scholarly journals Cytotoxic Activity of 2-O-β-glucopyranosil Cucurbitacin D from Benalu Batu (Begonia sp.) Growing in Morowali, Central Sulawesi

2020 ◽  
Vol 20 (4) ◽  
pp. 766
Author(s):  
Muhammad Sulaiman Zubair ◽  
Walied Mohamed Alarif ◽  
Mohamed Ali Ghandourah ◽  
Syariful Anam ◽  
Ibrahim Jantan
Keyword(s):  
Cytotoxic Activity ◽  
Annexin V ◽  
Preparative Thin Layer Chromatography ◽  
Human Colon ◽  
Breast Adenocarcinoma ◽  
Apoptosis Induction ◽  
Cucurbitacin D ◽  
Hct 116 ◽  
Central Sulawesi ◽  
Mcf 7

Benalu batu (Begonia sp.) had been used traditionally as an anticancer medicinal plant by Wana tribe in Morowali, Central Sulawesi, This study aims to evaluate the cytotoxic activity of 2-O-β-glucopyranosil cucurbitacin D, isolated from the ethyl acetate soluble fraction of Benalu batu (Begonia sp.) and to determine its action on apoptosis induction. Benalu batu (Begonia sp.) herb was extracted by maceration using ethanol 96% as a solvent. Vacuum liquid column chromatography and preparative thin layer chromatography have been applied on fractionation and isolation of the compound. The structure elucidation was performed by extensive analysis of 1D/2D nuclear magnetic resonance (NMR) and Mass Spectrophotometer (MS). Cytotoxic activity against human breast adenocarcinoma (MCF-7) and human colon colorectal carcinoma (HCT-116) cell lines were performed by 5-diphenyltetrazolium bromide (MTT) method. Annexin V-FITC assay was employed to determine the apoptosis induction. 2-O-β-glucopyranosil cucurbitacin D showed potent cytotoxic activity against MCF-7 and HCT-116 with the IC50 of 19.913 and 0.002 μg/mL, respectively. Annexin V-FITC assay clearly exhibited the cytotoxic mechanism on MCF-7 and HCT-116 via apoptosis induction with a significant percentage of early and late apoptosis of 75.8 and 78.4%, respectively. This study reveals the potential cytotoxic activity of 2-O-β-glucopyranosil cucurbitacin D isolated from Benalu batu and its mechanism via apoptosis induction.

scholarly journals Cytotoxic Activity and Metabolic Profiling of Fifteen Euphorbia Species

Metabolites ◽  
2020 ◽  
Vol 11 (1) ◽  
pp. 15
Author(s):  
Seham S. El-Hawary ◽  
Rabab Mohammed ◽  
Ahmed F. Tawfike ◽  
Nadia M. Lithy ◽  
Sameh Fekry AbouZid ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Metabolic Profiling ◽  
Colon Adenocarcinoma ◽  
Human Colon ◽  
Breast Adenocarcinoma ◽  
Molecular Formula ◽  
Metabolic Pattern ◽  
Hepg2 Cell Lines ◽  
Mcf 7

Euphorbia is a large genus of flowering plants with a great diversity in metabolic pattern. Testing the cytotoxic potential of fifteen Euphorbia species revealed highest activity of E. officinarum L. against human colon adenocarcinoma (CACO2) cell line (IC50 7.2 µM) and of E. lactea Haw. against human hepatoma (HepG2) and human breast adenocarcinoma (MCF-7) cell lines (IC50 5.2 and 5.1 µM, respectively). Additionally, metabolic profiling of the fifteen tested species, using LC-HRMS, for dereplication purposes, led to the annotation of 44 natural compounds. Among the annotated compounds, diterpenoids represent the major class. Dereplication approach and multivariate data analysis are adopted in order to annotate the compounds responsible for the detected cytotoxic activity. Results of Principle component analysis (PCA) come in a great accordance with results of biological testing, which emphasized the cytotoxic properties of E. lactea Haw. A similarity correlation network showed that the two compounds with the molecular formula C16H18O8 and C20H30O10, are responsible for cytotoxic activity against MCF-7 and HepG2 cell lines. Similarly, the compound with molecular formula C18H35NO correlates with cytotoxic activity against CACO2.

