Differential Pharmacologic Properties of the Two C75 Enantiomers: (+)-C75 Is a Strong Anorectic Drug; (−)-C75 Has Antitumor Activity

Chirality ◽  
2013 ◽  
Vol 25 (5) ◽  
pp. 281-287 ◽  
Author(s):  
Kamil Makowski ◽  
Paula Mera ◽  
David Paredes ◽  
Laura Herrero ◽  
Xavier Ariza ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Anorectic Drug

710: TNF-Related Apoptosis Inducing Ligand (TRAIL/APO-2L): A Novel Mechanism for BCG-Induced Antitumor Activity

2004 ◽  
Vol 171 (4S) ◽  
pp. 188-189
Author(s):  
Aaron T. Ludwig ◽  
Jill M. Moore ◽  
Yi Luo ◽  
Xiaohong Chen ◽  
Michael A. O’Donnell ◽  
...  
Keyword(s):  
Antitumor Activity

Antitumor activity of tricin, a flavone isolated from leaves of Casearia arborea (Salicaceae)

2017 ◽  
Author(s):  
P Sartorelli ◽  
A Santos ◽  
C Figueiredo ◽  
J Lago ◽  
M Soares
Keyword(s):  
Antitumor Activity

Adaptive NK cells with decreased antitumor activity are expanded in HBV-associated HCC

2018 ◽  
Vol 56 (01) ◽  
pp. E2-E89
Author(s):  
C Rennert ◽  
C Tauber ◽  
B Zecher ◽  
A Schuch ◽  
M Hofmann ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Nk Cells

Synthesis of Some New Tetracyclic Pyrimidine Derivatives Using Exocyclic α,β-Unsaturated Ketone and Evaluation of Their Antitumor Activities

2016 ◽  
Vol 12 (8) ◽  
pp. 311-317
Author(s):  
Kamelia El-Mahdy
Keyword(s):  
Antitumor Activity ◽  
Spectroscopic Data ◽  
Acid Hydrazide ◽  
Chloroacetic Acid ◽  
Equimolar Amount ◽  
Unsaturated Ketone ◽  
Cyanoacetic Acid ◽  
Antitumor Activities ◽  
Pyrimidine Derivatives ◽  
Cyanoacetic Acid Hydrazide

Thiazolopyrimidine 2 was obtained from the reaction of dihydropyrimidinone with chloroacetic acid and benzaldehyde. Thiazolopyrimidine 2 containing an α,β-unsaturated ketonic function [-CH=CH-CO-] has been used as a component of Michael addition with an equimolar amount of dinucleophiles to give a series of novel tetracyclic pyrimidine derivatives. Treatment of thiazolopyrimidine 2 with uracil, aminotriazole, cyanoacetic acid hydrazide, o-phenylenediamine or diaminopyridine afforded the corresponding pyridopyrimidine, triazolopyrimidine, pyrazolone, benzodiazepine and triazepine derivative, respectively. The detailed synthesis, spectroscopic data, and antitumor activity for synthesized compounds were reported.

COMPARATIVE STUDY OF THE EFFECTS OF NOS INHIBITOR T1023 AND BEVACIZUMABUM ON GROWTH AND MORPHOLOGY OF LEWIS LUNG CARCINOMA

2019 ◽  
pp. 89-98
Author(s):  
М.В. Филимонова ◽  
В.В. Южаков ◽  
А.С. Филимонов ◽  
В.М. Макарчук ◽  
Л.Н. Бандурко ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Growth Inhibition ◽  
Tumor Cells ◽  
Lung Carcinoma ◽  
Comparative Studies ◽  
Lewis Lung Carcinoma ◽  
Lewis Lung ◽  
Vegf Inhibitor ◽  
Nos Inhibitor ◽  
Experimental Group

