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1.
Chem Pharm Bull (Tokyo) ; 72(4): 389-392, 2024.
Article in English | MEDLINE | ID: mdl-38644164

ABSTRACT

Chagas disease, a neglected tropical disease caused by the protozoan Trypanosoma cruzi poses a significant health challenge in rural areas of Latin America. The current pharmacological options exhibit notable side effects, demand prolonged administration, and display limited efficacy. Consequently, there is an urgent need to develop drugs that are safe and clinically effective. Previously, we identified a quinone compound (designated as compound 2) with potent antiprotozoal activity, based on the chemical structure of komaroviquinone, a natural product renowned for its antitrypanosomal effects. However, compound 2 was demonstrated considerably unstable to light. In this study, we elucidated the structure of the light-induced degradation products of compound 2 and probed the correlation between the quinone ring's substituents and its susceptibility to light. Our findings led to the discovery of quinones with significantly enhanced light stability, some of which exhibiting antitrypanosomal activity. The most promising compound was evaluated for drug efficacy in a mouse model of Chagas disease, revealing where a notable reduction in blood parasitemia.


Subject(s)
Chagas Disease , Quinones , Trypanocidal Agents , Trypanosoma cruzi , Chagas Disease/drug therapy , Animals , Trypanosoma cruzi/drug effects , Mice , Trypanocidal Agents/pharmacology , Trypanocidal Agents/chemistry , Quinones/chemistry , Quinones/pharmacology , Parasitic Sensitivity Tests , Molecular Structure , Light , Disease Models, Animal , Structure-Activity Relationship
2.
Micromachines (Basel) ; 10(2)2019 Feb 20.
Article in English | MEDLINE | ID: mdl-30791588

ABSTRACT

We propose a wireless pressure sensor composed of a graphene sheet and a transmitter coil integrated with a polydimethylsiloxane (PDMS) tube. The pressure inside the tube was monitored wirelessly using an external receiver coil. We then monitored the typical blood pressure range, 12⁻20 kPa, using this fabricated sensor by changing the turn number of the receiver coil and the overlapping length of the coils. Furthermore, we demonstrated wireless blood pressure measurement by connecting our sensor to the blood vessel of a rat. Our results suggested that this sensor can be easily inserted between an implantable medical device and blood vessels for in vivo blood pressure monitoring. The proposed wireless pressure sensor could also be suitable for monitoring in vivo implanted medical systems, such as artificial organs and pump systems.

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