Discovery of new fluorescent thiazole–pyrazoline derivatives as autophagy inducers by inhibiting mTOR activity in A549 human lung cancer cells

Lin, Zhao‐Min; Wang, ZhaoYang; Zhou, Xinming; Zhang, Ming; Gao, Dongfang; Zhang, Lu; Wang, Peng; Yuan, Chen; Lin, Yuxing; Zhao, Bao‐Xiang; Jiang, Miao; Kong, Feng

doi:10.1038/s41419-020-02746-w

Cited by 20 publications

(7 citation statements)

References 55 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Though, extreme autophagy may result in the cell necrosis in many cancer cells, preserving the regular cellular mechanisms via stimulating autophagy ( Lorente et al, 2018 ). Nonetheless, autophagy has the pro-survival impact, hence exploring the hopeful options to provoke the autophagy was believed to be hopeful target to inhibit the tumor development ( Lin et al, 2020 ). The present research has focused to discover the anticancer role of geraniin against the NPC C666-1 cells via up-regulating autophagic biomarker expressions.…”

Section: Discussionmentioning

confidence: 99%

Geraniin inhibits cell growth and promoted autophagy-mediated cell death in the nasopharyngeal cancer C666-1 cells

Chen

Gong

Liu

et al. 2022

Saudi Journal of Biological Sciences

View full text Add to dashboard Cite

Background Nasopharyngeal carcinoma (NPC) is a rare malignant tumor developing from epithelial linings of nasopharynx, and 10–50 out of 100,000 NPC cases were recorded globally particularly in the Asian countries. Methodology The cytotoxicity of geraniin against the NPC C666-1 cells were analyzed using MTT assay. The influences of geraniin on the C666-1 cell viability with the presence of ROS and apoptosis inhibitors were also studied. The expressions of PI3K, Akt, mTOR, and autophagic markers LC3, ATG7, P62/SQSTM1 expressions in the C666-1 cells were studied by western blotting analysis. The ROS production was assayed using DCFH-DA staining. The immunofluorescence assay was performed to detect the NF-κB and β-catenin expressions in the C666-1 cells. Results The cell viability of C666-1 cells were appreciably prevented by the geraniin. The geraniin treatment also inhibited the C666-1 cell growth with the presence of apoptotic inhibitor Z-VAD-FMK. The geraniin-treatment effectively improved the ROS production and inhibited the NF-κB and β-catenin expressions in the C666-1 cells. Geraniin appreciably modulated the PI3K/Akt/mTOR signaling axis and improved the autophagy-mediated cell death via improving the autophagic markers LC3 and ATG7 expressions in the C666-1 cells. Conclusion In conclusion, our results proved that geraniin inhibits C666-1 cell growth and initiated autophagy-mediated cell death via modulating PI3K/Akt/mTOR cascade and improving LC3 and ATG7 expressions in the C666-1. Geraniin and it could be a hopeful and efficient candidate to treat the human NPC in the future.

show abstract

Section: Discussionmentioning

confidence: 99%

Geraniin inhibits cell growth and promoted autophagy-mediated cell death in the nasopharyngeal cancer C666-1 cells

Chen

Gong

Liu

et al. 2022

Saudi Journal of Biological Sciences

View full text Add to dashboard Cite

show abstract

“…The title compounds were synthesized by Claisen-Schmidt condensation in accordance with the procedure reported [25,42] in the literature. All of these intermediate compounds (3a-j) were recorded in the literature [43][44][45][46][47][48][49]. Briefly, a mixture of suitable acetophenone (1 mmol) and benzo[d] [1,3]dioxole-5-carbaldehyde (1 mmol) was dissolved in ethanol (5 mL).…”

Section: Synthesis Of Chalcone Compounds 3a-j 3-(benzo[d][13]dioxol-5-yl)-1-arylprop-2-en-1-one (Figure 2)mentioning

confidence: 99%

Synthesis and biological evaluation of new pyrazolebenzene-sulphonamides as potential anticancer agents and hCA I and II inhibitors

