scholarly journals Development of HPLC Method for Quantification of Sinigrin from Raphanus sativus Roots and Evaluation of Its Anticancer Potential

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 4947
Author(s):  
Anroop B. Nair ◽  
Dipal Gandhi ◽  
Snehal S. Patel ◽  
Mohamed A. Morsy ◽  
Bapi Gorain ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cell Lines ◽  
Mtt Assay ◽  
Raphanus Sativus ◽  
Caspase 3 ◽  
Human Cancer ◽  
Biological Activities ◽  
Hplc Method ◽  
Human Cancer Cell Lines ◽  
Rp Hplc

Sinigrin, a precursor of allyl isothiocyanate, present in the Raphanus sativus exhibits diverse biological activities, and has an immense role against cancer proliferation. Therefore, the objective of this study was to quantify the sinigrin in the R. sativus roots using developed and validated RP-HPLC method and further evaluated its’ anticancer activity. To achieve the objective, the roots of R. sativus were lyophilized to obtain a stable powder, which were extracted and passed through an ion-exchange column to obtain sinigrin-rich fraction. The RP-HPLC method using C18 analytical column was used for chromatographic separation and quantification of sinigrin in the prepared fraction, which was attained using the mobile phase consisting of 20 mM tetrabutylammonium: acetonitrile (80:20%, v/v at pH 7.0) at a flow rate of 0.5 mL/min. The chromatographic peak for sinigrin was showed at 3.592 min for pure sinigrin, where a good linearity was achieved within the concentration range of 50 to 800 µg/mL (R2 > 0.99), with an excellent accuracy (−1.37% and −1.29%) and precision (1.43% and 0.94%), for intra and inter-day, respectively. Finally, the MTT assay was performed for the sinigrin-rich fraction using three different human cancer cell lines, viz. prostate cancer (DU-145), colon adenocarcinoma (HCT-15), and melanoma (A-375). The cell-based assays were extended to conduct apoptotic and caspase-3 activities, to determine the mechanism of action of sinigrin in the treatment of cancer. MTT assay showed IC50 values of 15.88, 21.42, and 24.58 µg/mL for DU-145, HCT-15, and A-375 cell lines, respectively. Increased cellular apoptosis and caspase-3 expression were observed with sinigrin-rich fraction, indicating significant increase in overexpression of caspase-3 in DU-145 cells. In conclusion, a simple, sensitive, fast, and accurate RP-HPLC method was developed for the estimation of sinigrin in the prepared fraction. The data observed here indicate that sinigrin can be beneficial in treating prostate cancer possibly by inducing apoptosis.

scholarly journals A New Cycloartane Glucoside from Rhizophora stylosa

2014 ◽  
Vol 9 (9) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Phan Thi Thanh Huong ◽  
Chau Ngoc Diep ◽  
Nguyen Van Thanh ◽  
Vu Anh Tu ◽  
Tran Hong Hanh ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Lung Adenocarcinoma ◽  
Cell Lines ◽  
Caspase 3 ◽  
Methanol Extract ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Rhizophora Stylosa ◽  
Human Cancer Cell Lines ◽  
C Nmr

Nine secondary metabolites, including a new cycloartane glucoside, rhizostyloside (1), were isolated from a methanol extract of Rhizophora stylosa leaves through several chromatographic experiments. The structures of the compounds were determined on the basis of NMR spectroscopic (1H and 13C NMR, HSQC, HMBC, 1H-1H COSY, NOESY) and HR-ESI-MS data and by comparison with literature values. Compound 1 exhibited significant cytotoxicity against three human cancer cell lines: KB (epidermoid carcinoma), LU-1 (lung adenocarcinoma), and SK-Mel-2 (melanoma). In addition, 1 strongly activated caspase-3/7 in LU-1 cells.

scholarly journals Cytotoxic Constituents from the Rhizomes ofCurcuma zedoaria

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Omer Abdalla Ahmed Hamdi ◽  
Syarifah Nur Syed Abdul Rahman ◽  
Khalijah Awang ◽  
Norhanom Abdul Wahab ◽  
Chung Yeng Looi ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Mtt Assay ◽  
Apoptotic Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Chemical Components ◽  
Curcuma Zedoaria ◽  
Human Cancer Cell Lines ◽  
Mcf 7

