scholarly journals Polyacetylenes from the Roots of Swietenia macrophylla King

Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1291 ◽  
Author(s):  
Cheng-Neng Mi ◽  
Hao Wang ◽  
Hui-Qin Chen ◽  
Cai-Hong Cai ◽  
Shao-Peng Li ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Carcinoma Cell ◽  
Leukemia Cell ◽  
Cancer Cell Lines ◽  
Carcinoma Cell Line ◽  
Leukemia Cell Line ◽  
Swietenia Macrophylla ◽  
Ic50 Values

A phytochemical investigation of the roots of Swietenia macrophylla led to the isolation of seven polyacetylenes, including five new compounds (15) and two known ones (67). Their structures were elucidated by extensive spectroscopic analysis and detailed comparison with reported data. All the isolates were tested for their cytotoxicity against the human hepatocellular carcinoma cell line BEL-7402, human myeloid leukemia cell line K562, and human gastric carcinoma cell line SGC-7901. Compounds 1 and 6 showed moderate cytotoxicity against the above three human cancer cell lines with IC50 values ranging from 14.3 to 45.4 μM. Compound 4 displayed cytotoxicity against the K562 and SGC-7901 cancer cell lines with IC50 values of 26.2 ± 0.4 and 21.9 ± 0.3 μM, respectively.

scholarly journals HERBAL NANOSUSPENSION: IN VITRO CANCER STUDY AGAINST DIFFERENT CELL LINES

2020 ◽  
pp. 25-29
Author(s):  
MITHRA MM ◽  
KRISHNAKUMAR K ◽  
SMITHA K NAIR
Keyword(s):  
Epithelial Cell ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Carcinoma Cell ◽  
Carcinoma Cell Line ◽  
Myelogenous Leukemia ◽  
Leukemia Cell Line ◽  
Epithelial Cell Line

Herbal formulations marketed in India for many years providing its therapeutic benefits in health problems. Medicinal plants or their phytoconstituents are less toxic and free from side effects than synthetic drugs. However, formulation aspects of these phytoconstituents are limited due to its low solubility. Nanotechnology is a promising technique to increase the solubility of herbal drugs. This will lead to a subsequent reduction in drug dose. Nanoformulations such as nanosuspension increase the solubility of poorly soluble drugs and also have good targeting effects on different cells. The efficacy of herbal nanosuspensions evaluated using different cell lines. Here, hepatocellular carcinoma cell line (SMMC-7721), human prostate cancer cell line, human myelogenous leukemia cell line, human epithelial cell line, human breast cancer cell lines (4T1, MCF-7, and MDA-MB-453), carcinomic human alveolar basal epithelial cell line (A549), human umbilical vein endothelial cell line, human colorectal adenocarcinoma cell line (HT-29), and human epithelial carcinoma cell line (HeLa) are used in the evaluation procedures. In vitro assays help in the determination of the dose range of drugs for the activity. The present review highlights the in vitro cancer studies of herbal nanosuspensions using different cell lines.

scholarly journals Evaluation of Anticancer Action of Martynia annua Linn Root Extract on Different Human Cancer Cell Lines

2021 ◽  
pp. 96-109
Author(s):  
Rahul Kumar Gupta ◽  
Renu Bharat Rathi
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Leukemia Cell ◽  
Cancer Cell Line ◽  
Ethanolic Extract ◽  
Cancer Cell Lines ◽  
Leukemia Cell Line ◽  
Human Leukemia ◽  
Human Leukemia Cell Line

Background: In the last few decades, plants have been playing a vital role in treating cancer and infectious diseases. Natural products have been rediscovered as effective methods of drug production amid advances in combinatorial chemistry. Roots of Martynia annua are being used as a folklore remedy for the treatment of cancer and rheumatism successfully. Aims of the Study: In the present study, ethanolic, aqueous and hydro-ethanolic root extracts of Martynia annua were screened for in vitro cytotoxicity activity using different cell lines. Settings and Design: In the experiment, lung cancer cell lines (A549), leukemia cancer cell lines (K562), oral cancer cell lines (SCC-40), breast cancer cell lines (MCF-7) & cervix cancer cell lines (SiHa) were studied on the extracts. Materials and Methods: The method used was Sulforhodamine B (SRB) assay technique in which growth inhibition of 50% (GI50) was analyzed by comparing it with standard drug Adriamycin (ADR) (doxorubicin). Results: Aqueous & ethanolic extract of Martynia annua root had shown high anticancer activity with GI50 value 11.3µg/ml and 20.4µg/ml respectively on human leukemia cell line K-562 but for human breast cancer cell line MCF-7, human lung cancer cell line A-549, human squamous cell carcinoma SCC-40 and human cervical cancer cell line SiHa the extracts showed activity in more than 80µg/ml. Conclusion: The anticancer activity of aqueous extract of Martynia annua root was found superior than the ethanolic extract in Human Leukemia Cell Line K-562. The study indicates that the Martynia annua root extracts are most effective against the fast proliferative cells (Leukemic cells) and possibly a cell cycle arrest (needed to be proved as future perspective) is the mode of action of the extract. To study its effect on targeted cancers, specific in vivo scientific studies and clinical trials should be carried out by further researchers.

