Cleome Viscosa Exhibits Cytotoxicity in Vitro and improves Tumor Inhibitory Properties in Vivo in Liquid Tumor Model

2021 ◽  
pp. 5397-5404
Author(s):  
K Usha S Pai ◽  
Yadav D. Bodke ◽  
M Manjunath Setty ◽  
Savaliya Mihir ◽  
Keerthi Priya ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Petroleum Ether ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Tumor Model ◽  
Scientific Data ◽  
Chemotherapeutic Regimen ◽  
Cleome Viscosa

Cancer is one of the major causes of death in the world today. Although chemotherapeutic regimen remains the prime treatment of cancer, it is important to explore for newer compounds due to their adverse reactions and the growing rate of resistance. Traditionally, some plants are used for the treatment of cancers in India. However, no scientific data backing the evidence exists for the same. Among such plants is Cleome viscosa Linn, which is used in the Indian system of medicine for cancer treatment. To test its anticancer activity and generate scientifically reliable data, the extraction of whole plant has been carried out using methanol and fractions were generated using petroleum ether, dichloromethane, ethyl acetate and n-butanol. The fractions were first tested in vitro for their antiproliferative activity and mechanistic studies. In this paper, we report the anticancer potential of the fractions by a preliminary cytotoxicity activity in vitro using cell lines followed by the liquid tumor (EAC) model in mice. Upon screening on a panel of cancer cell lines, the fractions of petroleum ether, dichloromethane and ethyl acetate were found to possess significant cytotoxic activity on Hela and U343 cell lines. With this evidence, we have then tested the in vivo activity on mice using the liquid tumor model in which the fractions of pet ether, dichloromethane and ethyl acetate exhibit a potential anticancer activity which is evident in characteristics like inhibition of tumor progression, increase in the mean survival time and percentage increased life span along with a decrease in tumor volume. The fractions also showed significant anti-oxidant properties.

„IN VITRO“ AND „IN VIVO“ ANTITUMOR ACTIVITY OF PLATINUM(II) COMPLEXES WITH MALONIC ACID ON BREAST AND COLORECTAL CARCINOMA CELL LINES

2021 ◽  
Author(s):  
Andjela Franich ◽  
◽  
Milica Dimitrijević Stojanović ◽  
Snežana Rajković ◽  
Marina Jovanović ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Colorectal Carcinoma ◽  
Cell Lines ◽  
Tumor Model ◽  
Carcinoma Cells ◽  
Spectroscopic Techniques ◽  
Murine Cell Line ◽  
In Vivo Antitumor Activity

Four Pt(II) complexes of the general formula [Pt(L)(5,6-epoxy-1,10-phen)], where L is anion of malonic (mal, Pt1), 2-methylmalonic (Me-mal, Pt2), 2,2-dimethylmalonic (Me2-mal, Pt3) or 1,1- cyclobutanedicarboxylic (CBDCA, Pt4) acid while 5,6-epoxy-1,10-phen is bidentately coordinated 5,6-epoxy-5,6-dihydro-1,10-phenanthroline were synthesized and characterized by elemental microanalysis, IR, UV-Vis and NMR (1H and 13C) spectroscopic techniques. In vitro anticancer activity of novel platinum(II) complexes have been investigated on human and murine cancer cell lines, as well as normal murine cell line by MTT assay. The obtained results indicate that studied platinum(II) complexes exhibited strong cytotoxic activity against murine breast carcinoma cells (4T1), human (HCT116) and murine (CT26) colorectal carcinoma cells. Complex Pt3 display stronger selectivity toward carcinoma cells in comparison to other tested platinum(II) complexes exhibiting beneficial antitumor activity mainly via the induction of apoptosis, as well as inhibition of cell proliferation and migration. Further study showed that Pt3 complex also carry significant in vivo antitumor activity in orthotopical 4T1 tumor model without detected liver, kidney, lung, and heart toxicity. All results imply that these novel platinum(II) complexes have a good anti-tumor effect on breast and colorectal cancer in vivo and in vitro and the affinity to become possible candidates for treatment in anticancer therapy.