Ligand-Based Drug Design: Synthesis and Biological Evaluation of Substituted Benzoin Derivatives as Potential Antitumor Agents

2019 ◽  
Vol 15 (4) ◽  
pp. 417-429 ◽  
Author(s):  
Dima A. Sabbah ◽  
Ameerah H. Ibrahim ◽  
Wamidh H. Talib ◽  
Khalid M. Alqaisi ◽  
Kamal Sweidan ◽  
...  
Keyword(s):  
Cell Lines ◽  
Antiproliferative Activity ◽  
Inhibitory Activity ◽  
Colon Adenocarcinoma ◽  
Human Colon ◽  
T47d Cell ◽  
Breast Adenocarcinoma ◽  
Glide Docking ◽  
Hct 116 ◽  
Mcf 7

Background: Phosphoinositide 3-kinase α (PI3Kα) has emerged as a promising target for anticancer drug design. Objectives: Target compounds were designed to investigate the effect of the p-OCH3 motifs on ligand/PI3Kα complex interaction and antiproliferative activity. Methods: Synthesis of the proposed compounds, biological examination tests against human colon adenocarcinoma (HCT-116), breast adenocarcinoma (MCF-7), and breast carcinoma (T47D) cell lines, along with Glide docking studies. Results: A series of 1,2-bis(4-methoxyphenyl)-2-oxoethyl benzoates was synthesized and characterized by means of FT-IR, 1H and 13C NMR, and by elemental analysis. Biological investigation demonstrated that the newly synthesized compounds exhibit antiproliferative activity in human colon adenocarcinoma (HCT-116), breast adenocarcinoma (MCF-7), and breast carcinoma (T47D) cell lines possibly via inhibition of PI3Kα and estrogen receptor alpha (ERα). Additionally, results revealed that these compounds exert selective inhibitory activity, induce apoptosis, and suppress VEGF production. Compound 3c exhibited promising antiproliferative activity in HCT-116 interrogating that hydrogen bond-acceptor mediates ligand/PI3Kα complex formation on m- position. Compounds 3e and 3i displayed high inhibitory activity in MCF-7 and T47D implying a wide cleft discloses the o-attachment. Furthermore, compound 3g exerted selective inhibitory activity against T47D. Glide docking studies against PI3Kα and ERα demonstrated that the series accommodate binding to PI3Kα and/or ERα. Conclusion: The series exhibited a potential antitumor activity in human carcinoma cell lines encoding PI3Kα and/or ERα.

CYTOTOXIC ACTIVITY OF LUVUNGA SCANDENS AGAINST HUMAN CANCER CELL LINES

2016 ◽  
Vol 78 (10) ◽  
Author(s):  
Putri Nur Hidayah Al-Zikri ◽  
Muhammad Taher ◽  
Deny Susanti ◽  
Solachuddin Jauhari Arief Ichwan
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
A549 Cell ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Breast Adenocarcinoma ◽  
Human Cancer Cell Lines ◽  
Mcf 7

Luvunga scandens belongs to the family of Rutaceae which usually inhabit tropical and moist environment. This plant is known as ‘Mengkurat Jakun’ among locals and used traditionally to treat fever and fatigue via decoction. The aim of this study was to investigate the cytotoxic activity of the leaves and stems extracts of L. scandens extract. Extracts of the leaves and stems were obtained from sequential extraction procedures by various organic solvents. All extracts were subjected to cytotoxic study by 3-(4, 5-dimethylthaizol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. In in vitro cytotoxicity assay, all L. scandens extracts exhibited cytotoxicity against human breast adenocarcinoma (MCF-7) and human lung adenocarcinoma (A549) cell lines. The IC50 values of dichloromethane and methanol extracts from the leaves of L. scandens against MCF-7 cell line were 62.5 µg/mL and 88.0 µg/mL, respectively, whereas IC50 of methanol extract from stem was 81.0 µg/mL. All extracts were less active against A549 cell line where IC50 value were not be determined. The present findings revealed the potential of L. scandens as a cytotoxic agent against MCF-7 cell line. However, further studies should be planned to evaluate role of the plant in cytotoxic activity.

