Antitumor Agents, 119. Kansuiphorins A and B, Two Novel Antileukemic Diterpene Esters from Euphorbia kansui

1991 ◽  
Vol 54 (3) ◽  
pp. 823-829 ◽  
Author(s):  
Tian-Shung Wu ◽  
Yuh-Meei Lin ◽  
Mitsumasa Haruna ◽  
De-Ji Pan ◽  
Tetsuro Shingu ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Diterpene Esters ◽  
Euphorbia Kansui

Vitamin D as potential therapeutic anticancer agent

2018 ◽  
pp. 1-3
Keyword(s):  
Vitamin D ◽  
Anticancer Activity ◽  
Anticancer Agent ◽  
Antitumor Agents ◽  
Metastatic Potential ◽  
Anticancer Properties ◽  
Chemotherapy Agents

The role of vitamin D is implicated in carcinogenesis through numerous biological processes like induction of apoptosis, modulation of immune system inhibition of inflammation and cell proliferation and promotion of cell differentiation. Its use as additional adjuvant drug with cancer treatment may be novel combination for improved outcome of different cancers. Numerous preclinical, epidemiological and clinical studies support the role of vitamin D as an anticancer agent. Anticancer properties of vitamin D have been studied widely (both in vivo and in vitro) among various cancers and found to have promising results. There are considerable data that indicate synergistic potential of calcitriol and antitumor agents. Possible mechanisms for modulatory anticancer activity of vitamin D include its antiproliferative, prodifferentiating, and anti-angiogenic and apoptic properties. Calcitriol reduces invasiveness and metastatic potential of many cancer cells by inhibiting angiogenesis and regulating expression of the key molecules involved in invasion and metastasis. Anticancer activity of vitamin D is synergistic or additive with the antineoplastic actions of several drugs including cytotoxic chemotherapy agents like paclitaxel, docetaxel, platinum base compounds and mitoxantrone. Benefits of addition of vitamin D should be weighed against the risk of its toxicity.

Restoration of intestinal mucosal in Euphorbia kansui-treated severe acute pancreatitis rats is based on HMGB1/MFG-E8 expression

2020 ◽  
Vol 21 ◽  
Author(s):  
Chengjiang Qiu ◽  
Kairui Liu ◽  
Xuguang Li ◽  
Weirun Chen ◽  
Sheng Zhang ◽  
...  
Keyword(s):  
Acute Pancreatitis ◽  
Severe Acute Pancreatitis ◽  
Serum Amylase ◽  
Intestinal Barrier ◽  
Enzyme Linked Immunosorbent Assay ◽  
Inflammatory Factor ◽  
Apoptotic Cells ◽  
Rat Ileum ◽  
Plasma Endotoxin ◽  
Euphorbia Kansui

Background: The pathogenesis of severe acute pancreatitis (SAP) is mediated substantially by dysfunctions in the intestinal barrier. Euphorbia kansui (EK) is a medicinal plant used widely in traditional Chinese medicine to treat inflammation; however, its efficacy and mechanism of action in SAP treatment is not yet well understood. Objective: To investigate the role of EK in intestinal barrier tissue repair and in the pathogenesis and development of SAP. Methods: The rat SAP model was established by a retrograde injection of sodium taurocholate into the pancreatic bile duct. The SAP model group and the SAP + EK treatment groups were divided into 6 subgroups according to timing: 2, 6, 12, 24, 48, or 72 h after inducing SAP. The progression of the SAP rats and of the rats receiving the EK treatment was evaluated using the ascites volume, serum amylase and plasma endotoxin levels, and histological grading of intestinal mucosal damage. In addition, serum inflammatory factor contents were measured using enzyme-linked immunosorbent assay (ELISA) tests and apoptotic cells in damaged ileum tissue were detected using TUNEL staining. Apoptosis markers and other signaling proteins in intestinal mucosal cells were detected by immunohistochemical assays and then validated by combining these data with quantitative polymerase chain reactions and western blotting. Results: Compared with the results of the SAP model rats, the results of the rats that received EK treatment demonstrated that EK could effectively reduce the ascites volume and serum amylase and plasma endotoxin levels. EK treatment also greatly reduced the abnormal intestinal morphological alterations in the rat SAP model and significantly downregulated the serum contents of interleukin (IL)-1β, IL-6, and tumor necrosis factor-α. EK treatment inhibited the elevation of capapse-3, inhibited the decrease of the Bcl-2 protein, and decreased the number of apoptotic cells in rat ileum tissue. Finally, EK treatment abrogated the increase of HMGB1 and the suppression of MFG-E8 protein expression in the SAP + EK rat ileum tissue. Conclusion: EK suppresses SAP pathogenesis by restoring intestinal barrier function and modulating the HMGB1/MFG-E8 signaling axis.