Curcuma zedoariaalso known asTemu putihis traditionally used in food preparations and treatment of various ailments including cancer. The cytotoxic activity of hexane, dichloromethane, ethyl acetate, methanol, and the methanol-soxhlet extracts ofCurcuma zedoariarhizomes was tested on two human cancer cell lines (Ca Ski and MCF-7) and a noncancer cell line (HUVEC) using MTT assay. Investigation on the chemical components in the hexane and dichloromethane fractions gave 19 compounds, namely, labda-8(17),12 diene-15,16 dial (1), dehydrocurdione (2), curcumenone (3), comosone II (4), curcumenol (5), procurcumenol (6), germacrone (7), zerumbone epoxide (8), zederone (9), 9-isopropylidene-2,6-dimethyl-11-oxatricyclo[6.2.1.01,5]undec-6-en-8-ol (10), furanodiene (11), germacrone-4,5-epoxide (12), calcaratarin A (13), isoprocurcumenol (14), germacrone-1,10-epoxide (15), zerumin A (16), curcumanolide A (17), curcuzedoalide (18), and gweicurculactone (19). Compounds (1–19) were evaluated for their antiproliferative effect using MTT assay against four cancer cell lines (Ca Ski, MCF-7, PC-3, and HT-29). Curcumenone (3) and curcumenol (5) displayed strong antiproliferative activity (IC50=8.3±1.0and9.3±0.3 μg/mL, resp.) and were found to induce apoptotic cell death on MCF-7 cells using phase contrast and Hoechst 33342/PI double-staining assay. Thus, the present study provides basis for the ethnomedical application ofCurcuma zedoariain the treatment of breast cancer.

scholarly journals Terpenoids from Glechoma hederacea var. longituba and Their Biological Activities

2022 ◽  
Author(s):  
Dong Hyun Kim ◽  
Zahra Khan ◽  
Sun Yeou Kim ◽  
Sang Un Choi ◽  
Chung Sub Kim ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Human Cancer ◽  
Biological Activities ◽  
2D Nmr ◽  
C6 Glioma Cells ◽  
No Production ◽  
M Cell ◽  
Human Cancer Cell Lines ◽  
Glechoma Hederacea

Glechoma hederacea var. longituba (common name: ground-ivy) has been used for the treatment of asthma, bronchitis, cholelithiasis, colds, and inflammation. In the present study, three new sesquiterpene glycosides (1–3), two new diterpene glycosides (4–5), and four known compounds (6–9) were isolated from its MeOH extract. Structure elucidation was performed for the five new compounds (1–5) using 1D and 2D NMR, HRESIMS, ECD calculation, and chemical methods. All the isolates (1–9) were assessed for their anti-neuroinflammatory activity on nitric oxide (NO) production in lipopolysaccharide (LPS)-activated BV-2 cells, nerve growth factor (NGF) secretion stimulation activity in C6 glioma cells, and cytotoxic activity against four human cancer cell lines (A549, SK-OV-3, SK-MEL-2, and HCT15). Compounds 2 and 5–7 exhibited inhibitory effects on NO production with IC50 values of 52.21, 47.90, 61.61, and 25.35 μM, respectively. Compound 5 also exhibited a significant stimulating effect on NGF secretion (122.77 ± 8.10%). Compound 9 showed potent cytotoxic activity against SK-OV-3 (IC50 3.76 μM) and SK-MEL-2 (IC50 1.48 μM) cell lines, while 7 displayed a strong cytotoxic activity against SK-MEL-2 (IC50 9.81 μM) cell line

Recent development of tetrahydro-quinoline/isoquinoline based compounds as anticancer agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Pratik Yadav ◽  
Ashish Kumar ◽  
Ismail Althagafi ◽  
Vishal Nemaysh ◽  
Reeta Rai ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Biological Activities ◽  
Cancer Cell Lines ◽  
New Drugs ◽  
Anticancer Activities ◽  
Human Cancer Cell Lines ◽  
Anticancer Properties