Antioxidant effects and in vitro cytotoxicity on human cancer cell lines of flavonoid-rich Flamboyant (Delonix regia (Bojer) Raf.) flower extract

2020 ◽  
Vol 21 ◽  
Author(s):  
Putthiporn Khongkaew ◽  
Phanphen Wattanaarsakit ◽  
Konstantinos I. Papadopoulos ◽  
Watcharaphong Chaemsawang
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Leukemia Cell ◽  
Leukemia Cell Line ◽  
Flower Extract ◽  
Dependent Inhibition ◽  
Dose Dependent Inhibition ◽  
Murine Leukemia Cell ◽  
Dose Dependent

Background: Cancer is a noncommunicable disease with increasing incidence and mortality rates both worldwide and in Thailand. Its apparent lack of effective treatments is posing challenging public health issues. Introduction: Encouraging research results indicating probable anti-cancer properties of the Delonix regia flower extract (DRE) have prompted us to evaluate the feasibility of developing a type of product for future cancer prevention or treatment. Methods and Results: In the present report, using High Performance Liquid Chromatography (HPLC), we demonstrate in the DRE, the presence of high concentrations of three identifiable flavonoids, namely rutin 4.15±0.30 % w/w, isoquercitrin 3.04±0.02 %w/w, and myricetin 2.61±0.01 % w/w respectively while the IC50 of DPPH and ABTS assay antioxidation activity was 66.88±6.30 µg/ml and 53.65±7.24 µg/ml respectively. Discussion: Our cancer cell line studies using the MTT assay demonstrated DREs potent and dose dependent inhibition of murine leukemia cell line (P-388: 35.28±4.07% of cell viability remaining), as well as of human breast adenocarcinoma (MCF-7), human cervical carcinoma (HeLa), human oral cavity carcinoma (KB), and human colon carcinoma (HT-29) cell lines in that order of magnitude. Conclusion: Three identifiable flavonoids (rutin, isoquercitrin and myricetin) with high antioxidation activity and potent and dose dependent inhibition of murine leukemia cell line and five other cancer cell lines were documented in the DRE. The extract’s lack of cytotoxicity in 3 normal cell lines is a rare advantage not usually seen in current antineoplastic agents. Yet another challenge of the DRE was its low dissolution rate and long-term storage stability, issues to be resolved before a future product can be formulated.

scholarly journals A clear cancer cell line (150057) derived from human endometrial carcinoma harbors two novel mutations

BMC Cancer ◽  
2020 ◽  
Vol 20 (1) ◽  
Author(s):  
Yu-Hsun Chang ◽  
Dah-Ching Ding
Keyword(s):  
Endometrial Cancer ◽  
Cell Carcinoma ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Clear Cell ◽  
Carcinoma Cell ◽  
Clear Cell Carcinoma ◽  
Carcinoma Cell Line ◽  
Novel Mutations

Abstract Background Cell lines are extremely useful for both basic and clinical research. Thus, establishing endometrial cancer cell lines with malignant histology is important. This study aimed to extensively characterize an endometrial clear cell carcinoma cell line. Methods This cell line, named 150,057, was derived from the endometrial clear cell cancer of a 63-year-old woman. The morphology, chromosomes, chemosensitivity, tumor markers, xenotransplantation characteristics, and cancer-related genes of the cell line were characterized. Results This cell line exhibited adequate growth, being passaged more than 70 times. The morphology of the cells was polygonal with a cobblestone-like appearance. Karyotyping of the cell line revealed a hypodiploid chromosomal number. 150057 cells expressed CA19–9 and CA125. The cell line was sensitive to doxorubicin, paclitaxel, carboplatin, and cisplatin. After the cells were transplanted into the subcutaneous region of non-obese diabetic-severe combined immunodeficiency mice, they generated xenograft tumors with similar histology as the original tumor. A total of 59 somatic nucleotide mutations were identified in 25 of the 53 examined tumor suppressor genes and oncogenes. Two novel mutations were found in FGFR3 and ARID1A. Conclusion We established and characterized an endometrial clear cell carcinoma cell line that may be useful in carcinogenesis and treatment research for endometrial cancer.