scholarly journals Polyisoprenylated Acylphloroglucinols from Garcinia nervosa

2018 ◽  
Vol 13 (3) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Alfarius Eko Nugroho ◽  
Hitomi Nakamura ◽  
Daisuke Inoue ◽  
Yusuke Hirasawa ◽  
Chin Piow Wong ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Cytotoxic Activity ◽  
Spectroscopic Data ◽  
Human Lung ◽  
Carcinoma Cells ◽  
Breast Adenocarcinoma ◽  
Human Breast ◽  
Human Breast Adenocarcinoma ◽  
Human Hepatocellular Carcinoma Cells ◽  
Mcf 7

Two new polyisoprenylated acylphloroglucinols, 7- epi-isoxanthochymol and 7- epi-cycloxanthochymol (1 – 2), were isolated from the barks of Garcinia nervosa together with their 7-epimers isoxanthochymol (3) and cycloxanthochymol (4). Their structures were determined on the basis of NMR spectroscopic data. The cytotoxic activity of the isolated compounds against HL-60, MCF-7 (human breast adenocarcinoma), A549 (human lung adenocarcinoma) and HepG2 (human hepatocellular carcinoma) cells were evaluated, and all compounds showed cytotoxic activity against all cell lines.

scholarly journals One-Pot Multicomponent Synthesis and Cytotoxic Evaluation of Novel 7-Substituted-5-(1H-Indol-3-yl)Tetrazolo[1,5-a] Pyrimidine-6-Carbonitrile

Molecules ◽  
2020 ◽  
Vol 25 (2) ◽  
pp. 255
Author(s):  
Mohamed A. A. Radwan ◽  
Fahad M. Alminderej ◽  
Hanem M. Awad
Keyword(s):  
Human Cancer ◽  
Human Colon ◽  
Human Lung Cancer ◽  
Multicomponent Synthesis ◽  
Anticancer Activities ◽  
Human Colon Cancer ◽  
One Pot ◽  
Human Cancer Cell Lines ◽  
Hct 116 ◽  
Mcf 7

A series of novel 7-substituted-5-(1H-indol-3-yl)tetrazolo[1,5-a]pyrimidine-6-carbonitrile was synthesized via a one-pot, three-multicomponent reaction of appropriate aldehydes, 1H-tetrazole-5-amine and 3-cyanoacetyl indole in catalytic triethylamine. The cytotoxic activity of the new synthesized tetrazolopyrimidine-6-carbonitrile compounds was investigated against HCT-116, MCF-7, MDA-MB-231, A549 human cancer cell lines and one human healthy normal cell line (RPE-1) using the MTT cytotoxicity assay. Compounds 4h, 4b, 4c, 4i and 4a showed potent anticancer activities against human colon cancer. Additionally, all the compounds showed potent anticancer activities on human lung cancer.

scholarly journals Synthesis and Cytotoxic Activity of New 1,3,4-Thiadiazole Thioglycosides and 1,2,3-Triazolyl-1,3,4-Thiadiazole N-glycosides

Molecules ◽  
2019 ◽  
Vol 24 (20) ◽  
pp. 3738 ◽  
Author(s):  
Alminderej ◽  
Elganzory ◽  
El-Bayaa ◽  
Awad ◽  
El-Sayed
Keyword(s):  
Cell Lines ◽  
Human Cancer ◽  
Breast Adenocarcinoma ◽  
Cytotoxic Activities ◽  
Acetylenic Derivative ◽  
Thiol Compounds ◽  
Reference Drug ◽  
Human Cancer Cells ◽  
Hct 116 ◽  
Mcf 7

New 1,3,4-thiadiazole thioglycosides linked to substituted arylidine systems were synthesized via glycosylation of the prepared 1,3,4-thiadiazole thiol compounds. Click strategy was also used for the synthesis of new 1,3,4-thiadiazole and 1,2,3-triazole hybrid glycosides by reaction of the acetylenic derivatives with different glycosyl azids followed by deacetylation process. The cytotoxic activities of the prepared compounds were studied against HCT-116 (human colorectal carcinoma) and MCF-7 (human breast adenocarcinoma) cell lines using the MTT assay. The results showed that the key thiadiazolethione compounds 2 and 3, the triazole glycosides linked to p-methoxyarylidine derivatives 14 and 15 in addition to the free hydroxyl glycoside 20 were found potent in activity comparable to the reference drug doxorubicin against MCF-7 human cancer cells. The acetylenic derivative 2 and glycoside 20 were also found highly active against HCT-116 cell lines.

