scholarly journals A New Sterol From Sporoderm-Broken Ganoderma sinense Spores and Its Anticancer Activity

2019 ◽  
Vol 14 (12) ◽  
pp. 1934578X1989512
Author(s):  
Danhong Lian ◽  
Xin Zhong ◽  
Yimei Zheng ◽  
Sha Zhou ◽  
Li Gu ◽  
...  

A new sterol, ganodermaside E (1), and 4 known sterols, (22 E,24 R)-3β,5α-dihydroxyergosta-7,22-dien-6-one (2), (22 E,24 R)-3β,5α,9α-trihydroxyergosta-7,22-diene-6-one (3), (22 E,24 R)-ergosta-7,9(11),22-triene-3β,5α,6β-triol (4), and (22 E,24 R)-ergosta-7,22-diene-3β,5α,6α-triol (5), were isolated for the first time from the sporoderm-broken spores of Ganoderm sinense Zhao, Xu et Zhang. Their structures were determined by spectroscopic techniques such as nuclear magnetic resonance spectroscopy and mass spectrometry. Furthermore, all the compounds were evaluated for their in vitro cytotoxicity and migration inhibition on human non-small-lung cancer A549 cells. Compound 1 exhibited cytotoxicity with a half-maximal inhibitory concentration value of 21.12 ± 1.46 µM. Compound 5 exhibited the strongest and most significant antimetastatic activity at concentrations of 100 and 200 µM.

2018 ◽  
Vol 21 (4) ◽  
pp. 262-270 ◽  
Author(s):  
Zehao Huang ◽  
Na Li ◽  
Kaifeng Rao ◽  
Cuiting Liu ◽  
Zijian Wang ◽  
...  

Background: More than 2,000 chemicals have been used in the tannery industry. Although some tannery chemicals have been reported to have harmful effects on both human health and the environment, only a few have been subjected to genotoxicity and cytotoxicity evaluations. Objective: This study focused on cytotoxicity and genotoxicity of ten tannery chemicals widely used in China. Materials and Methods: DNA-damaging effects were measured using the SOS/umu test with Salmonella typhimurium TA1535/pSK1002. Chromosome-damaging and cytotoxic effects were determined with the high-content in vitro Micronucleus test (MN test) using the human-derived cell lines MGC-803 and A549. Conclusion: The cytotoxicity of the ten tannery chemicals differed somewhat between the two cell assays, with A549 cells being more sensitive than MGC-803 cells. None of the chemicals induced DNA damage before metabolism, but one was found to have DNA-damaging effects on metabolism. Four of the chemicals, DY64, SB1, DB71 and RR120, were found to have chromosome-damaging effects. A Quantitative Structure-Activity Relationship (QSAR) analysis indicated that one structural feature favouring chemical genotoxicity, Hacceptor-path3-Hacceptor, may contribute to the chromosome-damaging effects of the four MN-test-positive chemicals.


Materials ◽  
2021 ◽  
Vol 14 (4) ◽  
pp. 825
Author(s):  
Saman Sargazi ◽  
Mohammad Reza Hajinezhad ◽  
Abbas Rahdar ◽  
Muhammad Nadeem Zafar ◽  
Aneesa Awan ◽  
...  

In this research, tin ferrite (SnFe2O4) NPs were synthesized via hydrothermal route using ferric chloride and tin chloride as precursors and were then characterized in terms of morphology and structure using Fourier-transform infrared spectroscopy (FTIR), Ultraviolet–visible spectroscopy (UV-Vis), X-ray power diffraction (XRD), Scanning electron microscopy (SEM), Transmission electron microscopy (TEM), and Brunauer–Emmett–Teller (BET) method. The obtained UV-Vis spectra was used to measure band gap energy of as-prepared SnFe2O4 NPs. XRD confirmed the spinel structure of NPs, while SEM and TEM analyses disclosed the size of NPs in the range of 15–50 nm and revealed the spherical shape of NPs. Moreover, energy dispersive X-ray spectroscopy (EDS) and BET analysis was carried out to estimate elemental composition and specific surface area, respectively. In vitro cytotoxicity of the synthesized NPs were studied on normal (HUVEC, HEK293) and cancerous (A549) human cell lines. HUVEC cells were resistant to SnFe2O4 NPs; while a significant decrease in the viability of HEK293 cells was observed when treated with higher concentrations of SnFe2O4 NPs. Furthermore, SnFe2O4 NPs induced dramatic cytotoxicity against A549 cells. For in vivo study, rats received SnFe2O4 NPs at dosages of 0, 0.1, 1, and 10 mg/kg. The 10 mg/kg dose increased serum blood urea nitrogen and creatinine compared to the controls (P < 0.05). The pathology showed necrosis in the liver, heart, and lungs, and the greatest damages were related to the kidneys. Overall, the in vivo and in vitro experiments showed that SnFe2O4 NPs at high doses had toxic effects on lung, liver and kidney cells without inducing toxicity to HUVECs. Further studies are warranted to fully elucidate the side effects of SnFe2O4 NPs for their application in theranostics.