Activity of mTOR-Inhibitor Rad001 (everolimus) in differentiated and anaplastic thyroid cancer cell lines

2009 ◽  
Vol 27 (15_suppl) ◽  
pp. e14608-e14608
Author(s):  
T. Behlendorf ◽  
W. Voigt ◽  
T. Mueller ◽  
K. Jordan ◽  
D. Arnold ◽  
...  
Keyword(s):  
Thyroid Cancer ◽  
Drug Interaction ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Mtor Inhibitor ◽  
Cancer Cell Lines ◽  
Thyroid Cancer Cell ◽  
Ic50 Values ◽  
Thyroid Cancer Cell Lines

e14608 Background: Recent data suggest that aberrant activation of PIK3/AKT-pathway and mTOR are involved in the development of thyroid cancer, particularly of anaplastic (ATC) and follicular (FTC) subtype. Therefore, mTOR could be a potential treatment target in thyroid cancer. Methods: To asses the potential role of mTOR as target for the treatment of thyroid cancer, two human ATC cell lines SW1736 and 8505C, the papillary thyroid cancer (PTC) cell line BCPAP and the FTC cell line FTC133 were exposed for 96h to increasing concentrations of the mTOR inhibitor RAD001 (Everolimus, kindly provided by Novartis, Switzerland). For combination experiments 10 nM of RAD001 were combined with increasing concentrations of either doxorubicin (DOX) or cisplatin (CDDP) continuously. Cytotoxicity was measured using the sulforhodamine B assay. IC50-values were calculated with Sigma Plot (Jandel Scientific) and drug interaction was determined by the model of Drewinko. Results: The observed IC50-values of RAD001 were 1nM (FTC133), 10 nM (BCPAP), 1000 nM (SW1736) and 9400 nM (8505C). In contrast to the pronounced differences in sensitivity as assessed on the basis of IC50, a growth inhibitory effect ≥ 25 % was seen in all cell lines at a concentration of 1 nM of RAD001. IC50 for CDDP ranged from 1,3–4,8 μM and for DOX from 8–40 nM. Combination of 10 nM RAD001 with either DOX or CDDP resulted in additive drug interaction with the exception in cell line 8505C where significant synergy was found for the combination with CDDP. Conclusion: RAD001 exerted interesting preclinical activity in two differentiated thyroid cancer cell lines. Mainly additive drug interaction in thyroid cancer cell lines was observed for combinations with CDDP and DOX. Mechanistic investigations are underway and will be presented at the meeting. At least for differentiated thyroid cancer mTOR-inhibition appeared promising, further evaluation in thyroid cancer seems warranted. No significant financial relationships to disclose.

Targeting of Heat Shock Protein 32 (Hsp32) in Neoplastic Cells by Styrene Maleic Acid Zinc Protoporphyrin (SMA-ZnPP) Is Associated with Reduced Growth and Induction of Apoptosis.

Blood ◽  
2006 ◽  
Vol 108 (11) ◽  
pp. 4323-4323
Author(s):  
Karoline V. Gleixner ◽  
Mayerhofer Matthias ◽  
Anja Vales ◽  
Alexander Gruze ◽  
Michael Kneidinger ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Myeloid Leukemia ◽  
Carcinoma Cell ◽  
Leukemia Cell ◽  
Cancer Cell Line ◽  
Leukemia Cell Line ◽  
Zinc Protoporphyrin ◽  
Neoplastic Cells ◽  
Induction Of Apoptosis

