Assessment of Anti-inflammatory Activity of 3-Acetylmyricadiol in LPSStimulated Raw 264.7 Macrophages.

BACKGROUND: Pentacyclic triterpenoids are a biologically active class of phytoconstituents with diverse pharmacological activities, including anti-inflammatory action. OBJECTIVE: In the current study, we isolated 3-Acetylmyricadiol, a pentacyclic triterpenoid, from the ethyl acetate bark extract of Myrica esculenta and evaluated it for anti-inflammatory potential. METHODS: The ethyl acetate bark extract of the M. esculenta was subjected to column chromatography to isolate 3-Acetylmyricadiol. MTT assay was performed to check cell viability. The production of proinflammatory mediators like nitric oxide, IL-6, TNF-α were observed after the administration of 5, 10, 20 µM of 3-Acetylmyricadiol in LPS-activated raw 246.7 macrophages by the reported methods. RESULTS: MTT assay indicated more than 90% cell viability up to 20 µM of 3-Acetylmyricadiol. The administration of 3-Acetylmyricadiol inhibited the production of nitric oxide, IL-6, TNF-α in a dose-dependent manner significantly in comparison to LPS treated cells. The maximum effect was observed at 20 µM of 3-Acetylmyricadiol which resulted in 52.37, 63.10, and 55.37 % inhibition of nitric oxide, IL-6, and TNF-α, respectively. CONCLUSION: Our study demonstrated the anti-inflammatory action of 3-Acetylmyricadiol and can serve as a potential candidate in the development of the clinically efficient anti-inflammatory molecule.

Bioactive Heterocyclic Compounds as Potential Therapeutics in the Treatment of Gliomas: A Review.

Cancer is one of the most alarming diseases, with an estimation of 9.6 million deaths in 2018. Glioma occurs in glial cells surrounding nerve cells. The majority of the patients with gliomas have a terminal prognosis, and the ailment has significant sway on patients and their families, be it physical, psychological, or economic wellbeing. As Glioma exhibits, both intra and inter tumour heterogeneity with multidrug resistance and current therapies are ineffective. So the development of safer anti gliomas agents is the need of hour. Bioactive heterocyclic compounds, eithernatural or synthetic, are of potential interest since they have been active against different targets with a wide range of biological activities, including anticancer activities. In addition, they can cross the biological barriers and thus interfere with various signalling pathways to induce cancer cell death. All these advantages make bioactive natural compounds prospective candidates in the management of glioma. In this review, we assessed various bioactive heterocyclic compounds, such as jaceosidin, hispudlin, luteolin, silibinin, cannabidiol, tetrahydrocannabinol, didemnin B, thymoquinone, paclitaxel, doxorubicin, and cucurbitacins for their potential anti-glioma activity. Also, different kinds of chemical reactions to obtain various heterocyclic derivatives, e.g. indole, indazole, benzimidazole, benzoquinone, quinoline, quinazoline, pyrimidine, and triazine, are listed.