Mechanism of streptomyces albidoflavus STV1572a derived 1-heneicosanol as an inhibitor against squalene epoxidase of Trichophyton mentagrophytes

Thekkangil, Aswani; George, Benu; Prakash, Sagunthala Murugesan Udaya; Suchithra, T. V.

doi:10.1016/j.micpath.2021.104853

Cited by 7 publications

(4 citation statements)

References 25 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Similarly, diterpene phenol, ferruginol has pharmacological properties such as inhibition of the growth rate of cancer cells [37]. Other compounds which have also been reported to have anticancer activity include 1-octadecene, 1heneicosanol, and 2,4-di-tert-butylphenol [38][39][40]. Given that these compounds are found in the ethyl acetate fraction of E. ingens, we suggest that they may be responsible for the demonstrated antiproliferative effects of the plant on DU-145 cells.…”

Section: Discussionmentioning

confidence: 85%

Antiproliferative Activity of Euphorbia ingens Extract against Prostate Cancer Cell Line: An in silico and in vitro Analysis

Okpako¹,

Ng’ong’a²,

Kyama³

et al. 2023

Preprint

View full text Add to dashboard Cite

Euphorbia ingens is traditionally used to treat and manage cancer in Ambeere community of Embu County in Kenya. Whilst research has demonstrated the bioactivities of E. ingens including antimicrobial, antitubercular and antifungal activities, scientific validation of its anticancer properties is limited. This study evaluated the antiproliferative potentials of E. ingens on human prostate cancer cell line (DU-145). The 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay was used to assess the antiproliferative activity, chemical constituents were analysed by qualitative colour method and Gas Chromatography-Mass Spectrometry analysis. At the same time, the investigation of putative molecular targets and mechanisms of action of E. ingens was done through network pharmacological analysis. Reverse transcription-quantitative polymerase chain reaction (RT-qPCR) was carried out to validate the network predictions of putative targets. Our result showed E. ingens ethyl acetate inhibited DU-145 growth (IC50 of 9.71 ± 0.4 µg/ml) with a high selectivity index of 8.26. There was the presence of phenols, terpenoids, flavonoids, tannins, sterols, and saponins; additional 18 compounds were identified by the GC-MS approach. ESR1, IL6, MMP9, CDK2, MAP2K1, AR, PRKCD, CDK1, CDC25B, and JAK2 were indicated as key targets of E. ingens against prostate cancer with the PI3K-AKT, MAPK, and p53 signalling pathways identified as the most probable mechanisms of action. There was significant downregulation of AR and BCL2, and upregulation of p53 and caspase-3 in E. ingens-treated DU-145 cells compared to 0.2 % DMSO negative control. Our results suggest that E. ingens has phytochemical compounds efficacious at inhibiting the proliferation of DU-145 cells; therefore, the plant can be considered a potential source of compounds that may be used to manage and treat prostate cancer; however, further in vivo evaluations are needed.

show abstract

Section: Discussionmentioning

confidence: 85%

Antiproliferative Activity of Euphorbia ingens Extract against Prostate Cancer Cell Line: An in silico and in vitro Analysis

Okpako¹,

Ng’ong’a²,

Kyama³

et al. 2023

Preprint

View full text Add to dashboard Cite

show abstract

“…Detailed information of the five target proteins involved in dermatophytosis induced by T. mentagrophytes are retrieved from UniProt Database and the corresponding proteins such as glucan 1,3‐beta‐glucosidases ARB_02797 (UniProt Id D4B2W4), probable class II chitinase ARB_00204 (UniProt Id D4AVJ0), squalene monooxygenase (UniProt Id A0A289Z0K1), actin (UniProt Id H6X152), ubiquitin (UniProt Id Q9Y736) [10] are depicted for in silico study (Table 1).…”

Section: Resultsmentioning

confidence: 99%

“…Details of these targeted genes are obtained from UniProt database [9] and selected for in silico study. Five proteins such as glucan 1,3‐beta‐glucosidase ARB_02797, Probable class II chitinase ARB_00204, squalene monooxygenase, actin, and ubiquitin are considered as targets of T. mentagrophytes [10].…”

Section: Methodsmentioning

confidence: 99%

Phytochemical inhibitors from Leucas aspera against the target proteins induced by Trichophyton mentagrophytes using computational techniques

