stevioside was first isolated from leaves of Stevia rebaudiana Bertoni, a perennial herb belongs to family asteraecea [1]. Stevioside are effective in controlling obesity, atherosclerosis [3], hypertension, diabetes mellitus [4], cancer, inflammation [5], and free radical scavenging activities [6] Based on their wide spectrum in both medicine and food, two derivatives of steviol glycosides, namely isosteviol 16-Oxime (IO) and isosteviol 16-2, 4 dinitrophenyl hydrazine (ID) were utilized in this research. After in-silico screening, IO and ID were evaluated for in-vivo experimentation in determining their analgesic and antiinflammatory potential in different animal models as acetic acid induced pain, thermal nociception, carrageenan and formalin mediated paw inflammation. After 30 min of treatment with saline, test compound and diclofenac sodium chronic inflammation was induced by sub-aponeurotic injection of formalin (0.1 mL). ANOVA with post-hoc Tukey’s test was applied to interpret data. p < 0.05 was considered as significant
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