scholarly journals Anticancer Activity of Cynomorium coccineum

Cancers ◽  
2018 ◽  
Vol 10 (10) ◽  
pp. 354 ◽  
Author(s):  
Mouna Sdiri ◽  
Xiangmin Li ◽  
William Du ◽  
Safia El-Bok ◽  
Yi-Zhen Xie ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Death ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cell Cycle Progression ◽  
Cycle Progression

The extensive applications of Cynomorium species and their rich bioactive secondary metabolites have inspired many pharmacological investigations. Previous research has been conducted to examine the biological activities and numerous interesting pharmaceutical activities have been reported. However, the antitumor activities of these species are unclear. To understand the potential anticancer activity, we screened Cynomorium coccineum and Cynomorium songaricum using three different extracts of each species. In this study, the selected extracts were evaluated for their ability to decrease survival rates of five different cancer cell lines. We compared the cytotoxicity of the three different extracts to the anticancer drug vinblastine and one of the most well-known medicinal mushrooms Amaurederma rude. We found that the water and alcohol extracts of C. coccineum at the very low concentrations possessed very high capacity in decreasing the cancer cells viability with a potential inhibition of tumorigenesis. Based on these primitive data, we subsequently tested the ethanol and the water extracts of C. coccineum, respectively in in vitro and in vivo assays. Cell cycle progression and induction of programmed cell death were investigated at both biological and molecular levels to understand the mechanism of the antitumor inhibitory action of the C. coccineum. The in vitro experiments showed that the treated cancer cells formed fewer and smaller colonies than the untreated cells. Cell cycle progression was inhibited, and the ethanol extract of C. coccineum at a low concentration induced accumulation of cells in the G1 phase. We also found that the C. coccineum’s extracts suppressed viability of two murine cancer cell lines. In the in vivo experiments, we injected mice with murine cancer cell line B16, followed by peritoneal injection of the water extract. The treatment prolonged mouse survival significantly. The tumors grew at a slower rate than the control. Down-regulation of c-myc expression appeared to be associated with these effects. Further investigation showed that treatment with C. coccineum induced the overexpression of the tumor suppressor Foxo3 and other molecules involved in inducing autophagy. These results showed that the C. coccineum extract exerts its antiproliferative activity through the induction of cell death pathway. Thus, the Cynomorium plants appear to be a promising source of new antineoplastic compounds.

scholarly journals Anticancer Activity Of Plant Genus Clerodendrum (Lamiaceae): A Review

2017 ◽  
Vol 22 (3) ◽  
pp. 182
Author(s):  
Donald Emilio Kalonio ◽  
Rini Hendriani ◽  
Elisabeth N. Barung
Keyword(s):  
Molecular Docking ◽  
Anticancer Activity ◽  
Docking Simulation ◽  
Scientific Data ◽  
Anticancer Effect ◽  
Literature Study ◽  
Molecular Docking Simulation ◽  
Chemical Content

Plants of the genus Clerodendrum (Lamiaceae) is widespread in tropical and subtropical regions. Plants of this genus are used both empirically and scientifically as anti-inflammatory, antidiabetic, antimalarial, antiviral, antihypertensive, hypolipidemic, antioxidant, and antitumor. Results of the molecular docking simulation of chemical content of these plants could potentially provide an anticancer effect. This paper aims to review the anticancer activity of plant genus Clerodendrum based on scientific data. The method used in this study is the literature study. Searches were conducted online (in the database PubMed, Science Direct and Google Scholar) and on various books (Farmakope Herbal Indonesia and PROSEA). A total 12 plants of the genus Clerodendrum have anticancer activity in vitro and in vivo, thus potentially to be developed as a source of new active compounds with anticancer activity.

scholarly journals Ad-VT enhances the sensitivity of chemotherapy-resistant lung adenocarcinoma cells to gemcitabine and paclitaxel in vitro and in vivo

