Cytotoxic Effects of Some Flavonoids and Imatinib on the K562 Chronic Myeloid Leukemia Cell Line: Data Analysis Using the Combination Index Method

Kalındemirtaş, Ferdane Danışman; Birman, Hüsniye; Çandöken, Eda; Gazioğlu, Sema Bilgiş; Melikoğlu, Gülay; Kuruca, Serap Erdem

doi:10.4274/balkanmedj.galenos.2018.2017.1244

Cited by 16 publications

(11 citation statements)

References 37 publications

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“…Sinensetin inhibitory activity was observed in the presence of vincristine which is also a good substrate of P-gp. The inhibitory effect of sinensetin on P-gp was well-supported by other studies ( Mertens-Talcott et al, 2007 ; Bai et al, 2019 ; Danisman Kalindemirtas et al, 2019 ). However, there was no chemosensitizing activity of sinensetin against MRP-overexpressing cancer cells AML-2/DX100 ( Choi et al, 2002 ).…”

Section: Introductionsupporting

confidence: 79%

Sinensetin: An Insight on Its Pharmacological Activities, Mechanisms of Action and Toxicity

et al. 2021

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Sinensetin, a plant-derived polymethoxylated flavonoid found in Orthosiphon aristatus var. aristatus and several citrus fruits, has been found to possess strong anticancer activities and a variety of other pharmacological benefits and promising potency in intended activities with minimal toxicity. This review aims to compile an up-to-date reports of published scientific information on sinensetin pharmacological activities, mechanisms of action and toxicity. The present findings about the compound are critically analyzed and its prospect as a lead molecule for drug discovery is highlighted. The databases employed for data collection are mainly through Google Scholar, PubMed, Scopus and Science Direct. In-vitro and in-vivo studies showed that sinensetin possessed strong anticancer activities and a wide range of pharmacological activities such as anti-inflammatory, antioxidant, antimicrobial, anti-obesity, anti-dementia and vasorelaxant activities. The studies provided some insights on its several mechanisms of action in cancer and other disease states. However, more detail mechanistic studies are needed to understand its pharmacological effects. More in vivo studies in various animal models including toxicity, pharmacokinetic, pharmacodynamic and bioavailability studies are required to assess its efficacy and safety before submission to clinical studies. In this review, an insight on sinensetin pharmacological activities and mechanisms of action serves as a useful resource for a more thorough and comprehensive understanding of sinensetin as a potential lead candidate for drug discovery.

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Section: Introductionsupporting

confidence: 79%

Sinensetin: An Insight on Its Pharmacological Activities, Mechanisms of Action and Toxicity

et al. 2021

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“…Previous reports indicated a 5 μM concentration as calculated IC50 value for imatinib as a proven first choice chemical agent against the CML on K562 cells. Comparing the anti-proliferation potency of PDG with other natural compounds including apigenin (IC50 = 140 μM) and luteolin (IC50 = 100 μM) also supports this idea that PDG might be a potent agent in the inhibition of K562 cells proliferation ( 17 ).…”

Section: Discussionmentioning

confidence: 74%

Prodigiosin induced the caspase-dependent apoptosis in human chronic myelogenous leukemia K562 cell

et al. 2021

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Background and purpose: Chronic myeloid leukemia (CML) as a myeloproliferative disease is characterized by increased cellularity of bone marrow. Implementing the latest treatment protocols is currently accompanied by serious and life-threatening side effects. There are worldwide attempts to find new effective and potent therapeutic agents with minimal side effects on CML patients. This in vitro study was carried out to discover the potential antiproliferative and apoptotic effects of naturally produced prodigiosin (PDG) on K562 cells as an accepted model of CML. Experimental approach: The anti-proliferative effect of PDG was measured by MTT assay. To highlight the mechanism of cytotoxicity, the apoptotic cell death pathway was investigated by morphological and biochemical assessments. The dual acridine orange/ethidium bromide staining technique and western blotting method were applied to assess the mechanism of the potential apoptotic impact of PDG on K562 cells. Findings/Results: PDG-induced time- and concentration-dependent anti-proliferative effects were revealed with an estimated IC 50 value of 54.06 μM. The highest cell viability reduction (60%) was recorded in cells, which were exposed to 100 μM concentration. Further assays demonstrated that in the dual acridine orange/ethidium bromide staining method the cell population in the late apoptosis phase was increased in a concentration-dependent manner, which was confirmed with remarkable DNA fragmentation. Conclusion and implications: We found that the PDG-induced apoptosis in K562 cells is mediated through the caspase-3 activation both in mRNA and protein levels. Our results suggest that PDG could be a potent compound for further pharmacokinetic and pharmacodynamics studies in the in vivo model of CML.

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“…5b) and Prosopis cineraria) (figure 5c) showed better cytotoxicity in both AML and CML cell lines (HL-60 and K562) [287]. Danışman et.al, 2019 reported combination of flavonoids (apigenin, luteolin, 5-desmethyl sinensetin) and imatinib mesylate were able to enhance the cytotoxic effect on K562 cells in CML [288]. Fucoidan (complex polysaccharide from brown seaweeds) inhibited proliferation of the SKM-1 AML cell line via the activation of apoptotic pathways and production of ROS [289] and also induced apoptosis in U937 Cells through activation of p38 MAPK and modulation of Bcl-2 Family [290].…”

Section: Podophyllotoxinsmentioning

confidence: 95%

Complementary and Alternative Treatments for Cancer Prevention and Cure [Part 1]

Mohiuddin¹

2019

JCRCT

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Many lay people along with some so called “key opinion leaders” have a common slogan “There's no answer for cancer”. Again, mistake delays proper treatment and make situation worse, more often. Compliance is crucial to obtain optimal health outcomes, such as cure or improvement in QoL. Patients may delay treatment or fail to seek care because of high out-of- pocket expenditures. Despite phenomenal development, conventional therapy falls short in cancer management. There are two major hurdles in anticancer drug development: dose-limiting toxic side effects that reduce either drug effectiveness or the QoL of patients and complicated drug development processes that are costly and time consuming. Cancer patients are increasingly seeking out alternative medicine and might be reluctant to disclose its use to their oncology treatment physicians. But there is limited available information on patterns of utilization and efficacy of alternative medicine for patients with cancer. As adjuvant therapy, many traditional medicines shown efficacy against brain, head and neck, skin, breast, liver, pancreas, kidney, bladder, prostate, colon and blood cancers. The literature reviews non-pharmacological interventions used against cancer, published trials, systematic reviews and meta-analyses.

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Cytotoxic Effects of Some Flavonoids and Imatinib on the K562 Chronic Myeloid Leukemia Cell Line: Data Analysis Using the Combination Index Method

Cited by 16 publications

References 37 publications

Sinensetin: An Insight on Its Pharmacological Activities, Mechanisms of Action and Toxicity

Sinensetin: An Insight on Its Pharmacological Activities, Mechanisms of Action and Toxicity

Prodigiosin induced the caspase-dependent apoptosis in human chronic myelogenous leukemia K562 cell

Complementary and Alternative Treatments for Cancer Prevention and Cure [Part 1]

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