Oxazole: A Promising Building Block for the Development of Potent Antitumor Agents

2016 ◽  
Vol 16 (30) ◽  
pp. 3582-3589 ◽  
Author(s):  
Hua Zhou ◽  
Jiang-Qun Cheng ◽  
Zhi-Sen Wang ◽  
Fei-Hu Chen ◽  
Xin-Hua Liu
Keyword(s):  
Building Block ◽  
Antitumor Agents

Design, Synthesis, In vitro and In silico Evaluation of New Hydrazonebased Antitumor Agents as Potent Akt Inhibitors

2020 ◽  
Vol 17 (11) ◽  
pp. 1380-1392
Author(s):  
Emine Merve Güngör ◽  
Mehlika Dilek Altıntop ◽  
Belgin Sever ◽  
Gülşen Akalın Çiftçi
Keyword(s):  
Cell Line ◽  
Anticancer Agents ◽  
In Silico ◽  
Antitumor Agents ◽  
Colorimetric Assay ◽  
Fibroblast Cell ◽  
Lipinski’S Rule ◽  
In Silico Docking ◽  
Embryonic Fibroblast

Background: Akt is overexpressed or activated in a variety of human cancers, including gliomas, lung, breast, ovarian, gastric and pancreatic carcinomas. Akt inhibition leads to the induction of apoptosis and inhibition of tumor growth and therefore extensive efforts have been devoted to the discovery of potent antitumor drugs targeting Akt. Objectives: The objective of this work was to identify potent anticancer agents targeting Akt. Methods: New hydrazone derivatives were synthesized and investigated for their cytotoxic effects on 5RP7 H-ras oncogene transformed rat embryonic fibroblast and L929 mouse embryonic fibroblast cell lines. Besides, the apoptotic effects of the most active compounds on 5RP7 cell line were evaluated using flow cytometry. Their Akt inhibitory effects were also investigated using a colorimetric assay. In silico docking and Absorption, Distribution, Metabolism and Excretion (ADME) studies were also performed using Schrödinger’s Maestro molecular modeling package. Results and Discussion: Compounds 3a, 3d, 3g and 3j were found to be effective on 5RP7 cells (with IC50 values of <0.97, <0.97, 1.13±0.06 and <0.97 μg/mL, respectively) when compared with cisplatin (IC50= 1.87±0.15 μg/mL). It was determined that these four compounds significantly induced apoptosis in 5RP7 cell line. Among them, N'-benzylidene-2-[(4-(4-methoxyphenyl)pyrimidin- 2-yl)thio]acetohydrazide (3g) significantly inhibited Akt (IC50= 0.5±0.08 μg/mL) when compared with GSK690693 (IC50= 0.6±0.05 μg/mL). Docking studies suggested that compound 3g showed good affinity to the active site of Akt (PDB code: 2JDO). According to in silico ADME studies, the compound also complies with Lipinski's rule of five and Jorgensen's rule of three. Conclusion: Compound 3g stands out as a potential orally bioavailable cytotoxic agent and apoptosis inducer targeting Akt.

