scholarly journals Antiproliferative Effects of a Series of Pyrazolines on Lung Cancer

Proceedings ◽  
2018 ◽  
Vol 2 (25) ◽  
pp. 1574
Author(s):  
Belgin Sever ◽  
Mehlika Dilek Altıntop ◽  
Elif Kaya Tilki ◽  
Miriş Dikmen ◽  
Ahmet Özdemir

Lung cancer is one of the most diagnosed cancers worldwide and the development of anticancer agents for the treatment of lung cancer is an important task for researchers. For this purpose, herein pyrazoline-based compounds 1–18 were investigated for their cytotoxic effects on A549 human lung adenocarcinoma and CCD-19Lu human lung fibroblast cell lines using MTT assay. According to the results, 1-(4-methoxyphenyl)-3-(2-furanyl)-5-(4-methylphenyl)-2-pyrazoline (7) was identified as the most promising anticancer agent due to its selective inhibitory effect on A549 cell line with an IC50 value of 138.63 µg/mL when compared with cyclophosphamide (IC50 = 309.97 µg/mL).

2018 ◽  
Vol 37 (5) ◽  
pp. 849-864 ◽  
Author(s):  
Malgorzata Kucinska ◽  
Helena Mieszczak ◽  
Hanna Piotrowska-Kempisty ◽  
Mariusz Kaczmarek ◽  
Walter Granig ◽  
...  

2021 ◽  
pp. 37-40

Purpose: The rapid growth, morbidity and mortality of lung cancer and the lack of effective treatment have attracted great interest from researchers to find new cancer treatments aimed at the effect of gossypine on cell proliferation and apoptosis of A549 cells. The most used of these products are flavonoids. Gossypin is a potential chemo preventive and therapeutic agent for lung cancer. Material and Method: We investigated the effect of Gossypin anticancer activity on A549 cell proliferation with MTT method, depending on dose and time. In addition, mRNA expression levels of the apoptotic markers caspase-3 (CAS-3) and caspase-9 (CAS-9) were investigated by real-time PCR. In our study, six groups were used as control, gossypin (10, 20, 40 μM), cisplatin 5 μg/mL and cisplatin 5 μg/mL+gossypin 40 μM combine concentrations. The proliferative and antiapoptotic effects of gossypin at 24, 48 and 72 hours were investigated. Results were analyzed and presented as cell viability (%). Results: In our results, it was determined that gossypin especially at a dose of 40 μM and at 72 hours showed almost as much effect on A549 cells, but the highest inhibitory effect was seen in the 40 combined group of cisplatin 5 μg / mL + gossypin. In addition, gossypin caused a significant increase in apoptosis genes (CASP-3, CASP-9) compared to control. Conclusion: Our study showed that gossypin significantly increases the chemosensitivity of cisplatin. Based on this, it is predicted that gossypin can be used as a supportive therapy that increases the effectiveness of anticancer agents. However, more detailed research should be done for this.


Biomolecules ◽  
2020 ◽  
Vol 10 (4) ◽  
pp. 569 ◽  
Author(s):  
Ausana Mapook ◽  
Allan Patrick G. Macabeo ◽  
Benjarong Thongbai ◽  
Kevin D. Hyde ◽  
Marc Stadler

Pseudopalawania siamensis gen. et sp. nov., from northern Thailand, is introduced based on multi-gene analyses and morphological comparison. An isolate was fermented in yeast malt culture broth and explored for its secondary metabolite production. Chromatographic purification of the crude ethyl acetate (broth) extract yielded four tetrahydroxanthones comprised of a new heterodimeric bistetrahydroxanthone, pseudopalawanone (1), two known dimeric derivatives, 4,4′-secalonic acid D (2) and penicillixanthone A (3), the corresponding monomeric tetrahydroxanthone paecilin B (4), and the known benzophenone, cephalanone F (5). Compounds 1–3 showed potent inhibitory activity against Gram-positive bacteria. Compounds 2 and 3 were inhibitory against Bacillus subtilis with minimum inhibitory concentrations (MIC) of 1.0 and 4.2 μg/mL, respectively. Only compound 2 showed activity against Mycobacterium smegmatis. In addition, the dimeric compounds 1–3 also showed moderate cytotoxic effects on HeLa and mouse fibroblast cell lines, which makes them less attractive as candidates for development of selectively acting antibiotics.


2019 ◽  
Vol 120 (10) ◽  
pp. 18066-18076 ◽  
Author(s):  
Fatih Oltulu ◽  
Duygu Ç. Kocatürk ◽  
Yasemin Adalı ◽  
Berrin Özdil ◽  
Eda Açikgöz ◽  
...  

2013 ◽  
Vol 39 (6) ◽  
pp. 644-649 ◽  
Author(s):  
Sarah Fernandes Teixeira ◽  
Isabella dos Santos Guimarães ◽  
Klesia Pirola Madeira ◽  
Renata Dalmaschio Daltoé ◽  
Ian Victor Silva ◽  
...  

OBJECTIVE: To test the effectiveness of combining conventional antineoplastic drugs (cisplatin and etoposide) with metformin in the treatment of non-small cell lung cancer in the NCI-H460 cell line, in order to develop new therapeutic options with high efficacy and low toxicity.METHODS: We used the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and calculated the combination index for the drugs studied.RESULTS: We found that the use of metformin as monotherapy reduced the metabolic viability of the cell line studied. Combining metformin with cisplatin or etoposide produced a synergistic effect and was more effective than was the use of cisplatin or etoposide as monotherapy.CONCLUSIONS: Metformin, due to its independent effects on liver kinase B1, had antiproliferative effects on the NCI-H460 cell line. When metformin was combined with cisplatin or etoposide, the cell death rate was even higher.


Planta Medica ◽  
2018 ◽  
Vol 85 (05) ◽  
pp. 394-405 ◽  
Author(s):  
Shao-Fang Xing ◽  
Lin-Hua Liu ◽  
Ma-Li Zu ◽  
Man Lin ◽  
Xin-Fang Zhai ◽  
...  

AbstractDamulin B, a dammarane-type saponin from steamed Gynostemma pentaphyllum, exhibits the strongest activity against human lung carcinoma A549 cells among the isolated active saponins. In this study, the structure-activity relationship of a series of saponin compounds was discussed. The inhibitory effect of damulin B on human lung cancer A549 and H1299 cells was investigated from apoptosis, cell cycle, and migration aspects. In vitro, human lung cancer cells were more susceptible to damulin B treatment than human normal fibroblasts. Damulin B exhibited a strong cytotoxic effect, as evidenced by the increase of apoptosis rate, reduction of mitochondrial membrane potential (MMP), generation of reactive oxygen species, and G0/G1 phase arrest. Furthermore, damulin B activated the following: both intrinsic and extrinsic apoptosis pathways along with early G1 phase arrest via the upregulation of the Bax, Bid, tBid, cleaved caspase-8, and p53 expression levels; downregulation of the procaspase-8/-9, CDK4, CDK6, and cyclin D1 expression levels; and more release of cytochrome c in the cytoplasm. In addition, antimigratory activities and suppressive effects on metastasis-related factors, such as MMP-2 and MMP-9, accompanied by the upregulation of IL-24 were revealed. Altogether, the results proved that damulin B could inhibit human lung cancer cells by inducing apoptosis, blocking the cell cycle at early G0/G1 phase and suppressing the migration. Hence, damulin B has potential therapeutic efficacy against lung cancer.


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