Giri,

Parida

2024

J Basic Microbiol

View full text Add to dashboard Cite

Dermatophytosis is a cutaneous infection that is able to degrade the keratinized tissues of the animal/human body, like skin, nails, and hair, causing chronic or subacute infection with the contact of some specific fungal strains. Trichophyton mentagrophytes are the most potential fungal pathogen causing dermatophytoses. The present study focuses on computationally based in silico antifungal activity of selected phytocompounds of Leucas aspera (Willd.) Link. against dermatophytic fungus, T. mentagrophytes. Validation and screening of derived phytocompounds is performed using Lipinski rule of five and toxicity test through Protox‐II. Five target genes involved in dermatophytosis, induced by T. mentagrophytes are retrieved from the UniProt Database, and the corresponding proteins such as glucan 1,3‐beta‐glucosidase ARB_02797, Probable class II chitinase ARB_00204, squalene monooxygenase, actin, and ubiquitin are selected for in silico study. Three‐dimensional structures of the target protein were computationally determined and validated through modeling tools and techniques due to the lack of validated protein structures in the database. Then, these proteins are used for in silico molecular docking through the AutoDock Vina tool to find out the promising phytocompounds. This study could be utilized in designing more effective drugs against T. mentagrophytes. Based on this work, a plant‐based natural alternative can be added to the treatment of dermatophytosis rather than synthetic supplements.

show abstract

“…The inoculum was made using a sterile saline solution with 95 % of transmission at 530 nm. Accordingly, the inoculum concentration ranging 1 × 10 6 CFU/mL was achieved (16).…”

Section: Preparation Of Inoculums Clinical Isolates Ofmentioning

confidence: 99%

Effect of fluconazole and terbinafine nanoparticles on the treatment of dermatophytosis induced by Trichophyton mentagrophytes in guinea pig

Lalvand

Hashemi

Bayat

2021

IJM

View full text Add to dashboard Cite

Background and Objectives: Dermatophytosis induced by Trichophyton mentagrophytes is a major human and animal fun- gal contamination. Antifungals like terbinafine and fluconazole are widely used to treat dermatophytosis; nevertheless, the prevalence of drug resistance has increased. Hence, novel curative strategies are needed. In the present study, we compared the efficacies of conventional and nanoform of antifungals agents in guinea pig model of dermatophytosis. Materials and Methods: Guinea pigs (n=36) were injected (the posterior dorsal portion) with Trichophyton mentagrophytes conidia. The guinea pigs were divided into 6 groups (positive control, negative control, fluconazole 0.5% treated group, na- no-fluconazole treated group, terbinafine 1% treated group, and nano-terbinafine treated group), then were scored both clin- ically (redness and lesion intensity) and mycologically (microscopy and culture) until day 40 of inoculation. The treatment started 5 days after the inoculation and continued until day 40 of inoculation. Results: Assessment of the mean score of clinical lesions in groups treated with nano-drug forms of fluconazole and terbin- afine on the first day of treatment showed a score of 3 (significant redness with large scaling) and for the conventional form of terbinafine and fluconazole had a score of 4 (ulcer and scar). The decrease in lesion score in nano-drug treated groups was observed between days 15 and 20 and continued until day 40. On day 40, all groups had zero scores except the positive control group. Conclusion: This study indicated that nano-drugs are more suitable for the treatment of dermatophytosis and could be con- sidered as future alternatives for the treatment of dermatophytosis.

show abstract

Mechanism of streptomyces albidoflavus STV1572a derived 1-heneicosanol as an inhibitor against squalene epoxidase of Trichophyton mentagrophytes

Cited by 7 publications

References 25 publications

Antiproliferative Activity of Euphorbia ingens Extract against Prostate Cancer Cell Line: An in silico and in vitro Analysis

Antiproliferative Activity of Euphorbia ingens Extract against Prostate Cancer Cell Line: An in silico and in vitro Analysis

Phytochemical inhibitors from Leucas aspera against the target proteins induced by Trichophyton mentagrophytes using computational techniques

Effect of fluconazole and terbinafine nanoparticles on the treatment of dermatophytosis induced by Trichophyton mentagrophytes in guinea pig

Contact Info

Product

Resources

About