Abstract:
:Considering the therapeutic values of bioflavonoids in colon cancer treatment, six 2'-hydroxy chalcones (C1-C6) were synthesized, characterized and screened for in vitro cytotoxicity on human colon carcinoma (HCT116) and African green monkey kidney epithelial cells (Vero). Only C5 showed selective cytotoxicity against HCT116 cells. Other potent cytotoxic compounds were C1, C2 and C3. Further screening included enzyme inhibition studies on histone deacetylase (HDAC) enzyme where C1 showed lowest IC50 value (105.03 µM). Based on cytotoxicity data C1, C2 and C3 were selected for further in vitro mechanistic studies, namely apoptotic studies (Acridine orange/Ethidium bromide (AO/EB) and Annexin V), cell cycle analysis using propidium iodide (PI) stain and in vivo anticancer efficacy in 1,2-dimethyl hydrazine (DMH) induced colorectal carcinoma in Wistar rats. The compounds induced apoptosis in more than 30 % cells in AO/EB and Annexin V staining. They also showed cell cycle arrest in G2/M phase with PI staining. They showed a significant reduction in aberrant crypt foci formation and adenocarcinoma count along with a significant (p<0.05) reduction in TNF-α levels as compared to DMH control at 100 mg/kg dose. Thus, it can be concluded that the synthesized 2'-hydroxychalcones were effective against colon adenocarcinoma in in vitro and in vivo studies.
journal_name
EXCLI Jjournal_title
EXCLI journalauthors
Pande AN,Biswas S,Reddy ND,Jayashree BS,Kumar N,Rao CMdoi
10.17179/excli2016-643subject
Has Abstractpub_date
2017-04-03 00:00:00pages
448-463issn
1611-2156pii
Doc448journal_volume
16pub_type
杂志文章相关文献
EXCLI Journal文献大全abstract::Phoenix sylvestris (Arecaceae family) known as Indian Date Palm has been identified as a component of traditional medicine against various ailments. The present study was focused on phytochemical screening of crude hexane, dichloromethane and methanol leaf extracts. The crude extracts showed the presence of alkaloids,...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:10.17179/excli2015-689
更新日期:2016-02-05 00:00:00
abstract::Genome editing technologies include techniques used for desired genetic modifications and allow the insertion, modification or deletion of specific DNA fragments. Recent advances in genome biology offer unprecedented promise for interdisciplinary collaboration and applications in gene editing. New genome editing techn...
journal_title:EXCLI journal
pub_type: 杂志文章,评审
doi:10.17179/excli2020-3070
更新日期:2021-01-04 00:00:00
abstract::Achillea eriophora (Asteraceae) is a medicinal plant commonly used in Iran. This study was performed to determine the cardiovascular effects of hydroethanolic extract of A. eriophora (HEAE) and the underlying mechanisms in anaesthetized rats. The acute effects of intravenous (i.v.) administration of different doses of...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:10.17179/excli2016-529
更新日期:2016-12-07 00:00:00
abstract::The liver is famous for its strong regenerative capacity, employing different modes of regeneration according to type and extent of injury. Mature liver cells are able to proliferate in order to replace the damaged tissue allowing the recovery of the parenchymal function. In more severe scenarios hepatocytes are belie...
journal_title:EXCLI journal
pub_type: 杂志文章,评审
doi:10.17179/excli2014-576
更新日期:2015-01-06 00:00:00
abstract::Bladder cancer (BC) is the sixth most common malignancy in men and 17th in women. Exosomal long non-coding RNAs (lncRNAs) have been defined as a novel biomarker for BC. The aim of this study is to evaluate the clinical significance of urine exosomal PVT-1, ANRIL and PCAT-1 as a biomarker in BC patients with tumors cla...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:10.17179/excli2019-1683
更新日期:2020-03-04 00:00:00
abstract::Hepatitis C is a major global health burden and Egypt has the highest prevalence of hepatitis C virus (HCV) worldwide. The current study was designed to evaluate the beneficial therapeutic effects of ethanolic extracts of Nigella sativa, Zingiber officinale and their mixture in Egyptian HCV patients. Sixty volunteer p...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:
更新日期:2013-11-11 00:00:00
abstract::We present the case of a 77 year old male patient with metastatic pancreatic neuroendocrine tumor (NET). The patient was initially treated by extensive surgical resection that however, led to severe complications with delayed recovery. During follow-up, a number of new liver metastases were detected, one of which was ...
