Primary study of muscone's effect on cardiovascular system

Objective To investigate the effect of muscone on cardiovascular system.Methods Experimental animals to divide muscone high、middle、low dose group(the mouse is 20 mg·kg-1,10 mg·kg-1,5.0 mg·kg-1;the rat is 10 mg·kg-1,5.0 mg·kg-1,2.5 mg·kg-1),GT group(the mouse is 1/12 mg·kg-1;the rat is 1/24 mg·kg-1)and NS group.Intragastric administration in a week,do the mouse ant-hypoxia experiment、the drug(Pit.)produce the rat myocardial ischemia experiment and obstruct coronary artery to produce the rat myocardial ischemia experiment.The mice's survival time(t),the rat's variation of T in electrocardiogram、creatinkinase(CK)and lactate dehydrogenase(LDH)were recorded,respectively.Results The effect of Muscone is significant difference between GT and NS in a dose variation manner.Conclusions Muscone has the effect of ant-hypoxia,cutting down T peak value,reducing CK and LDH.The muscone has effect to inhibiting myocardial ischemia.

Effect of Muscone on Neuronal Glutamate Transporter EAAC1 Expression in Rats with Acute Cerebral Ischemia

Objective: To investigate muscone's neuroprotective action and it s mechanism in rats with acute cerebral ischemic injury. Methods: Rat focal ischemic model of middle cerebral artery occlusion(MCAO) was establi shed by thread inserting method. TTC staining, RT PCR and Western blot analys is were used to study the effects of muscone on infracted volume, EAAC1mRNA and protein levels.Results: Infarcted volume in the muscone treated gr oup was significantly lower than that in the model control group. Compared with normal group, EAAC1 mRNA level increased in the model control group at 6 and 24 hrs, and protein level increased at 24 hrs after modelling, muscone could reduc e the increased expression in model rats. Conclusion: Muscone po ssesses the action of neuroprotection, its mechanism may be related to reduction of EAAC1 and protein expressions.

Enantioselective Hydrogenation of α,β-Unsaturated Cyclic Ketones by Double Asymmetric Induction Preparation of (R)-Muscone

By ketal formation with chiral glycols like methyl or ethyl ester of tartaric acid,hydrogenation of ketals from the correspondingα,β-unsaturated 15-membered cyclic ketone produces (R)-muscone in good chemical and optical yield in the presence of chiral catalysts

Biomimetic synthesis for precursor of muscone

Muscone is a precious fragrant compound scarce in nature. Many attempts have been made to synthesize this unique natural product. In this work, the one-carbon unit transfer reaction of tetrahydrofolate coenzyme was initiated. Benzimidazolium salt was used as the tetrahydrofolate coenzyme model at formic acid oxidation level and di-Grignard reagent as the nucleophile to which one-carbon unit was transferred; the biomimetic synthesis of 2,15-hexade-canedione, a precursor of muscone, was successfully accomplished by using the addition-hydrolysis reaction of benzimidazolium salt with Grignard reagent. And an important useful method for the synthesis of muscone is provided.

Synthesis of(R)-(−)-Muscone from(R)-5-Bromo-4-methylpentanoate:A Chiron Approach

A synthesis of(R)-muscone(1),a valuable musk odorant,is presented.The stereogenic center of muscone was introduced from methyl(R)-5-bromo-4-methylpentanoate(5),a chiral pool molecule developed in our group,and the macrocyclic ring was prepared by ring-closing metathesis(RCM)reaction.

Compatible stability study of Xing NaoJing injection based on physical-chemical properties analysis

Objective:The clinical treatment of brain diseases is urgent. Xingnaojing (XNJ) injection is often used in combination with other injection drugs. Due to the possible interaction between the injections in vivo, the particle size, osmotic pressure, pH value change and component stability decrease, that is one of the important factors causing various adverse reactions. Based on the above situation, this study investigated the physical properties and chemical composition changes of XNJ injection and its compatibility solvent and 13 kinds of clinical injection, speculated the possible interactions between the drugs in vivo from the perspective of in vitro compatibility stability, find out the safety risks of adverse reactions and provide guidance for the safe and rational use of XNJ injection. Methods:According to the clinical application, XNJ injection was mixed with 13 combination injections based on 250 mL 5% glucose injection, and placed at room temperature for 6 h. Then, the clarity, particle size, pH, osmolality, and the contents of camphor, d-borneol, and muscone of the compatible solutions were detected at 0, 1, 2, 4, and 6 h, respectively. Results:The results showed that the physical-chemical properties of compatibility solution were slightly influenced when XNJ was combined with Alprostadil injection and Danhong injection. The change of particle size and the degradation of muscone content were the main factors affecting the compatibility stability of XNJ injection, indicating that there are some problems in compatibility stability, which may be one of the causes of clinical adverse reactions. Conclusion:This study suggests that XNJ injection in combination with other injections during intravenous administration should be performed cautiously.