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Antiprotozoal Effects of Wild Plants
Published in Mahendra Rai, Shandesh Bhattarai, Chistiane M. Feitosa, Ethnopharmacology of Wild Plants, 2021
Muhammad Subbayyal Akram, Rao Zahid Abbas, José L. Martinez
Maesa balansae (Figure 7.9) is a shrub that belongs to Primulaceae family and grows naturally in the forests of the northern areas of Vietnam. Traditionally, it has been used for the treatments of headache, allergies, worm infections, sprains and skin ulcers in Vietnamese medicines. Polar extracts and bioassay-guided fractionation of M. balansae leaves help in isolation and characterization of its compounds, which divulges the presence of six oleane triterpenoid saponins mesabalides I–VI. These six triterpenoid saponins were separated by liquid chromatography and each was separately evaluated against leishmaniasis (Leonard et al. 2003). Each mesabalides has the capability to halt specifically leishmaniasis but most potent are Maesabalide III and IV with IC50 values of 7 and 14 ng/ml against intracellular amastigotes. In vivo studies show more than 90% reduction in the burden of amastigotes just after one week of subcutaneous single dose at 0.2–0.4 mg/kg. No cytotoxicity was observed in the human fibroblast (MRC-5) cell line even at CC50 > 32 μg/ml (Germonprez et al. 2005).
The Renewal of Interest in Nitroaromatic Drugs
Published in Venkatesan Jayaprakash, Daniele Castagnolo, Yusuf Özkay, Medicinal Chemistry of Neglected and Tropical Diseases, 2019
Nicolas Primas, Caroline Ducros, Patrice Vanelle, Pierre Verhaeghe
DNDI-0690 (24) has now been selected and is in preclinical development. The first in human phase I study of safety, tolerability, and pharmacokinetics after single oral ascending doses of DNDI-0690 (24) was submitted to UK authorities in February 2019 (DNDi 2019b).IC50 in jiM values for inhibition of the growth of L. donovani and L. infantum (in mouse macrophages), T. cruzi (on MRC-5 cells), and T. brucei, or for cytotoxicity toward human lung fibroblasts (MRC-5 cells).
Pomegranate: a role in health promotion and AIDS?
Published in Ronald R. Watson, NUTRIENTS and FOODS in AIDS, 2017
Jeongmin Lee, Ronald R. Watson
A mixture of a ferrous salt and an extract of pomegranate rind completely inhibited the growth of fungus, powdery mildew, in the apple leaves within 24 h.13 Through microscopic test, both spores and mycellium of powdery mildew treated with the mixture were destroyed after 1 h at room temperature. The 144 μg of the mixture was tested to identify the effect on the growth of poliovirus, herpes simplex virus type 1 (HSV-1), and human immunodeficiency virus type 1 (HIV-1).13 In the cell culture assays using HT-29 cells for poliovirus, MRC-5 cells for HSV-1 and IIUT-78 cells for HIV-1, there was complete reduction of infectivity of these viruses, which indicated that the extract of pomegranate could be used to control the spread of herpes and as protection against HIV-1. However, there was no apparent cytopathogenic effect on MRC-5 cells or HT-29 cells.
Application of the Mannich reaction in the structural modification of natural products
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Miao-Xia Pu, Hong-Yan Guo, Zhe-Shan Quan, Xiaoting Li, Qing-Kun Shen
Phenoxodiol, an isoflavone analogue, is clinically used to treat drug-resistant ovarian and prostate cancers. Chen et al.8 reported a series of Mannich base derivatives obtained through the Mannich reaction using phenoxodiol, primary amines, and formaldehyde as reactants and methanol as solvent at room temperature. All 25 compounds inhibited tumour cell proliferation in a dose-dependent manner (Table 1). Compared with the lead compound, phenoxodiol, the majority of compounds exhibited higher antiproliferative activity against the MDA MB-231 breast cancer cell line, among which compound 5 (Figure 2) exhibited the highest antiproliferative activity with an IC50 of 0.7 µM, which was 50-fold higher than that of phenoxodiol (IC50 = 35.6 µM). Compound 5 showed low toxicity to the MRC-5 cell line (IC50 = 197.0 µM), and its specificity value to the MDA-MB-231 cell line was 266. Therefore, compound 5 should be considered for further in-depth studies.
Evaluation of genotoxic potential of tert-butylquinone and its derivatives in prokaryotic and eukaryotic test models
Published in Drug and Chemical Toxicology, 2020
Jelena Đorđević, Stoimir Kolarević, Jovana Jovanović, Jovana Kostić-Vuković, Irena Novaković, Marko Jeremić, Dušan Sladić, Branka Vuković-Gačić
Having in mind that metabolic activation could contribute to the reactivity of the studied compound, two cell lines were chosen for assessment of genotoxic potential in eukaryotic model. MRC-5 was chosen as a model of a healthy cell line, while the human hepatoma cell line HepG2 was chosen as model for cancerous cell line and cell line with higher metabolic activity. Prior to comet assay, subtoxic concentration range was determined for both cell lines. MRC-5 cells were more sensitive to TBQ in comparison with HepG2 cells. Generally, for derivatives we have not observed significant difference in response among the studied cell lines which is in compliance of the study of Jeremić et al. (2016) showing that 2,6-disubstituted derivatives do not exhibit profound selectivity in action depended on the cell line (healthy versus cancerous lines). Among the studied derivatives, derivative 4C exhibited the highest activity in both cell lines which is again in compliance with previous findings of Jeremić et al. (2016) showing that 2,6-disubstituted derivatives exhibit higher cytotoxicity than the 2,5-disubstituted derivatives.
14-3-3β Is necessary in the regulation of polarization and directional migration of alveolar myofibroblasts by lipopolysaccharide
Published in Experimental Lung Research, 2020
Cell culture and transfection. Myofibroblasts culture was performed in accordance with previous methods.39 Normal embryonic lung fibroblasts(MRC-5) were purchased from Cell Bank, Chinese Academy of Sciences [GNHu41]. Cells were cultured in minimum essential medium (MEM) medium supplied with 10% fetal bovine serum(GIBCO, Gaithersburg, MD; 10099141) and antibiotics (100 U of penicillin, 100 μg of streptomycin) Cells were grown at 37 °C with 5% CO2 in air and were routinely passaged with trypsin (0.25%)/EDTA (1 mM)when they reached 80–90% confluence. For inducing myofibroblasts, cells were counted after trypsinization and passaged at 103cells/ml (5cells/mm2). Myofibroblasts were identified and distinguished from fibroblasts by expression of α-SMA. For 14-3-3β siRNA, the sequence is: 14-3-3β 5′-UUUGUCCAACAGCUCCAGCTT-3′. Control siRNA is scrambled sequence of the siRNA. Clone the annealed oligos that contain the siRNA-expressing sequence into the pSUPER. Retro. Neo + gfp vector(OligoEngine, USA). Transfection of vector was performed using Lipofectamine 2000 (Invitrogen; 11668027).