Application progress on anti-skin aging effect of traditional Chinese medicine / 药学学报

With the aging of population intensifies and the level of population health have improved, thus much attention has been directed to how to delaying or preventing skin aging. Skin aging is associated with age, ultraviolet and lifestyle, mainly characterized as skin sagging, wrinkles, pigmentation, so it is urgent to seek traditional Chinese medicine and related cosmetics to solve the problem of skin aging. Traditional Chinese medicine has the functions of anti-oxidation, enhancing human immunity, promoting body metabolism and regulating endocrine, therefore, it has become a research focus in anti-skin aging. This article reviews the skin aging mechanism and the research advances of traditional Chinese medicine anti-skin aging, in order to provide a reference for future research and development of anti-aging traditional Chinese medicine.

Research progress and thinking on improving physicochemical properties and efficacy of the active ingredients in traditional Chinese medicine based on crystal structure / 药学学报

The active ingredients in traditional Chinese medicine have been reported to possess significant pharmacological activity and played an important role in clinical treatments. However, lots of the active ingredients in traditional Chinese medicine suffer from disadvantages such as low solubility, high melting point and low stability that results in low bioavailability and limit its clinical application. Crystal structure plays an important role in improving physicochemical properties and efficacy of the active ingredients in traditional Chinese medicine. This review concludes the research advances of several crystal forms used in the active ingredients in traditional Chinese medicine in terms of polymorph, cocrystal, amorphous/coamorphous and nanocrystal. And the effects of crystal forms on the physicochemical properties and efficacy of the active ingredients in traditional Chinese medicine were reviewed. This research may be useful for the formulation preparation and development of the active ingredients in traditional Chinese medicine.

Design and synthesis of 3'-methyl-furanonucleosides and their anti-tumor activities / 药学学报

Taking 3'-Me-Ado (3'-methyladenosine) and Cladribine as the leading compounds, seventeen 3'-C-methyl-furanonucleosides were designed and synthesized. All the structures were confirmed by 1H NMR and MS. The target compounds were tested in vitro against human pulmonary carcinoma A549, human colon carcinoma LOVO and human leukemia CEM by MTT assay. The results showed that these compounds possessed moderate cytotoxicities.

Synthesis and antibacterial activities of 7-{4-2-2-substituted-4-((5S)-5-acetylaminomethyl-2-oxo-oxazolidin-3-yl)}-phenyl -ethyl-piperazin-1-yl}-fluoroquinolones / 药学学报

<p><b>AIM</b>To find out new oxazolidinone-fluoroquinolone derivatives with high antibacterial activity.</p><p><b>METHODS</b>Some 7-{4-[2-[2-substituted-4-((5S)-5- acetylaminomethyl-2-oxo-oxazolidin-3-yl)-phenyl]-ethyl]-piperazin-1-yl}-fluoroquinolones were designed and synthesized, and their antibacterial activities were tested in vitro.</p><p><b>RESULTS</b>Twenty target compounds were obtained and their structures were confirmed by 1H NMR and MS. The target compounds had high antibacterial activities in vitro, especially, the activity of compound 22 against Enterococcus faecium was 16-fold and 64-fold more potent than that of linezolid and norfloxacin, respectively, and its MIC value against Staphylococcus aureus was 4-fold lower than that of linezolid.</p><p><b>CONCLUSION</b>The oxazolidinone-fluoroquinolone derivatives improved the antibacterial activities.</p>

Synthesis and antibacterial activity of (S) -5-acetylaminomethyl-3-(4-substituted-aminomethyl) phenyl -2-oxazolindinone derivatives / 药学学报

<p><b>AIM</b>To synthesize oxazolindinone derivatives and test their antibacterial activities.</p><p><b>METHODS</b>3-Halo-4-methylaniline was acylated with benzyl chloroformate, followed by cyclization with (R)-glycidyl butyrate, acylation with methanesulfonyl chloride, substitution with NaN3, reduction with H2 + Pd/C or P(OMe)3 + HCl, acylation with Ac2O, and bromination with NBS to form bromides VIIIa and VIIIb, Substitution of the bromides with various amines including aliphatic amine and aromatic amine provided the target compounds IXa and IXb. The in vitro antibacterial activity of the target compounds was tested.</p><p><b>RESULTS</b>Fifty one new compounds were designed and synthesized. And their structures were confirmed by 1H NMR and elemental analyses or MS. Some physical constants such as [alpha]D25 were reported also. Compounds VIIb, IXa1, IXa2, IXa7, IXb1, IXb3, IXb10, IXb16 and IXb23 had moderate in vitro antibacterial activity against G+ bacteria but they were less active than linezolid or norfloxacin.</p><p><b>CONCLUSION</b>Insertion of methylene group between 4-position of phenyl and morpholinyl group in linezolid derivatives can not increase the antibacterial activity.</p>