scholarly journals Molecular attributes and apoptosis-inducing activities of a putative serine protease isolated from Tiger Milk mushroom (Lignosus rhinocerus) sclerotium against breast cancer cells in vitro

PeerJ ◽  
2018 ◽  
Vol 6 ◽  
pp. e4940 ◽  
Author(s):  
Hui Yeng Y. Yap ◽  
Nget Hong Tan ◽  
Szu Ting Ng ◽  
Chon Seng Tan ◽  
Shin Yee Fung
Keyword(s):  
Cold Water ◽  
Water Extract ◽  
Cancer Therapeutics ◽  
Breast Adenocarcinoma ◽  
Activity Measurement ◽  
Cytotoxic Activities ◽  
Nucleotide Polymorphisms ◽  
Anticancer Activities ◽  
Mcf7 Cells

Background The highly valued medicinal tiger milk mushroom (also known as Lignosus rhinocerus) has the ability to cure numerous ailments. Its anticancer activities are well explored, and recently a partially purified cytotoxic protein fraction termed F5 from the mushroom’s sclerotial cold water extract consisting mainly of fungal serine proteases was found to exhibit potent selective cytotoxicity against a human breast adenocarcinoma cell line (MCF7) with IC50 value of 3.00 μg/ml. However, characterization of its cell death-inducing activity has yet to be established. Methods The mechanism involved in the cytotoxic activities of F5 against MCF7 cells was elucidated by flow cytometry-based apoptosis detection, caspases activity measurement, and expression profiling of apoptosis markers by western blotting. Molecular attributes of F5 were further mined from L. rhinocerus’s published genome and transcriptome for future exploration. Results and Discussion Apoptosis induction in MCF7 cells by F5 may involve a cross-talk between the extrinsic and intrinsic apoptotic pathways with upregulation of caspase-8 and -9 activities and a marked decrease of Bcl-2. On the other hand, the levels of pro-apoptotic Bax, BID, and cleaved BID were increased accompanied by observable actin cleavage. At gene level, F5 composed of three predicted non-synonymous single nucleotide polymorphisms (T > C) and an alternative 5′ splice site. Conclusions Findings from this study provide an advanced framework for further investigations on cancer therapeutics development from L. rhinocerus.

scholarly journals Natural Compounds Isolated from Stachybotrys chartarum Are Potent Inhibitors of Human Protein Kinase CK2

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4453
Author(s):  
Samer Haidar ◽  
Franziska M. Jürgens ◽  
Dagmar Aichele ◽  
Annika Jagels ◽  
Hans-Ulrich Humpf ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Natural Compounds ◽  
Breast Adenocarcinoma ◽  
Stachybotrys Chartarum ◽  
Mcf7 Cells ◽  
A431 Cells ◽  
Ic50 Values ◽  
Human Lung Carcinoma ◽  
Kinase Ck2

A large number of secondary metabolites have been isolated from the filamentous fungus Stachybotrys chartarum and have been described before. Fourteen of these natural compounds were evaluated in vitro in the present study for their inhibitory activity towards the cancer target CK2. Among these compounds, stachybotrychromene C, stachybotrydial acetate and acetoxystachybotrydial acetate turned out to be potent inhibitors with IC50 values of 0.32 µM, 0.69 µM and 1.86 µM, respectively. The effects of these three compounds on cell proliferation, growth and viability of MCF7 cells, representing human breast adenocarcinoma as well as A427 (human lung carcinoma) and A431 (human epidermoid carcinoma) cells, were tested using EdU assay, IncuCyte® live-cell imaging and MTT assay. The most active compound in inhibiting MCF7 cell proliferation was acetoxystachybotrydial acetate with an EC50 value of 0.39 µM. In addition, acetoxystachybotrydial acetate turned out to inhibit the growth of all three cell lines completely at a concentration of 1 µM. In contrast, cell viability was impaired only moderately, to 37%, 14% and 23% in MCF7, A427 and A431 cells, respectively.