2022 ◽  
Author(s):  
Gaojie Song ◽  
Chao Shang ◽  
Lili Sun ◽  
Yiquan Li ◽  
Yilong Zhu ◽  
...  
Keyword(s):  
Cell Lines ◽  
A549 Cells ◽  
Resistance Index ◽  
Tumor Model ◽  
Resistant Cell ◽  
Drug Resistant ◽  
Chemotherapeutic Drugs ◽  
Drug Resistant Cell

SummaryBackground One of the main challenges in the clinical treatment of lung cancer is resistance to chemotherapeutic drugs. P-glycoprotein (P-gp)-mediated drug resistance is the main obstacle to successfully implementing microtubule-targeted tumor chemotherapy. Purpose In this study, we explored the effect of Ad-hTERTp-E1a-Apoptin (Ad-VT) on drug-resistant cell lines and the molecular mechanism by which Ad-VT combined with chemotherapy affects drug-resistant cells and parental cells. Methods In vitro, cell proliferation, colony formation, resistance index (RI), apoptosis and autophagy assays were performed. Protein expression was analyzed by Western blotting. Finally, a xenograft tumor model in nude mice was used to detect tumor growth and evaluate histological characteristics. Results Our results showed that Ad-VT had an obvious killing effect on A549, A549/GEM and A549/Paclitaxel cancer cells, and the sensitivity of drug-resistant cell lines to Ad-VT was significantly higher than that of parental A549 cells. Compared with A549 cells, A549/GEM and A549/Paclitaxel cells had higher autophagy levels and higher viral replication ability. Ad-VT decreased the levels of p-PI3k, p-Akt and p-mTOR and the expression of P-gp. In vivo, Ad-VT combined with chemotherapy can effectively inhibit the growth of chemotherapy-resistant tumors and prolong the survival of mice. Conclusions Thus, the combination of Ad-VT and chemotherapeutic drugs will be a promising strategy to overcome chemoresistance.

scholarly journals Simultaneous Multi-Organ Metastases from Chemo-Resistant Triple-Negative Breast Cancer Are Prevented by Interfering with WNT-Signaling

Cancers ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 2039 ◽  
Author(s):  
Iram Fatima ◽  
Ikbale El-Ayachi ◽  
Hilaire C. Playa ◽  
Jackelyn A. Alva-Ornelas ◽  
Aysha B. Khalid ◽  
...  
Keyword(s):  
Cell Lines ◽  
Triple Negative ◽  
De Novo ◽  
Tumor Model ◽  
Model Systems ◽  
Breast Cancers ◽  
Primary Tumors ◽  
Multiple Organs

Triple-negative breast cancers (TNBCs), which lack specific targeted therapy options, evolve into highly chemo-resistant tumors that metastasize to multiple organs simultaneously. We have previously shown that TNBCs maintain an activated WNT10B-driven network that drives metastasis. Pharmacologic inhibition by ICG-001 decreases β-catenin-mediated proliferation of multiple TNBC cell lines and TNBC patient-derived xenograft (PDX)-derived cell lines. In vitro, ICG-001 was effective in combination with the conventional cytotoxic chemotherapeutics, cisplatin and doxorubicin, to decrease the proliferation of MDA-MB-231 cells. In contrast, in TNBC PDX-derived cells doxorubicin plus ICG-001 was synergistic, while pairing with cisplatin was not as effective. Mechanistically, cytotoxicity induced by doxorubicin, but not cisplatin, with ICG-001 was associated with increased cleavage of PARP-1 in the PDX cells only. In vivo, MDA-MB-231 and TNBC PDX orthotopic primary tumors initiated de novo simultaneous multi-organ metastases, including bone metastases. WNT monotherapy blocked multi-organ metastases as measured by luciferase imaging and histology. The loss of expression of the WNT10B/β-catenin direct targets HMGA2, EZH2, AXIN2, MYC, PCNA, CCND1, transcriptionally active β-catenin, SNAIL and vimentin both in vitro and in vivo in the primary tumors mechanistically explains loss of multi-organ metastases. WNT monotherapy induced VEGFA expression in both tumor model systems, whereas increased CD31 was observed only in the MDA-MB-231 tumors. Moreover, WNT-inhibition sensitized the anticancer response of the TNBC PDX model to doxorubicin, preventing simultaneous metastases to the liver and ovaries, as well as to bone. Our data demonstrate that WNT-inhibition sensitizes TNBC to anthracyclines and treats multi-organ metastases of TNBC.