journal_title:EXCLI journal
pub_type:
doi:10.17179/excli2019-1220
更新日期:2019-05-21 00:00:00
abstract::This study investigated the effect of the serotonin selective reuptake inhibitors (SSRIs) fluoxetine, sertraline, fluvoxamine and the tricyclic antidepressant (TCA) impiramine on oxidative stress in brain and liver induced by lipopolysaccharide administration in mice. Each drug was administered subcutaneously at doses...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:
更新日期:2011-12-08 00:00:00
abstract::To investigate whether offspring sex ratio at birth (SRB) was associated with maternal breast cancer risk, the present case-control study and a meta-analysis of literature were done. A total of 389 female breast cancer patients who had at least one offspring participated in the study. From general population 356 healt...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:
更新日期:2010-07-26 00:00:00
abstract::Aromatase is a rate-limiting enzyme for estrogen biosynthesis that is overproduced in breast cancer tissue. To block the growth of breast tumors, aromatase inhibitors (AIs) are employed to bind and inhibit aromatase in order to lower the amount of estrogen produced in the body. Although a number of synthetic aromatase...
journal_title:EXCLI journal
pub_type: 杂志文章,评审
doi:10.17179/excli2018-1417
更新日期:2018-07-20 00:00:00
abstract::The aim of this study was to evaluate the effect of acute and chronic physical and psychological stressors on the induction of oxidative stress in male rat liver. Male Wistar rats were randomly divided into 3 groups as following: control, physical and psychological stress groups. Stress was induced by communication bo...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:
更新日期:2014-02-24 00:00:00
abstract::Vitamin D deficiency, common in the population with irritable bowel syndrome (IBS), can induce the main factors that lead to IBS clinical symptoms, such as depression, anxiety, and inflammation. Serotonin (5-HT) plays an important role in the pathophysiology of IBS, and its production and secretion are increased from ...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:10.17179/excli2020-2247
更新日期:2020-05-19 00:00:00
abstract::Exposure to microgravity leads to orthostatic intolerance in astronauts and differential vascular structural and functional adaptations have been implicated in its occurrence. The present study tended to clarify the characteristics of vascular inflammation and oxidative stress in hindlimb unweighting (HU) rat vasculat...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:
更新日期:2010-12-23 00:00:00
abstract::Presently, functional foods and nutraceuticals are gaining immense importance in the prevention of various maladies through dietary regimen module. Consumption of fruits and vegetables based diet has pursuit a range of bioactive components, especially phytochemicals targeting life threatening ailments. In this context...
journal_title:EXCLI journal
pub_type: 杂志文章,评审
doi:
更新日期:2014-06-03 00:00:00
abstract::The aim of this study was to determine the effects of caffeine and chlorogenic acid supplementation on gut microbiota, and metabolic disturbances in patients with NAFLD and diabetes. In this randomized, placebo-controlled, clinical trial, 26 patients with diabetes and NAFLD were randomly assigned to four groups to rec...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:10.17179/excli2019-2021
更新日期:2020-03-02 00:00:00
abstract::Everolimus (EVR), as a rapamycin analog, is a selective inhibitor of the mammalian target of rapamycin (mTOR) kinase and its associated signaling pathway. mTOR is a serine/threonine protein kinase and its hyperactivity is involved in the pathophysiology of Alzheimer's disease (AD) and associated cognitive deficits. Th...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:10.17179/excli2018-1626
更新日期:2018-10-29 00:00:00
abstract::The essential oil obtained from leaves of Melissa officinalis L. (Family of Lamiaceae) growing in Algeria, was investigated for its chemical composition and in vitro antimicrobial activity. The chemical composition was determined by hydrodistillation and analyzed by GC/MS and GC-FID. Sixty-three compounds were identif...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:
更新日期:2014-07-17 00:00:00
abstract::Prosopis cineraria (L.) Druce (Leguminosae) (syn. Prosopis spicigera L.) has antidiabetic and antioxidant potential. Earlier we reported its hypolipidemic activity obtained from ethanol extract (ET-PCF). Object of this work was to isolate ferulic acid (FA) from ET-PCF and evaluate hypolipidemic activity against high-f...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:10.17179/excli2016-394
更新日期:2016-10-25 00:00:00
