IN VIVO ANTITUMOR ACTIVITY OF PHYTOCHEMICAL PITC-2 OBTAINED FROM TISSUE CULTURED PLANT PLUCHEA INDICA ON SARCOMA-180 SOLID TUMOR MICE MODEL

Objective: PITC-2 was isolated from the methanolic root extract of tissue cultured medicinal plant Pluchea indica (L.) Less. PITC-2 is a thiophene derivative which is 2-(Prop-1-ynyl)-5(5,6-dihydroxyhexa-1,3-diynyl)-thiophene. The main objective of the study is to evaluate the in vivo antitumor activity of PITC 2 against sarcoma-180 cancer cell in Swiss albino mice.Methods: The antitumor activity was evaluated by treatment with PITC-2 at a dose of 2.5 and 5 mg/kg b.w for 21 days on sarcoma-180 mice model. Cell viability was studied using 3-(4, 5- dimethylthiazol -2-yl)-2, 5-diphenyl tetrazolium bromide assay and cell apoptosis, G1 cell cycle arrest and reduction in tumor cell proliferation were evaluated by histopathological analysis and Bcl-2, cyclic-D1, and Ki-67 protein expression through immunohistochemistry study.Results: Precisely, PITC-2 had a cytotoxic effect on various in vitro cancer cells. Significant decreases in solid tumor volume and weight along with increase lifespan also observed. The histopathological and immunohistopathological examination indicates that PITC-2 induces apoptosis, typical morphological changes and suppresses tumor cell proliferation along with G1 cell cycle arrest through the downregulation of the intratumoral expression of Bcl-2, cyclic D1, and Ki-67 and thus highlighting antiproliferative and apoptotic properties against sarcoma-180 in vivo solid tumor model.Conclusion: The present results clearly demonstrate that PITC-2 significantly inhibits sarcoma-180 cell growth in a dose-dependent manner in in vivo mice model. Besides this, the study reveals a comprehensive perception of the possible mechanism behind the antitumor activity of PITC-2 by significant changes in the morphological, hematological, biochemical parameters in sarcoma-180 cells.

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Chemical composition, antitumor activity, and toxicity of essential oil from the leaves of Lippia microphylla

Zeitschrift für Naturforschung C ◽

10.1515/znc-2014-4138 ◽

2015 ◽

Vol 70 (5-6) ◽

pp. 129-137 ◽

Cited By ~ 5

Author(s):

Aline L. Xavier ◽

João Carlos L.R. Pita ◽

Monalisa T. Brito ◽

Déborah R.P. Meireles ◽

Josean F. Tavares ◽

...

Keyword(s):

Chemical Composition ◽

Antitumor Activity ◽

Liver Function ◽

Essential Oil ◽

Pharmacological Study ◽

Hematological Toxicity ◽

Sarcoma 180 ◽

Hemolytic Assay ◽

In Vivo Antitumor Activity

Abstract The chemical composition, antitumor activity and toxicity of the essential oil from Lippia microphylla leaves (OEL) were investigated. The major constituents were thymol (46.5%), carvacrol (31.7%), p-cymene (9%), and γ-terpinene (2.9%). To evaluate the toxicity of OEL in non-tumor cells, the hemolytic assay with Swiss mice erythrocytes was performed. The concentration producing 50% hemolysis (HC50) was 300 μg/mL. Sarcoma 180 tumor growth was inhibited in vivo 38% at 50 mg/kg, and 60% at 100 mg/kg, whereas 5-FU at 50 mg/kg caused 86% inhibition. OEL displays moderate gastrointestinal and hematological toxicity along with causing some alteration in liver function and morphology. However, the changes were considered reversible and negligible in comparison to the effects of several anticancer drugs. In summary, OEL displays in vivo antitumor activity and a moderate toxicity, which suggests further pharmacological study.

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Design, synthesis and pharmacological evaluation of novel 2-chloro-3-(1H-benzo[d]imidazol-2-yl)quinoline derivatives as antitumor agents: in vitro and in vivo antitumor activity, cell cycle arrest and apoptotic response

RSC Advances ◽

10.1039/c8ra04640a ◽

2018 ◽

Vol 8 (43) ◽

pp. 24376-24385 ◽

Cited By ~ 4

Author(s):

Wen-Bin Kuang ◽

Ri-Zhen Huang ◽

Yi-Lin Fang ◽

Gui-Bin Liang ◽

Chen-Hui Yang ◽

...

Keyword(s):

Antitumor Activity ◽

Antitumor Agents ◽

Quinoline Derivatives ◽

Apoptotic Response ◽

Design Synthesis ◽

Cycle Arrest ◽

In Vivo Antitumor Activity ◽

Combination Principle

A series of novel 2-chloro-3-(1H-benzo[d]imidazol-2-yl)quinoline derivatives were designed and synthesized as antitumor agents under the combination principle. The antitumor activity and mechanisms were then evaluated.