scholarly journals Composition and in-vitro CytotoxicActivities of the Leaf Essential Oil of Beilschmiedia erythrophloia from Taiwan

2013 ◽  
Vol 8 (1) ◽  
pp. 1934578X1300800
Author(s):  
Yu-Chang Su ◽  
Chen-Lung Ho
Keyword(s):  
Chemical Composition ◽  
Essential Oil ◽  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Cytotoxic Activities ◽  
Anticancer Activities ◽  
Leaf Essential Oil ◽  
Main Components ◽  
Type Apparatus

This study investigated the chemical composition and in-vitro cytotoxic activities of the essential oil isolated from the leaf of Beilschmiedia erythrophloia. The essential oil was isolated using hydrodistillation in a Clevenger-type apparatus, and characterized by GC-FID and GC-MS. Fifty-five compounds were identified, representing 100% of the oil. The main components identified were β-caryophyllene (22.6%), α-humulene (21.9%), terpinen-4-ol (5.3%), cis-β-ocimene (5.1%), sabinene (5.0%) and limonene (4.5%). The anticancer activities of oil were evaluated. The results showed that the oil exhibited cytotoxic activity against human oral, liver, lung, colon, melanoma, and leukemic cancer cells.

scholarly journals Synthesis, Biological Assessment, and Structure Activity Relationship Studies of New Flavanones Embodying Chromene Moieties

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 544 ◽  
Author(s):  
Eman Assirey ◽  
Azhaar Alsaggaf ◽  
Arshi Naqvi ◽  
Ziad Moussa ◽  
Rawda M. Okasha ◽  
...  
Keyword(s):  
In Silico ◽  
Biological Assessment ◽  
Diffusion Method ◽  
Breast Adenocarcinoma ◽  
Cytotoxic Activities ◽  
Human Pathogens ◽  
Bacterial Strains ◽  
Human Carcinoma ◽  
In Silico Studies

Novel flavanones that incorporate chromene motifs are synthesized via a one-step multicomponent reaction. The structures of the new chromenes are elucidated by using IR, 1H-NMR, 13C-NMR, 1H-1H COSY, HSQC, HMBC, and elemental analysis. The new compounds are screened for their in vitro antimicrobial and cytotoxic activities. The antimicrobial properties are investigated and established against seven human pathogens, employing the agar well diffusion method and the minimum inhibitory concentrations. A majority of the assessed derivatives are found to exhibit significant antimicrobial activities against most bacterial strains, in comparison to standard reference drugs. Moreover, their cytotoxicity is appraised against four different human carcinoma cell lines: human colon carcinoma (HCT-116), human hepatocellular carcinoma (HepG-2), human breast adenocarcinoma (MCF-7), and adenocarcinoma human alveolar basal epithelial cell (A-549). All the desired compounds are subjected to in-silico studies, forecasting their drug likeness, bioactivity, and the absorption, distribution, metabolism, and excretion (ADME) properties prior to their synthetic assembly. The in-silico molecular docking evaluation of all the targeted derivatives is undertaken on gyrase B and the cyclin-dependent kinase. The in-silico predicted outcomes were endorsed by the in vitro studies.

scholarly journals Ajwa Date (Phoenix dactylifera L.) Extract Inhibits Human Breast Adenocarcinoma (MCF7) Cells In Vitro by Inducing Apoptosis and Cell Cycle Arrest

PLoS ONE ◽  
2016 ◽  
Vol 11 (7) ◽  
pp. e0158963 ◽  
Author(s):  
Fazal Khan ◽  
Farid Ahmed ◽  
Peter Natesan Pushparaj ◽  
Adel Abuzenadah ◽  
Taha Kumosani ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Cycle Arrest ◽  
Phoenix Dactylifera ◽  
Breast Adenocarcinoma ◽  
Human Breast ◽  
Mcf7 Cells ◽  
Human Breast Adenocarcinoma ◽  
Cycle Arrest ◽  
Phoenix Dactylifera L

scholarly journals ANTIMICROBIAL, CYTOTOXIC AND HEMOLYTIC ACTIVITIES OF MARINE ALGAE-ASSOCIATED FUNGAL ISOLATES IN VIETNAM

