scholarly journals FORMULATION AND CHARACTERIZATION OF CYCLODEXTRIN BASED CURCUMIN LOADED NANOSPONGE

2022 ◽  
pp. 130-138
Author(s):  
ANUP M. AKARTE ◽  
PRAKASH H. PATIL
Keyword(s):  
Melting Point ◽  
Breast Cancer Cells ◽  
Combination Index ◽  
In Vitro Cytotoxicity ◽  
Index Analysis ◽  
Ic50 Value ◽  
Poorly Soluble ◽  
Mcf 7

Objective: The aim of proposed work is to develop and screen cyclodextrin based Nanosponge loaded with poorly soluble anticancer drug and to optimize most suitable Nanosystem with increased solubility and dissolution rate. Methods: Cyclodextrinnanosponge (CDNS) was prepared using pyromelliticdianhydride as a crosslinker for beta cyclodextrin monomer. Cyclodextrinnanosponge and curcumin were taken in 1:1 w/w proportion. The resultant curcumin loaded nanosponges were dried at 50±0.5 °C for 24 h. Results: The absorbance maxima for Curcumin was seen at 424.0 nm and for cyclodextrin was seen at 290.0 nm, The average melting point of pure drug is 181 °C which is complies with Stander melting point of drug and the aspect ratio of the nanosponge was found 1.037. Zeta potential noticed for CUR-CD-NS were more negative contrasted with separate plain CUR (−20.1±1.57) demonstrating solidness of the nanodispersion. Curcumin release from CUR-CDNS was upgraded to very nearly 10 folds toward the finish of 8 hour. Treatment with a combination of CUR-CDNS at 1:1 and 1:3 ratios resulted in an IC50 value was found 14.98 μg/ml. Conclusion: In vitro cytotoxicity study and combination index analysis showed the synergistic effect of CUR-CDNS against MCF-7 cells. The present study reveals that the combination of curcumin results in higher cytotoxicity against breast cancer cells.

scholarly journals Spectral analysis, in vitro cytotoxicity and antibacterial studies of bioactive principles from the leaves of Conocarpus lancifolius, a common tree of Jazan, Saudi Arabia

2023 ◽  
Vol 83 ◽  
Author(s):  
S. S. Moni ◽  
M. F. Alam ◽  
M. H. Sultan ◽  
H. A. Makeen ◽  
H. A. Alhazmi ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Breast Cancer Cells ◽  
In Vitro Cytotoxicity ◽  
Coumaric Acid ◽  
Ic50 Value ◽  
Ft Ir ◽  
Ir Analysis ◽  
Common Tree ◽  
Mcf 7

Abstract The objective of the present study was to analyse the bioactive compounds of the leaves of Conocarpus lancifolius (C. lancifolius). The GC-MS analysis of the hot methanolic extract of the leaves (HMEL) of C. lancifolius exhibited the bioactive compounds such as 1-(3-Methoxy-2-nitrobenzyl) iso quinoline, morphin-4-ol-6,7-dione, 1-bromo-N-methyl-, phytol, hexadecanoic acid, 2,3-dihydroxypropyl ester, 2,2':4',2”-terthiophene, ethyl iso-allocholate, caryophyllene oxide, campesterol, epiglobulol, cholestan-3-ol, 2-methylene-, (3á,5à)-, dasycarpidan-1-methanol, acetate (ester) and oleic acid, eicosyl ester. The FT-IR analysis of HMEL of C. lancifolius showed a unique peak at 3184, 2413, 1657 cm-1 representing coumaric acid, chlorogenic acid and ferulic acid. The HMEL of C. lancifolius was actively inhibiting the proliferation of breast cancer cells MCF-7 ATCC at the concentration of 72.66 ± 8.21 µg/ml as IC50 value. The HMEL of C. lancifolius also revealed a good spectrum of activity against Gram-positive and Gram-negative bacterial cultures screened in this work. The activity observed has shown more or less similar effects against screened bacteria. However, the magnitude of potentiality was significantly lesser compared to standard ciprofloxacin disc at p< 0.001 level (99% confidence intervals). Furthermore, the study demonstrating the bioactive compounds can be isolated from the leaves of C. lancifolius.

scholarly journals In Vitro Cytotoxicity of the Synthesized Gallic Acid Derivatives (N-Alkyl Gallamide) Against Breast MCF-7 Cancer Cells

2018 ◽  
Vol 34 (5) ◽  
pp. 2268-2272
Author(s):  
Maurin Marcelia ◽  
Ade Arsianti ◽  
Jilly Octaria Tagore Chan ◽  
Stevano Julio Wijoyo ◽  
Fadilah Fadilah ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Gallic Acid ◽  
Cytotoxic Effect ◽  
Linear Regression Analysis ◽  
Cancer Cell Line ◽  
In Vitro Cytotoxicity ◽  
Tert Butyl ◽  
Ic50 Value ◽  
Mcf 7