RSC Advances ◽  
2016 ◽  
Vol 6 (53) ◽  
pp. 47520-47529 ◽  
Author(s):  
Mohammad H. Sakr ◽  
Najeeb M. Halabi ◽  
Leen N. Kalash ◽  
Sara I. Al-Ghadban ◽  
Mayyasa K. Rammah ◽  
...  

We demonstrate the effective cytotoxic properties of a dye-sensitized metal oxide in an in vitro model of a human lung cancer cell line (A549 cells) upon light irradiation, where a type I mechanism photo-dynamic therapy is realized exclusively.


2021 ◽  
pp. 002203452110453
Author(s):  
G. Yuan ◽  
C. Fu ◽  
S.T. Yang ◽  
D.Y. Yuh ◽  
G. Hajishengallis ◽  
...  

Periodontitis is a complex inflammatory disease affecting the supporting structures of teeth and is associated with systemic inflammatory disorders. Regulator of G-protein signaling 12 (RGS12), the largest protein in the RGS protein family, plays a crucial role in the development of inflammation and bone remodeling. However, the role and mechanism(s) by which RGS12 may regulate periodontitis have not been elucidated. Here, we showed that ablation of RGS12 in Mx1+ hematopoietic cells blocked bone loss in the ligature-induced periodontitis model, as evidenced morphometrically and by micro–computed tomography analysis of the alveolar bone. Moreover, hematopoietic cell-specific deletion of RGS12 inhibited osteoclast formation and activity as well as the production of inflammatory cytokines such as IL1β, IL6, and TNFα in the diseased periodontal tissue. In the in vitro experiments, we found that the overexpression of RGS12 promoted the reprogramming of macrophages to the proinflammatory M1 type, but not the anti-inflammatory M2 type, and enhanced the ability of macrophages for migration. Conversely, knockdown of RGS12 in macrophages inhibited the production of inflammatory cytokines and migration of macrophages in response to lipopolysaccharide stimulation. Our results demonstrate for the first time that inhibition of RGS12 in macrophages is a promising therapeutic target for the treatment of periodontitis.


Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2464
Author(s):  
Ramiro Quintanilla-Licea ◽  
Javier Vargas-Villarreal ◽  
María Julia Verde-Star ◽  
Verónica Mayela Rivas-Galindo ◽  
Ángel David Torres-Hernández

Amebiasis caused by Entamoeba histolytica is nowadays a serious public health problem worldwide, especially in developing countries. Annually, up to 100,000 deaths occur across the world. Due to the resistance that pathogenic protozoa exhibit against commercial antiprotozoal drugs, a growing emphasis has been placed on plants used in traditional medicine to discover new antiparasitics. Previously, we reported the in vitro antiamoebic activity of a methanolic extract of Lippia graveolens Kunth (Mexican oregano). In this study, we outline the isolation and structure elucidation of antiamoebic compounds occurring in this plant. The subsequent work-up of this methanol extract by bioguided isolation using several chromatographic techniques yielded the flavonoids pinocembrin (1), sakuranetin (2), cirsimaritin (3), and naringenin (4). Structural elucidation of the isolated compounds was achieved by spectroscopic/spectrometric analyses and comparing literature data. These compounds revealed significant antiprotozoal activity against E. histolytica trophozoites using in vitro tests, showing a 50% inhibitory concentration (IC50) ranging from 28 to 154 µg/mL. Amebicide activity of sakuranetin and cirsimaritin is reported for the first time in this study. These research data may help to corroborate the use of this plant in traditional Mexican medicine for the treatment of dyspepsia.


2020 ◽  
Vol 11 (7) ◽  
Author(s):  
Wei Sun ◽  
Fang Zhao ◽  
Yu Xu ◽  
Kai Huang ◽  
Xianling Guo ◽  
...  

