scholarly journals Improving Dissolution and Cytotoxicity by Forming Multidrug Crystals

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1343
Author(s):  
Xufei Bian ◽  
Lan Jiang ◽  
Jing Zhou ◽  
Xiaoshu Guan ◽  
Jingyu Wang ◽  
...  

Both rosiglitazone and metformin have effects on blood glucose regulation and the proliferation of liver cancer cells. Combination therapy with these two drugs is common and effective for the treatment of diabetes in the clinic, however, the application of these two drugs is influenced by the poor dissolution of rosiglitazone and the gastrointestinal side-effect of metformin resulting from a high solubility. The formation of a multidrug crystal form (Rsg-Met) by a solvent evaporation method can solve the solubility issue. Crystal structure data and intramolecular hydrogen bonds were detected by X-ray diffraction and infrared spectroscopy. Surprisingly, Rsg-Met shortens the time spent in solubility equilibrium and multiplies the dissolution rate of Rsg. Finally, we found that a low concentration of Rsg-Met enhanced the proliferation inhibition effect on liver cancer cells (HepG2, SK-hep1) compared with rosiglitazone, without affecting the human normal cell line LO2.

2021 ◽  
Vol 2021 ◽  
pp. 1-6
Author(s):  
Zhenshan Guo ◽  
Jun Zhen ◽  
Zhoujia Yao ◽  
Yemeng Wang ◽  
Chenlu Jin

Employing the flexible hexacarboxylate ligand of 1,3,5-triazine-2,4,6-triamine hexaacetic acid (H6TTHA) to assemble with Co(NO3)2·6H2O, we have acquired a novel coordination compound, i.e., [Co2(H2TTHA)(H2O)]n·6n(H2O) (1). The analysis of single X-ray diffraction indicated that the H2TTHA2- ligand μ5-bridges connected the Co(II) ions into a two-dimensional layered architecture. Moreover, the magnetic property of 1 was also investigated between 2 and 300 K under 1000 Oe applied magnetic field. The novel compound’s inhibitory activity against the viability of cancer cell was determined through CCK-8 assay, and the expression of miRNA31 in liver cancer cells was detected via the real-time RT-PCR.


2012 ◽  
Vol 50 (01) ◽  
Author(s):  
A Henrici ◽  
R Montalbano ◽  
K Quint ◽  
M Ocker ◽  
P Di Fazio

Author(s):  
Lili Yao ◽  
Zhen-hua Sui ◽  
Yan-Kun Liu ◽  
Hong Xie ◽  
Hui-jie Gao ◽  
...  

2020 ◽  
Vol 16 (4) ◽  
pp. 337-343
Author(s):  
Shaimaa E. Abdel-Ghany ◽  
Eman El-Sayed ◽  
Nour Ashraf ◽  
Nada Mokhtar ◽  
Amany Alqosaibi ◽  
...  

Background: Hepatocellular carcinoma is the second leading cause of cancer-related deaths among other types of cancer due to lack of effective treatments and late diagnosis. Nanocarriers represent a novel method to deliver chemotherapeutic drugs, enhancing their bioavailability and stability. Methods: In the present study, we loaded gold nanoparticles (AuNPs) and titanium oxide nanoparticles (TiO2NPs) with ERL to investigate the efficiency of the formed composite in inducing apoptosis in HepG2 liver cancer cells. Cytotoxicity was assessed using MTT assay and cell phase distribution was assessed by flow cytometry along with apoptosis detection. Results: Data obtained indicated the efficiency of the formed composite to significantly induce cell death and arrest cell cycle and G2/M phase. IRF4 was downregulated after treatment with loaded ERL. Conclusion: Our data showed that loading ERL on TiO2NPs was more efficient than AuNPs. However, both nanocarriers were efficient compared with control.


2021 ◽  
Author(s):  
Novi Angeline ◽  
Sung-Sik Choo ◽  
Cheol-Hwi Kim ◽  
Suk Ho Bhang ◽  
Tae-Hyung Kim

2021 ◽  
Vol 165 ◽  
pp. 54
Author(s):  
Patricia de la Cruz-Ojeda ◽  
M. Ángeles Rodríguez-Hernández ◽  
Elena Navarro-Villarán ◽  
Paloma Gallego ◽  
Pavla Staňková ◽  
...  

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Wen Li ◽  
Jing Zhou ◽  
Yajie Zhang ◽  
Jing Zhang ◽  
Xue Li ◽  
...  

Abstract Background Echinacoside (ECH) is the main active ingredient of Cistanches Herba, which is known to have therapeutic effects on metastatic tumors. However, the effects of ECH on liver cancer are still unclear. This study was to investigate the effects of ECH on the aggression of liver cancer cells. Methods Two types of liver cancer cells Huh7 and HepG2 were treated with different doses of ECH at different times and gradients. MTT and colony formation assays were used to determine the effects of ECH on the viability of Huh7 and HepG2 cells. Transwell assays and flow cytometry assays were used to detect the effects of ECH treatment on the invasion, migration, apoptosis and cell cycle of Huh7 and HepG2 cells. Western blot analysis was used to detect the effects of ECH on the expression levels of TGF-β1, smad3, smad7, apoptosis-related proteins (Caspase-3, Caspase-8), and Cyto C in liver cancer cells. The relationship between miR-503-3p and TGF-β1 was detected using bioinformatics analysis and Luciferase reporter assay. Results The results showed that ECH inhibited the proliferation, invasion and migration of Huh7 and HepG2 cells in a dose- and time-dependent manner. Moreover, we found that ECH caused Huh7 and HepG2 cell apoptosis by blocking cells in S phase. Furthermore, the expression of miR-503-3p was found to be reduced in liver tumor tissues, but ECH treatment increased the expression of miR-503-3p in Huh7 and HepG2 cells. In addition, we found that TGF-β1 was identified as a potential target of miR-503-3p. ECH promoted the activation of the TGF-β1/Smad signaling pathway and increased the expression levels of Bax/Bcl-2. Moreover, ECH could trigger the release of mitochondrial Cyto C, and cause the reaction Caspases grade. Conclusions This study demonstrates that ECH exerts anti-tumor activity via the miR-503-3p/TGF-β1/Smad aixs in liver cancer, and provides a safe and effective anti-tumor agent for liver cancer.


2021 ◽  
Vol 9 (4) ◽  
pp. 1833-1841
Author(s):  
Lian‐Hui Wei ◽  
Yan Dong ◽  
Yu‐Feng Sun ◽  
Xue‐Song Mei ◽  
Xue‐Song Ma ◽  
...  

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