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Antitumor Activity of Leaves from Hyptis mutabilis (A. Rich.) Briq. (Lamiaceae) in Mice Bearing Tumor

Dataset Papers in Pharmacology ◽

10.7167/2013/169357 ◽

2013 ◽

Vol 2013 ◽

pp. 1-3 ◽

Cited By ~ 2

Author(s):

Rafael Matos Ximenes ◽

Antônio Mario Melo ◽

Lucimeri Paulino Machado Magalhães ◽

Ivone Antonia de Souza ◽

Julianna Ferreira Cavalcanti de Albuquerque

Keyword(s):

Antitumor Activity ◽

Solid Tumor ◽

Folk Medicine ◽

Positive Control ◽

Hot Water ◽

Phytochemical Analysis ◽

Aqueous Extracts ◽

Sarcoma 180 ◽

Anticancer Compounds

The Hyptis genus has more than 400 species, many of them being used in folk medicine to treat several conditions. Some anticancer compounds have been isolated from plants of this genus, and for that reason we decided to investigate the potential in vivo antitumor activity of extracts of leaves of Hyptis mutabilis with different polarities (hexane, methanol, water, and hot water) against two mice tumors: sarcoma 180 and Ehrlich solid tumor. Phytochemical analysis revealed strong presence of steroids, saponins, flavonoids (mainly dihydroflavanols), and catechins. Acute toxicity was perfomed according to the up-and-down method showing LD50 values ranging from 100 up to 2500 mg/kg. Antitumor activity was investigated using 10% of the LD50 for each extract. Methotrexate was used as positive control. Both aqueous extracts showed strong inhibition of tumor growth with values up to 70% of inhibition growth for sarcoma 180. Ehrlich solid tumor was only slight inhibited by hexane extract (38.6%). In conclusion, the aqueous extracts of H. mutabilis showed promising results against sarcoma 180 mice tumor.

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In Vitro and In Vivo Anticancer Activity of Root Extracts ofSansevieria libericaGerome and Labroy (Agavaceae)

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2015/560404 ◽

2015 ◽

Vol 2015 ◽

pp. 1-11 ◽

Cited By ~ 16

Author(s):

Abidemi J. Akindele ◽

Zahoor A. Wani ◽

Sadhana Sharma ◽

Girish Mahajan ◽

Naresh K. Satti ◽

...

Keyword(s):

Antitumor Activity ◽

Anticancer Activity ◽

Solid Tumor ◽

Cytotoxicity Assay ◽

Sarcoma 180 ◽

Lymphoid Leukemia ◽

Root Extracts ◽

Hct 116

Introduction. Sansevieria libericaGerome and Labroy (Agavaceae) is a perennial plant widely distributed in tropical Africa. Preparations of the plant are commonly used across Nigeria for the treatment of inflammatory conditions. Based on the fact that herbal medicine is a strong component of integrative medicine, this study was conducted to evaluate the anticancer activity of root extracts ofSansevieria liberica. Methods.Sulforhodamine B (SRB) in vitro cytotoxicity assay, Sarcoma-180 (S-180) ascites and solid tumor, and L1210 lymphoid leukemia in vivo models were used in this study.Results.SL-A002 (IC5023 µg/mL with HeLa), SL-A003 (IC5022 µg/mL with HCT-116), and SL-A004 (IC5023 and 18 µg/mL with A549 and THP-1, resp.) demonstrated significant activity in the SRB cytotoxicity assay. Potency was highest with the following pairs of extract : cancer cell line: SL-A002 : HeLa (IC5023 µg/mL), SL-A003 : HCT-116 (IC5022 µg/mL), and SL-A004 : THP-1 (IC5018 µg/mL). SL-A002 demonstrated significant dose-dependent antitumor activity in the Sarcoma-180 (S-180) ascites model with peak effect produced at the dose of 120 mg/kg (i.p.) with inhibition of 89.36% compared to 97.96% for 5-FU (20 mg/kg i.p.). The inhibition of tumor growth by SL-A002 in the S-180 solid tumor model was 47.40% compared to a value of 50.18% for 5-FU. SL-A002 was also significantly active in the L1210 lymphoid leukemia model with 158.33% increase in mean survival time, the same value for 5-FU.Conclusions.The hydroethanolic extract ofSansevieria liberica, SL-A002, possesses significant anticancer activity to warrant further extensive study to identify, isolate, and characterize the specific bioactive molecules responsible for the observed antitumor activity and the precise mechanism(s) of action.

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