Chemical Characterization and Anti-Inflammatory Activity of Phytoconstituents from Swertia alata.

Sakshi Bajaj,Himangini Bansal,Dhanalekshmi Unnikrishnan Meenakshi,Neeraj Kumar Fuloria,Satish Manchanda,Sharad Wakode,Shivkanya Fuloria,Vetriselvan Subramaniyan,Avneet Kaur,Sachin Kumar

doi:10.3390/plants10061109

Abstract

Swertia alata C.B Clarke (Gentianaceae) is a well-reported plant in the traditional system of medicine. The present study was intended to isolate the phytoconstituents from the ethanolic extract of the aerial parts of S. alata; and evaluate for in vitro COX-1/COX-2 inhibition activity, in vivo anti-inflammatory and ulcerogenic activity. Phytoisolation involved partitioning of S. alata ethanolic extract into petroleum ether and chloroform soluble fractions using silica gel-based column chromatography. The isolation afforded two phytoisolates, namely oleanolic acid (SA-1) and 3-hydroxylup-12-(13)-ene-17-carboxylic acid (SA-4). Phytoisolates structures were established by melting point, ultraviolet (UV), attenuated total reflection-Fourier-transform infrared (ATR-FTIR), nuclear magnetic resonance (1H-NMR, 13C-NMR and HMBC) and mass spectrometry. Phytoisolates were further evaluated for in vitro cyclooxygenase (COX-1/COX-2) inhibitory activity, in vivo anti-inflammatory and ulcerogenic activity. The study revealed SA-4 (COX-1/COX-2 inhibition activity of 104/61.68 µM with % inhibition of 61.36) to be more effective than SA-1 (COX-1/COX-2 inhibition activity of 128.4/87.25 µM, with % inhibition of 47.72). SA-1 and SA-4, when subjected to ulcerogenic study, exhibited significant gastric tolerance. The current study reports chromatographic isolation and spectrometric characterization of SA-1 and SA-4. The present study concludes that compound SA-4 possess significant anti-inflammatory activity and less irritant property over gastric mucosa with no significant ulcerogenicity in comparison to indomethacin.

Highlights

The structural elucidations of isolated compounds were achieved by melting point, ultraviolet (UV), attenuated total reflection-Fourier-transform infrared (ATR-FTIR), nuclear magnetic resonance (1H-NMR, 13C-NMR and HMBC), and mass spectrometry
Results of the present study revealed that the phytoisolates SA-1 and SA-4 exhibit dose-dependent anti-inflammatory activity by suppressing the rat paw edema
Macroscopical examination suggests that 24 mg/kg of S. alata can be an effective treatment for the management of inflammatory responses. These results suggest that phytoisolate of SA-4 could be a potent action for the anti-inflammatory effects

Summary

Introduction

Swertia alata C.B Clarke (Gentianaceae) is a perennial herb and widely distributed plant in the west and north-west Himalayas, in Kashmir to Kumaon, Mussorie, Dehradun, and the Nainital region of India [1]. Numerous species of Swertia are being used as substituents or adulterants of S. chirata. S. alata is used and unknowingly collected as S. chirata by traders for the preparation of several ayurvedic drugs [2]. S. alata is widely used in indigenous medicine as it possesses various properties. The bitterness, anthelmintic, hypoglycemic, and antipyretic properties are attributed to amarogentin, swerchirin, swertiamarin, and other active principles of the herb [3]. The most potential specie of Swertia genus is S. chirata, which is nearly extinct from India.

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