OBJECTIVE:To determine the content of acetic acid in Octreotide acetate for injection by IEC,and provide reference for the improvement of pharmacopoeia standards. METHODS:The column was Rezex ROA-Organic Acid H+ with mobile phase of 0.002 5 mol/L sulfuric acid at a flow rate of 0.5 ml/min,the detection wavelength was 210 nm,column temperature was 45℃,and in-jection volume was 100 μl. RESULTS:The linear range of acetic acid was 0.394 4 μg/ml-78.89 μg/ml(r=0.999 9);RSDs of preci-sion,stability and reproducibility tests were all lower than 2%;the limit of quantification was 197.2 ng/ml,and limit of detection was 78.89 ng/ml;recovery was 104.71%-109.78%(RSD=1.34%,n=9). CONCLUSIONS:The method is environmental and simple with good accuracy and precision,and suitable for the content determination of acetic acid in Octreotide acetate for injection.

Cycloheximide (CHX) inhibits protein synthesis in most eukaryotic cells and it is a well-known tool commonly used in biochemical research. In this paper, the antiviral spectrum of CHX against several DNA and RNA viruses have been evaluated. CHX showed strong inhibitory activities against several RNA viruses such as HIV-1, influenza viruses, coxsackie B virus, enterovirus (EV71) and several DNA viruses such as HSV and HCMV. Especially the strong inhibitory activities of CHX against coxsackie B virus and enterovirus caught our attention, since effective drugs available in clinic are limited. The SAR of CHX derivatives also has been discussed in the paper. The hydroxyl group at C-2' and carbonyl group at C-2" of CHX are essential for its antiviral activity. And modification to these groups results its derivatives' antiviral activities reduced or lost.

OBJECTIVE: To observe the clinical efficacy of methycobal iontophoresis combined with balance acupuncture in the treatment of peripheral facial paralysis. METHODS: A total of 108 patients with peripheral facial paralysis were randomly divided into a methycobal iontophoresis combined with balance acupuncture group (a combined group), a methycobal iontophoresis group and a simple balance acupuncture group, 36 cases in each one. Basic medical treatment were given in the three groups. The simple balance acupuncture was applied at contralateral lumbago acupoint, rhinitis acupoint, stomachache acupoint in the simple balance acupuncture group. Methycobal through iontophoresis anodic introduction therapy was given in the methycobal iontophoresis group. On the basic treatment of methycobal iontophoresis, in the combined group, acupuncture was supplied at contralateral lumbago acupoint, rhinitis acupoint and stomachache acupoint. The treatment in all groups was given once a day, for 2 weeks. The House-Brackmann grading scale and the modified portmann score (RPA) method were used to observe the degree of nerve function and facial paralysis before and after treatment, and the clinical efficacy of each group was evaluated. RESULTS: The total effective rate of the combined group was 97.2% (35/36), which was higher than 83.3% (30/36) in the methycobal iontophoresis group and 88.9% (32/36) in the simple balance acupuncture group (all <0.05). After treatment, the H-B classification of the combined group was significantly different from those of the methycobal iontophoresis group and simple balance acupuncture group (both <0.05). There was no significant difference between the methycobal iontophoresis group and simple balance acupuncture group (>0.05). The RPA score of the combined group was higher than those in the methycobal iontophoresis group and simple balance acupuncture group (both <0.05), and there was no significant difference in the RPA score between the methycobal iontophoresis group and simple balance acupuncture group (>0.05). CONCLUSION Compared with methycobal iontophoresis and simple balance acupuncture therapy, methycobal iontophoresis combined with balance acupuncture therapy can effectively improve the clinical symptoms and signs of peripheral facial paralysis.
Acupuncture Therapy ; Facial Paralysis ; Humans ; Iontophoresis ; Treatment Outcome

A series of novel indole-2-carboxylate derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities. The biological results showed that some of the synthesized compounds exhibited potent broad-spectrum antiviral activity. Notably, compound 8f showed the highest SI value (17.1) to Cox B3 virus. Compound 14f showed both potent inhibitory activity against influenza A (IC50=7.53 μmol/L) and the highest SI value (12.1). SAR results showed that the alkyloxy at the 4-position of indole ring was not crucial to the antiviral activities. Incorporation of an acetyl substituent at the amino group disfavored antiviral activity towards RNA viruses.

A series of novel N-phenylbenzamide and N-phenylacetophenone compounds were synthesized and evaluated for their antiviral activity against HCV and EV71 (strain SZ-98). The biological results showed that three compounds (23, 25 and 41) exhibited considerable anti-HCV activity (IC50=0.57-7.12 μmol/L) and several compounds (23, 28, 29, 30, 31 and 42) displayed potent activity against EV71 with the IC50 values lower than 5.00 μmol/L. The potency of compound 23 (IC50=0.57 μmol/L) was superior to that of reported compounds IMB-1f (IC50=1.90 μmol/L) and IMB-1g (IC50=1.00 μmol/L) as anti-HCV agents, and compound 29 possessed the highest anti-EV71 activity, comparable to the comparator drug pirodavir. The efficacy in vivo and antiviral mechanism of these compounds warrant further investigations.

Polymyxin B and polymyxin E (colistin) are presently considered the last line of defense against human infections caused by multidrug-resistant Gram-negative organisms such as carbapenemase-producer Enterobacterales, Acinetobacter baumannii, and Klebsiella pneumoniae. Yet resistance to this last-line drugs is a major public health threat and is rapidly increasing. Polymyxin S₂ (S₂) is a polymyxin B analogue previously synthesized in our institute with obviously high antibacterial activity and lower toxicity than polymyxin B and colistin. To predict the possible resistant mechanism of S₂ for wide clinical application, we experimentally induced bacterial resistant mutants and studied the preliminary resistance mechanisms. Mut-S, a resistant mutant of K. pneumoniae ATCC BAA-2146 (Kpn2146) induced by S₂, was analyzed by whole genome sequencing, transcriptomics, mass spectrometry and complementation experiment. Surprisingly, large-scale genomic inversion (LSGI) of approximately 1.1 Mbp in the chromosome caused by IS26 mediated intramolecular transposition was found in Mut-S, which led to mgrB truncation, lipid A modification and hence S₂ resistance. The resistance can be complemented by plasmid carrying intact mgrB. The same mechanism was also found in polymyxin B and colistin induced drug-resistant mutants of Kpn2146 (Mut-B and Mut-E, respectively). This is the first report of polymyxin resistance caused by IS26 intramolecular transposition mediated mgrB truncation in chromosome in K. pneumoniae. The findings broaden our scope of knowledge for polymyxin resistance and enriched our understanding of how bacteria can manage to survive in the presence of antibiotics.