scholarly journals Cytotoxic Effects of Compounds Isolated from Ricinodendron heudelotii

Molecules ◽  
2019 ◽  
Vol 24 (1) ◽  
pp. 145 ◽  
Author(s):  
Omolara F. Yakubu ◽  
Abiodun H. Adebayo ◽  
Titilope M. Dokunmu ◽  
Ying-Jun Zhang ◽  
Emeka E.J. Iweala
Keyword(s):  
Ethyl Acetate ◽  
Gallic Acid ◽  
Cell Lines ◽  
Cancer Cell ◽  
Ethyl Acetate Fraction ◽  
Cytotoxic Effects ◽  
Ic50 Value ◽  
Ricinodendron Heudelotii ◽  
Galloyl Glucose ◽  
Mcf 7

This study was designed to explore the in vitro anticancer effects of the bioactive compounds isolated from Ricinodendron heudelotii on selected cancer cell lines. The leaves of the plant were extracted with ethanol and partitioned in sequence with petroleum ether, ethyl acetate, and n-butanol. The ethyl acetate fraction was phytochemically studied using thin layer chromatography (TLC) and column chromatography (CC). Structural elucidation of pure compounds obtained from the ethyl acetate fraction was done using mass spectra, 1H-NMR, and 13C-NMR analysis. The isolated compounds were subsequently screened using five different cancer cell lines: HL-60, SMMC-7721, A-549, MCF-7, SW-480, and normal lung epithelial cell line, BEAS-2B, to assess their cytotoxic effects. Nine compounds were isolated and structurally elucidated as gallic acid, gallic acid ethyl ester, corilagin, quercetin-3-O-rhamnoside, myricetin-3-O-rhamnoside, 1,4,6-tri-O-galloyl glucose, 3,4,6-tri-O-galloyl glucose, 1,2,6-tri-O-galloyl glucose, and 4,6-di-O-galloyl glucose. Corilagin exhibited the most cytotoxic activity with an IC50 value of 33.18 μg/mL against MCF-7 cells, which were comparable to cisplatin with an IC50 value of 27.43 µg/mL. The result suggests that corilagin isolated from R. heudelotii has the potential to be developed as an effective therapeutic agent against the growth of breast cancer cells.

Novel Conjugated Quinazolinone-Based Hydroxamic Acids: Design, Synthesis and Biological Evaluation

2020 ◽  
Vol 16 ◽  
Author(s):  
Tran Khac Vu ◽  
Nguyen Thi Thanh ◽  
Nguyen Van Minh ◽  
Nguyen Huong Linh ◽  
Nguyen Thi Phương Thao ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Cell Lines ◽  
Cancer Cell ◽  
Hdac Inhibitors ◽  
Cancer Cell Lines ◽  
Hydroxamic Acids ◽  
Biological Evaluation ◽  
Hdac Inhibition ◽  
Ic50 Value ◽  
Mcf 7

Background: Target-based approach to drug discovery currently attracts a great deal of interest from medicinal chemists in anticancer drug discovery and development. Histone deacetylase (HDAC) inhibitors represent an extensive class of targeted anti-cancer agents. Among the most explored structure moieties, hydroxybenzamides and hydroxypropenamides have been demonstrated to have potential HDAC inhibitory effects. Several compounds of these structural classes have been approved for clinical uses to treat different types of cancer, such as vorinostat and belinostat. Aims: This study aims at developing novel HDAC inhibitors bearing conjugated quinazolinone scaffolds with potential cytotoxicity against different cancer cell lines. Method: A series of novel N-hydroxyheptanamides incorporating conjugated 6-hydroxy-2 methylquinazolin-4(3H)- ones (15a-l) was designed, synthesized and evaluated for HDAC inhibitory potency as well as cytotoxicity against three human cancer cell lines, including HepG-2, MCF-7 and SKLu-1. Molecular simulations were finally performed to gain more insight into the structure-activity. relationships. Results: It was found that among novel conjugated quinazolinone-based hydroxamic acids synthesized, compounds 15a, 15c and 15f were the most potent, both in terms of HDAC inhibition and cytotoxicity. Especially, compound 15f displayed up to nearly 4-fold more potent than SAHA (vorinostat) in terms of cytotoxicity against MCF-7 cell line with IC50 value of 1.86 µM, and HDAC inhibition with IC50 value of 6.36 µM. Docking experiments on HDAC2 isozyme showed that these compounds bound to HDAC2 with binding affinities ranging from -10.08 to -14.93 kcal/mol compared to SAHA (-15.84 kcal/mol). It was also found in this research that most of the target compounds seemed to be more cytotoxic toward SKLu-1than MCF-7 and HepG-2. Conclusion: The resesrch results suggest that some hydroxamic acids could emerge for further evaluation and the results are well served as basics for further design of more potent HDAC inhibitors and antitumor agents.

