Most chemical medicines have polymorphs. The difference of medicine polymorphs in physicochemical properties directly affects the stability, efficacy, and safety of solid medicine products. Polymorphs is incomparably important to pharmaceutical chemistry, manufacturing, and control. Meantime polymorphs is a key factor for the quality of high-end drug and formulations. Polymorph prediction technology can effectively guide screening of trial experiments, and reduce the risk of missing stable crystal form in the traditional experiment. Polymorph prediction technology was firstly based on theoretical calculations such as quantum mechanics and computational chemistry, and then was developed by the key technology of machine learning using the artificial intelligence. Nowadays, the popular trend is to combine the advantages of theoretical calculation and machine learning to jointly predict crystal structure. Recently, predicting medicine polymorphs has still been a challenging problem. It is expected to learn from and integrate existing technologies to predict medicine polymorphs more accurately and efficiently.

Objective To investigate the difference of complication incidence, death rate, quantity of lymphadeneetomy, lymphatic metastasis rate and long-term survival rate in thoracic squamons cell carcinoma of esophagus between three fields lymphadenectomy (3-FL) and traditional method. Methods Homoehronous 96 esophageal cancer patients were fractionated in two groups, 46 patients for 3-FL, the other 50 patients for traditional method. Results The average quantity of lymphadenectomy was 39.28 pieces per patient in 3-FL, and was significantly higher than 13.30 pieces per patient in traditional method (P <0.01). The rate of metastatic lymphatic nodes was 73.91%(34/46) in 3-FL patients, significantly higher than38.00%(19/50) in traditional method patients. For incidence of postoperative complications, recurrent laryngeal nerve damage and respiratory complication in 3-FL patients was significantly higher than patients in traditional method (P <0.05). The chest fluid obviously inereasod in 3-FL patients than in traditional method patients. There was significant contrast in 3-year survival rate between 3-FL patients and traditional method patients. Conclusion The there fields lymphadenectomy expand scope of lymphdenectomy effectually, accurate the staging of thoracic esophageal carcinoma. At the same time, a lot of evidence was found in raising survival rate for 3-FL. Disadvantage of 3-FL was severe surgical trauma, high incidence of complication, and a long recovery time after operation.

Objective: To review the systematic reviews of acupuncture for diabetic peripheral neuropathy (DPN) and to provide evidence for clinical decisions. Methods: Published systematic reviews targeting acupuncture treatment of DPN were searched using computer through both Chinese and English databases till July 1, 2019. Two researchers screened the papers based on inclusion and exclusion criteria and conducted report quality evaluation, methodological quality assessment and evidence quality grading using the preferred reporting items for systematic reviews and meta-analyses (PRISMA), assessment of multiple systematic review 2 (AMSTAR 2) and grading of recommendations assessment, development and evaluation (GRADE). Results: Ten systematic reviews were included, involving 11 outcome measures. According to PRISMA, 6 items were sufficiently reported while 1 item was not; AMSTAR 2 appraised that all the included systematic reviews were of low quality in the methodological evaluation; according to GRADE, of the 30 clinical evidences, only 5 were graded moderate while the remained were graded low or extremely low. Descriptive analysis showed that acupuncture can significantly improve DPN symptoms, accelerate the conduction velocities of sensory and motor nerves, and up-regulate the content of plasma nitric oxide (NO), while the adverse reaction rate was low. Conclusion: Acupuncture can produce satisfactory clinical efficacy in treating DPN, but the existing problems, such as low-quality evidence, unitary outcome measures, poor methodological quality of systematic reviews and nonstandard reporting, need to be treated cautiously; meanwhile, more high-quality clinical trials are required to elevate the level of evidence.

Objective To compare the expression of nitric oxide synthase (NOS ) in patients with gastroesophageal reflex disease (GERD)and healthy controls.Methods The distribution and relative protein amount of two NOS subtypes (nNOS and iNOS)were determined with immunohistological method,and their mRNA levels were measured with real-time PCR method.Results The nNOS and iNOS were mostly distributed in the cytoplasm in epithelia of esophageal mucosa.The nNOS and iNOS in reflux esophagitis (RE)were significantly higher than in non-erosive reflux disease (NERD)patients and healthy controls (P <0.05 ).The mRNA levels of nNOS and iNOS were also significantly higher in RE patients than in NERD patients and healthy controls (P <0.05).Conclusion The expressions of nNOS and iNOS were increased in the esophagus of RE patients,which may be related to the effects of NO on the onset of GERD.

OBJECTIVETo explore the correlation between Pi and Shen by observing the relationship between the metabolism of aristolochic acid (AA) and mRNA and protein expression levels of organic anion transporting polypeptide (oatp) superfamily member 2a1 and 2 b1 (oatp2al and oatp2bl) in renal, small intestinal, and large intestinal tissues of Pi deficiency syndrome (PDS) model rats.

