scholarly journals Chemical Constituents of Anacardium occidentale as Inhibitors of Trypanosoma cruzi Sirtuins

Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1299 ◽  
Author(s):  
Tanira Matutino Bastos ◽  
Helena Mannochio Russo ◽  
Nilmar Silvio Moretti ◽  
Sergio Schenkman ◽  
Laurence Marcourt ◽  
...  

Benznidazole and nifurtimox, the only drugs available for the treatment of Chagas disease, have limited efficacy and have been associated with severe adverse side effects. Thus, there is an urgent need to find new biotargets for the identification of novel bioactive compounds against the parasite and with low toxicity. Silent information regulator 2 (Sir2) enzymes, or sirtuins, have emerged as attractive targets for the development of novel antitrypanosomatid agents. In the present work, we evaluated the inhibitory effect of natural compounds isolated from cashew nut (Anacardium occidentale, L. Anacardiaceae) against the target enzymes TcSir2rp1 and TcSir2rp3 as well as the parasite. Two derivates of cardol (1, 2), cardanol (3, 4), and anacardic acid (5, 6) were investigated. The two anacardic acids (5, 6) inhibited both TcSir2rp1 and TcSir2rp3, while the cardol compound (2) inhibited only TcSir2rp1. The most potent sirtuin inhibitor active against the parasite was the cardol compound (2), with an EC50 value of 12.25 µM, similar to that of benznidazole. Additionally, compounds (1, 4), which were inactive against the sirtuin targets, presented anti-T. cruzi effects. In conclusion, our results showed the potential of Anacardium occidentale compounds for the development of potential sirtuin inhibitors and anti-Trypanosoma cruzi agents.

2010 ◽  
Vol 58 (9) ◽  
pp. 5341-5346 ◽  
Author(s):  
Jennifer Trox ◽  
Vellingiri Vadivel ◽  
Walter Vetter ◽  
Wolfgang Stuetz ◽  
Veronika Scherbaum ◽  
...  

2011 ◽  
Vol 128 (4) ◽  
pp. 1094-1099 ◽  
Author(s):  
Jennifer Trox ◽  
Vellingiri Vadivel ◽  
Walter Vetter ◽  
Wolfgang Stuetz ◽  
Dietmar R. Kammerer ◽  
...  

2017 ◽  
Vol 2017 ◽  
pp. 1-12 ◽  
Author(s):  
Yoon Kyoung Lee ◽  
Eun Young Hong ◽  
Wan Kyunn Whang

Blocking the polyol pathway plays an important role preventing diabetic complications. Therefore, aldose reductase (AR) and advanced glycation endproducts (AGEs) formation has significant effect on diabetic complications. Artemisia iwayomogi has long been used as treatment of various diseases in Korea. However, no literatures have reported on AR and AGEs formation inhibitory activities of A. iwayomogi. For these reasons, we aimed to assess that A. iwayomogi had potential as anti-diabetic complications agents. We led to isolation of two coumarins (1 and 2), nine flavonoids (3–11), five caffeoylquinic acids (12–16), three diterpene glycosides (17–19), and one phenolic compound (20) from A. iwayomogi. Among them, hispidulin (4), 6-methoxytricin (6), arteanoflavone (7), quercetin-3-gentiobioside (10), 1,3-di-O-caffeoylquinic acid (13), and suavioside A (18) were first reported on the isolation from A. iwayomogi. Not only two coumarins (1 and 2), nine flavonoids (3–11), and five caffeoylquinic acids (12–16) but also extracts showed significant inhibitor on AR and AGEs formation activities. We analyzed contents of major bioactive compounds in Korea’s various regions of A. iwayomogi. Overall, we selected Yangyang, Gangwon-do, from June, which contained the highest amounts of bioactive compounds, as suitable areas for cultivating A. iwayomogi as preventive or therapeutic agent in the treatment of diabetic complications.


2020 ◽  
Vol 157 ◽  
pp. 104686 ◽  
Author(s):  
Ana Beatriz Zanqui ◽  
Claudia Marques da Silva ◽  
Jéssica Barrionuevo Ressutte ◽  
Damila Rodrigues de Morais ◽  
Jandyson Machado Santos ◽  
...  

Author(s):  
N. I. Chalisova ◽  
V. K. Kozlov ◽  
A. B. Mulik ◽  
E. P. Zatsepin ◽  
T. A. Kostrova

An urgent problem is the search for substances that can provide a protective effect in cases of DNA synthesis and repair disorders that arise as a result of side effects of cytostatic drugs used in the treatment of cancer. The aim of this work was to study the effect of 20 encoded amino acids in the presence of Cyclophosphane on the development of organotypic culture of rat liver tissue. The results obtained indicate that Cyclophosphane; which simulates the action of such cytostatic substances; inhibits cell proliferation in the liver tissue. It was also found that the encoded amino acids: asparagine; arginine; and glutamic acid; eliminate the inhibitory effect of Cyclophosphane in liver tissue culture. The growth zone of explants after combined exposure to Cyclophosphane (whose isolated action suppressed the growth zone) and these amino acids increased significantly and reached control values. Thus; the experimental data create the basis for the development of methods for the therapeutic use of the three studied amino acids for the removal of side effects in the treatment with cytostatic drugs.


2020 ◽  
Author(s):  
Laura Lafon-Hughes

BACKGROUND COVID-19 pandemic prompts the study of coronavirus biology and search of putative therapeutic strategies. OBJECTIVE To compare SARS-CoV-2 genome-wide structure and proteins with other coronaviruses, focusing on putative coronavirus-specific or SARS-CoV-2 specific therapeutic designs. METHODS The genome-wide structure of SARS-CoV-2 was compared to that of SARS and other coronaviruses in order to gain insights, doing a literature review through Google searches. RESULTS There are promising therapeutic alternatives. Host cell targets could be modulated to hamper viral replication, but targeting viral proteins directly would be a better therapeutic design, since fewer adverse side effects would be expected. CONCLUSIONS Therapeutic strategies (Figure 1) could include the modulation of host targets (PARPs, kinases) , competition with G-quadruplexes or nucleoside analogs to hamper RDRP. The nicest anti-CoV options include inhibitors of the conserved essential viral proteases and drugs that interfere ribosome slippage at the -1 PRF site.


Planta Medica ◽  
2021 ◽  
Author(s):  
Qian Yang ◽  
An Jia ◽  
Xizi Liu ◽  
Shiyi Han ◽  
Siyang Fan

AbstractA new sesquiterpene, chlorantholide G (1), a new sesquiterpene dimer, elatiolactone (2), and 2 new diterpenes, elatiorlabdane B (3) and elatiorlabdane C (4), together with 51 known compounds, were isolated from the aerial parts of Chloranthus elatior. The new structures including their absolute configurations were mainly established by mass spectrometric, NMR, and electronic circular dichroism experiments. All isolated compounds were tested for their anti-hDHODH activity. (4S,6R)-4-hydroxy-6-isopropyl-3-methylcyclohex-2-enone (5) and (4S,5R,9S,10R)-8(17),12,14-labdatrien-18-oic acid (29) were the most active compounds with IC50 values of 18.7 and 30.7 µM, respectively.


The Analyst ◽  
2021 ◽  
Author(s):  
Chang Shu ◽  
Tengfei Li ◽  
Duo Li ◽  
Zhong-Qiu Li ◽  
Xing-Hua Xia

Protein drugs showing strong pharmaceutical activity, high specificity, low toxicity and side effects, have drawn extensive attention from the field of life science and medicine. Precise evaluation of the function...


Sign in / Sign up

Export Citation Format

Share Document