Dergiler / Journal of the Turkish Chemical Society Section A: Chemistry / 2021 / Cilt: 8 - Sayı: 1

Cytotoxic effects of Mannich bases via induction of caspase-3 pathway on human oral squamous cell carcinoma

Sayfa
187–194
Yayın Tarihi
2021-02-28
DOI
—
🏛️Bu makalenin bibliyografik verileri ve tam metin bağlantısı DergiPark üzerinden sağlanmıştır.
DergiPark Kaydı ↗
✨

Yapay Zeka Hızlı Bakış & Çıkarımlar

AI Insight
⚡ TL;DR(1 Cümlede Hızlı Çıkarım)

These results may suggest that the apoptosis pathway may be one of the possible mechanisms of the actions and lead compound 7 can be subjected to further bioassays.

📌 3 Maddede Bu Makale

🎯
Amaç & Hipotez:In anticancer drug research, there is a need for the synthesis of compounds with selective cytotoxicity compared to the drugs in the market.
📊
Temel Bulgular & Veri:The current study aimed to determine the cytotoxicities of the bis Mannich bases 1-9 towards human oral squamous cell carcinoma (OSCC).
💡
Sonuç & Katkı:These results may suggest that the apoptosis pathway may be one of the possible mechanisms of the actions and lead compound 7 can be subjected to further bioassays.
🔬Tür:Araştırma Makalesi
📍Kapsam:Genişletilmiş Akademik Örneklem
⚙️Değişkenler:Mannich · anticancer · apoptosis

Abstract

In anticancer drug research, there is a need for the synthesis of compounds with selective cytotoxicity compared to the drugs in the market. The current study aimed to determine the cytotoxicities of the bis Mannich bases 1-9 towards human oral squamous cell carcinoma (OSCC). Mannich bases showed cytotoxicity in low micromolar in the range of 1.7-27 µM against OSCC cell lines. The compounds 5 with the highest potency selectivity expression (PSE) value (318.1) and 7 with the highest tumor selectivity (TS) values (TS1:11.2, TS2:15.8) showed promising selective cytotoxicity towards cancer cell lines. According to Western blot analysis, representative compound 7 induced the activation of caspase-3 in HSC-2 cells. These results may suggest that the apoptosis pathway may be one of the possible mechanisms of the actions and lead compound 7 can be subjected to further bioassays.

🔖

Bu Makaleye Atıf Yap

YAMALI, C., GÜL, H. İ. (2021). Cytotoxic effects of Mannich bases via induction of caspase-3 pathway on human oral squamous cell carcinoma. Journal of the Turkish Chemical Society Section A: Chemistry, Cilt: 8 - Sayı: 1, 187–194. https://ajindex.com/articles/781164

📄 Tam Metin PDF Okuyucu

📄

PDF görüntüleyici hazırlanıyor...

Kaynakça (11)

  1. Siegel RL, Miller KD, Jemal A. Cancer statistics, 2019. CA: A Cancer Journal for Clinicians. 2019
  2. 69(1):7-34. Doi:10.3322/caac.21551 2. American Cancer Society. Cancer facts and figures 2020. 2020:1-76 3. Tewari D, Rawat P, Singh PK. Adverse drug reactions of anticancer drugs derived from natural sources. Food and Chemical Toxicology. 2019
  3. Doi:10.1016/j.fct.2018.11.041 4. Roman G. Mannich bases in medicinal chemistry and drug design. European Journal of Medicinal Chemistry. 2015
  4. Doi: 10.1016/j.ejmech.2014.10.076 5. Dimmock JR, Chamankhah M, Seniuk A, Allen TM, Kao GY, Halleran S. Synthesis and cytotoxic evaluation of some Mannich bases of alicyclic ketones. Pharmazie. 1995
  5. 50(10):668-71. 6. Dimmock JR, Kandepu NM, Hetherington M, Quail JW, Pugazhenthi U, Sudom AM, et al. Cytotoxic activities of Mannich bases of chalcones and related compounds. Journal of Medicinal Chemistry. 1998
  6. 41(7):1014-26. Doi: 10.1021/jm970432t 7. Gul M, Gul HI, Das U, Hanninen O. Biological evaluation and structure-activity relationships of bis-(3-aryl-3-oxo-propyl)methylamine hydrochlorides and 4-aryl-3-arylcarbonyl-1-methyl-4-piperidinol hydrochlorides as potential cytotoxic agents and their alkylating ability towards cellular glutathione in human leukemic T cells. Arzneimittelforsch. 2005
  7. 55(6):332-7. Doi: 10.1055/s-0031-1296868. 8. Gul M, Gul HI, Hanninen O. Effects of Mannich bases on cellular glutathione and related enzymes of Jurkat cells in culture conditions. Toxicology in Vitro. 2002
  8. 16(2):107-12. Doi: 10.1016/S0887-2333(01)00115-1 9. Gul M, Gul HI, Vepsalainen J, Erciyas E, Hanninen O. Effect of acetophenone derived Mannich bases on cellular glutathione level in jurkat cells - A possible mechanism of action. Arzneimittel-Forsch. 2001
  9. 51(8):679-82. Doi: 10.1055/s-0031-1300100 10. Yerdelen KO, Gul HI, Sakagami H, Umemura N. Synthesis and biological evaluation of 1,5-bis(4-hydroxy-3-methoxyphenyl)penta-1,4-dien-3-one and its aminomethyl derivatives. Journal of Enzyme Inhibition and Medicinal Chemistry. 2015
  10. 30(3):383-8. Doi: 10.3109/14756366.2014.940934 11. Yamali C, Gul HI, Sakagami H, Supuran CT. Synthesis and bioactivities of halogen bearing phenolic chalcones and their corresponding bis Mannich bases. Journal of Enzyme Inhibition and Medicinal Chemistry. 2016
  11. 31(sup4):125-31. Doi: 10.1080/14756366.2016.1221825. 12. Tugrak M, Yamali C, Sakagami H, Gul HI. Synthesis of mono Mannich bases of 2-(4-hydroxybenzylidene)-2,3-dihydroinden-1-one and eval