Цель исследования - изучение механизмов противоопухолевой активности ингибитора NOS Т1023 и оценка перспективности его дальнейшей разработки. Методика. В качестве опухолевой модели использована эпидермоидная КЛЛ, штамм которой получен из банка опухолевых материалов ФГБУ РОНЦ им. Н.Н. Блохина и поддерживался на самцах мышей C57BL6j. КЛЛ трансплантировали самцам мышей F1 (CBA´C57BL6j) путем подкожного введения 1,5×106 клеток карциномы в 0,1 мл суспензии на основе среды 199 в область латеральной поверхности правого бедра. Для сравнительной оценки противоопухолевой эффективности использовали ингибитор NOS под шифром Т1023, синтезированный в лаборатории радиационной фармакологии МРНЦ им. А.Ф. Цыба, и VEGF-ингибитор бевацизумаб (БВЗ). Животным первой опытной группы ежедневно, со 2 по 20 сутки вводили соединение Т1023 (60 мг/кг, в/б); второй опытной группы - трижды, на 2, 5 и 10 сут вводили БВЗ (12 мг/кг, в/б); третьей опытной группы - по этим схемам и в таких же дозах вводили и Т1023, и БВЗ (при комбинированном применении Т1023 вводили через 4 ч после введения БВЗ). Контрольным животным в качестве плацебо со 2 по 20 сутки вводили 0,9% раствор натрия хлорида (0,2 мл, в/б). Противоопухолевые эффекты оценивали, сравнивая размеры опухолевых узлов, длительность задержки роста и индекс торможения роста опухоли у контрольных и опытных животных. Гистологические методы исследования включали иммуноокрашивание на PCNA, CD31, пимонидазол и морфометрический анализ микроскопических изображений. Результаты сравнительных исследований показали, что соединение Т1023 и VEGF-ингибитор бевацизумаб (БВЗ) оказывают однонаправленное влияние на карциному легких Льюис (КЛЛ), сопровождающееся торможением роста и подавлением метастазирования неоплазии. Воздействие и Т1023, и БВЗ вызывало снижение содержания сосудов в перитуморальных зонах и в «горячих точках» ангиогенеза, усиливало гипоксию паренхимы КЛЛ и стимулировало апоптоз опухолевых клеток. При комбинированном применении Т1023 и БВЗ их антинеопластическая эффективность в отношении ингибирования ангиогенеза и девитализации опухолевых клеток соответствовала аддитивному действию. Заключение. Результаты позволяют предполагать, что основой противоопухолевой активности Т1023 является антиангиогенное действие и свидетельствуют о перспективности применения ингибиторов NOS в ангиостатической терапии солидных злокачественных новообразований в сочетании с имеющимися антинеоваскулярными средствами. The aim. Study of mechanisms of NOS inhibitor T1023 antitumor activity and estimation of its prospects for further development. Methods. Epidermoid Lewis lung carcinoma (LLC) from N.N. Blokhin NMRCO bank of tumor materials was used as a tumor model. Maintenance of tumor cell culture was provided by intramuscular injection of tumor cells suspension to C57BL6j mice every 14 days. Then LLC cells were transplanted to male F1 mice (CBA´C57BL6j) by subcutaneous injection of 1,5×106 cells in 0,1 ml of 199 medium into the lateral surface of the right hip. Comparative studies of antitumor efficacy were carried out using NOS inhibitor T1023, synthesized in the laboratory of radiation pharmacology of A.F. Tsyb MRRC, and VEGF inhibitor Bevacizumab (BVZ). Mice from the first experimental group were injected intraperitoneally (ip) with compound T1023 at dose 60 mg / kg from day 2 to 20; animals from the second experimental group were treated with BVZ at dose 12 mg / kg ip at days 2, 5 and 10; the third experimental group received T1023 in combination with BVZ according to these schemes and at the same doses (T1023 was administered 4 hours after administration of BVZ). Mice from the control group received 0,9% sodium chloride solution (0,2 ml, ip) as a placebo daily from 2 to 20 days. Antitumor effects were assessed by comparing the tumor size, duration of tumor growth delay and the index of tumor growth inhibition in control and experimental groups. Histological examination methods included immunostaining on PCNA, CD31, pimonidazole and morphometric analysis of microscopic images. Results. Comparative studies have shown that compound T1023 and VEGF inhibitor Bevacizumab (BVZ) have unidirectional effects on Lewis lung carcinoma (LLC), accompanied by growth inhibition and suppression of metastasis of neoplasia. The effect of both T1023 and BVZ caused a decrease in vascular content in the peritumoral zones and in the “hot spots” of angiogenesis, increased the hypoxia in the LLC parenchyma, and stimulated apoptosis of tumor cells. The combined use of T1023 and BVZ, caused the antineoplastic efficacy against inhibition of angiogenesis and devitalization of tumor cells which was estimated as additive effect. Conclusion. The results suggest that the basis of antitumor activity of T1023 is the anti-angiogenic effect and indicate the prospects of using NOS inhibitors in the angiostatic therapy of solid malignant neoplasms in combination with available anti-neovascular agents.

SKRINING FITOKIMIA DAN UJI AKTIVITAS ANTIOKSIDAN DAN ANTITUMOR 20 TUMBUHAN OBAT ASAL KABUPATEN MANOKWARI

2008 ◽  
Vol 7 (1) ◽  
Author(s):  
Bimo Budi Santoso
Keyword(s):  
Antioxidant Activity ◽  
Medicinal Plants ◽  
Antitumor Activity ◽  
Traditional Method ◽  
Extraction Efficiency ◽  
Phenolic Content ◽  
Antioxidant Activities ◽  
Total Phenolic ◽  
Phenolic Contents ◽  
Total Phenolic Contents

<strong><em>Flavanoid, steroid, and terpenoid contents of 20 Manokwari medicinal plants were analyzed.  The antioxidant activity, total phenolic contents and antitumor activity of 20 Manokwari medicinal plants were also evaluated. The result shows that 83% positif to flavanoid test, 59% positif to terpenoid test and only 25% positif steroid. Antioxidant activity and total phenolic contents evaluated using Ferric Thiocianate (FTC) and Folin-Ciocalteu methods respectively. Antioxidant activity and total phenolic contents of medicinal plants were extracted by the traditional method, boiling in water and also in 80% methanol. Twenty plants evaluated in both exstracts have significantly varies of antioxidant activities and phenolic contents,  A significant and linier correlation coefficient between the antioxidant activity and the total phenolic content was found in both aqueous (R<sup>2</sup>= 0,77) and methanol (R<sup>2</sup> = 0,85). Antitumor activity was tested using cell maurine P-388 and only 2 of medicinal plants are active to inhibit cell maurine P-388. Comparing extraction efficiency of the two methods, the methanol extracted phenolic compounds more efficiently, and antioxidant activity of the extract was higher.</em></strong>

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