abstract::A reliable biomarker has not been identified to predict the outcome of traumatic brain injury (TBI) in children. Therefore, the present systematic review and meta-analysis aimed to assess the association between neuron specific enolase (NSE) and traumatic brain injury (TBI) in children. Two independent reviewers searc...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:10.17179/excli2017-405
更新日期:2017-07-03 00:00:00
abstract::The purpose of the present study was to investigate whether the markers of oxidative stress could be altered in workers exposed to asbestos. A comparative cross-sectional research was conducted in a group of 50 subjects exposed to asbestos and another group of 50 with the same age and sex unexposed to asbestos. Malond...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:10.17179/excli2015-469
更新日期:2015-09-28 00:00:00
abstract::The present study deals with the isolation and partial purification of bioactive compounds from the crude methanol extracts of the leaves of Ageratum houstonianum (Asteraceae). The quantification and the identification of compounds in the crude extract and active bands isolated by preparative TLC were accomplished usi...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:
更新日期:2012-02-28 00:00:00
abstract::The chemical composition of the essential oils of different Allium nigrum L. organs and the antibacterial activity were evaluated. The study is particularly interesting because hitherto there are no reports on the antibacterial screening of this species with specific chemical composition. Therefore, essential oils fro...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:
更新日期:2014-05-13 00:00:00
abstract::Lack of data on safety of herbal medicines have endangered human health and life. The present study evaluated the genotoxic and mutagenic effect of Kalanchoe laciniata to access the safety and usefulness of the medicinal plant. Aqua-methanolic and n-hexane extracts of K. laciniata were evaluated for the genotoxic pote...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:10.17179/excli2016-748
更新日期:2017-04-24 00:00:00
abstract::The traditional uses of Portulaca oleracea L. (PO) with anti-inflammatory and anti-cancer activity as well as antioxidants properties were expressed previously. Glioma is considered the most common primary brain tumor and its malignant form is the most lethal adult brain tumor, that glioblastoma covers about 50 % of g...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:10.17179/excli2019-1063
更新日期:2019-03-20 00:00:00
abstract::There are abundant studies indicating that blocking gap junctions (GJs) containing connexin 36 (Cx36) inhibit seizures. However, recent evidences demonstrate proconvulsant effect of such intervention. Electrical coupling between GABAergic interneurons in CA1 region of hippocampus is mediated through Cx36 GJs. We inves...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:
更新日期:2013-03-14 00:00:00
abstract::To date, a number of significant herbal drug interactions have their origins in the alteration of cytochrome P450 (CYP) activity by various phytochemicals. Among the most noteworthy are those involving St. John's wort and drugs metabolized by human CYP3A4 enzyme. This review article is the continued work from our prev...
journal_title:EXCLI journal
pub_type: 杂志文章,评审
doi:
更新日期:2014-08-20 00:00:00
abstract::Metabolic syndrome (MS) is a condition associated with metabolic abnormalities that are characterized by central obesity (e.g. waist circumference or body mass index), hypertension (e.g. systolic or diastolic blood pressure), hyperglycemia (e.g. fasting plasma glucose) and dyslipidemia (e.g. triglyceride and high-dens...
journal_title:EXCLI journal
pub_type: 杂志文章,评审
doi:10.17179/excli2017-911
更新日期:2018-01-10 00:00:00
abstract::Toxoplasma gondii is a common protozoan parasite, which infects warm-blooded mammals, including mice and humans, throughout the world. The negative effects of T. gondii infection on the human reproductive system have been documented, especially in females. However, only few studies have examined the effects of T. gond...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:10.17179/excli2020-2052
更新日期:2020-08-24 00:00:00
abstract::[This retracts the article DOI: 10.17179/excli2015-642.]. ...
journal_title:EXCLI journal
pub_type: 杂志文章,撤回出版物
doi:10.17179/excli2016-570
更新日期:2016-09-19 00:00:00
abstract::Patients with diabetes tend to have an increased risk of osteoporosis that may be related to hyperglycemia. In vitro evidence has shown that high glucose can affect the proliferation and osteogenic differentiation of mesenchymal stem cells (MSCs). Tissue regeneration depends mainly on MSCs. However, the exact mechanis...
journal_title:EXCLI journal
pub_type: 杂志文章
doi:
更新日期:2013-06-27 00:00:00