scholarly journals Anticancer Activity of 2-O-caffeoyl Alphitolic Acid Extracted from the Lichen, Usnea barbata 2017-KL-10

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3937
Author(s):  
Hae-Jung Chae ◽  
Geum-Jin Kim ◽  
Barsha Deshar ◽  
Hyun-Jin Kim ◽  
Min-Ji Shin ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Biological Activities ◽  
Biological Effects ◽  
Cancer Cell Line ◽  
Colorectal Cancer Cell Line ◽  
Migration And Invasion ◽  
Dependent Manner ◽  
Anticancer Activities ◽  
Concentration Dependent Manner ◽  
Mortality And Morbidity

Colorectal cancer is one of the life-threatening ailments causing high mortality and morbidity worldwide. Despite the innovation in medical genetics, the prognosis for metastatic colorectal cancer in patients remains unsatisfactory. Recently, lichens have attracted the attention of researchers in the search for targets to fight against cancer. Lichens are considered mines of thousands of metabolites. Researchers have reported that lichen-derived metabolites demonstrated biological effects, such as anticancer, antiviral, anti-inflammatory, antibacterial, analgesic, antipyretic, antiproliferative, and cytotoxic, on various cell lines. However, the exploration of the biological activities of lichens’ metabolites is limited. Thus, the main objective of our study was to evaluate the anticancer effect of secondary metabolites isolated from lichen (Usnea barbata 2017-KL-10) on the human colorectal cancer cell line HCT116. In this study, 2OCAA exhibited concentration-dependent anticancer activities by suppressing antiapoptotic genes, such as MCL-1, and inducing apoptotic genes, such as BAX, TP53, and CDKN1A(p21). Moreover, 2OCAA inhibited the migration and invasion of colorectal cancer cells in a concentration-dependent manner. Taken together, these data suggest that 2OCAA is a better therapeutic candidate for colorectal cancer.

scholarly journals Cytotoxic Effect of Resveratrol on Colorectal Cancer Cell Line

2020 ◽  
Vol 44 (1) ◽  
pp. 68-74
Author(s):  
Hussein A. Khayoon
Keyword(s):  
Colorectal Cancer ◽  
Cell Line ◽  
Cytotoxic Effect ◽  
Driving Forces ◽  
Cancer Cell Line ◽  
Negative Control ◽  
Significant Inhibition ◽  
Colorectal Cancer Cell Line ◽  
Dependent Manner ◽  
Concentration Dependent Manner

This study aimed to examine the cytotoxic effect of resveratrol as an anticancer in human colorectal cancer (HRT) cell line by assessment of its half-maximal inhibitory concentration (IC50) and its ability to inhibit the growth of these cancerous cells. Resveratrol inhibited the proliferation of HRT cell lines when used at different increased concentrations in this study (25, 50, 100, 200, 300) μmol respectively. These increased concentrations of resveratrol caused a corresponding significant inhibition in the growth percentage of the tested cancerous cell line (13%, 31.33%, 53.66%, 63.66 %, and 76.33%) respectively when compared with DMSO0.1% as negative control, in a concentration-dependent manner. Resveratrol at 300 μmol concentration showed the highest significant increase in the growth inhibitory percentage (76.33%). Moreover, resveratrol IC50 against (HRT) cell line was determined as 75.63 μmol. The study suggested a promising anticancer activity of resveratrol which can interfere with many dysregulated signaling pathways in transformed cells which are proposed to be driving forces for its anticancer effect.

scholarly journals Semi-Synthesis and In Vitro Anti-Cancer Evaluation of Magnolol Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4302
Author(s):  
Xiao-Long Sun ◽  
Mei-Lin Zhu ◽  
Yi-Qun Dai ◽  
Hong-Mei Li ◽  
Bo-Han Li ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
Biological Activities ◽  
Migration And Invasion ◽  
Dependent Manner ◽  
Anticancer Activities ◽  
Antitumor Effects ◽  
Concentration Dependent Manner ◽  
Human Cancer Cell Lines

Magnolol (MAG), a biphenolic neolignan, has various biological activities including antitumor effects. In this study, 15 MAG derivatives were semi-synthesized and evaluated for their in vitro anticancer activities. From these derivatives, compound 6a exhibited the best cytotoxic activity against four human cancer cell lines, with IC50 values ranging from 20.43 to 28.27 μM. Wound-healing and transwell assays showed that compound 6a significantly inhibited the migration and invasion of MDA-MB-231 cells. In addition, Western blotting experiments, performed using various concentrations of 6a, demonstrated that it downregulates the expression of HIF-1α, MMP-2, and MMP-9 in a concentration-dependent manner. Overall, these results suggest that substituting a benzyl group having F atoms substituted at the C2 position on MAG is a viable strategy for the structural optimization of MAG derivatives as anticancer agents.

