دورية أكاديمية

Synthesis of Rhodamine-Conjugated Lupane Type Triterpenes of Enhanced Cytotoxicity

التفاصيل البيبلوغرافية
العنوان: Synthesis of Rhodamine-Conjugated Lupane Type Triterpenes of Enhanced Cytotoxicity
المؤلفون: Toni C. Denner, Niels V. Heise, Sophie Hoenke, René Csuk
المصدر: Molecules, Vol 29, Iss 10, p 2346 (2024)
بيانات النشر: MDPI AG, 2024.
سنة النشر: 2024
المجموعة: LCC:Organic chemistry
مصطلحات موضوعية: betulinic acid, platanic acid, rhodamine hybrids, cytotoxicity, Organic chemistry, QD241-441
الوصف: Various conjugates with rhodamines were prepared by starting with betulinic acid (BA) and platanic acid (PA). The molecules homopiperazine and piperazine, which were identified in earlier research, served as linkers between the rhodamine and the triterpene. The pentacyclic triterpene’s ring A was modified with two acetyloxy groups in order to possibly boost its cytotoxic activity. The SRB assays’ cytotoxicity data showed that conjugates 13–22, derived from betulinic acid, had a significantly higher cytotoxicity. Of these hybrids, derivatives 19 (containing rhodamine B) and 22 (containing rhodamine 101) showed the best values with EC50 = 0.016 and 0.019 μM for A2780 ovarian carcinoma cells. Additionally, based on the ratio of EC50 values, these two compounds demonstrated the strongest selectivity between malignant A2780 cells and non-malignant NIH 3T3 fibroblasts. A375 melanoma cells were used in cell cycle investigations, which showed that the cells were halted in the G1/G0 phase. Annexin V/FITC/PI staining demonstrated that the tumor cells were affected by both necrosis and apoptosis.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 1420-3049
Relation: https://www.mdpi.com/1420-3049/29/10/2346; https://doaj.org/toc/1420-3049
DOI: 10.3390/molecules29102346
URL الوصول: https://doaj.org/article/decc1abf7fba45c386e305971d1771a9
رقم الأكسشن: edsdoj.1abf7fba45c386e305971d1771a9
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:14203049
DOI:10.3390/molecules29102346