Tuğrak¹,

Gül²,

Sakagami³

et al. 2021

Turk J Chem

View full text Add to dashboard Cite

IntroductionCancer is a disease characterized by the continuous growth of cells without obeying the rules that normal healthy cells do. It is second amongst the reasons for death after cardiovascular diseases [1][2][3][4]. Based on the World Healthy Organization (WHO) report in 2018, 18.1 million people around the world had cancer, and 9.6 million died from the disease. It will reach 29.4 million in 2040. Although several therapeutic approaches are available, such as chemotherapy, which includes drug therapy and has great importance, development of new chemotherapeutics is needed since the available drugs in the market have numerous side effects, resistance development to itself, or selectivity problems [1,3,5].Oral cancer is ranked as the sixth most common malignancy worldwide [6][7][8]. The main carcinogens for oral squamous cell carcinoma (OSCC) are cigarette and alcohol products [9,10]. Understanding the molecular mechanisms of tumorigenesis and metastasis process for OSCC can lead researchers to discover new chemotherapeutic strategies and improve the treatment of oral cancer.Although there are several types of anticancer therapeutic products, novel aryl sulphonamides have recently been reported to have anticancer properties and can be used to treat different types of cancers. Among them, pazopanib, a tyrosine kinase inhibitor for renal cell carcinoma and soft tissue sarcoma, belinostat, a histone deacetylase inhibitor for peripheral T-cell lymphoma, and dabrafenib, a BRAF inhibitor for metastatic melanoma, have been approved for in the clinic treatment of patients [11] (Figure 1).As another well-known pharmacophore in drugs or bioactive compounds are pyrazoline and its analogs. Their numerous bioactivities have been reported including their anticancer/cytotoxic activities [12][13][14].

show abstract

“…Images were captured using Cool Snap CCD camera and the pictures were analyzed using ImageJ 1.44p, NIH, USA. [23] Reverse transcription-PCR Human Neuroblastoma cell line cells from 25 cm 2 culture flask were homogenized in TRI Reagent (Sigma). Total RNA was extracted and reverse transcriptized according to the manufacturer's instruction.…”

Section: Immunocytochemistrymentioning

confidence: 99%

Untitled

Sarvananda¹

2021

IJPSCR

View full text Add to dashboard Cite

Neurodegenerative movement disorder of the central nervous system (CNS) (Parkinson's disease [PD]) is characterized by necrosis of dopaminergic neurons in the substantia nigra pars compacta region of the midbrain. The etiology of PD is still unknown and is believed to be multifactorial, oxidative stress and mitochondrial dysfunction are widely considered major consequences, which provide important clues to the disease mechanisms. Studies have showed the role of free radicals and oxidative stress that contributes to the cascade of events leading to dopamine cell degeneration in PD. In general, in-built protective mechanisms consisting of enzymatic and non-enzymatic antioxidants in the CNS play decisive roles in preventing neuronal cell loss due to free radicals. However, the ability to produce these antioxidants decreases with aging. Therefore, antioxidant therapy alone or in combination with current treatment methods may represent an attractive strategy for treating or preventing the neurodegeneration seen in PD. Here, we summarize the recent discoveries of potential antioxidant compounds for modulating free-radical mediated oxidative stress leading to neurotoxicity in PD.

show abstract

Discovery of new fluorescent thiazole–pyrazoline derivatives as autophagy inducers by inhibiting mTOR activity in A549 human lung cancer cells

Cited by 20 publications

References 55 publications

Geraniin inhibits cell growth and promoted autophagy-mediated cell death in the nasopharyngeal cancer C666-1 cells

Geraniin inhibits cell growth and promoted autophagy-mediated cell death in the nasopharyngeal cancer C666-1 cells

Synthesis and biological evaluation of new pyrazolebenzene-sulphonamides as potential anticancer agents and hCA I and II inhibitors

Untitled

Contact Info

Product

Resources

About