2019 ◽  
Vol 18 (4) ◽  
pp. 406-412
Author(s):  
Hoang Kim Chi ◽  
Tran Thi Hong Ha ◽  
Le Huu Cuong ◽  
Tran Thi Nhu Hang ◽  
Nguyen Dinh Tuan ◽  
...  
Keyword(s):  
Natural Products ◽  
Human Cancer ◽  
Biological Activities ◽  
Breast Adenocarcinoma ◽  
Cytotoxic Activities ◽  
Marine Microorganisms ◽  
Fungal Strains ◽  
Fungal Isolates ◽  
Fungal Extracts

In the context of sources for natural products discovery are going scarcer, exploiting biotechnologically potential compounds from marine microbial symbionts is considered a relatively new trend. In our study a total of fifteen fungal strains were isolated from marine algal samples belonging to species Kappaphycus cottonii, K. striatus, Gracilaria eucheumatoides and Betaphycus gelatinus collected in Nha Trang in 2017. The in vitro biological activities, including antimicrobial, cytotoxic and hemolytic activities of ethyl acetate extracts of the fungal strains were determined. From fifteen fungal extracts, six displayed antimicrobial activity against at least one test strain. At 20 μg.ml-1, four fungal extracts were found to express cytotoxic activity on two human cancer cell lines hepatocellular carcinoma (Hep-G2) and breast adenocarcinoma (MCF-7), with G. eucheumatoides being the source of the highest number of producer strains. Hemolytic activity was observed in rabbit erythrocytes under almost all fungal extracts’ effect. No apparent relationship was observed between the biological activities of fungal isolates. The biological assessments uncovered several fungal candidates, such as Bge-1.1, Kco-2.1 and Geu-1.1 with relatively potent antimicrobial and cytotoxic activities while expressing less hemolytic effect at concentrations from 20 μg.ml-1 to 200 μg.ml-1. The results evidenced the potential of exploiting natural products from associated marine microorganisms, especially those for the purpose of pharmaceutical applications.

Effective Pharmacophore for CDC25 Phosphatases Enzyme Inhibitors: Newly Synthesized Bromothiazolopyrimidine Derivatives

2020 ◽  
Vol 20 ◽  
Author(s):  
Mahmoud El-Shahat ◽  
Mowafia A.M. Salama ◽  
Ahmed F. El-Farargy ◽  
Mamdouh M. Ali ◽  
Dalia M. Ahmed
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Enzyme Inhibitors ◽  
Wide Spectrum ◽  
Hct116 Cell ◽  
Cytotoxic Activities ◽  
The Novel ◽  
Anticancer Activities ◽  
Starting Compound

Background: Thiazolopyrimidine analogues are versatile synthetic scaffold possessing wide spectrum of biological interests involving potential anticancer activity. Objective: To report the synthesis of novel bromothiazolopyrimidine derivatives and the study of both molecular modeling and in-vitro anticancer activity. Method: Novel bromothiazolopyrimidine derivatives 5–18 have been prepared from 2-bromo-3-(4-chlorophenyl)-1-(3,4- dimethylphenyl)-propenone 3 as a key starting compound. The anti-cancer activities of the new compounds were evaluated against HepG2, MCF-7, A549 and HCT116 cell lines. Results: The compounds 16, 17 and 18 showed cytotoxic and growth inhibitory activities on both colon and lung cells. The cytotoxic activities of the novel synthetic compounds 8, 9, 11, 16, 17 and 18 were due to CDC25 phosphatases inhibition as shown by the enzymatic binding assay. Although compounds 8, 9 and 11 have only demonstrated CDC25B phosphatases inhibition. Conclusion: The novel bromothiazolopyrimidine derivatives showed promising in vitro anticancer activities against colon cancer HCT116 and lung cancer A549 cell lines comparable to the anticancer drug doxorubicin.