Cytotoxic Activity and Apoptosis Induction by Gaillardin

2013 ◽  
Vol 68 (3-4) ◽  
pp. 108-112 ◽  
Author(s):  
Maryam Hamzeloo Moghadam ◽  
Farzaneh Naghibi ◽  
Azadeh Atoofi ◽  
Mitra Asgharian Rezaie ◽  
Mahboobeh Irani ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Carcinoma Cell ◽  
Carcinoma Cell Line ◽  
Terminal Deoxynucleotidyl Transferase ◽  
Breast Adenocarcinoma ◽  
Adenocarcinoma Cell Line ◽  
Cell Lung Carcinoma ◽  
Adenocarcinoma Cell ◽  
Mcf 7

Cytotoxic activity of gaillardin, a sesquiterpene lactone isolated from Inula oculus-christi L. (Asteraceae), was assessed in the human breast adenocarcinoma cell line MCF-7, human hepatocellular carcinoma cell line HepG-2, human non-small cell lung carcinoma cell line A-549, and human colon adenocarcinoma cell line HT-29, resulting in IC50 values of 6.37, 6.20, 4.76, and 1.81 μg/mL, respectively, in the microculture tetrazolium-formazan MTT assay. In vitro apoptosis-inducing properties of gaillardin were also evaluated in MCF-7 cells with the terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate nickend labeling (TUNEL) assay. The results suggest gaillardin as a candidate for further studies in cancer therapy

scholarly journals Antibacterial and Cytotoxic Potential of Two Steroids from the Indonesian Soft Coral Sinularia polydactila

2021 ◽  
Vol In Press (In Press) ◽  
Author(s):  
Masteria Yunovilsa Putra ◽  
Firmansyah Karim ◽  
Aji Nugroho
Keyword(s):  
Cytotoxic Activity ◽  
Brine Shrimp ◽  
Soft Coral ◽  
Human Colon ◽  
2D Nmr ◽  
Moderate Activity ◽  
Human Colon Cancer ◽  
Brine Shrimp Lethality ◽  
Brine Shrimp Lethality Assay ◽  
Hct 116

Background: Soft corals of the genus Sinularia are well recognized as a rich source of steroidal compounds. These constituents, mainly steroids, have been reported as possessing antitumor, antimicrobial, and antiviral activities. Objectives: This study was designed to isolate and elucidate antibacterial and cytotoxic compounds from the soft coral Sinularia polydactila. Methods: Structure elucidation of steroids was determined based on spectroscopic data through 1D and 2D NMR analyses and mass spectrometry, with the results compared to data in the literature. Antibacterial activity was determined using four human bacterial pathogens, namely B. subtilis (ATCC 6633), P. aeruginosa (ATCC 27853), S. aureus (ATCC 25923), and E. coli (ATCC 25922). Cytotoxic activity was evaluated using the human colon cancer cell HCT 116 and brine shrimp lethality assay (BSLA). Results: Two steroids (Compounds 1 - 2) were isolated from the Indonesian soft coral Sinularia polydactila. (22R,23R,24R)-22,23-methylene-24-methylcholest-6-en-5α,8α-epidioxy-3β-ol (1) and 5α,8α-Epidioxy-24(R)-methylcholesta-6,22-dien-3α-ol (2) showed moderate activity against colon carcinoma cancer HCT 116 at the concentrations of 24.8 and 27.3 μg/mL, respectively. Furthermore, compounds 1 and 2 showed cytotoxic activity using the brine shrimp lethality assay with the concentrations of 57.1 and 121.3 3 μg/mL, respectively. Compound 2 showed moderate activity against S. aureus and B. subtilis at the 250 μg/mL concentration. Conclusions: Two steroids isolated from soft coral Sinularia polydactila were found to possess moderate cytotoxic and antibacterial activities.

Sign in / Sign up

Export Citation Format

Share Document