Dose-dependent proliferative and cytotoxic effects of melatonin on human epidermoid carcinoma and normal skin fibroblast cells

2018 ◽  
Vol 829-830 ◽  
pp. 50-60 ◽  
Author(s):  
Abdurrahim Kocyigit ◽  
Eray Metin Guler ◽  
Ersin Karatas ◽  
Hifa Caglar ◽  
Huri Bulut
Keyword(s):  
Skin Fibroblast ◽  
Normal Skin ◽  
Epidermoid Carcinoma ◽  
Fibroblast Cells ◽  
Cytotoxic Effects ◽  
Normal Skin Fibroblast ◽  
Dose Dependent ◽  
Human Epidermoid Carcinoma

scholarly journals Synthesis and Antiproliferative Activity of Marine Bromotyrosine Purpurealidin I and Its Derivatives

Marine Drugs ◽  
2018 ◽  
Vol 16 (12) ◽  
pp. 481 ◽  
Author(s):  
Chinmay Bhat ◽  
Polina Ilina ◽  
Irene Tilli ◽  
Manuela Voráčová ◽  
Tanja Bruun ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Skin Fibroblast ◽  
Melanoma Cell Line ◽  
Normal Skin ◽  
Selectivity Index ◽  
Cytotoxic Agents ◽  
Fibroblast Cells ◽  
Human Malignant Melanoma ◽  
Structure Activity ◽  
Normal Skin Fibroblast

The first total synthesis of the marine bromotyrosine purpurealidin I (1) using trifluoroacetoxy protection group and its dimethylated analog (29) is reported along with 16 simplified bromotyrosine derivatives lacking the tyramine moiety. Their cytotoxicity was evaluated against the human malignant melanoma cell line (A-375) and normal skin fibroblast cells (Hs27) together with 33 purpurealidin-inspired simplified amides, and the structure–activity relationships were investigated. The synthesized simplified analogs without the tyramine part retained the cytotoxic activity. Purpurealidin I (1) showed no selectivity but its simplified pyridin-2-yl derivative (36) had the best improvement in selectivity (Selectivity index 4.1). This shows that the marine bromotyrosines are promising scaffolds for developing cytotoxic agents and the full understanding of the elements of their SAR and improving the selectivity requires further optimization of simplified bromotyrosine derivatives.

Overexpression of miR-340-5p Inhibits Skin Fibroblast Proliferation by Targeting Kruppel-like Factor 2

2019 ◽  
Vol 20 (13) ◽  
pp. 1147-1154 ◽  
Author(s):  
Ling Chen ◽  
Qian Li ◽  
Xun Lu ◽  
Xiaohua Dong ◽  
Jingyun Li
Keyword(s):  
Gene Ontology ◽  
Skin Fibroblast ◽  
Kegg Pathway ◽  
Normal Skin ◽  
Skin Fibroblasts ◽  
Differentially Expressed ◽  
Luciferase Reporter ◽  
Fibroblast Proliferation ◽  
Pathway Analyses ◽  
Normal Skin Fibroblast

<P>Objective: MicroRNA (miR)-340-5p has been identified to play a key role in several cancers. However, the function of miR-340-5p in skin fibroblasts remains largely unknown. </P><P> Methods: Gain of function experiments were performed by infecting normal skin fibroblast cells with a lentivirus carrying 22-bp miR-340-5p. Cell proliferation was detected by Cell Counting Kit-8 (CCK-8) assay. To uncover the mechanisms, mRNA-seq was used. Differentially expressed mRNAs were further determined by Gene Ontology and KEGG pathway analyses. The protein levels were analysed by Western blotting. A dual-luciferase reporter assay was used to detect the direct binding of miR-340-5p with the 3&#039;UTR of Kruppel-like factor 2 (KLF2). </P><P> Results: MiR-340-5p lentivirus infection suppressed normal skin fibroblast proliferation. The mRNAseq data revealed that 41 mRNAs were differentially expressed, including 22 upregulated and 19 downregulated transcripts in the miR-340-5p overexpression group compared with those in the control group. Gene Ontology and KEGG pathway analyses revealed that miR-340-5p overexpression correlated with the macromolecule biosynthetic process, cellular macromolecule biosynthetic process, membrane, and MAPK signalling pathway. Bioinformatics analysis and luciferase reporter assays showed that miR-340-5p binds to the 3&#039;UTR of KLF2. Forced expression of miR-340-5p decreased the expression of KLF2 in normal skin fibroblasts. Overexpression of KLF2 restored skin fibroblast proliferation in the miR-340-5p overexpression group. </P><P> Conclusion: This study demonstrates that miR-340-5p may suppress skin fibroblast proliferation, possibly through targeting KLF2. These findings could help us understand the function of miR-340-5p in skin fibroblasts. miR-340-5p could be a therapeutic target for preventing scarring.</P>