scholarly journals Determination of the Wound Healing Potentials of Medicinal Plants Historically Used in Ghana

2017 ◽  
Vol 2017 ◽  
pp. 1-6 ◽  
Author(s):  
Sara H. Freiesleben ◽  
Jens Soelberg ◽  
Nils T. Nyberg ◽  
Anna K. Jäger
Keyword(s):  
Wound Healing ◽  
Medicinal Plants ◽  
Plant Species ◽  
Cold Water ◽  
Water Extract ◽  
Scratch Assay ◽  
3T3 Fibroblasts ◽  
Nih 3T3 ◽  
Wound Healing Activity

The present study was carried out to investigate the wound healing potentials of 17 medicinal plants historically used in Ghana for wound healing. Warm and cold water extracts were prepared from the 17 dried plant species and tested in vitro in the scratch assay with NIH 3T3 fibroblasts from mice. The wound healing scratch assay was used to evaluate the effect of the plants on cell proliferation and/or migration in vitro, as a test for potential wound healing properties. After 21 hours of incubation increased proliferation and/or migration of fibroblasts in the scratch assay was obtained for 5 out of the 17 plant species. HPLC separation of the most active plant extract, which was a warm water extract of Philenoptera cyanescens, revealed the wound healing activity to be attributed to rutin and a triglycoside of quercetin. The present study suggests that Allophylus spicatus, Philenoptera cyanescens, Melanthera scandens, Ocimum gratissimum, and Jasminum dichotomum have wound healing activity in vitro.

scholarly journals Synthesis and in vitro anticancer activities of substituted N -(4′-nitrophenyl)- l -prolinamides

2020 ◽  
Vol 7 (9) ◽  
pp. 200906
Author(s):  
Adejoke Osinubi ◽  
Josephat Izunobi ◽  
Xiaoguang Bao ◽  
Olayinka Asekun ◽  
Jiehong Kong ◽  
...  
Keyword(s):  
Biological Properties ◽  
Lower Percentage ◽  
Cytotoxic Activities ◽  
Anticancer Activities ◽  
One Pot ◽  
Human Carcinoma ◽  
Carcinoma Cell Lines ◽  
Hct 116 ◽  
Cell Inhibition

Prolinamides are present in secondary metabolites and have wide-ranging biological properties as well as antimicrobial and cytotoxic activities. N -(4′-substituted phenyl)- l -prolinamides 4a – 4w were synthesized in two steps, starting from the condensation of p -fluoronitrobenzene 1a – 1b with l -proline 2a – 2b , under aqueous–alcoholic basic conditions to afford N -aryl- l -prolines 3a – 3c , which underwent amidation via a two-stage, one-pot reaction involving SOCl 2 and amines, to furnish l -prolinamides in 20–80% yield. The cytotoxicities of 4a – 4w against four human carcinoma cell lines (SGC7901, HCT-116, HepG2 and A549) were evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay; with good tumour inhibitory activities (79.50 ± 1.24%–50.04 ± 1.45%) against HepG2. 4a exhibited the best anti-tumour activity against A549 with percentage cell inhibition of 95.41 ± 0.67% at 100 µM. Likewise, 4s (70.13 ± 3.41%) and 4u (83.36 ± 1.70%) displayed stronger antineoplastic potencies against A549 than the standard, 5-fluorouracil (64.29 ± 2.09%), whereas 4a (93.33 ± 1.36%) and 4u (81.29 ± 2.32%) outperformed the reference (81.20 ± 0.08%) against HCT-116. SGC7901 showed lower percentage cell viabilities with 4u (8.02 ± 1.54%) and 4w (27.27 ± 2.38%). These results underscore the antiproliferative efficacies of l -prolinamides while exposing 4a and 4u as promising broad-spectrum anti-cancer agents. Structure-activity relationship studies are discussed.

scholarly journals New Values of Teucrium species: in Vitro Study of Cytotoxic Activities of Secondary Metabolites