scholarly journals Cytotoxic Constituents of Pachyrhizus Tuberosus from Peruvian Amazon

2013 ◽  
Vol 8 (10) ◽  
pp. 1934578X1300801 ◽  
Author(s):  
Olga Leuner ◽  
Jaroslav Havlik ◽  
Milos Budesinsky ◽  
Vladimir Vrkoslav ◽  
Jessica Chu ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Mtt Assay ◽  
Human Cancer ◽  
Chemical Constituents ◽  
Human Fibroblasts ◽  
Cancer Cell Lines ◽  
Cytotoxic Effects ◽  
Hct 116 ◽  
Mcf 7

Investigations into the chemical constituents of the seeds of the neglected tuber crop Pachyrhizus tuberosus (Leguminosae) resulted in the isolation of seven components: five rotenoids [12a-hydroxyerosone (1), 12a-hydroxydolineone (2), erosone (3), 12a-hydroxyrotenone (4) and rotenone (6)], a phenylfuranocoumarin [pachyrrhizine (5)] and an isoflavanone [neotenone (7)]. The compounds were isolated using several chromatography techniques and characterized and verified by NMR and HPLC/MS. The MTT assay was used to examine the selective cytotoxic effects of the methanolic P. tuberosus extract and isolated compounds in two human cancer cell lines [breast (MCF-7) and colorectal (HCT-116)] and in non-transformed human fibroblasts (MRC-5); IC50 values were calculated. The methanolic P. tuberosus extract displayed respectable cytotoxic effects against HCT-116 and MCF-7 cells with IC50 values of 7.3 and 6.3 μg/mL, respectively. Of the compounds, 6 exacted greatest cytotoxicity and selectivity towards the cancer cell lines tested, yielding IC50 values of 0.3 μg/mL against both MCF-7 and HCT-116 cells, and a 6-fold reduced activity against MRC-5 fibroblasts. Compound 4 also demonstrated cytotoxicity against MCF-7 and HCT-116 (1.1 and 1.8 μg/mL, respectively), and reduced cytotoxicity towards MRC-5 cells (7.5 μg/mL). The results revealed from the in vitro cytotoxic MTT assay are worthy of further antitumor investigation.

scholarly journals Cytotoxic Alkaloids from Leaves and Twigs of Dasymaschalon sootepense

2014 ◽  
Vol 9 (7) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Sakchai Hongthong ◽  
Chutima Kuhakarn ◽  
Vichai Reutrakul ◽  
Surawat Jariyawat ◽  
Pawinee Piyachaturawat ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Cell Lines ◽  
Cancer Cell ◽  
Methanol Extract ◽  
Ethyl Acetate Fraction ◽  
Cancer Cell Lines ◽  
Spectroscopic Methods ◽  
Aporphine Alkaloid ◽  
First Report ◽  
Bioassay Guided Fractionation

Bioassay-guided fractionation of the cytotoxic ethyl acetate fraction of the sequential methanol extract from the leaves and twigs of Dasymaschalon sootepense led to the isolation of a new 7-hydroxy aporphine alkaloid, 6a,7-dehydrodasymachaline (1) along with the five known compounds (-)-nordicentrine (2), dicentrinone (3), (-)-sinactine (4), aristolactam AII (5) and epiberberine (6). Their structures were elucidated by spectroscopic methods. This is the first report of alkaloids 1–2 and 5–6 from the genus Dasymaschalon. Compounds 1 and 5 showed cytotoxicity against a panel of cancer cell lines.