: Tetrahydroquinoline and isoquinoline scaffolds are important class heterocyclic compounds, which is implied for the development of new drugs and diagnostic for therapeutic function. Naturally occurring as well as synthetic tetrahydroquinolines/isoquinolines possess many different biological activities and have been testified as remarkable cytotoxic and potency in human cancer cell lines. Tetrahydroquinoline/isoquinolines based compounds displayed a key role in the development of anticancer drugs or lead molecules and acting through various mechanisms such as cell proliferation, apoptosis, DNA fragmentation, inhibition of tubulin polymerization, induced cell cycle arrest, interruption of cell migration, and modulation. The number of tetrahydroquinoline/isoquinoline derivatives has been reported as potent anticancer agents. Due to promising anticancer activities and wide-ranging properties of these molecules, we have compiled the literature for the synthesis and anticancer properties of various tetrahydroquinolines and isoquinolines. We have reported the synthesis of potent tetrahydroquinoline/isoquinoline molecules of the last 10 years with their anticancer properties in various cancer cell lines and stated their half-maximal inhibitory concentration (IC50). In addition, we also considered the discussion of molecular docking and structural activity relationship wherever provided to understand the possible mode of activity a target involved and structural feature responsible for the better activity, so the reader can directly find the detail for designing new anticancer agents.

scholarly journals In vitro and In silico Evaluation of Structurally Diverse Benzyl-pyrrolidine-3-ol Analogues as Apoptotic Agents via Caspase Activation

2021 ◽  
Vol 68 (3) ◽  
pp. 667-682
Author(s):  
Tahira Naqvi ◽  
Asif Amin ◽  
Shujat Ali ◽  
Mohsin Y. Lone ◽  
Nadeem Bashir ◽  
...  
Keyword(s):  
Cell Lines ◽  
In Silico ◽  
Caspase 3 ◽  
Human Cancer ◽  
Md Simulations ◽  
Human Cancer Cell Lines ◽  
Lead Compounds ◽  
Model Protein ◽  
The Stability

The activation of caspases is central to apoptotic process in living systems. Defects in apoptosis have been implicated with carcinogenesis. Need to develop smart agents capable of inducing apoptosis in tumor cells is obvious. With this motive, diversity oriented synthesis of 1-benzylpyrrolidin-3-ol analogues was envisaged. The multi component Ugi reaction synthesized library of electronically diverse analogues was explored for cytotoxic propensity towards a panel of human cancer cell lines at 10 μM. The lead compounds exhibit a selective cytotoxicity towards HL-60 cells as compared to cell lines derived from solid tumors. Besides, their milder cytotoxic effect on non-cancerous cell lines reaffirm their selective action towards cancer cells only.The lead molecules were tested for their ability to target caspase-3, as a vital protease triggering apoptosis. The lead compounds were observed to induce apoptosis in HL-60 cells around 10 μM concentration. The lead compounds exhibited various non-covalent supra type interactions with caspase-3 key residues around the active site. The binding ability of lead compounds with caspase-3 was studied via molecular docking and molecular dynamic (MD) simulations. MD simulations indicated the stability of compound-caspase-3 complex throughout the 50 ns simulation run. The stability and bio-availability of the lead compounds under physiological conditions was assessed by their interaction with Bovine Serum Albumin (BSA) as model protein. BSA interactions of lead compounds were studied by various bio-physical methods and further substantiated with in silico MD simulations.

scholarly journals Triterpenic Acid Content and Cytotoxicity of Some Salvia Species From Iran

2019 ◽  
Vol 14 (5) ◽  
pp. 1934578X1984272 ◽  
Author(s):  
Hoda Abdollahi-Ghehi ◽  
Ali Sonboli ◽  
Samad Nejad Ebrahimi ◽  
Mohammad Ali Esmaeili ◽  
Mohammad Hossein Mirjalili
Keyword(s):  
Cell Lines ◽  
High Performance ◽  
Human Cancer ◽  
Biological Activities ◽  
Dry Weight ◽  
Leaf Length ◽  
Array Detector ◽  
Human Cancer Cell Lines ◽  
Wide Range ◽  
Commercial Species

