Morpho-functional indicators changes of rats’ myocardium in experimental doxorubicin-induced chronic heart failure and its pharmacological modulation with new 4-amino-1,2,4-triazole derivative

Bromide 1 - (β-phenylethyl)-4-amino-1,2,4-triazolium (Hypertril) has the properties of a beta-blocker and of NO-mimetic, is assigned to the IV class of toxicity. All these effects make Hypertril a promising drug for the treatment of cardiovascular diseases. The aim of this paper was to study the cardioprotective action of Hypertril in terms of the effect on the morpho-functional parameters of the myocardium in rats with experimental chronic heart failure (CHF). CHF was modeled on 80 white outbred rats weighing 190–220g by administering doxorubicin at a cumulative dose of 15 mg/kg. Hypertril and the reference drug metoprolol succinate were administered within 30 days after CHF modeling, intragastrically at doses of 3.5 mg/kg and 15 mg/kg. Morphometric analysis of the cellular structure of the myocardium was carried out on an Axioskop microscope (Zeiss, Germany), in an automatic mode using a macro program developed in a specialized programming environment VIDAS-2.5 (Kontron Elektronik, Germany). The administration of Hypertril to animals with CHF led to an increase in the density of nuclei of cardiomyocytes, the area of myocardiocyte nuclei, an increase in the nuclear cytoplasmic ratio and an increase in the concentration of RNA in the nuclei and cytoplasm of cardiomyocytes compared with the group of untreated animals, which indicated the presence of a pronounced cardioprotective effect in the drug candidate. In terms of such indicators as the density of surviving cardiomyocytes and the content of RNA in them, the nuclear-cytoplasmic ratio of Hypertril is significantly (p < 0.05) superior to metoprolol.

Design and Synthesis of New Acridone-Based Nitric Oxide Fluorescent Probe

Nitric oxide (NO) is an important signaling molecule involved in a wide range of physiological and pathological processes. Fluorescent imaging is a useful tool for monitoring NO concentration, which could be essential in various biological and biochemical studies. Here, we report the design of a novel small-molecule fluorescent probe based on 9(10H)acridone moiety for nitric oxide sensing. 7,8-Diamino-4-carboxy-10-methyl-9(10H)acridone reacts with NO in aqueous media in the presence of O2, yielding a corresponding triazole derivative with fivefold increased fluorescence intensity. The probe was shown to be capable of nitric oxide sensing in living Jurkat cells.

Lubrication and Anti-Rust Properties of Jeffamine-Triazole Derivative as Water-Based Lubricant Additive

With the worldwide concern of environmental protection, water-based lubricants exhibit extensive potential applications due to their advantages of energy-conservation, innocuity, and competitive price. Nonetheless, the common lubricating additives currently available in the market are mainly oil-based, while multifunctional water lubricants are rare. This paper reports a sulfur- and phosphorus-free multifunctional additive with high water-solubility, which is applicable for multitype material surfaces. Specifically, through the Mannich reaction method, a Jeffamine-triazole derivative was synthesized from olyetheramine and benzotriazole. Compared with distilled water, the derivative exhibited superior friction reduction and wear resistance properties in water, with the friction reduction rate up to 72.7% and 70.2% for steel/steel and steel/aluminum contacts, respectively, when the concentration of the JD2000 is 2 wt.%. Remarkably, the wear resistance property for steel/aluminum contact is improved by 88.2%. Moreover, the additive showed corrosion inhibition on the metal surface by 75.5%. We further revealed the lubrication and anti-rust mechanisms: the additives are adsorbed on the surfaces through nitrogen atoms, and the long-chain structure of polyether can cover the sliding surfaces, forming a stable viscoelastic film to prevent the severe damages caused by the direct contact between rough friction pairs. Concurrently, the dense protective film can resist the corrosion of environmental media on the metal surface and delay the metal rust. This research may provide a candidate for an ecofriendly multifunctional water-based lubricating additive.