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Recent Advancements of Curcumin Analogs and Curcumin Formulations in Context to Modern Pharmacotherapeutics Perspectives
Published in Debarshi Kar Mahapatra, Cristóbal Noé Aguilar, A. K. Haghi, Applied Pharmaceutical Practice and Nutraceuticals, 2021
Animeshchandra G. M. Haldar, Kanhaiya M. Dadure, Debarshi Kar Mahapatra
Five series of sulfonamides conjugated curcuminoids have been designed and prepared by Jaggi Lal et al.74. The prepared entities have been evaluated for in vitro antibacterial activity against Gram-(+) and Gram-(−) bacterial species viz. Bacillus cereus, S. typhi, S. aureus, Escherichia coli, and Pseudomonas aeruginosa. Antifungal activities of new entities have been marked against few pathogenic fungal species, viz., Trichoderma viride, Aspergillus flavus, Curvularia, and Aspergillus niger lunata. The cytotoxicity has been marked against human cell lines HeLa, Hep G2, QG-56, and HCT-116 by measuring IC50. Some compounds displayed higher cytotoxicity than curcumin. The sulfonamides conjugated curcuminoids were also evaluated for anti-inflammatory activity in vivo.
Regulation of α1-Acid glycoprotein genes and Relationship to Other Type 1 Acute Phase Plasma Proteins
Published in Andrzej Mackiewicz, Irving Kushner, Heinz Baumann, Acute Phase Proteins, 2020
Heinz Baumann, Karen R. Prowse, Kwang-Ai Won, Sanja Marinkovic-Pajovic
In order to gain an experimental system for studying potential posttranscriptional regulation of AGP mRNA the entire structural rat AGP gene has been placed under control of the highly active and hormone-independent immediate early promoter of human cytomegalovirus. This gene construct was transiently introduced into Hep G2 cells.45 Treatment of these cells with IL-1, IL-6, and dexamethasone caused a three- to fivefold increase of the transcription rate of the endogenous human AGP gene and a 20- to 30-fold increase of human AGP mRNA. However, the steady-state concentration of the mature rat AGP mRNA, derived from the transgene construct, was unaffected by the same treatments. Although this experimental system has not provided supportive evidence for posttranscriptional AGP regulation, alternative approaches have to be pursued (e.g., use of different AGP gene constructs and cell targets, and analysis of nuclear precursor DNAs) in order to document the presence and define the mode of the proposed regulatory system.
Antiproliferative Potential of Medicinal Plants—an Evaluation by in Vivo, in Vitro, and in Silico Approaches
Published in V. R. Mohan, A. Doss, P. S. Tresina, Ethnomedicinal Plants with Therapeutic Properties, 2019
Hepatoblastoma is an embryonal malignancy of hepatocellular origin and the common primary liver tumor of childhood. The HepG2 cell line was originally established in 1979 by Barbara Knowles and colleagues and was wrongly reported as hepatocellular carcinoma (Aden et al., 1979). A primary culture of HepG2 cells was grown to confluency in a 60-mm petri plate or 25 cm2 flask containing 5 mL DMEM (Dulbecco’s modified Eagle’s medium). In liver cancer, HepG2 cells represent a mainstay of liver cancer biology. Therefore, they are frequently employed in experimental manipulations, including drug treatment, mechanistic studies, and various high-throughput applications (Qiu et al., 2015). There are also various other cell lines like capan-1, SNU-182, SNU-423, SNU-449, LMH/2A, SNU-398, Hep 3B, MH1C1, etc. The cytotoxic role of the active ethyl acetate fraction of A. marmelos was evident in HepG2 cells. The oxidative stress was significantly inhibited and enhanced apoptosis by regulating up the p53 and caspase 3 expressions and simultaneously regulating down NF-κB. Thus, the extract increased nuclear condensation and DNA fragmentation and the ability of the active fraction from A. marmelos was potent to induce apoptosis by a multiprolonged cascade of events suggesting that it might be an ideal therapeutic for solid tumors of liver.