Abstract Chondroitin polymerizing factor (CHPF) is an important member of glycosyltransferases involved in the biosynthesis of chondroitin sulfate (CS). However, the relationship between CHPF and malignant melanoma (MM) is still unknown. In this study, it was demonstrated that CHPF was up-regulated in MM tissues compared with the adjacent normal skin tissues and its high expression was correlated with more advanced T stage. Further investigations indicated that the over-expression/knockdown of CHPF could promote/inhibit proliferation, colony formation and migration of MM cells, while inhibiting/promoting cell apoptosis. Moreover, knockdown of CHPF could also suppress tumorigenicity of MM cells in vivo. RNA-sequencing followed by Ingenuity pathway analysis (IPA) was performed for exploring downstream of CHPF and identified CDK1 as the potential target. Furthermore, our study revealed that knockdown of CDK1 could inhibit development of MM in vitro, and alleviate the CHPF over-expression induced promotion of MM. In conclusion, our study showed, as the first time, CHPF as a tumor promotor for MM, whose function was carried out probably through the regulation of CDK1.


Animals ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 281
Author(s):  
Adrian Zaragoza-Bastida ◽  
Saudy Consepcion Flores-Aguilar ◽  
Liliana Mireya Aguilar-Castro ◽  
Ana Lizet Morales-Ubaldo ◽  
Benjamín Valladares-Carranza ◽  
...  

Rattlesnakes have venoms with a complex toxin mixture comprised of polypeptides and proteins. Previous studies have shown that some of these polypeptides are of high value for the development of new medical treatments. The aim of the present study is to evaluate, in vitro, the antibacterial and hemolytic activity of Crotalus triseriatus and Crotalus ravus venoms. A direct field search was conducted to obtain Crotalus triseriatus and Crotalus ravus venom samples. These were evaluated to determine their antibacterial activity against Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa through the techniques of Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC). Hemolytic activity was also determined. Antibacterial activity was determined for treatments (Crotalus triseriatus 2) CT2 and (Crotalus ravus 3) CR3, obtaining a Minimum Inhibitory Concentration of 50 µg/mL and a Minimum Bactericidal Concentration of 100 µg/mL against Pseudomonas aeruginosa. CT1 (Crotalus triseriatus 1), CT2, and CR3 presented hemolytic activity; on the other hand, Crotalus ravus 4 (CR4) did not show hemolytic activity. The results of the present study indicate for the first time that Crotalus triseriatus and Crotalus ravus venoms contain some bioactive compounds with bactericidal activity against Pseudomonas aeruginosa which could be used as alternative treatment in diseases caused by this pathogenic bacterium.


1998 ◽  
Vol 3 (1) ◽  
pp. 49-53 ◽  
Author(s):  
J. Enrico Lazaro ◽  
Frederick Gay

The microculture tetrazolium assay using 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) was used to estimate the 50% inhibitory concentration of chloroquine, quinine, artemisinin, and atovaquone using a Plasmodium falciparum in vitro culture system. The MTT assay was compared to the standard tritiated hypoxan-thine assay and to a previously described method, the 2,2′-di-p-nitrophenyl-5,5′-diphenyl-3,3′-[3,3′-dimethoxy-4,4′-diphenylenel-ditetrazolium chloride (NBT) assay. In general, the results show that the three assays generate comparative results. The results of this study suggest that the MTT method is able to give a profile of cytotoxic dose response effects over a wide range of concentrations of a drug. The method may be used in work that does not require extreme pre-cision and sensitivity, for instance, as a portable rapid screen to assay natural products for in vitro cytotoxic ac-tivity against Plasmodium falciparum.


2008 ◽  
Vol 2008 ◽  
pp. 1-5 ◽  
Author(s):  
Vasilios I. Balas ◽  
Sotiris K. Hadjikakou ◽  
Nick Hadjiliadis ◽  
Nikolaos Kourkoumelis ◽  
Mark E. Light ◽  
...  

A novel tri-n-butyl(IV) derivative of 2-thiobarbituric acid (HTBA) of formula[(n-Bu)3Sn(TBA)⋅H2O](1) has been synthesized and characterized by elemental analysis and119Sn-NMR and FT-IR spectroscopic techniques. The crystal structure of complex1has been determined by single crystal X-ray diffraction analysis at 120(2) K. The geometry around Sn(IV) is trigonal bipyramidal. Threen-butyl groups and one oxygen atom from a deprotonated 2-thiobarbituric ligand are bonded to the metal center. The geometry is completed with one oxygen from a water molecule. Compound1exhibits potent, in vitro, cytotoxicity against sarcoma cancer cells (mesenchymal tissue) from the Wistar rat, polycyclic aromatic hydrocarbons (PAH, benzo[a]pyrene) carcinogenesis. In addition, the inhibition caused by1, in the rate of lipoxygenase (LOX) catalyzed oxidation reaction of linoleic acid to hyperoxolinoleic acid, has been also kinetically and theoretically studied. The results are compared to that of cisplatin.


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