Synthesis, X-ray structures and cytotoxic effects of a Cu(II)- and a Zn(II) thiosemicarbazones on human epidermoid carcinoma cell A431

2021 ◽  
Vol 133 (2) ◽  
Author(s):  
Chinmoy Biswas ◽  
Arnab Chatterjee ◽  
Sonali Bhattacharya ◽  
Deba Prasad Mandal ◽  
Shamee Bhattacharjee ◽  
...  
Keyword(s):  
Carcinoma Cell ◽  
Epidermoid Carcinoma ◽  
Cytotoxic Effects ◽  
X Ray ◽  
Human Epidermoid Carcinoma

ROLE OF PHENERGAN IN ABNORMAL SCARS AND KELOIDS

2004 ◽  
Vol 12 (04) ◽  
pp. 471-482
Author(s):  
J. VENUGOPAL ◽  
V. JAYARAMAN ◽  
MARY BABU ◽  
S. RAMAKRISHNA
Keyword(s):  
Dna Synthesis ◽  
Hypertrophic Scar ◽  
Skin Fibroblast ◽  
Collagen Synthesis ◽  
Normal Skin ◽  
Compression Therapy ◽  
Matrix Proteins ◽  
Intralesional Corticosteroid ◽  
Normal Skin Fibroblast

Hypertrophic scar and keloids have affected patients and frustrated physicians for centuries. Hypertrophic scar (HSc) and keloids are a major problem for patients who survive extensive thermal and traumatic skin injuries. HSc and other fibroproliferative disorders are associated with excessive accumulation of collagen and extracellular matrix proteins due to an imbalance between synthesis and degradation. The therapeutic management of hypertrophic scars and keloids include occlusive dressings, compression therapy, intralesional corticosteroid injections, cryosurgery, excision, radiation therapy, laser therapy, interferon therapy and other promising lesser known therapies directed at collagen synthesis. In this study we investigated the effect of phenergan (promethazine hydrochloride) as one of the most potent histamine antagonists on cell proliferation, DNA synthesis and collagen production in fibroblast isolated from human post burn hypertrophic scar, keloids and normal skin. The proliferation of normal skin fibroblast was slightly decreased but hypertrophic scar and keloids showed significant (p<0.001) level of decrease after 72 hours of phenergan (750 μM) treatment. The results of DNA synthesis also significantly (p<0.001) decreased in hypertrophic scar and keloid fibroblasts. Phenergan (1.5 mM) decreased the collagen synthesis upto 61% and 66% in HSc and keloids in comparison to normal skin fibroblast, which showed reduction of 38% after 72 hours. Improved understanding of such regulatory mechanisms may eventually be of therapeutic significance in the control of hypertrophic scar and keloids.

Anti-Trypanosomal Activity of Diarylheptanoids Isolated from the Bark ofAlnus japonica

2014 ◽  
Vol 42 (05) ◽  
pp. 1245-1260 ◽  
Author(s):  
Nguyen Huu Tung ◽  
Mitsuko Suzuki ◽  
Takuhiro Uto ◽  
Osamu Morinaga ◽  
Kofi D. Kwofie ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Normal Skin ◽  
Leukemia Cells ◽  
Fibroblast Cells ◽  
Colon Cancer Cells ◽  
Alnus Japonica ◽  
Chemical Methods ◽  
Structure Activity ◽  
Normal Skin Fibroblast

The crude extract of Alnus japonica bark exhibited a strong effect on the growth of Trypanosoma brucei. Subsequent chromatographic separation resulted in the isolation of two novel diarylheptanoids, known as alnuside C (2) and alnuside D (3), and three known compounds, 1-(3,4-dihydroxyphenyl)-7-(4-hydroxyphenyl)-heptan-3(R)-O-β-D-glucopyranoside (1), oregonin (4) and hirsutanone (5). The structures of the isolates were elucidated based on the use of extensive spectroscopic and chemical methods. Among the isolated diarylheptanoids, oregonin (4) (a major component of plant bark) and hirsutanone (5) exhibited potent in vitro inhibitory activity against T. brucei growth in the bloodstream with IC50values of 1.14 and 1.78 μM, respectively. We confirmed that oregonin (4) and hirsutanone (5) were not toxic to human normal skin fibroblast cells (NB1RGB) and colon cancer cells (HCT-15) at a concentration of 50 μM; however, lower levels of toxicity were observed for leukemia cells. To determine the structure activity relationships of the isolated components, we performed Conformation Search and found that the 3-oxo function of the heptane chain in the diarylheptanoid molecule is required for their trypanocidal activity.

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