Abstract Heat shock protein 32 (Hsp32), also known as heme oxygenase-1 (HO-1), is a stress-related survival factor that has recently been implicated in enhanced survival of neoplastic cells. We here show that Hsp32/HO-1 is expressed abundantly in primary neoplastic cells in various solid tumors and hematopoietic neoplasms such as acute myeloid leukemia (AML) or chronic myeloid leukemia (CML), and in respective cell lines including the AML cell lines HL60, KG1, KG1a, and U937, CML cell lines K562 and KU812, eosinophilic leukemia cell line EOL-1, mast cell leukemia cell line HMC-1, myeloma cell lines RPMI8226 and U266, breast cancer cell line MDA MB 231, lung cancer cell line A549, pancreatic carcinoma cell line BxPC-3, colon carcinoma cell lines COLO201, COLO205, COLO320DM, and DLD-1, and the ovarian carcinoma cell line OVCAR-3. Expression of Hsp32 mRNA was demonstrable by RT-PCR and Northern blotting, and expression of the Hsp32 protein by Western blotting and immunocytochemistry. The CML-specific oncoprotein BCR/ABL and the transforming oncoprotein KIT D816V that is expressed in neoplastic mast cells, were found to promote expression of Hsp32 in Ba/F3 cells. In order to examine the functional role of Hsp32 in neoplastic cells, a specific siRNA was employed. Expression of Hsp32 siRNA resulted in reduced viability and induction of apoptosis in all cell lines tested. To further explore the value of Hsp32 as a target in neoplastic cells, a novel specific Hsp32-targeting compound, styrene maleic acid copolymer zinc protoporphyrin micelles (SMA-ZnPP) was applied. Exposure to SMA-ZnPP resulted in a significant decrease in proliferation determined by 3H-thymidine uptake, in all cell lines as well as in all primary neoplastic cells tested (AML, n=5; CML, n=5; mastocytosis, n=3; breast cancer, n=2; lung cancer, n=1). As assessed by AnnexinV-staining, Tunel assay and electron microscopy, the growth-inhibitory effects of SMA-ZnPP were found to be associated with induction of apoptosis. In each cell type, the effect of SMA-ZnPP on growth was dose-dependent and found to occur at pharmacologic concentrations (IC50 1–30 μM). Moreover, SMA-ZnPP was found to synergize with various anti-neoplastic drugs (tumor cell lines: cisplatin, leukemias: cytarabine, myeloma: bortezomib) in producing growth inhibition. In summary, these data show that Hsp32/HO-1 is an important survival factor and novel interesting target in various hematopoietic and non-hematopoietic neoplasms. Based on these data, it seems desirable to explore the value of the Hsp32-targeting drug SMA-ZnPP in clinical trials in patients with leukemias and solid tumors.

scholarly journals Cytotoxic Potential of a-Azepano- and 3-Amino-3,4-SeCo-Triterpenoids

2021 ◽  
Vol 22 (4) ◽  
pp. 1714
Author(s):  
Oxana Kazakova ◽  
Irina Smirnova ◽  
Elena Tret’yakova ◽  
René Csuk ◽  
Sophie Hoenke ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Acid Amide ◽  
Leukemia Cell ◽  
Human Tumor ◽  
Cancer Cell Lines ◽  
Leukemia Cell Line

Semi-synthetic triterpenoids, holding an amino substituted seven-membered A-ring (azepano-ring), which could be synthesized from triterpenic oximes through a Beckmann type rearrangement followed by a reduction of lactame fragment, are considered to be novel promising agents exhibiting anti-microbial, alpha-glucosidase, and butyrylcholinesterase inhibitory activities. In this study, in an attempt to develop new antitumor candidates, a series of A-ring azepano- and 3-amino-3,4-seco-derivatives of betulin, oleanolic, ursolic, and glycyrrhetinic acids were evaluated for their cytotoxic activity against five human cancer cell lines and non-malignant mouse fibroblasts by means of a colorimetric sulforhodamine assay. Azepanoallobetulinic acid amide derivative 11 was the most cytotoxic compound of this series but showed little selectivity between the different human tumor cell lines. Flow cytometry experiments showed compound 11 to act mainly by apoptosis (44.3%) and late apoptosis (21.4%). The compounds were further screened at the National Cancer Institute towards a panel of 60 cancer cell lines. It was found that compounds 3, 4, 7, 8, 9, 11, 15, 16, 19, and 20 showed growth inhibitory (GI50) against the most sensitive cell lines at submicromolar concentrations (0.20–0.94 μM), and their cytotoxic activity (LC50) was also high (1–6 μM). Derivatives 3, 8, 11, 15, and 16 demonstrated a certain selectivity profile at GI50 level from 5.16 to 9.56 towards K-562, CCRF-CEM, HL-60(TB), and RPMI-8226 (Leukemia), HT29 (Colon cancer), and OVCAR-4 (Ovarian cancer) cell lines. Selectivity indexes of azepanoerythrodiol 3 at TGI level ranged from 5.93 (CNS cancer cell lines SF-539, SNB-19 and SNB-75) to 14.89 for HCT-116 (colon cancer) with SI 9.56 at GI50 level for the leukemia cell line K-562. The present study highlighted the importance of A-azepano-ring in the triterpenic core for the development of novel antitumor agents, and a future aim to increase the selectivity profile will thus lie in the area of modifications of azepano-triterpenic acids at their carboxyl group.

