Factorial design based curcumin ethosomal nanocarriers for the skin cancer delivery: <i>in vitro</i> evaluation

Peram, Malleswara Rao; Jalalpure, Sunil; Kumbar, Vijay; Patil, Sachin; Joshi, Sumit; Bhat, K. Ishwar; Diwan, Prakash V.

doi:10.1080/08982104.2018.1556292

Cited by 72 publications

(32 citation statements)

References 52 publications

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“…Cell preparations were analyzed by flow cytometry (BD Accuri™ C5 flow cytometer, BD Biosciences, CA, USA). Cytometry data were analyzed by FlowJo software (version 10.1, Ashland, OR, USA) [62].…”

Section: Apoptosis Studies By Flowcytometry-mentioning

confidence: 99%

Discovery of novel N-substituted thiazolidinediones (TZDs) as HDAC8 inhibitors: in-silico studies, synthesis, and biological evaluation

Upadhyay

Tilekar

Jänsch³

et al. 2020

Bioorganic Chemistry

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Epigenetics plays a fundamental role in cancer progression, and developing agents that regulate epigenetics is crucial for cancer management. Among Class I and Class II HDACs, HDAC8 is one of the essential epigenetic players in cancer progression. Therefore, we designed, synthesized, purified, and structurally characterized novel compounds containing N-substituted TZD (P1-P25). Cell viability assay of all compounds on leukemic cell lines (CEM, K-562, and KCL22) showed the cytotoxic potential of P8, P9, P10, P12, P19, and P25. In-vitro screening of different HDACs isoforms revealed that P19 was the most potent and selective inhibitor for HDAC8 (IC 50-9.3 μM). Thermal shift analysis (TSA) confirmed the binding of P19 to HDAC8. In-vitro screening of all compounds on the transport activity of GLUT1, GLUT4, and GLUT5 indicated that P19 inhibited GLUT1 (IC 50-28.2 μM). P10 and P19 induced apoptotic cell death in CEM cells (55.19% and 60.97% respectively) and P19 was less cytotoxic on normal WBCs (CC 50-104.2 μM) and human fibroblasts (HS27) (CC 50-105.0 μM). Thus, among this novel series of TZD *

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Section: Apoptosis Studies By Flowcytometry-mentioning

confidence: 99%

Discovery of novel N-substituted thiazolidinediones (TZDs) as HDAC8 inhibitors: in-silico studies, synthesis, and biological evaluation

Upadhyay

Tilekar

Jänsch³

et al. 2020

Bioorganic Chemistry

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“…Less than the 50 μg/ml of compounds was treated at 48 h. After the incubation, the cells were washed with PBS and fixed with 4% paraformaldehyde for 30 min. Twenty microliters of DAPI (0.1 μg/ml) was incubated for 5 min at room temperature in the dark and examined under fluorescent microscope, randomly selecting the fields in the microscope and counted the number of cells undergone apoptosis and then calculated the percentage of apoptotic cells [31].…”

Section: Diffusion Studiesmentioning

confidence: 99%

Design and characterization of camptothecin gel for treatment of epidermoid carcinoma

Galatage¹,

Hebalkar²,

Gote³

et al. 2020

Futur J Pharm Sci

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Background: The objective of present research work is to design and characterize camptothecin gel using Carbopol-934 for the treatment of epidermoid carcinoma. Optimized herbal gel formulations were evaluated for homogeneity and appearance, viscosity, extrudability, spreadability, drug content, drug release, pH, and in vitro skin cancer activity on A431 cell lines. Results: Mass and Infrared Spectra respectively conforms molecular weight and functional groups present in camptothecin. All the formulations F1 to F5 showed good homogeneity, pH from 6.68 to 6.90, spreadability in the range of 15.81-23.37 gm.cm/s, extrudability 85.51-90.45% w/w, drug content 89.12-96.64%, and in vitro diffusion 88.36-98.40%, respectively. The drug release study showed that all the formulations followed a diffusion-controlled, zero-order release mechanism. Anticancer activity results indicate that camptothecin gel induce cell death in A-439 cells having IC 50 48.03 μg and % apoptosis 54.67 ± 4.58. Conclusion: Topical delivery of camptothecin alleviates the side effects caused by systemic chemotherapy; hence, the developed herbal gel formulation can be effectively useful to deliver camptothecin in the treatment of epidermoid carcinoma on A-431 cells.

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“…The synthesized compounds were screened for their toxicity against normal Human Embryonic kidney cell line (HEK293) [41] . As depicted in Table 1, the compounds have exhibited moderate to low levels of cytotoxicity with IC 50 values in the range of 195.4–581.1 μg/mL.…”

Section: Resultsmentioning

confidence: 99%

Synthesis of 1,2‐Disubstituted Imidazole Derivatives as Potent Inhibitors of Mycobacterium tuberculosis and Their In Silico Studies

et al. 2021

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A multi‐step synthetic protocol was employed to accomplish the synthesis of (2Z)‐2‐((E)‐4‐(benzylideneamino)phenyl)‐3‐(1‐methyl‐1H‐imidazol‐2‐yl)acrylonitrile derivatives. The title compounds were screened for antitubercular activity. Amongst them, three of the compounds appeared promising with a MIC value 0.2 to 0.4 μg/mL whereas the other compounds have also exhibited lower MIC than the standards. Docking study was performed to check their binding interaction and to deduce the possible mechanism of action involved in the inhibition process which revealed that the newly synthesized molecules act by inhibiting the DprE1 enzymatic pathway.

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Factorial design based curcumin ethosomal nanocarriers for the skin cancer delivery: in vitro evaluation

Cited by 72 publications

References 52 publications

Discovery of novel N-substituted thiazolidinediones (TZDs) as HDAC8 inhibitors: in-silico studies, synthesis, and biological evaluation

Discovery of novel N-substituted thiazolidinediones (TZDs) as HDAC8 inhibitors: in-silico studies, synthesis, and biological evaluation

Design and characterization of camptothecin gel for treatment of epidermoid carcinoma

Synthesis of 1,2‐Disubstituted Imidazole Derivatives as Potent Inhibitors of Mycobacterium tuberculosis and Their In Silico Studies

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