scholarly journals 596 Armed myxoma virus demonstrates therapeutic activity in xenograft models

2020 ◽  
Vol 8 (Suppl 3) ◽  
pp. A631-A631
Author(s):  
Lino Torres-Dominguez ◽  
Lina Franco ◽  
Mario Abrantes ◽  
Benjamin Walker ◽  
Zachary Tacner ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Myxoma Virus ◽  
Human Cancer Cell Lines ◽  
Cancer Models ◽  
Oncolytic Activity

BackgroundOncolytic Viruses (OV) selectively replicate in and lyse tumor cells and provide stimulation to the immune system. This represents a promising therapeutic option for cancer patients that do not respond well to treatment with immune checkpoint inhibitors. Myxoma virus (MYXV) is a member of the Pox family of double stranded DNA viruses. The natural host of MYXV is a subset of rabbits and hares, but MYXV is able to infect cancer cell lines of humans and other species. The genome of MYXV is relatively large and is amenable to engineering for expression of transgenic proteins making it an excellent oncolytic virus for introduction of immunomodulatory proteins.MethodsThe current work describes the in vitro oncolytic activity and transgene production capability in human cancer cell lines, and in vivo activity of armed myxoma viruses in xenograft human cancer models.ResultsArmed Myxoma viruses demonstrate transgene production and oncolytic activity in multiple human cancer cell lines in vitro and in vivoConclusionsArmed Myxoma viruses present a novel oncolytic viral therapy with ability to modulate immune responses in human cancer modelsEthics ApprovalThis study was approved by OncoMyx Therapeutics and the TD2 IACUC

scholarly journals COTI-2, a novel small molecule that is active against multiple human cancer cell lines in vitro and in vivo

Oncotarget ◽  
2016 ◽  
Vol 7 (27) ◽  
pp. 41363-41379 ◽  
Author(s):  
Kowthar Y. Salim ◽  
Saman Maleki Vareki ◽  
Wayne R. Danter ◽  
Serban San-Marina ◽  
James Koropatnick
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Small Molecule ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

scholarly journals In vitro and in vivo anticancer efficacy of Adiantum capillus-veneris L. against some selected human cancer cell lines and on EAC mouse model

2020 ◽  
pp. 267-274
Author(s):  
Zeenat Ayoub ◽  
Sumera Banoo Malik ◽  
Archana Mehta
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Ethanolic Extract ◽  
Cancer Cell Lines ◽  
Hexane Fraction ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

Adiantum capillus-veneris, commonly known as maidenhair fern belongs to family Pteridaceae, has traditionally been used in various medicinal preparations as demulcent, expectorant, emmenagogue, diuretic etc. in the form of oil, paste, decoction and powder. It has also prominent role in hair growing and has anti-microbial, anti-inflammatory, anti-diabetic, anti-nociceptive and antioxidant properties of therapeutic interest. This study aimed to investigate the in vitro cytotoxic activity of fractions of ethanolic extract isolated from the aerial part of A. capillus-veneris against some human cancer cell lines such as colon (HCT-116), lung (A549), breast (MCF-7) and pancreatic (MIA PaCa-2) and tumor cell proliferation/inhibition was assessed using MTT assay. The in vivo anticancer activity of hexane fraction was also evaluated against murine Ehrlich ascites carcinoma (EAC) model. The results confirmed that all the fractions of ethanolic extract exhibited promising in vitro inhibition of tumor cell proliferation when tested against different human cancer cell lines. Among all, hexane fraction proved to be more effective having IC50 values 21.72, 22.67, 26.25 μg/mL, for HCT- 116, A-549, MCF-7, respectively, but chloroform fraction revealed to be more cytotoxic against Mia-PACA-2 having IC50 value 14.72 μg/mL. Higher cytotoxic activity is found to be associated with lower IC50 values. The findings showed that all five fractions exhibited dose-dependent killing capabilities in various human derived cancer cell lines at 48 h of treatment. Hexane fraction was found to inhibit tumour growth development by 16.95%, 41.12% and 82.07% at 50, 100 and 200 mg/kg body weight, respectively. Additionally, this fraction was predicted to be non-toxic at the tested doses. The findings indicate that A. capillus-veneris herb is an antineoplastic agent and suggest that further studies evaluating the isolation of active antitumor compounds from A. capillus-veneris and their mechanism(s) of action are necessary.