2015 ◽  
Vol 43 (1) ◽  
pp. 41-46 ◽  
Author(s):  
Milan S. STANKOVIĆ ◽  
Tatjana Lj. MITROVIĆ ◽  
Ivana Z. MATIĆ ◽  
Marina D. TOPUZOVIĆ ◽  
Slaviša M. STAMENKOVIĆ
Keyword(s):  
Cell Survival ◽  
Cytotoxic Effect ◽  
Mononuclear Cells ◽  
In Vitro Study ◽  
K562 Cells ◽  
Myelogenous Leukemia ◽  
Breast Adenocarcinoma ◽  
Cytotoxic Activities ◽  
Peripheral Blood Mononuclear

The cytotoxicity of seven Teucrium species, a long time ago used as a food spices, for beverages and teas preparing, as well as therapeutics for digestive and respiratory diseases, were examined against human cervix adenocarcinoma HeLa, human melanoma Fem-x, human chronic myelogenous leukemia K562 and human breast adenocarcinoma MDA-MB-361 cells. MTT assay was used for determination of target cell survival. The most prominent cytotoxic effect was observed against K562 cells, especially by T. scordioides, T. montanum and T. botrys. All Teucrium extracts showed good cytotoxic activity on HeLa cells, but very low cytotoxic effect on MDA-MB-361 cells. In addition, the cytotoxic activities of T. scordioides and T. montanum extract were tested on healthy resting and phytohaemagglutinin-stimulated peripheral blood mononuclear cells (PHA-stimulated PBMC). T. scordioides and T. montanum extracts at concentration of 200 µg/ml reduced the resting PBMC and PHA-stimulated PBMC survival up to 10% and 20%, while the reduction of K562 cell survival at the same concentration of extracts was 94% and 97%, respectively. These results point to selectivity in their antitumor actions. Teucrium species can be regarded as promising candidates for natural plant sources of effective biological compounds as a supplements in the food industry, as well as for therapeutic use.

scholarly journals Host-Guest Complexation of Oxaliplatin and Para-Sulfonatocalix[n]Arenes for Potential Use in Cancer Therapy

Molecules ◽  
2020 ◽  
Vol 25 (24) ◽  
pp. 5926
Author(s):  
Sherif Ashraf Fahmy ◽  
Fortuna Ponte ◽  
Iten M. Fawzy ◽  
Emilia Sicilia ◽  
Udo Bakowsky ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Cancer Therapeutics ◽  
Breast Adenocarcinoma ◽  
Cytotoxic Activities ◽  
Therapeutic Drugs ◽  
Plot Analysis ◽  
The Stability ◽  
Reaction Stoichiometry ◽  
Potential Use ◽  
Mcf 7

P-sulfonatocalix[n]arenes have demonstrated a great potential for encapsulation of therapeutic drugs via host-guest complexation to improve solubility, stability, and bioavailability of encapsulated drugs. In this work, guest-host complexes of a third-generation anticancer drug (oxaliplatin) and p-4-sulfocalix[n]arenes (n = 4 and 6; p-SC4 and p-SC6, respectively) were prepared and investigated, using 1H NMR, UV, Job’s plot analysis, and DFT calculations, for use as cancer therapeutics. The peak amplitude of the prepared host-guest complexes was linearly proportional to the concentration of oxaliplatin in the range of 1.0 × 10−5 M−1 to 2.1 × 10−4 M−1. The reaction stoichiometry between either p-SC4 or p-SC6 and oxaliplatin in the formed complexes was 1:1. The stability constants for the complexes were 5.07 × 104 M−1 and 6.3 × 104 M−1. These correspond to complexation free energy of −6.39 and −6.52 kcal/mol for p-SC4 and p-SC6, respectively. Complexation between oxaliplatin and p-SC4 or p-SC6 was found to involve hydrogen bonds. Both complexes exhibited enhanced biological and high cytotoxic activities against HT-29 colorectal cells and MCF-7 breast adenocarcinoma compared to free oxaliplatin, which warrants further investigation for cancer therapy.

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