Gallic acid is a phenolic compound distributed in plants and fruits which has been reported to have cytotoxic effect on MCF-7 breast cancer cell line. In this research, we investigated in vitro cytotoxic effect of six synthesized compounds of gallic acid derivatives (N-alkyl gallamide), namely N-methyl gallamide (2); N-ethyl gallamide (3); N-butyl gallamide (4); N-sec-butyl gallamide (5); N-tert-butyl gallamide (6) and N-hexyl gallamide (7) against breast MCF-7 cells by MTT assay. Linear regression analysis is utilized to analyze data to regenerate IC50 value. The results will be compared with gallic acid as an original compound and doxorubicin as a positive control.Among six synthesized compounds, N-tert-butyl gallamide (6) with IC50 value of 2.1 µg/mL, and N-hexyl gallamide (7) with IC50 value of 3.5µg/mL,showed the stronger cytotoxicity against breast MCF-7 cells compared to gallic acid and doxorubicin. Thus,N-tert-butyl gallamide (6) and N-hexyl gallamide (7) are potential to be further developed as a promising anti-breast cancer agents.

Synthesis, Characterization, Molecular Docking, In Vitro Biological Evaluation and In Vitro Cytotoxicity Study of Novel Thiazolidine-4-One Derivatives as Anti-Breast Cancer Agents‏‏

2021 ◽  
Vol 21 ◽  
Author(s):  
Zainab Y. Kadhim ◽  
Hasanain G.J. Alqaraghuli ◽  
Muna Tawfeeq Abd
Keyword(s):  
Breast Cancer ◽  
Antibacterial Activity ◽  
Molecular Docking ◽  
Cell Growth ◽  
Breast Cancer Cells ◽  
Docking Study ◽  
In Vitro Cytotoxicity ◽  
T1 And T2 ◽  
Mcf 7

Background: Thiazolidine-4-one is a promising class of heterocyclic compounds with interesting pharmacological and biological activities, such as anticancer and antibacterial. Therefore, many researchers have synthesized thiazolidine-4-ones and evaluated their biological potential for developing new drugs. Objective: In this study, two novel thiazolidine-4-one derivatives (T1 and T2) were synthesized and evaluated for their antibacterial activity toward Staphylococcus aureus, Escherichia coli and Proteus mirabilis. Also, the cytotoxic activities of compounds T1 and T2 were estimated against MCF-7 (HER2+, ER+ and ER+) and MDA-MB-231 (triple-negative) human breast cancer cell lines. The chemical structure of compounds T1 and T2 was proven using spectral techniques (FT-IR, 1HNMR, and 13C-NMR) and CHN elemental analysis. Methods: The synthesis of thiazolidine-4-one compounds was performed in two steps. The first step consisted of the formation of Schiff bases S1 and S2. In the second step, the synthesized Schiff bases were reacted with thioglycolic acid to prepared thiazolidine-4-one compounds T1 and T2. Hemolysis assay, molecular docking, cytotoxicity activity (MTT assay) and antibacterial activity (disc diffusion assay) were studied. Results: The hemolysis study demonstrated that the hemolytic ratio of compounds T1 and T2 at (1, 2 and 3) mg/ml was less than 4%. MTT assay showed that 100 µg/ml of compounds T1 and T2 diminish the MCF-7 cell growth up to 80.05 ± 1.72 and 69.85 ± 3.26 respectively after 72 hrs, while the same concentration of compounds T1 and T2 reduces the MDA-MB-231 cell growth up 70.28 ± 2.31 and 57.15 ± 1.49, respectively. The inhibition zone of compounds T1 and T2 were 12 mm at 50 mg/ml and 10 mm at 5 mg/ml in E. coli bacteria. Furthermore, a docking study was carried out to investigate the affinity and binding mode of compounds T1 and T2 towards the ERα, VEGF, and HER2 protein receptors in breast cancer cells. Data obtained from the docking study were exactly identical to that obtained from in vitro cytotoxicity assay. Conclusion: The results proved that compound T1 is an optimal anticancer agent toward breast cancer cells and the hemolysis study indicates the use of safety inside the body for compound T1. Synthesized compound T1 was most effective against MCF-7 cells compared to MDA-MB-231 cells and more effective than the reference drug tamoxifen in breast cell lines. The high cytotoxicity of compound T1 on the growth of MCF‐7 cells because T1 binds with a high degree of affinity to the estrogen and HER2 receptors, which in turn inhibits cell proliferation and induces apoptosis.