scholarly journals Correction: COTI-2, a novel small molecule that is active against multiple human cancer cell lines in vitro and in vivo

Oncotarget ◽  
2017 ◽  
Vol 8 (36) ◽  
pp. 60724-60724
Author(s):  
Kowthar Y. Salim ◽  
Saman Maleki Vareki ◽  
Wayne R. Danter ◽  
Serban San-Marina ◽  
James Koropatnick
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Small Molecule ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

Synthesis and Cytotoxicity Assessment of Novel 7-O- and 14-O-Derivatives of Glaucocalyxin A

2020 ◽  
Vol 20 (10) ◽  
pp. 1241-1249
Author(s):  
Hong-Chuan Liu ◽  
Li-Ming Qiao ◽  
Wei Zheng ◽  
Zhao-Bao Xiang ◽  
Hai-Sheng Chen ◽  
...  
Keyword(s):  
Acute Toxicity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Folk Medicine ◽  
A549 Cells ◽  
Cancer Cell Lines ◽  
Human Cancer Cell Lines ◽  
Derivatives Of

Background: Rabdosia japonica has been historically used in China as a popular folk medicine for the treatment of cancer, hepatitis, and gastricism. Glaucocalyxin A (GLA), an ent-kaurene diterpene isolated from Rabdosia japonica, is one of the main active ingredients showing potent inhibitory effects against several types of tumor cells. To the best of our knowledge, studies regarding the structural modification and Structure- Activity Relations (SAR) of this compound have not yet been reported. Objective: The aim of this study was to discover more potent derivatives of GLA and investigate their SAR and cytotoxicity mechanisms. Methods: Novel 7-O- and 14-O-derivatives of GLA were synthesized by condensation of acids or acyl chloride. The anti-tumor activities of these derivatives against various human cancer cell lines were evaluated in vitro by MTT assays. Apoptosis assays of compound 17 (7,14-diacylation product) were performed on A549 and HL-60 cells by flow cytometry and TUNNEL. The acute toxicity of this compound was tested on mice, at the dose of 300mg per kg body weight. Results: Seventeen novel 7-O- and 14-O-derivatives of GLA (1-17) were synthesized. These compounds showed potent cytotoxicity against the tested cancer cell lines, and almost all of them were found to be more cytotoxic than GLA and oridonin. Of the synthesized derivatives, compound 17 presented the greatest cytotoxicity, with IC50 values of 0.26μM and 1.10μM in HL-60 and CCRF-CEM cells, respectively. Furthermore, this compound induced weak apoptosis of A549 cells but showed great potential in stimulating the apoptosis of HL- 60 cells. Acute toxicity assays indicated that compound 17 is relatively safer. Conclusion: The results reported herein indicate that the synthesized GLA derivatives exhibited greater cytotoxicity against leukemia cells than against other types of tumors. In particular, 7,14-diacylation product of GLA was found to be an effective anti-tumor agent. However, the cytotoxicity mechanism of this product in A549 cells is expected to be different than that in other tumor cell lines. Further research is needed to confirm this hypothesis.

scholarly journals Discovery of New Pyrazolopyridine, Furopyridine, and Pyridine Derivatives as CDK2 Inhibitors: Design, Synthesis, Docking Studies, and Anti-Proliferative Activity

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3923
Author(s):  
Adel A.-H. Abdel-Rahman ◽  
Amira K. F. Shaban ◽  
Ibrahim F. Nassar ◽  
Dina S. EL-Kady ◽  
Nasser S. M. Ismail ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Molecular Docking Study ◽  
Human Cancer Cell Lines ◽  
Hct 116 ◽  
Mcf 7