For prosperous domestication, breeding, and cultivation of a herbal species, it is important to screen its medicinally valuable compounds as well as its referred biological activity. Salvia L. species (Lamiaceae), distributed throughout the world, contain a wide range of secondary metabolites including terpenoids and phenolic derivatives. Betulinic acid (BA), oleanolic acid (OA), and ursolic acid (UA) are highly valuable triterpenic acids (TAs) because of their wide range of biological activities. The objective of the present work was to evaluate the BA, OA, and UA contents among 22 Salvia species native to Iran. TA content in the studied Salvia species was compared with that in Salvia officinalis as a commercial species. High-performance liquid chromatography with photodiode array detector results showed that the maximum content of BA (3.12 ± 0.03 mg/g dry weight [DW]) and OA (1.96 ± 0.05 mg/g DW) was determined in Salvia multicaulis. The highest content of UA (4.34 ± 0.1 mg/g DW) was quantified in S. officinalis L. followed by S. multicaulis (3.71 ± 0.08 mg/g DW). Salvia multicaulis exhibited significantly higher agro-morphological values than S. officinalis in traits related to plant width, leaf length, internode length, and inflorescence length. The cytotoxicities of both species were determined against human cancer cell lines using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. The methanolic extract of S. multicaulis and S. officinalis showed cytotoxic effects against SH-SY5Y and MCF-7 cell lines, respectively. Both species were equally cytotoxic against the HL-60 cell line. This study provides scope for the selection of high-yielding species and genetic improvement through breeding and biotechnological programs in the future.

A saccharinate-bridged palladacyclic dimer with a Pd–Pd bond: experimental and molecular docking studies of the interaction with DNA and BSA and in vitro cytotoxicity against human cancer cell lines

2018 ◽  
Vol 42 (1) ◽  
pp. 574-586 ◽  
Author(s):  
Kazem Karami ◽  
Moloud Alinaghi ◽  
Zahra Amirghofran ◽  
Janusz Lipkowski ◽  
Amir Abbas Momtazi-borojeni
Keyword(s):  
Molecular Docking ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Activities ◽  
Docking Studies ◽  
In Vitro Cytotoxicity ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

The synthesis, characterization and biological activities of a saccharinate-bridged palladacyclic dimer are reported in this work.

scholarly journals SYNTHESIS OF TAMOXIFEN DERIVATIVES AND THEIR BIOLOGICAL ACTIVITIES

2020 ◽  
Vol 21 (supplement 1) ◽  
Author(s):  
Nitin Tandon ◽  
Nitin Tandon ◽  
Runjhun Tandon
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Gold Standard ◽  
Human Cancer ◽  
Biological Activities ◽  
Biological Properties ◽  
Synthetic Methods ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

Tamoxifen has remained the gold standard for the treatment of the breast cancer and extensive research is going on for the synthesis of the various novel tamoxifen analogs for their evaluation as anticancer agents against various human cancer cell lines. The main aim of this review is to summarize the various synthetic methods for the preparation of the tamoxifen analogs and their biological properties.

scholarly journals The Novel Benzothiazole Derivative PB11 Induces Apoptosis via the PI3K/AKT Signaling Pathway in Human Cancer Cell Lines

2021 ◽  
Vol 22 (5) ◽  
pp. 2718
Author(s):  
Jinsun Kim ◽  
Sung Hee Hong ◽  
So Hyun Jeon ◽  
Min Ho Park ◽  
Cha-Gyun Shin
Keyword(s):  
Cancer Cells ◽  
Cell Lines ◽  
Caspase 3 ◽  
Human Cancer ◽  
Akt Signaling ◽  
Nuclear Condensation ◽  
Continuous Administration ◽  
Human Cancer Cell Lines ◽  
Benzothiazole Derivative ◽  
Anti Cancer

Among several anti-cancer therapies, chemotherapy can be used regardless of the stage of the disease. However, development of anti-cancer agents from potential chemicals must be executed very cautiously because of several problems, such as safety, drug resistance, and continuous administration. Most chemotherapeutics selectively cause cancer cells to undergo apoptosis. In this study, we tested the effects of a novel chemical, the benzothiazole derivative N-[2-[(3,5-dimethyl-1,2-oxazol-4-yl)methylsulfanyl]-1,3-benzothiazol-6-yl]-4-oxocyclohexane-1-carboxamide (PB11) on the human cell lines U87 (glioblastoma), and HeLa (cervix cancer). It was observed that this chemical was highly cytotoxic for these cells (IC50s < 50 nM). In addition, even 40 nM PB11 induced the classical apoptotic symptoms of DNA fragmentation and nuclear condensation. The increase of caspase-3 and -9 activities also indicated an increased rate of apoptosis, which was further confirmed via Western blotting analysis of apoptosis-associated proteins. Accordingly, PB11 treatment up-regulated the cellular levels of caspase-3 and cytochrome-c, whereas it down-regulated PI3K and AKT. These results suggest that PB11 induces cytotoxicity and apoptosis in cancer cells by suppressing the PI3K/AKT signaling pathways and, thus, may serve as an anti-cancer therapeutic.

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