DEVELOPMENT AND CHARACTERIZATION OF A NANOCARRIER FOR QUERCETIN

2009 ◽  
Vol 08 (01n02) ◽  
pp. 175-179 ◽  
Author(s):  
MAN-YI WONG ◽  
GIGI N. C. CHIU
Keyword(s):  
Breast Cancer Cells ◽  
Water Solubility ◽  
Storage Temperature ◽  
In Vitro Cytotoxicity ◽  
Cytotoxic Compound ◽  
Naturally Occurring ◽  
Quercetin Concentration ◽  
Fold Stability

Quercetin is a naturally occurring cytotoxic compound where clinical use has been limited by its low water solubility. Therefore, liposomes were explored for solubilizing quercetin. Liposomes composed of DPPC (1,2 dipalmitoyl-sn-glycerol-3-phosphocholine)/DSPE-PEG2000 (1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(polyethylene glycol)2000])/quercetin (90:5:5 mole ratio) incorporated quercetin efficiently at 100.9 ± 4.6% and increased quercetin concentration in water 11.2-fold. Stability studies at storage temperature of 4°C showed that the liposomes were stable for up to 16 weeks, without any significant changes in diameters. Liposomal quercetin showed a delayed release profile and reduced quercetin degradation. In vitro cytotoxicity tests also showed that the ED50 of liposomal quercetin was 17.6 times lower than free quercetin in MDA-MB-231 breast cancer cells. In conclusion, the DPPC/DSPE-PEG-based liposomes were stable and were capable of solubilizing quercetin, preventing quercetin degradation, and increasing quercetin in vitro cytotoxicity. Hence, liposomes are a suitable nanocarrier for quercetin.

scholarly journals Cytotoxicity of Kelakai (Stenochlaena palustris) Extract to MCF-7 Breast Cancer Cell

2020 ◽  
Vol 7 (3) ◽  
pp. 5-9
Author(s):  
Harlyanti Muthma'innah Mashar ◽  
Itma Annah
Keyword(s):  
Breast Cancer ◽  
Breast Cancer Cells ◽  
Chemical Constituents ◽  
Ethanol Extract ◽  
Positive Control ◽  
Cytotoxicity Assay ◽  
Ic50 Value ◽  
Mtt Reduction ◽  
Mcf 7

Breast cancer is reported to rank fifth among all types of cancer with a case of death of 6.6%. In the Central Kalimantan region, early examinations of cancers including breast cancer were carried out and 247 tumors in the breast were identified (1.76%). Kelakai (Stenochlaena palustris) as one of the typical plants of Kalimantan which contain natural chemical constituents has been reported to be effective as an anti-inflammatory and antioxidant, so that with this potential can be developed to overcome diseases associated with it, one of them is breast cancer. This study aimed to examine the cytotoxicity of MCF-7 breast cancer cells using ethanol extract. The cytotoxicity assay of kelakai extract against MCF-7 cells conducted in vitro by the MTT reduction method. The variation of concentration used is 1000; 500; 250; 125; 62.5; 31.5; and 15.625 µg/ml, doxorubicin as a positive control was performed in a concentration of 1 μg / ml. The results of the cytotoxicity assay showed that the kelakai extract had a toxic effect on MCF-7 cells with an IC50 value of 493.57 µg / ml.

scholarly journals Ursolic Acid Enhances Doxorubicin Cytotoxicity on MCF-7 Cells Mediated by G2/M Arrest

2012 ◽  
Vol 3 (3) ◽  
pp. 410
Author(s):  
Ibrahim Arifin ◽  
Adam Hermawan ◽  
Muthi' Ikawati ◽  
Sari Haryanti ◽  
Anindyajati Anindyajati ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Cycle ◽  
Cancer Cells ◽  
Ursolic Acid ◽  
Breast Cancer Cells ◽  
Chemotherapeutic Agent ◽  
Ic50 Value ◽  
Combinational Treatment ◽  
Mcf 7

Ursolic acid has been widely known to possess biological activity against numerous tumor cell lines. Previous studies revealed its cytotoxicity on several cancer cells in vitro by either inducing apoptosis or cell cycle modulation. This study was conducted to investigate ursolic acid’s cytotoxicity solely and in combination with a chemotherapeutic agent, doxorubicin, on MCF-7 breast cancer cells, followed by observation on its mechanism. Cytotoxicity of single and combinational treatment of ursolic acid and doxorubicin on MCF-7 breast cancer cells were conducted by using MTT assay. Single treatment was then evaluated by determining IC50 value, while combinational treatment was evaluated by analyzing cell viability and evaluating combination index (CI). To explore the mechanism underlying cytotoxic effect on respected cells, further analysis on cell cycle profile of single and combinational treatment was conducted by flow cytometry. Twenty four hours treatment of ursolic acid inhibited MCF-7 cells’ growth with IC50 value of 37 µM, while combinational treatment showed that several concentration combinations of ursolic acid and doxorubicin exhibited synergism of cytotoxic activity on MCF-7 cells, giving optimum CI value of 0.54. Flow cytometric analysis showed that combinational treatment induced G2/M arrest in MCF-7 cells. These results show that ursolic acid is promising to be developed as either single chemopreventive agent, or as doxorubicin’s co-chemotherapeutic agent in breast cancer treatment. Observation on the selectivity as part of safety aspect together with in silico, in vitro, and in vivo study on its molecular mechanism should be conducted.Keywords: ursolic acid, doxorubicin,co-chemotherapeutic agent, breast cancer, cell cycle

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