Design, Synthesis of Novel Quinazolone Alkaloids Derivatives as Potential Antitumor Agents

2011 ◽  
Vol 7 (4) ◽  
pp. 295-300
Author(s):  
Youguang Zheng ◽  
Min Sun ◽  
Yi Liu ◽  
Mingdong Li ◽  
Min Ji
Keyword(s):  
Antitumor Agents ◽  
Design Synthesis ◽  
Potential Antitumor

Synthesis and Biological Evaluation of Diaryl Ether Linked DC-81 Conjugates as Potential Antitumor Agents

2013 ◽  
Vol 13 (10) ◽  
pp. 1590-1600 ◽  
Author(s):  
Ahmed Kamal ◽  
A. Viswanath ◽  
M. Ramaiah ◽  
J. Murty ◽  
Farheen Sultana ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Biological Evaluation ◽  
Diaryl Ether ◽  
Synthesis And Biological Evaluation ◽  
Potential Antitumor

Copper(II) Complexes with Saccharinate and Glutamine as Antitumor Agents: Cytoand Genotoxicity in Human Osteosarcoma Cells

2017 ◽  
Vol 17 (3) ◽  
pp. 424-433 ◽  
Author(s):  
Juan Cadavid-Vargas ◽  
Ignacio Leon ◽  
Susana Etcheverry ◽  
Eduardo Santi ◽  
Maria Torre ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Osteosarcoma Cells ◽  
Human Osteosarcoma ◽  
Human Osteosarcoma Cells

A Review of Electroporation-based Antitumor Skin Therapies and Investigation of Betulinic Acid-loaded Ointment

2018 ◽  
Vol 18 (5) ◽  
pp. 693-701
Author(s):  
Monika Bakonyi ◽  
Szilvia Berko ◽  
Gabor Eros ◽  
Gabor Varju ◽  
Cristina A. Dehelean ◽  
...  
Keyword(s):  
Betulinic Acid ◽  
High Efficiency ◽  
Antitumor Agents ◽  
Ex Vivo ◽  
Mouse Skin ◽  
Chemotherapeutic Agents ◽  
Hairless Mouse ◽  
Promising Tool ◽  
Acid Formulation ◽  
Invasive Method

Background: Electrochemotherapy is a novel treatment for cutaneous and subcutaneous tumors utilizing the combination of electroporation and chemotherapeutic agents. Since tumors have an increasing incidence nowadays as a result of environmental and genetic factors, electrochemotherapy could be a promising treatment for cancer patients. Objective: The aim of this article is to summarize the novel knowledge about the use of electroporation for antitumor treatments and to present a new application of electrochemotherapy with a well-known plant derived antitumor drug betulinic acid. For the review we have searched the databases of scientific and medical research to collect the available publications about the use of electrochemotherapy in the treatment of various types of cancer. Method: By the utilization of the available knowledge, we investigated the effect of electroporation on the penetration of a topically applied betulinic acid formulation into the skin by ex vivo Raman spectroscopy on hairless mouse skin. Results: Raman measurements have demonstrated that the penetration depth of betulinic acid can be remarkably ameliorated by the use of electroporation, so this protocol can be a possibility for the treatment of deeper localized cancer nodules. Furthermore, it proved the influence of various treatment times, since they caused different spatial distributions of the drug in the skin. Conclusion: The review demonstrates that electrochemotherapy is a promising tool to treat different kinds of tumors with high efficiency and with only a few moderate adverse effects. Moreover, it presents a non-invasive method to enhance the penetration of antitumor agents, which can offer novel prospects for antitumor therapies.

Synthesis and Evaluation of A New Series of Thiazole Derivatives as Potential Antitumor Agents and MMP Inhibitors

2017 ◽  
Vol 17 (5) ◽  
pp. 674-681 ◽  
Author(s):  
Zafer Asim Kaplancikli ◽  
Mehlika Dilek Altıntop ◽  
Ozlem Atli ◽  
Belgin Sever ◽  
Merve Baysal ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Thiazole Derivatives ◽  
Mmp Inhibitors ◽  
Potential Antitumor
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