scholarly journals IN VITRO CYTOTOXIC ACTIVITY OF SECOISOLARICIRESINOL DIGLUCOSIDE ON HT-29, PA-1 CELL LINES, AND α-AMYLASE INHIBITORY ACTIVITY

2019 ◽  
pp. 168-173
Author(s):  
GUNABHUSHANA DADDALA ◽  
SWAROOPARANI A
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
Ovarian Cancer Cell Line ◽  
Cancer Cell Line ◽  
Secoisolariciresinol Diglucoside ◽  
Human Colon Cancer ◽  
Ht 29

Objective: The present study was conducted to evaluate the in vitro cytotoxic activity and α- amylase inhibitory activity of secoisolariciresinol diglucoside (SDG). Methods: The cytotoxic activity was conducted on HT-29 (human colon cancer cell line) and PA-1 (human ovarian cancer cell line) by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay and the α- amylase inhibitory activity using acarbose as a standard. Both the tests were evaluated at different concentrations, 3.125–100 μg/ml and 50–2000 μg correspondingly and the concentration required for a 50% inhibition of viability (IC50) was determined graphically. The effect of the samples on the proliferation of HT-29 and PA-1 was expressed as the percentage cell viability. Results: SDG exhibited a considerable dose- and time-dependent inhibition on both HT-29 and PA-1 and also observed a concentration-dependent α-amylase inhibitory activity that leads in reduction of starch hydrolysis and hence eventually to lowered glucose levels. Conclusion: The present in vitro study concluded that SDG can be a potent anticancer and moderate hyperglycemic component.

scholarly journals Monocyte Infiltration and Differentiation in 3D Multicellular Spheroid Cancer Models

Pathogens ◽  
2021 ◽  
Vol 10 (8) ◽  
pp. 969
Author(s):  
Natasha Helleberg Madsen ◽  
Boye Schnack Nielsen ◽  
Son Ly Nhat ◽  
Søren Skov ◽  
Monika Gad ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Dependent Manner ◽  
Multicellular Spheroid ◽  
Tumor Associated Macrophages ◽  
Cancer Models ◽  
Ht 29 ◽  
Mcf 7

Tumor-associated macrophages often correlate with tumor progression, and therapies targeting immune cells in tumors have emerged as promising treatments. To select effective therapies, we established an in vitro 3D multicellular spheroid model including cancer cells, fibroblasts, and monocytes. We analyzed monocyte infiltration and differentiation in spheroids generated from fibroblasts and either of the cancer cell lines MCF-7, HT-29, PANC-1, or MIA PaCa-2. Monocytes rapidly infiltrated spheroids and differentiated into mature macrophages with diverse phenotypes in a cancer cell line-dependent manner. MIA PaCa-2 spheroids polarized infiltrating monocytes to M2-like macrophages with high CD206 and CD14 expression, whereas monocytes polarized by MCF-7 spheroids displayed an M1-like phenotype. Monocytes in HT-29 and PANC-1 primarily obtained an M2-like phenotype but also showed upregulation of M1 markers. Analysis of the secretion of 43 soluble factors demonstrated that the cytokine profile between spheroid cultures differed considerably depending on the cancer cell line. Secretion of most of the cytokines increased upon the addition of monocytes resulting in a more inflammatory and pro-tumorigenic environment. These multicellular spheroids can be used to recapitulate the tumor microenvironment and the phenotype of tumor-associated macrophages in vitro and provide more realistic 3D cancer models allowing the in vitro screening of immunotherapeutic compounds.

scholarly journals Cytotoxicity of Standardized Curcuminoids Mixture against Epithelial Ovarian Cancer Cell Line SKOV-3

2020 ◽  
Vol 88 (1) ◽  
pp. 11 ◽  
Author(s):  
Heba Almosa ◽  
Mihal Alqriqri ◽  
Iuliana Denetiu ◽  
Mohammed A. Baghdadi ◽  
Mohammed Alkhaled ◽  
...  
Keyword(s):  
Ovarian Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Ovarian Cancer Cell ◽  
Ovarian Cancer Cell Line ◽  
Cancer Cell Line ◽  
Reversed Phase ◽  
Potential Contribution ◽  
Dependent Manner

Herbal medicine has been in use for centuries for a wide variety of ailments; however, the efficacy of its therapeutic agents in modern medicine is currently being studied. Curcuminoids are an example of natural agents, widely used due to their potential contribution in the prevention and treatment of cancer. In this study, the three main compounds of curcuminoids—curcumin, desmethoxycurcumin, and bisdesmethoxycurcumin—were determined by reversed-phase high performance liquid chromatography (HPLC) to quantify total content in a mixture. Subsequently, the effect of the three curcuminoids, employed as one sample, was evaluated, to study the proliferation, apoptosis, cell cycle, and migration of the human ovarian cancer cell line SKOV-3. The results reveal that curcuminoids inhibit the proliferation of SKOV-3 cells with concentration- and time-dependent mechanisms. The morphological analysis of the treated SKOV-3 cells showed a typical apoptotic phenotype—cell shrinkage and membrane blebbing in a dose-dependent manner. In addition, flow cytometry demonstrated an increase in apoptosis with an IC50 of 30 µM curcuminoids. The migration of SKOV-3 cells was also inhibited, reflected by a decrease in wound area. Furthermore, the curcuminoids were found to have no stimulation effect on the expression of cytokines TNF-α and IL-10. These results suggest that a curcuminoid mixture can effectively suppress epithelial cancer cell growth in vitro by inducing cellular changes and apoptosis.