scholarly journals Potent In Vitro and In Vivo Anticancer Activity of New Bipyridine and Bipyrimidine Gold (III) Dithiocarbamate Derivatives

Cancers ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 474 ◽  
Author(s):  
Muhammad Altaf ◽  
Naike Casagrande ◽  
Elena Mariotto ◽  
Nadeem Baig ◽  
Abdel-Nasser Kawde ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Ros Generation ◽  
Dna Breaks

We synthesized eight new bipyridine and bipyrimidine gold (III) dithiocarbamate-containing complexes (C1–C8) and tested them in a panel of human cancer cell lines. We used osteosarcoma (MG-63), lung (A549), prostate (PC3 and DU145), breast (MCF-7), ovarian (A2780 and A2780cis, cisplatin- and doxorubicin-resistant), and cervical (ME-180 and R-ME-180, cisplatin resistant) cancer cell lines. We found that C2, C3, C6, and C7 were more cytotoxic than cisplatin in all cell lines tested and overcame cisplatin and doxorubicin resistance in A2780cis and R-ME-180 cells. In the PC3 prostate cancer cell line, the gold (III) complex C6 ([Au2(BPM)(DMDTC)2]Cl4) induced apoptosis and double-stranded DNA breaks, modified cell cycle phases, increased Reactive Oxigen Species (ROS) generation, and reduced thioredoxin reductase and proteasome activities. It inhibited PC3 cell migration and was more cytotoxic against PC3 cells than normal human adipose-derived stromal cells. In mice bearing PC3 tumor xenografts, C6 reduced tumor growth by more than 70% without causing weight loss. Altogether, our results demonstrate the anticancer activity of these new gold (III) complexes and support the potential of C6 as a new agent for prostate cancer treatment.

Synthesis, In Silico and In Vivo Evaluation of Novel 1, 3, 4-Thiadiazole Analogues as Novel Anticancer Agents

2020 ◽  
Vol 17 (4) ◽  
pp. 434-444 ◽  
Author(s):  
Swathi Krishna ◽  
Byran Gowramma ◽  
Manal Mohammed ◽  
Rajagopal Kalirajan ◽  
Lakshman Kaviarasan ◽  
...  
Keyword(s):  
Vero Cell ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Binding Interaction ◽  
Standard Drug ◽  
Discovery Studio ◽  
Vero Cell Lines ◽  
Mcf 7

