Biological activity of a small molecule indole analog, 1-[(1H-indol-3-yl)methylene]-2-phenylhydrazine (HMPH), in chronic inflammation

Misra, Chandra Sekhar; Honnappa, Chethan Gejjalagere; Jitta, Srinivas Reddy; Gourishetti, Karthik; Daram, Prasanthi; Singh, Mahendra Pratap; Shrungeswara, Akhila Hosur; Nayak, Yogendra; Unnikrishnan, Mazhuvancherry Kesavan

doi:10.1016/j.cbi.2015.10.024

Cited by 9 publications

(3 citation statements)

References 39 publications

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“…In this study, the respective IC 50 values of EGCG for scavenging DPPH and ABTS were found to be 8.52 ± 1.24 μg/mL and 4.12 ± 0.89 μg/mL, which are not noticeably different from those reported previously (Abbas & Wink, 2009 ). Similarly the IC 50 values of curcumin observed with DPPH and ABTS (19.19 ± 2.13 and 15.03 ± 2.67 μg/mL, respectively) were also found to be closely comparable to those reported in a previous study (Misra et al, 2016 ). Transfersomal EGCG showed slightly higher, but not significantly different, IC 50 values in comparison with plain EGCG.…”

Section: Resultssupporting

confidence: 90%

Skin delivery of epigallocatechin-3-gallate (EGCG) and hyaluronic acid loaded nano-transfersomes for antioxidant and anti-aging effects in UV radiation induced skin damage

et al. 2017

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(2017) Skin delivery of epigallocatechin-3-gallate (EGCG) and hyaluronic acid loaded nano-transfersomes for antioxidant and anti-aging effects in UV radiation induced skin damage, Drug Delivery, 24:1, 61-74, DOI: 10.1080/10717544.2016 AbstractThe present work attempts to develop and statistically optimize transfersomes containing EGCG and hyaluronic acid to synergize the UV radiation-protective ability of both compounds, along with imparting antioxidant and anti-aging effects. Transfersomes were prepared by thin film hydration technique, using soy phosphatidylcholine and sodium cholate, combined with high-pressure homogenization. They were characterized with respect to size, polydispersity index, zeta potential, morphology, entrapment efficiency, Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD), in vitro antioxidant activity and ex vivo skin permeation studies. Cell viability, lipid peroxidation, intracellular ROS levels and expression of MMPs (2 and 9) were determined in human keratinocyte cell lines (HaCaT). The composition of the transfersomes was statistically optimized by Design of Experiments using Box-Behnken design with four factors at three levels. The optimized transfersome formulation showed vesicle size, polydispersity index and zeta potential of 101.2 ± 6.0 nm, 0.245 ± 0.069 and À44.8 ± 5.24 mV, respectively. FTIR and DSC showed no interaction between EGCG and the selected excipients. XRD results revealed no form conversion of EGCG in its transfersomal form. The optimized transfersomes were found to increase the cell viability and reduce the lipid peroxidation, intracellular ROS and expression of MMPs in HaCaT cells. The optimized transfersomal formulation of EGCG and HA exhibited considerably higher skin permeation and deposition of EGCG than that observed with plain EGCG. The results underline the potential application of the developed transfersomes in sunscreen cream/lotions for improvement of UV radiation-protection along with deriving antioxidant and anti-aging effects.

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Section: Resultssupporting

confidence: 90%

Skin delivery of epigallocatechin-3-gallate (EGCG) and hyaluronic acid loaded nano-transfersomes for antioxidant and anti-aging effects in UV radiation induced skin damage

et al. 2017

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“…Nacylhydrazones are well described in the literature as anti-inflammatory agents 9,32,33 and the indole heteroaromatic group was related to the maximal anti-inflammatory response in a carrageenan-induced paw edema assay, as described by Bhookya et al (2017). 34 In addition, the pharmacologic potential of hydrazone-indole compounds has been reported in models of acute and chronic inflammation 35 , which highlights the importance of these nuclei for the development of anti-inflammatory activity.…”

Section: Figmentioning

confidence: 93%

Synthesis, in vitro and in vivo biological evaluation, COX-1/2 inhibition and molecular docking study of indole-N-acylhydrazone derivatives

Moraes

Miranda

Jacob

et al. 2018

Bioorganic & Medicinal Chemistry

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“…5-Nitro-3-[(5-nonsubstituted/methyl-4-thiazolidinone-2ylidene) hydrazono]-1H-2-indolinones were prepared and tested for antiviral activities by Terzioğlu et al Compounds (Z)-4-allyl-1-(1-(morpholinomethyl)-5-nitro-2-oxoindolin-3-ylidene)thiosemicarbazide (9), (3Z,3E)-3-(2-(3-ethyl-4oxothiazolidin-2-ylidene)hydrazono)-5-nitroindolin-2-one (10), (3Z,3E)-5-nitro-3-(2-(4-oxo-3-phenylthiazolidin-2-ylidene)hydrazono)indolin-2-one (11), (3Z,3E)-3-(2-(3-(4-bromophenyl)-5-methyl-4-oxothiazolidin-2-ylidene)hydrazono)-5-nitroindolin-2-one (12) and (3Z,3E)-3-(2-(3-(4chlorophenyl)-5-methyl-4-oxothiazolidin-2-ylidene)hydrazono)-5-nitroindolin-2-one (13) prevented the development of bovine viral diarrhea virus in cells [9]. 7-Ethoxy-1-methyl-4, 9-dihydro-3H-pyrido [3, 4-b]indole derivatives were reported as anti-Herpes Simplex virus-1(HSV-1) compounds by El-sawy et al and derivatives ethyl (17) possessed considerable antiviral activity with IC 50 ranged between 5 and 6 μg/ml and substantial therapeutic indices (TI) of 80 and 83 were recorded [10].…”

Section: Giampieri Et Al Elaborated Reaction Of Indoles and 2-mentioning

confidence: 99%

A brief review of the biological potential of indole derivatives

2020

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Background Various bioactive aromatic compounds containing the indole nucleus showed clinical and biological applications. Indole scaffold has been found in many of the important synthetic drug molecules which gave a valuable idea for treatment and binds with high affinity to the multiple receptors helpful in developing new useful derivatives. Main text Indole derivatives possess various biological activities, i.e., antiviral, anti-inflammatory, anticancer, anti-HIV, antioxidant, antimicrobial, antitubercular, antidiabetic, antimalarial, anticholinesterase activities, etc. which created interest among researchers to synthesize a variety of indole derivatives. Conclusion From the literature, it is revealed that indole derivatives have diverse biological activities and also have an immeasurable potential to be explored for newer therapeutic possibilities.

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Biological activity of a small molecule indole analog, 1-[(1H-indol-3-yl)methylene]-2-phenylhydrazine (HMPH), in chronic inflammation

Cited by 9 publications

References 39 publications

Skin delivery of epigallocatechin-3-gallate (EGCG) and hyaluronic acid loaded nano-transfersomes for antioxidant and anti-aging effects in UV radiation induced skin damage

Skin delivery of epigallocatechin-3-gallate (EGCG) and hyaluronic acid loaded nano-transfersomes for antioxidant and anti-aging effects in UV radiation induced skin damage

Synthesis, in vitro and in vivo biological evaluation, COX-1/2 inhibition and molecular docking study of indole-N-acylhydrazone derivatives

A brief review of the biological potential of indole derivatives

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