A brief review of the biological potential of indole derivatives

Kumar, Sunil; Ritika, .

doi:10.1186/s43094-020-00141-y

Cited by 137 publications

(72 citation statements)

References 81 publications

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“…Given both the remarkable selectivity and antiviral activity of these compounds, we chose to continue expanding this library of tetrapodal SCRs in an effort to develop design rules that anticipate substrate selectivity and binding affinities for future use as antivirals, drug‐delivery agents, or as catalysts/ligands in glycan synthesis. Indoles are abundant in nature and they play an important role in cell biology and are found in various medically‐relevant natural products, [40] and several indole derivatives are currently being explored for their antiviral, anti‐inflammatory, anticancer, anti‐HIV, antioxidant, antimalarial, and antitubercular activities [41] . Taken together, these led us to further explore how indole structure affected SCR binding affinity and selectivity.…”

Section: Introductionmentioning

confidence: 99%

Regiochemical Effects on the Carbohydrate Binding and Selectivity of Flexible Synthetic Carbohydrate Receptors with Indole and Quinoline Heterocyclic Groups

et al. 2021

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Synthetic carbohydrate receptors (SCRs) that bind cell‐surface carbohydrates could be used for disease detection, drug‐delivery, and therapeutics, or for the site‐selective modification of complex carbohydrates, but their potential has not been realized because of remaining challenges associated with binding affinity and substrate selectivity. We have reported recently a series of flexible SCRs based upon a biaryl core with four pendant heterocyclic groups that bind glycans selectively through noncovalent interactions. Here we continue to explore the role of heterocycles on substrate selectivity by expanding our library to include a series of indole and quinoline heterocycles that vary in their regiochemistry of attachment to the biaryl core. The binding of these SCRs to a series of biologically‐relevant carbohydrates was studied by 1H NMR titrations in CD2Cl2 and density‐functional theory calculations. We find SCR030, SCR034 and SCR037 are selective, SCR031, SCR032, and SCR039 are strong binders, and SCR033, SCR035, SCR036, and SCR038 are promiscuous and bind weakly. Computational analysis reveals the importance of C−H⋅⋅⋅π and H‐bonding interactions in defining the binding properties of these new receptors. By combining these data with those obtained from our previous studies on this class of flexible SCRs, we develop a series of design rules that account for the binding of all SCRs of this class, and anticipate the binding of future, not‐yet imagined tetrapodal SCRs.

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Section: Introductionmentioning

confidence: 99%

Regiochemical Effects on the Carbohydrate Binding and Selectivity of Flexible Synthetic Carbohydrate Receptors with Indole and Quinoline Heterocyclic Groups

et al. 2021

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“…Biological actions of derivatives containing the indole core include antidiabetic, anticancer, antibacterial, anti-HIV, antiviral, anti-inflammatory, and antioxidant. Indole has a broad range of biological functions and offers a lot of potential when it comes to novel therapeutic options [ 45 ].…”

Section: Resultsmentioning

confidence: 99%

Immunomodulatory Efficacy-Mediated Anti-HCV and Anti-HBV Potential of Kefir Grains; Unveiling the In Vitro Antibacterial, Antifungal, and Wound Healing Activities

et al. 2022

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The utilization of fermented foods with health-promoting properties is becoming more popular around the world. Consequently, kefir, a fermented milk beverage made from kefir grains, was shown in numerous studies to be a probiotic product providing significant health benefits. Herein, we assessed the antibacterial and antifungal potential of kefir against a variety of pathogenic bacteria and fungi. This study also showed the effectiveness of kefir in healing wounds in human gastric epithelial cells (GES-1) by (80.78%) compared with control (55.75%) within 48 h. The quantitative polymerase chain reaction (qPCR) results of kefir-treated HCV- or HBV- infected cells found that 200 µg/mL of kefir can eliminate 92.36% of HCV and 75.71% of HBV relative to the untreated infected cells, whereas 800 µg/mL (the highest concentration) completely eradicated HCV and HBV. Moreover, the estimated IC50 values of kefir, at which HCV and HBV were eradicated by 50%, were 63.84 ± 5.81 µg/mL and 224.02 ± 14.36 µg/mL, correspondingly. Kefir can significantly suppress the elevation of TNF-α and upregulate IL-10 and INF-γ in both treated HCV- and HBV-infected cells. High-performance liquid chromatography (HPLC) and gas chromatography-mass spectrometry (GC-MS) analysis of kefir revealed the presence of numerous active metabolites which mainly contribute to the antimicrobial, antiviral, and immunomodulatory activities. This study demonstrated, for the first time, the anti-HBV efficacy of kefir while also illustrating the immunomodulatory impact in the treated HBV-infected cells. Accordingly, kefir represents a potent antiviral agent against both viral hepatitis C and B, as well as having antimicrobial and wound healing potential.

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“…The choice to use Cau in this study was based on its particular chemical structure, characterized by two indole nuclei. Indole, in fact, has been considered the most privileged scaffold in drug discovery [ 51 , 52 ] because of its anti-inflammatory, anti-cancer, antioxidant, anti-diabetic, antimicrobial, antiviral and anti-hypertensive roles [ 32 , 51 , 53 ]. In addition, the presence of two indole nuclei makes Cau similar to W-rich peptides, such as WRW 4 , which was found to interact with FPR2, exerting antagonistic effects [ 54 ].…”

Section: Discussionmentioning

confidence: 99%

Caulerpin Mitigates Helicobacter pylori-Induced Inflammation via Formyl Peptide Receptors

Cuomo

Medaglia

Allocca

et al. 2021

IJMS

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The identification of novel strategies to control Helicobacter pylori (Hp)-associated chronic inflammation is, at present, a considerable challenge. Here, we attempt to combat this issue by modulating the innate immune response, targeting formyl peptide receptors (FPRs), G-protein coupled receptors that play key roles in both the regulation and the resolution of the innate inflammatory response. Specifically, we investigated, in vitro, whether Caulerpin—a bis-indole alkaloid isolated from algae of the genus Caulerpa—could act as a molecular antagonist scaffold of FPRs. We showed that Caulerpin significantly reduces the immune response against Hp culture filtrate, by reverting the FPR2-related signaling cascade and thus counteracting the inflammatory reaction triggered by Hp peptide Hp(2–20). Our study suggests Caulerpin to be a promising therapeutic or adjuvant agent for the attenuation of inflammation triggered by Hp infection, as well as its related adverse clinical outcomes.

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A brief review of the biological potential of indole derivatives

Cited by 137 publications

References 81 publications

Regiochemical Effects on the Carbohydrate Binding and Selectivity of Flexible Synthetic Carbohydrate Receptors with Indole and Quinoline Heterocyclic Groups

Regiochemical Effects on the Carbohydrate Binding and Selectivity of Flexible Synthetic Carbohydrate Receptors with Indole and Quinoline Heterocyclic Groups

Immunomodulatory Efficacy-Mediated Anti-HCV and Anti-HBV Potential of Kefir Grains; Unveiling the In Vitro Antibacterial, Antifungal, and Wound Healing Activities

Caulerpin Mitigates Helicobacter pylori-Induced Inflammation via Formyl Peptide Receptors

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