scholarly journals Monarubins A–C from the Marine Shellfish-Associated Fungus Monascus ruber BB5

Marine Drugs ◽  
2020 ◽  
Vol 18 (2) ◽  
pp. 100
Author(s):  
Yan-Qin Ran ◽  
Wen-Jian Lan ◽  
Yi Qiu ◽  
Qi Guo ◽  
Gong-Kan Feng ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Carcinoma Cell ◽  
2D Nmr ◽  
Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Monascus Ruber ◽  
Carcinoma Cell Lines ◽  
Ic50 Values ◽  
New Compounds

Three new compounds, monarubins A–C (1, 6 and 13), together with ten known compounds, including four alkaloids (2–5), two isocoumarins (7 and 8) and four polyketides (9–12), were isolated from marine shellfish-associated fungus Monascus ruber BB5. The structures were determined on the basis of the 1D and 2D NMR, MS, UV and IR data. The absolute configurations of compounds 3, 6 and 13 were determined by ECD calculations. The NMR data of compounds deoxyhydroxyaspergillic acid (3) and 2-hydroxy-6-(1-hydroxy-1-methylpropyl)-3-sec-buthylpyrazine (4) were first reported. All of the isolated compounds were evaluated for their cytotoxic activities against human nasopharyngeal carcinoma cell lines CNE1, CNE2, SUNE1 and HONE1 and hepatocellular carcinoma cell lines QGY7701 and HepG2. Monarubin B (6) displayed potent cytotoxicities against the cancer cell lines HepG2 and QGY7701 with IC50 values of 1.72 and 0.71 μΜ, respectively; lunatinin (7) showed moderate cytotoxic activities against the cancer cell lines HepG2, QGY7701 and SUNE1 with the IC50 values of 9.60, 7.12 and 28.12 μΜ, respectively.

scholarly journals Design, Synthesis of Novel Tetrandrine-14-l-Amino Acid and Tetrandrine-14-l-Amino Acid-Urea Derivatives as Potential Anti-Cancer Agents

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1738
Author(s):  
Sheng-Cao Hu ◽  
Jin Yang ◽  
Chao Chen ◽  
Jun-Rong Song ◽  
Wei-Dong Pan
Keyword(s):  
Amino Acid ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Leukemia Cell ◽  
Leukemia Cell Line ◽  
Human Leukemia ◽  
Urea Derivatives ◽  
Anti Cancer

Tetrandrine, a dibenzyltetrahydroisoquinoline alkaloid isolated from the root of the traditional Chinese medicinal plant Stephania tetrandra S. Moore, a member of the Menispermaceae, showed anti-cancer activity by inhibiting cell proliferation, preventing cell cycle progress and induction of cell death and autophagy. In this study, twelve tetrandrine-l-amino acid derivatives and twelve tetrandrine-14-l-amino acid-urea derivatives were designed and synthesized, using C14-aminotetrandrine as raw material. Then the preliminary in vitro anti-cancer activities of these derivatives against human breast cancer cell line MDA-MB-231, human leukemia cell lines HEL and K562 were evaluated. The in vitro cytotoxicity results showed that these derivatives exhibited potent inhibitory effects on cancer cell growth, and the primary structure-activity relationships were evaluated. Notably, compound 3f exhibited satisfactory anticancer activity against all three cancer cell lines, especially the HEL cell line, with the IC50 value of 0.23 µM. Further research showed that 3f could induce G1/S cycle arrest and apoptosis in a dose- and time- dependent manner on the leukemia cell line HEL. The results suggested that 3f may be used as a potential anti-cancer agent for human leukemia.

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