A comprehensive insight on the biological potential of embelin and its derivatives

Basha, N. Jeelan; Basavarajaiah, S. M.; Baskaran, Swathi; Kumar, Prasanna

doi:10.1080/14786419.2021.1955361

Cited by 31 publications

(17 citation statements)

References 74 publications

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“…However, its cardiac side effects, leading to cardiomyopathy and congestive heart failure, have limited the clinical use of this potent anticancer drug. 56 Therefore, more effective therapeutic agents are needed considering previous reports of embelin against myocardial injury, 48 − 50 and since so far protective effects of embelin and embelin derivatives against anthracycline-induced cardiotoxicity have not been tested, 57 in the present study, we aimed to determine whether cardiotoxicity induced by chemotherapy could be attenuated by embelin derivatives when administrated in conjunction with chemotherapeutical agents.…”

Section: Results and Discussionmentioning

confidence: 99%

Synthesis of Quinoline and Dihydroquinoline Embelin Derivatives as Cardioprotective Agents

et al. 2023

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A set of new dihydroquinoline embelin derivatives was obtained from the reaction of the natural benzoquinone embelin ( 1 ) with anilines and aromatic aldehydes in the presence of AgOTf. The synthesis of these compounds involves the formation of a Knoevenagel adduct, followed by nucleophilic addition of aniline and subsequent electrocyclic ring closure. The scope of the reaction regarding the aldehydes and anilines was determined. Quinoline derivatives were also obtained from the corresponding dihydroquinolines under oxidation with DDQ. The cardioprotective activity of the synthesized compounds was screened using a doxorubicin-induced cardiotoxicity model in H9c2 cardiomyocytes. Some structure–activity relationships were outlined, and the best activities were achieved with quinoline-embelin derivatives having a 4-nitrophenyl group attached at the pyridine ring. The obtained results indicated that embelin derivatives 4i , 6a , 6d , 6k , and 6m could have potential as cardioprotective agents, as they attenuated a DOX-induced cardiotoxicity effect acting on oxidative stress and apoptosis.

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Section: Results and Discussionmentioning

confidence: 99%

Synthesis of Quinoline and Dihydroquinoline Embelin Derivatives as Cardioprotective Agents

et al. 2023

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“…10 Fused pyrrole analogs as potential anticancer agents I compound (32) showed significant antiproliferative activity in MDA-MB human cancer cell lines. Many natural products are known to possess potential anticancer activity [114,115]. One such natural product, pyrrolomycin, a polyhalogenated antibiotic (33 a), has potent anticancer activity.…”

Section: Anticancer Agentsmentioning

confidence: 99%

Therapeutic potential of pyrrole and pyrrolidine analogs: an update

Basha¹,

Basavarajaiah²,

Shyamsunder³

2022

Mol Divers

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The chemistry of nitrogen-containing heterocyclic compound pyrrole and pyrrolidine has been a versatile field of study for a long time for its diverse biological and medicinal importance . Biomolecules such as chlorophyll, hemoglobin, myoglobin, and cytochrome are naturally occurring metal complexes of pyrrole. These metal complexes play a vital role in a living system like photosynthesis, oxygen carrier, as well storage, and redox cycling reactions. Apart from this, many medicinal drugs are derived from either pyrrole, pyrrolidine, or by its fused analogs. This review mainly focuses on the therapeutic potential of pyrrole, pyrrolidine, and its fused analogs, more specifically anticancer, anti-inflammatory, antiviral, and antituberculosis. Further, this review summarizes more recent reports on the pyrrole, pyrrolidine analogs, and their biological potential. Graphical Abstract

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“…This compound is reported to have antibacterial activity against Staphylococcus aureus, Streptococcus pyogenes, Shigella flexneri, Shigella sonnei, Pseudomonas aeruginosa, Shigella boydii, and Proteus mirabilis [20]. In addition, Embelin is also reported to exhibit anticancer, antioxidant, antimalarial, antiviral, antidiabetic, and anti-inflammatory activity [23]. Therefore, it could suggest that Embelin is the active antibacterial compound in JSR, even though other compounds are also prospective to be explored, such as 2,6-diamino-4hexenoic acid, palmitamide, and 3-hydroxybutyric acid.…”

Section: Embelinmentioning

confidence: 99%

Antibacterial Activity of Jojoba Seed residue and Its Possible Active Compound

et al. 2022

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Jojoba (Simmondsia chinensis) (Link) C.K. is a shrub plant widely used in cosmetics, especially jojoba oil. The residue will remain when producing jojoba oil and become waste. This study aimed to determine the antibacterial activity of Jojoba seed residue (JSR) and its possible active antibacterial compounds. JSR was collected from Sudan and extracted by maceration with n-hexane, ethyl acetate, and 70% ethanol. The antibacterial activity was determined with the microdilution method against Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli). The 70% ethanol extract showed the value of MIC and MBC against E. coli, which was 7.8 mg/ml; meanwhile, against S. aureus was 3.9 mg/mL and 7.8 mg/mL, respectively. Fractionation of 70% ethanol extract using silica gel column chromatography with gradient elution produced ten fractions. Fraction 3 showed the MIC and MBC values in E. coli which were 3.1 mg/mL and 12 mg/ml, and in S. aureus, which were 3.1 mg/mL and 6.2 mg/mL. The fractionation continued to Fraction 3 using preparative thin layer chromatography to collect subfraction 3.2 at an Rf value of 0.76, actively based on contact autobiography against E. coli and S. aureus. Embelin was detected in Subfraction 3.2 using liquid chromatography-mass spectrometry (UHPLC-Q-Orbitrap HRMS) and suggested as the active antibacterial component in JSR.

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A comprehensive insight on the biological potential of embelin and its derivatives

Cited by 31 publications

References 74 publications

Synthesis of Quinoline and Dihydroquinoline Embelin Derivatives as Cardioprotective Agents

Synthesis of Quinoline and Dihydroquinoline Embelin Derivatives as Cardioprotective Agents

Therapeutic potential of pyrrole and pyrrolidine analogs: an update

Antibacterial Activity of Jojoba Seed residue and Its Possible Active Compound

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