Background: 1,3,4-thiadiazole is a lead molécule which is versatile for a wide variety of biological activities and in continuation of our interest in establishing some novel heterocyclic compounds for antitumor activity. Objective: The objective of the study was to synthesize series of 5-(1,3-benzodioxol-5-yl)-1,3,4- thiadiazol-2-amine derivative and evaluated for their possible in vitro and in vivo anticancer activity. Methods: The synthesis of 2-aminonaphthoxy-1,3,4-thiadiazole and 5-(1,3-benzodioxol-5-yl)-1,3,4- thiadiazol-2-amine as intermediates were carried out by cyclization method. A mixture of thiosemicarbazide and naphthoxyacetic acid/piperonylic acid and phosphoryl chloride were subjected to cyclization with phosphorous oxychloride to obtain compound 3. Further compounds 1 and 3 were reacted with different aromatic aldehydes in methanol to form compounds 2a-e and 4a-e. The compounds 2a-e and 4a-e were characterized for the melting points, IR, Proton NMR and Mass spectra. The compounds were further evaluated for their anticancer activity. The docking study was performed using Discovery studio 4.1 (Accelrys) software against DNA-binding domain of STAT3. The compounds were analyzed for the ligand-protein binding interaction(s) by molecular docking into the active site of STAT3β using the CDOCKER protocol of Discovery studio (v4.1). Results: The title compounds were screened for in vitro anticancer on human breastadenocarcinoma cells (MCF-7 and Vero). Compounds 4c, 4d and 2d against MCF 7 and 4d against Vero cell lines were found to be the most active dérivatives with IC50 values of 1.03, 2.81 and 3.45 µg/ml against MCF 7 and 31.81 µg/ml against Vero cell lines, respectively. Conclusion: From the in vivo anticancer studies, it was concluded that the synthesized compounds 4c and 4d displayed anticancer activity comparable to the standard drug, while the rest of the compounds demonstrated mild potency for anticancer studies.

Ru(III) complexes of pyrazolopyrimidines as anticancer agents: In vitro, in vivo anticancer activity and underlying multi-mechanisms

2022 ◽  
Author(s):  
Yunqiong Gu ◽  
Wen-Ying Shen ◽  
Qi-Yuan Yang ◽  
Zhen-Feng Chen ◽  
Hong Liang
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Human Liver ◽  
Normal Human Liver ◽  
Normal Human ◽  
Low Toxicity

Three ruthenium(III) complexes with pyrazolopyrimidine [Ru(Ln)(H2O)Cl3] (13, n=13) were prepared and characterized. These Ru(III) compounds show strong cytotoxicity against six cancer cell lines and low toxicity to normal human liver...

scholarly journals In vitro and in vivo evaluation of pharmacological potential of Begonia barbata Wall

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Mohammad Rashedul Haque ◽  
Mirazul Islam ◽  
Md. Ruhul Kuddus
Keyword(s):  
Acetic Acid ◽  
Ethyl Acetate ◽  
Petroleum Ether ◽  
Total Phenolic ◽  
Plant Samples ◽  
Tail Immersion ◽  
Thiopental Sodium ◽  
Pharmacological Potential

Abstract Background Begonia barbata Wall is an important medicinal plant in Bangladesh used to treat several human diseases. The intention of the existing work was to determine in vitro and in vivo pharmacological properties of petroleum-ether, dichloromethane, and ethyl acetate soluble fractions of methanol extract of B. barbata whole plant (MEBB). The total phenolic content (TPC) was determined by Folin-Ciocalteu test while antioxidant activity assay was performed by DPPH radical quenching process. Tail immersion and acetic acid-induced writhing methods were utilized to evaluate analgesic effect in albino mice. To evaluate the hypoglycemic potential, glucose tolerance test is used. Castor oil-induced diarrhea method is utilized to figure out the anti-diarrheal action in mice. Thiopental-sodium-induced sleeping time test was exploited for the appraisal of CNS antidepressant action. Results Antioxidant activities of the test materials followed the order: dichloromethane fraction (DCMF) > ethyl acetate fraction (EAF) > petroleum-ether fraction (PEF). The EAF yielded maximum amount of phenolic compounds (12.47 mg of GAE/g of sample). The DMF was most effective in terms of thrombolytic activity while the EAF protected the membrane integrity of erythrocyte by 63.47% inhibition of hemolysis induced by heat. Among all fractions, the PEF (400 mg/kg body weight) demonstrated highest analgesic activity in both tail immersion test (maximum elongations as 262.053%) and acetic acid-induced writhing method (66.02% writhing inhibition). During anti-diarrheal test, the plant samples significantly diminished the frequency of diarrheal episodes in mice. Similarly, the plant samples decreased the sleeping duration induced by thiopental sodium. Conclusion The above outcome exposed that B. barbata possesses significant pharmacological potential, which validates its use in Bangladesh folk medicinal practices.

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