scholarly journals Global transcriptome analysis reveals partial estrogen-like effects of karanjin in MCF-7 breast cancer cells

2021 ◽  
Author(s):  
Gaurav Bhatt ◽  
Akshita Gupta ◽  
Latha Rangan ◽  
Anil Mukund Limaye
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Target Genes ◽  
Biological Activities ◽  
Biological Effects ◽  
Dependent Manner ◽  
Cell Type ◽  
Concentration Dependent Manner ◽  
Mcf 7

Karanjin, an abundantly occurring furanoflavonoid in edible and non-edible legumes, exerts diverse biological effects in vivo, and in vitro. Its potential as an anticancer agent is also gaining traction following recent demonstrations of its anti-proliferative, cell cycle inhibitory, and pro-apoptotic effects. However, the universality of its anticancer potential is yet to be scrutinized, particularly so because flavonoids can act as selective estrogen receptor modulators (SERMs). Even the genomic correlates of its biological activities are yet to be examined in hormone responsive cells. This paper presents the early and direct transcriptomic footprint of 10 μM karanjin in MCF-7 breast cancer cells, using next generation sequencing technology (RNA-seq). We show that karanjin-modulated gene-expression repertoire is enriched in several hallmark gene sets, which include early estrogen-response, and G2/M checkpoint genes. Genes modulated by karanjin overlapped with those modulated by 1 nM 17β-estradiol (E2), or 1 μM tamoxifen. Karanjin altered the expression of selected estrogen-regulated genes in a cell-type, and concentration dependent manner. It downmodulated the expression of ERα protein in MCF-7 cells. Furthermore, ERα knockdown negatively impacted karanjins ability to modulate the expression of selected E2 target genes. Our data suggest that karanjin exerts its effects on ERα-positive breast cancer cells, at least in part, via ERα. The apparent SERM-like effects of karanjin pose a caveat to the anticancer potential of karanjin. In-depth studies on cell-type and concentration-dependent effects of karanjin may bring out its true potential in endocrine therapies.

Inhibition of Colorectal Cancer Cell Line CaCo-2 by Essential Oil of Eucalyptus camaldulensis Through Induction of Apoptosis

2020 ◽  
Author(s):  
Elham Taheri ◽  
Saba Ghorbani ◽  
Maryam Safi ◽  
Nasrin Seyyed Sani ◽  
Fatemeh Firouzi Amoodizaj ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Antioxidant Activity ◽  
Essential Oil ◽  
Cancer Cells ◽  
Cell Line ◽  
Cancer Cell Line ◽  
Eucalyptus Camaldulensis ◽  
Colorectal Cancer Cell Line ◽  
Dependent Manner ◽  
Induction Of Apoptosis

Treatment of colorectal cancer is one of the important challenges due to the increase of resistance to chemotherapeutic drugs. Isolated natural compounds from medicinal plants and other sources often are used as novel drugs for treatment of various human cancer. The aim of this study was to investigate the antioxidant and anticancer activity of Eucalyptus camaldulensis essential oil on colorectal cancer cell line Caco-2. The antioxidant activity of extracted E. camaldulensis essential oil (1000, 800, 400, 200, 100, 50, 25, 12.5, 6, and 3 μg/mL) was evaluated by free radicals inactivation method. Moreover, MTT assay was used to examine the cytotoxic effects of E. camaldulensis essential oil on the Caco-2 cell line. The mRNA expression of BAX and BCL-2 genes was studied using quantitative Real-Time PCR method, in treated cancer cells compared to untreated cells. We indicated a significant, impressive antioxidant activity in 1000 μg/mL of E. camaldulensis essential oil, in a concentration-dependent manner. In addition, we found that this product exerted a cytotoxic effect on cancer cells when 100 μg/mL concentration was considered as half-maximal inhibitory concentration (IC50). Also, the expression of BAX and BCL-2 genes were significantly upregulated and downregulated, respectively, in the treated Caco-2 cells with E. camaldulensis essential oil. In conclusion, our study showed significant antioxidant and anticancer activity in E. camaldulensis essential oil in a concentration and time-dependent manner, which may be due to the reduction of free radicals and induction of apoptosis process in colorectal cancer cells.