New pyridine, pyrazoloyridine, and furopyridine derivatives substituted with naphthyl and thienyl moieties were designed and synthesized starting from 6-(naphthalen-2-yl)-2-oxo-4-(thiophen-2-yl)-1,2-dihydropyridine-3-carbonitrile (1). The chloro, methoxy, cholroacetoxy, imidazolyl, azide, and arylamino derivatives were prepared to obtain the pyridine-−C2 functionalized derivatives. The derived pyrazolpyridine-N-glycosides were synthesized via heterocyclization of the C2-thioxopyridine derivative followed by glycosylation using glucose and galactose. The furopyridine derivative 14 and the tricyclic pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine 15 were prepared via heterocyclization of the ester derivative followed by a reaction with formamide. The newly synthesized compounds were evaluated for their ability to in vitro inhibit the CDK2 enzyme. In addition, the cytotoxicity of the compounds was tested against four different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549). The CDK2/cyclin A2 enzyme inhibitory results revealed that pyridone 1, 2-chloro-6-(naphthalen-2-yl)-4-(thiophen-2-yl)nicotinonitrile (4), 6-(naphthalen-2-yl)-4-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-amine (8), S-(3-cyano-6-(naphthaen-2-yl)-4-(thiophen-2-yl)pyridin-2-yl) 2-chloroethanethioate (11), and ethyl 3-amino-6-(naphthalen-2-yl)-4-(thiophen-2-yl)furo[2,3-b]pyridine-2-carboxylate (14) are among the most active inhibitors with IC50 values of 0.57, 0.24, 0.65, 0.50, and 0.93 µM, respectively, compared to roscovitine (IC50 0.394 μM). Most compounds showed significant inhibition on different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549) with IC50 ranges of 31.3–49.0, 19.3–55.5, 22.7–44.8, and 36.8–70.7 μM, respectively compared to doxorubicin (IC50 40.0, 64.8, 24.7 and 58.1 µM, respectively). Furthermore, a molecular docking study suggests that most of the target compounds have a similar binding mode as a reference compound in the active site of the CDK2 enzyme. The structural requirements controlling the CDK2 inhibitory activity were determined through the generation of a statistically significant 2D-QSAR model.

scholarly journals SPIONs/3D SiSBA-16 based Multifunctional Nanoformulation for target specific cisplatin release in colon and cervical cancer cell lines

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
B. Rabindran Jermy ◽  
Munther Alomari ◽  
Vijaya Ravinayagam ◽  
Sarah Ameen Almofty ◽  
Sultan Akhtar ◽  
...  
Keyword(s):  
Cervical Cancer ◽  
Magnetic Resonance ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Dapi Staining ◽  
Tem Analysis ◽  
Human Cancer Cell Lines

Abstract Multifunctional nanomaterials can be used for dual applications: drug delivery as well as in bioimaging. In current study, we investigated potential use of silica based supports; 3D cage type SiSBA-16 (S-16), monodispersed hydrophilic spherical silica (HYPS) and mesocellular foam (MSU-F) for cisplatin (Cp) delivery. To obtain magnetic resonance characteristics, 10 wt% iron oxide was loaded through enforced adsorption technique. For pH stimuli responsive release of Cp, 10 wt%SPIONs/S-16 was functionalized with 3-(Aminopropyl)triethoxysilane (A) and poly acrylic acid (PAA) termed as 10 wt%SPIONs/S-16-A-Cp and 10 wt%SPIONs/S-16-APAA-Cp. By TEM analysis, the average diameter of the SPIONs was found to range between 10–60 nm. VSM analysis showed saturation magnetization over S-16, HYPS and MSU-F were in the following order: 10 wt%SPIONs/HYPS (4.08 emug−1) > 10 wt%SPIONs /S-16 (2.39 emug−1) > 10 wt%SPIONs/MSU-F (0.23 emug−1). Cp release study using dialysis membrane in PBS solution over 10 wt%SPIONs/S-16 nanoformulations showed highest cumulative release (65%) than 10 wt%SPIONs/MSU-F-A-Cp (63%), 10 wt%SPIONs/HYPS-A-Cp (58%), and Cp-F127/S-16 (53%), respectively. 10 wt%SPIONs/S-16-A-Cp and 10 wt%SPIONs/S-16-APAA-Cp were evaluated for in vitro target anticancer efficiency in human cancer cell lines (colon cancer (HCT 116), cervical cancer (HeLa)) and normal cells (Human embryonic kidney cells (HEK293) using MTT and DAPI staining. 10 wt%SPIONs/S-16-A-Cp treated Hela and HCT116 cancerous cell lines showed significant control of cell growth, apoptotic activity and less cytotoxic effect as compared to Cp and 10 wt%SPIONs/S-16. Target specific Cp release in the cells shows that 10 wt%SPIONs/S-16-A-Cp can be easily upgraded for magnetic resonance imaging capability.

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