Isolation of Lupeol and Gallic acid with cytotoxic activity of two different extracts from the leaves of Iraqi Conocarpus erectus L.

2021 ◽  
pp. 3495-3503
Author(s):  
Tahany Amir Tawfeeq ◽  
Ghaith Ali Jasim ◽  
Abdulmutalib A. Nasser ◽  
Basma Talib Al-Sudani
Keyword(s):  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Gallic Acid ◽  
Cell Line ◽  
Ethyl Acetate Fraction ◽  
Hexane Fraction ◽  
High Concentration ◽  
Conocarpus Erectus ◽  
Mcf 7 ◽  
Ethyl Acetate Extracts

Conocarpus erectus L. is a perennial, evergreen shrub belonging to Combretaceae family. Conocarpus plant reported to contain phenolic acid, flavonoids, lignan, terpenes and tannins. Aim of study was to isolate lupeol from hexane fraction and gallic acid from ethyl acetate fraction and investigate the effects of (hexane and ethyl acetate) fractions on viability of pancreatic AsPC-1 and breast MCF-7 cell lines by MTT assay. The presence of lupeol in the hexane and gallic acid in the ethyl acetate extracts was detected by TLC. The identification of isolated lupeol and gallic acid by HPTLC and HPLC comparing with standard lupeol and gallic acid. Structural elucidation of isolated compounds done by FTIR and UV spectrophotometer. The cytotoxic activity showed more at high concentration (30µg/ml) in both ethyl acetate and hexane fractions against MCF-7 cell line, the percentage of cellular inhibition for ethyl acetate at 30mg/ml was (73% and 79%) more than the hexane fraction in which the inhibition was (60% and 76%) at 48hr and 72 hr respectively. Furthermore, the cytotoxic activity more at high concentration (30µg/ml) in both fractions against AsPC-1 cell line with cellular inhibition (58% and 70%) for ethyl acetate fraction and (50% and 66%) for hexane fraction in compared with Cisplatin.

Cytotoxic Evaluation of Daphne pontica L. Aerial Part Extracts on Three Cancerous Cell Lines by MTT Assay

2019 ◽  
Author(s):  
Behshad Eskandari ◽  
Maliheh Safavi ◽  
Seyede Nargess Sadati Lamardi ◽  
Mahdi Vazirian
Keyword(s):  
Ethyl Acetate ◽  
Cell Lines ◽  
Cancer Cell ◽  
Mtt Assay ◽  
Cytotoxic Effect ◽  
Ethyl Acetate Fraction ◽  
Chemotherapeutic Agents ◽  
Breast Cancer Cell Lines ◽  
Total Extract ◽  
Cancerous Cell

Nowadays, cancer is the second prevalent cause of mortality after cardiovascular diseases in developed and the third one in developing countries. Adverse effects of chemotherapeutic agents bring the necessity of investigating about new medications with fewer side effects. Daphne L. genus is one of the natural sources with valuable reported anticancer effects. This study aimed to assess the cytotoxic effect of some extracts from the aerial parts of Daphne pontica collected from North of Iran on cancer cell lines.Extraction of the plant material was performed by maceration (3×72 h) of 200 g of sample with petroleum ether, chloroform, ethyl acetate, and methanol, respectively. The total extract was also obtained by maceration of the sample with 80% ethanol. Different concentrations of the dried extracts were prepared to assess their cytotoxic effect by 24 h incubation of cell lines with different extracts and then MTT (dimethyl thiazolyl diphenyl tetrazolium) assay on three cancerous cell lines (MDA-MB-231, MCF-7 and T47D), performed in triplicate. IC50 was then estimated from curves constructed by plotting cell survival (%) versus sample concentration (µg/ml). Results indicated that ethyl acetate fraction of D. pontica had the most potent cytotoxic effect in MTT assay with IC50 = 977.46 µg/ml; while other fractions were weaker in toxicity (IC50>1000 µg/ml). By comparing to potent cytotoxic effects of other Daphne species, it seems that the cytotoxic properties of D. pontica is different from other species of this genus since according to this study, no significant antineoplastic properties against the three breast cancer cell lines were determined. Further studies on other pharmacological activities of this plant are recommended.