Chickpea (Cicer arietinum L.) Lectin Exhibit Inhibition of ACE-I, α-amylase and α-glucosidase Activity

2019 ◽  
Vol 26 (7) ◽  
pp. 494-501 ◽  
Author(s):  
Sameer Suresh Bhagyawant ◽  
Dakshita Tanaji Narvekar ◽  
Neha Gupta ◽  
Amita Bhadkaria ◽  
Ajay Kumar Gautam ◽  
...  
Keyword(s):  
Biological Effects ◽  
Exchange Chromatography ◽  
Health Concern ◽  
Carbohydrate Binding ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Ic50 Values ◽  
Chickpea Lectin

Background: Diabetes and hypertension are the major health concern and alleged to be of epidemic proportions. This has made it a numero uno subject at various levels of investigation. Glucosidase inhibitor provides the reasonable option in treatment of Diabetes Mellitus (DM) as it specifically targets post prandial hyperglycemia. The Angiotensin Converting Enzyme (ACE) plays an important role in hypertension. Therefore, inhibition of ACE in treatment of elevated blood pressure attracts special interest of the scientific community. Chickpea is a food legume and seeds contain carbohydrate binding protein- a lectin. Some of the biological properties of this lectin hitherto been elucidated. Methods: Purified by ion exchange chromatography, chickpea lectin was tested for its in vitro antioxidant, ACE-I inhibitory and anti-diabetic characteristic. Results: Lectin shows a characteristic improvement over the synthetic drugs like acarbose (oral anti-diabetic drug) and captopril (standard antihypertensive drug) when, their IC50 values are compared. Lectin significantly inhibited α-glucosidase and α-amylase in a concentration dependent manner with IC50 values of 85.41 ± 1.21 ҝg/ml and 65.05 ± 1.2 µg/ml compared to acarbose having IC50 70.20 ± 0.47 value of µg/ml and 50.52 ± 1.01 µg/ml respectively. β-Carotene bleaching assay showed antioxidant activity of lectin (72.3%) to be as active as Butylated Hydroxylanisole (BHA). In addition, lectin demonstrated inhibition against ACE-I with IC50 value of 57.43 ± 1.20 µg/ml compared to captopril. Conclusion: Lectin demonstrated its antioxidant character, ACE-I inhibition and significantly inhibitory for α-glucosidase and α-amylase seems to qualify as an anti-hyperglycemic therapeutic molecule. The biological effects of chickpea lectin display potential for reducing the parameters of medically debilitating conditions. These characteristics however needs to be established under in vivo systems too viz. animals through to humans.

scholarly journals Bioactivity-Guided Extract Optimization of Osmanthus fragrans var. aurantiacus Leaves and Anti-Inflammatory Activities of Phillyrin

Plants ◽  
2021 ◽  
Vol 10 (8) ◽  
pp. 1545
Author(s):  
Hwa-Young Song ◽  
Da-Eun Jeong ◽  
Mina Lee
Keyword(s):  
Biological Activities ◽  
Radical Scavenging ◽  
No Production ◽  
Dependent Manner ◽  
Optimal Method ◽  
Concentration Dependent Manner ◽  
Osmanthus Fragrans ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
Extracellular Regulated Kinase

The aim of this study was to identify the optimal extraction conditions for leaves of Osmanthus fragrans var. aurantiacus. Inhibitory effects of various extracts on NO production were compared. Antioxidant evaluations for total phenol and flavonoid contents were carried out using various extracts of O. fragrans var. aurantiacus leaves obtained under optimal extraction conditions that showed the greatest effect on NO production. The optimal method for extracting O. fragrans var. aurantiacus leaves resulted in an extract named OP OFLE. OP OFLE showed DPPH and ABTS radical scavenging activities in a concentration-dependent manner. Phillyrin (PH) was isolated as a major compound from OP OFLE by HPLC/DAD analysis. OP OFLE and PH reduced inducible nitric oxide (iNOS) and cyclooxygenase (COX)-2 protein expression and downregulated proinflammatory cytokines such as interleukin (IL)-1β, IL-6, IL-8, and tumor necrosis factor (TNF)-α in LPS-stimulated RAW 264.7 and HT-29 cells. To determine the signal pathway involved in the inhibition of NO production, a Western blot analysis was performed. Results showed that OP OFLE decreased phosphorylation of extracellular regulated kinase (pERK) 1/2 and the expression of nuclear factor-kappa B (NF-κB). Our results suggest that extracts of O. fragrans var. aurantiacus leaves and its major components have biological activities such as antioxidative and anti-inflammatory properties.

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