Keywords : COX2
In-vivo analgesic and anti-inflammatory evaluation of synthesised novel new chromane and its analogues
European Journal of Molecular & Clinical Medicine,
2023, Volume 10, Issue 1, Pages 2924-2934
The current research protocol was carried to evaluate biological activity of synthesised new chromane and itsanalogues. New chromane {3,5,7-trihydroxy2-(4-hydroxy benzyl) chroman-4-one} isolated from dried leaves of Dillenia indica Linn, family Dilleniaceae is structurally relating with various reported chroman-4-one derivatives displaying remarkable in-vivo analgesic and anti-inflammatory activity.But the literature reveals that 0.8 – 1.0% yield of pure new chromane was obtained in isolation. Followingreported literature data of synthesis and in-silico study (COX2 binding);synthesized new chromane and its derivatives (SI-SX) were investigated for in-vivoanalgesic and anti-inflammatory examination respectively.in-vivo analgesic study (Tail immersion and hot plate method) also displayed the significant analgesic potential of new chromane and its O-alkyl substituents (especially SI) while other synthesized compounds (SV-SX) reported for moderate to mild effects w.r.t. reference drug.Moreover, synthetic new chromane and O-alkyl substituent (SI) exhibited maximum anti-inflammatory activity also in terms of increment of paw volume and percentage inhibition of paw edema while others (SV-SX) showed mild anti-inflammatory action in comparison to referencedrug.
Anti-Inflammatory and Gene Expression Studies of Terminalia chebula Extracts against Interleukins and TNF
European Journal of Molecular & Clinical Medicine,
2020, Volume 7, Issue 2, Pages 229-237
Aims: Since ages, several plant extracts and Ayurvedic formulations were used to treat
ailments and such studies were well documented in the recent decades. Even some of
the plants were screened for their efficacy as immunomodulators to restore and
rejuvenate the immune system. The present study deals in screening for the possible
healing effects of Terminalia chebula on IL-2 and IFN-γ levels.
Methods: The raw and dried fruits of the sample were pulverized finely and extracted with
methanol. Following which their aqueous solutions are reextracted with hexane, ethyl
acetate and chloroform to study the possible cytotoxic effects. Lipopolysaccharide (LPS)-
stimulated macrophage cells were used throughout the study to measure the effect of
extracts on nitric oxide (NO) production using Griess method. Expression of
Cyclooxygenase-2 (COX2) and tumor necrosis factor (TNF)-α were studied by real time
PCR quantification along with estimation of IL-1β and IL-6 cytokine levels using the
enzyme-linked immunosorbent assay (ELISA).
Results: The chloroform extract showed maximum NO inhibition at about 18.31±
1.6μmol/L. In accordance to the above result, COX2 and TNF-α were found to be
downregulated by 12 and 7 fold respectively at 100μg/mL (P < 0.005). Chloroform extract
significantly reduced IL-1β levels to 21.23 ± 0.21pg/ml (100μg/mL) and also lowered the
levels of IL-6 to 45.67± 3.31pg/ml (100μg/ml)
Conclusion: The present study confirmed the positive effect of the chloroform extract in
reducing the NO secretion and also by showing an inhibition in the expression of COX2,
IL-1β, IL-6, and TNF-α. Thus to conclude Terminalia chebula could be used as the best antiinflammatory
candidate drug in addition to the many chemical compounds available in the
medical markets.