Assessments of in vitro and in vivo antineoplastic potentials of β-sitosterol-loaded PEGylated niosomes against hepatocellular carcinoma
Published in Journal of Liposome Research, 2020
Raquibun Nisha, Pranesh Kumar, Anurag Kumar Gautam, Hriday Bera, Bolay Bhattacharya, Poonam Parashar, Shubhini A. Saraf, Sudipta Saha
The procedure adopted for cytotoxicity assay using Hep-G2 cells (a human liver cancer cell line) has been described previously (Keshari et al.2017a). The cells were grown in Roswell Park Memorial Institute media (RPMI 1640) in standard condition (Parashar et al.2019). Later, 5 × 103 cells/well were treated with various concentrations (10, 20, 40, and 80 µg/mL) and incubated for 48 h. Following addition of SRB solution the absorbance was taken at a wavelength of 540 nm (690 nm reference wavelength over plate reader). GI50 was calculated using equation [(Ti-Tz)/(C-Tz)] × 100 = 50. GI50 is the drug concentration that results in a 50% reduction in the net protein increase (as measured by SRB staining) in control cells during the drug incubation.
Towards a clinical application of freeze-dried squalene-based nanomedicines
Published in Journal of Drug Targeting, 2019
Marie Rouquette, Karine Ser-Le Roux, Mélanie Polrot, Claudie Bourgaux, Jean-Philippe Michel, Fabienne Testard, Frédéric Gobeaux, Sinda Lepetre-Mouelhi
Moreover, liver safety had to be considered as SQAd NPs accumulate in the liver after intravenous injection [8]. Preliminary in vitro experiments were therefore performed on cultured hepatocytes. HepG2 cells were selected because they represent a well-accepted model of human hepatocytes and are easy to handle under in vitro conditions. In addition, the HepG2 cells have been used as a liver-specific cell line to predict hepatotoxicity of drugs in general [32] and nanoparticles in particular [33–35]. Lyophilised SQAd NPs did not exhibit any toxicity in vitro after 72 h of treatment on HepG2 cell line. While intravenous injection of freshly prepared SQAd NPs induced some mortality on liver injured mice, freeze-dried SQAd NPs were shown to be perfectly safe on the same animal model. Higher residual ethanol contents in freshly prepared NPs may explain this difference. This result further strengthens the progress towards SQAd NPs clinical application.
Inhibition of the lethality of Shiga-like toxin-1 by functional gold nanoparticles
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2018
Chun-Hsien Li, Yi-Ling Bai, Yu-Chie Chen
The uptake of POA-Au NPs by Hep G2 cells was also examined by using optical microscopy. Figure 6(A–F) show the optical images of Hep G2 cells under dark field that were obtained after being incubated with POA-Au NPs at the concentations of 0, 62.5, 125, 250, 500, and 1000 µgmL−1, respectively, for 6 h. The intensity of the scattering light derived from POA-Au NPs in the cells was apparently increased as the concentration of POA-Au NPs was increased. However, the location of the cell nuclei was hard to be observed because Hep G2 cells were aggregated to a large extent. Thus, blue fluorescent Hoechst 33342 was used to stain the cells and the cell nuclei were located. Figure 7(A–F) show the overlapped images of Hep G2 cells that were obtained by being incubated with POA-Au NPs with the concentrations of 0, 62.5, 125, 250, 500, and 1000 µgmL−1, respectively, for 6 h. The overlapped images were obtained by using optical microscopy under dark field and fluorescence microscopy. The blue colorindicated the cell nuclei and orange color indicated the distribution of POA-Au NPs. The blue color was too bright and suppressed the observation of the location of POA-Au NPs. Nevertheless, a red emission was derived from POA-Au NPs that surrounded the blue nuclei, as shown in Figure 7(D).