scholarly journals In vitro and in vivo evaluation of colon cancer targeted epichlorohydrin crosslinked Portulaca-alginate beads

2018 ◽  
Vol 9 (1) ◽  
pp. 190-199 ◽  
Author(s):  
Geet P. Asnani ◽  
Chandrakant R. Kokare
Keyword(s):  
Colon Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Colon Cancer Cell Line ◽  
Colon Cancer Cell ◽  
In Vivo Studies ◽  
Ht 29

AbstractThe aim of this study was to formulate a novel dual crosslinked hydrogel bead using Portulaca mucilage for colon-targeted delivery of 5-fluorouracil (5-FU) and evaluate its safety, specificity and efficacy. The ionotropic gelation technique was employed to prepare the hydrogel beads of Portulaca mucilage. For this, the mucilage was initially crosslinked with alginate and calcium ions. Epichlorohydrin was employed as a crosslinker in the second crosslinking step. The formulation was subjected to in vitro and in vivo studies to evaluate morphology, size, cytotoxicity, and organ distribution. Human HT-29 colon cancer cell-line was used for in vitro assays and in vivo studies were performed in Wistar rats to assess the usefulness and effectiveness of the formulation for colon cancer therapy. Microsphere sizes ranged from 930 to 977μm and possessed a high level of drug encapsulation efficiency (ca. 78% w/w). Compared with 5-FU solution (Tmax = 1.2 h, mean resident time: MRT = 3.3h) the dual crosslinked Portulaca microspheres exhibited sustained drug release after oral administration to rats (Tmax = 16h, MRT = 14h). The relative bioavailability of 5-FU solution and the microspheres were 100 and 93.6% respectively. Tissue distribution studies indicated high concentration of 5-FU in colon. In-vitro anticancer assay demonstrated IC50 value of 11.50 μg/ml against HT-29 colon cancer cell line. The epichlorohydrin cross-linked Portulaca microspheres prepared in this study provided sustained release of 5-FU up to 16h in the colonic region and enhanced the antitumor activity of the neoplastic drug. The formulation is hence an ideal carrier system for colon-targeted drug delivery.

scholarly journals Synthesis, Characterization, In Vitro Anticancer Potentiality, and Antimicrobial Activities of Novel Peptide–Glycyrrhetinic-Acid-Based Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4573
Author(s):  
Gaber O. Moustafa ◽  
Ahmed Shalaby ◽  
Ahmed M. Naglah ◽  
Marwa M. Mounier ◽  
Heba El-Sayed ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Micrococcus Luteus ◽  
Normal Skin ◽  
Cancer Cell Line ◽  
Glycyrrhetinic Acid ◽  
Pentacyclic Triterpenoids ◽  
Vitro Effect

Glycyrrhetinic acid (GA) is one of many interesting pentacyclic triterpenoids showing significant anticancer activity by triggering apoptosis in tumor cell lines. This study deals with the design and synthesis of new glycyrrhetinic acid (GA)–amino acid peptides and peptide ester derivatives. The structures of the new derivatives were established through various spectral and microanalytical data. The novel compounds were screened for their in vitro cytotoxic activity. The evaluation results showed that the new peptides produced promising cytotoxic activity against the human breast MCF-7 cancer cell line while comparing to doxorubicin. On the other hand, only compounds 3, 5, and 7 produced potent activity against human colon HCT-116 cancer cell line. The human liver cancer (HepG-2) cell line represented a higher sensitivity to peptide 7 (IC50; 3.30 μg/mL), while it appeared insensitive to the rest of the tested peptides. Furthermore, compounds 1, 3, and 5 exhibited a promising safety profile against human normal skin fibroblasts cell line BJ-1. In order to investigate the mode of action, compound 5 was selected as a representative example to study its in vitro effect against the apoptotic parameters and Bax/BCL-2/p53/caspase-7/caspase-3/tubulin, and DNA fragmentation to investigate beta (TUBb). Additionally, all the new analogues were subjected to antimicrobial assay against a panel of Gram-positive and Gram-negative bacteria and the yeast candida Albicans. All the tested GA analogues 1–8 exhibited more antibacterial effect against Micrococcus Luteus than gentamicin, but they exhibited moderate antimicrobial activity against the tested bacterial and yeast strains. Molecular docking studies were also simulated for compound 5 to give better rationalization and put insight to the features of its structure.

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