scholarly journals Cytotoxic Test of Extract and Fraction of Dendrophtoe Pentandra (L) Miq on T47D Cell

2019 ◽  
Vol 22 (3) ◽  
pp. 73-78
Author(s):  
Masayu Farah Diba ◽  
Salni Salni ◽  
Subandrate Subandrate
Keyword(s):  
Ethyl Acetate ◽  
Cytotoxic Effect ◽  
Linear Equations ◽  
Ethanol Extract ◽  
Ethyl Acetate Fraction ◽  
T47d Cell ◽  
Assay Method ◽  
Cytotoxic Effects ◽  
Ic50 Value ◽  
Ethanol Fraction

Indonesia has a variety of plants that have the potential for medicine. One of the plants used by the community as a drug with anticancer effects is Dendrophtoe petandra (L.) Miq. This study aims to determine the cytotoxic effect of ethanol extract, ethyl acetate fraction and water ethanol fraction of Dendrophtoe petandra (L.) Miq on T47D breast cancer cells. The cytotoxic effects of ethanol extract, ethyl acetate fraction and water ethanol fraction were carried out by MTT assay method using series concentration. Cytotoxic effects were assessed by calculating IC50 values using linear equations. Phytochemical test showed that Dendrophtoe petandra (L.) Miq contained saponins, terpenoids, flavonoids and tannins. The IC50 value of the ethanol extract, ethyl acetate fraction and water ethanol fraction were 417.506 μg/mL, 233.617 μg/mL, and 2748.357 μg/mL, respectively. The smaller the IC50 value means that the compound is more active. Water ethanol fraction of Dendrophtoe petandra (L.) Miq does not have a cytotoxic effect, whereas ethanol extract and ethyl acetate fraction of Dendrophtoe petandra (L.) Miq have cytotoxic effects in the medium strength category. The content of flavonoids and saponins in ethanol extract and ethyl acetate fraction of Dendrophtoe petandra (L.) Miq is thought to play role in causing T47D cell death. Cytotoxic effects of ethyl acetate fraction are stronger than ethanol extracts.

scholarly journals Indonesian Micromelum minutum Leave Extracts and Their Cytotoxic Activities toward Breast Cancer Cell Lines

2021 ◽  
Vol 53 (1) ◽  
pp. 109-117
Author(s):  
Ratna Asmah Susidarti ◽  
Edy Meiyanto ◽  
Muthi' Ikawati ◽  
Normaidah Normaidah ◽  
Nurramadhani A. Sida
Keyword(s):  
Breast Cancer ◽  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
4T1 Cells ◽  
Mcf 7

Isolation and identification of compounds and pharmacological activity of the Micromelum minutum grown in some countries has been done, but the Indonesian M. minutum has not been studied, either phytochemically or pharmacologically. This study aimed to determine the cytotoxic activity of Indonesian M. minutum leave extracts toward MCF-7 and 4T1 breast cancer cell lines. The leaves were obtained from M. minutum grow in Bantimurung National Park, Bulusaraung, South Sulawesi, and then were macerated gradually in hexane, ethyl acetate, and methanol. The cytotoxic activity of obtained extracts was determined by MTT assay. The extraction yielded hexane (HEM), ethyl acetate (EEM), and methanol (MEM) extracts of 2.65, 6.12, and 6.49%, respectively. HEM was the most potent extract with IC50 values of 148 and 87 µg/mL on MCF-7 and 4T1 cells, respectively, followed by EEM (185 and 170 µg/mL). MEM possessed a weak potency with an IC50 value of 384 µg/mL on MCF-7 cells and was not toxic toward 4T1 cells. Therefore, HEM is important to be further investigated for its active constituents.

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