METHODSTotally 46 Sprague-Dawley (SD) rats were randomly divided into four groups, i.e., the blank group (n = 12), the PDS group (n = 22), the AA-I group (n = 6), and the PDS AA-I group (n = 6). PDS model was established by subcutaneously injecting Reserpine at the daily dose of 5 mg/kg for 16 successive days. Carotid intubation was performed in 6 rats selected from the blank group and the PDS group. Pharmacokinetics of AA-I were detected at 5, 15, 30, 45, and 60 min after gastrogavage of AA-I. AA-I concentrations in renal, small intestinal, and large intestinal tissues of 10 rats selected from the PDS group were determined. Normal saline was administered to 6 rats selected from the PDS group and the blank group by gastrogavage. Renal, small intestinal, and large intestinal tissues were collected in the AA-I group and the PDS AA-I group at 60 min after gastrogavage of AA-I. mRNA and protein expression levels of oatp2a1 and oatp2b1 in each tissue were detected using real-time polymerase chain reaction (RT- PCR) and Western blot.

RESULTSCompared with the blank group, plasma concentrations of in vivo AA-I were obviously higher in the PDS group at 15, 30, 45, and 60 min after gastrogavage of AA-I with statistical difference (P < 0.05). Plasma concentrations of AA-I were obviously decreased at 60 min after gastrogavage of AA-I; AA-I concentrations in renal and large intestinal tissues were elevated; AA-I concentrations in small intestinal tissues were obviously reduced in the PDS group. There was no statistical difference in mRNA expression levels of oatp2a1 and oatp2b1 in the aforesaid three tissues of rats between the blank group and the PDS group. Compared with the blank group, mRNA expression levels of oatp2a1 and oatp2b1 decreased in small intestinal tissues of the AA-I group, and the mRNA expression level of oatp2a1 in large intestinal tissues significantly decreased (P < 0.05, P < 0.01). Compared with the PDS group, mRNA expression levels of oatp2a1 and oatp2b1 increased in renal tissues of the PDS AA-I group (P < 0.05); mRNA expression levels of oatp2b1 increased in large intestinal tissues of the PDS AA-I group (P < 0.05).

CONCLUSIONSThe difference in AA-I metabolism might be associated with changed expression levels of oatp2a1 and oatp2b1 in renal, small intestinal, and large intestinal tissues under Pi deficiency induced loss of transportation. Shen and Dachang played important roles in substance metabolism under Pi deficiency state, which proved Pi-Shen correlated in Chinese medical theories.

Animals ; Anions ; Aristolochic Acids ; metabolism ; Drugs, Chinese Herbal ; Kidney ; Medicine, Chinese Traditional ; Organic Cation Transport Proteins ; metabolism ; Peptides ; RNA, Messenger ; Rats ; Rats, Sprague-Dawley

Xiatianwu tablet is based on the theory of traditional Chinese medicine (TCM), combined with modern TCM pharmacology and selected 33 famous traditional Chinese crude drugs to compose. Its recipe helps cure rheumatism, relax tendons, promote blood circulation to relieve pain, et al. Although Xiatianwu tablets are widely applied to clinical remedy such as rheumatic arthritis, lumbar disc hernia, osteoarthritis and so on, there is no report about its application in fracture. This article is to observe the efficacy of compound Xiatianwu tablets in elderly patients with osteoporotic distal radius fractures and its impact on the wrist function and complications. 180 elderly patients with osteoporotic distal radius fractures, from January 2011 to June 2014, were divided into observation group and control group by the method of random number table, each group had 90 cases. The control group were gave Caltrate D after manipulative reduction and plaster immobilization, observation group were treated with compound Xiatianwu tablets in the basis of the control group. Efficacy, wrist function and complication rates were observed in two groups after treatment. The excellent and good rate was 95.56% in observation group better than 77.78% in control group, the difference was statistically significant (χ2 = 4.712, P < 0.05). The complication rate in observation group was significantly lower compared with the control group (P < 0.05). This study shows that compound Xiatianwu tablets can improve the efficacy in elderly patients with osteoporotic distal radius fractures, reduce the incidence of complications and relieve the pain of patients which plays a significant role in improving the quality of life.
Aged ; Aged, 80 and over ; Drugs, Chinese Herbal ; administration & dosage ; Female ; Fractures, Bone ; drug therapy ; Humans ; Male ; Middle Aged ; Osteoarthritis ; drug therapy ; Radius Fractures ; drug therapy ; Tablets ; administration & dosage ; Treatment Outcome

Adenocarcinoma ; genetics ; Adult ; Age Factors ; Aged ; Base Sequence ; Carcinoma, Squamous Cell ; genetics ; DNA, Mitochondrial ; genetics ; Female ; Humans ; Lung Neoplasms ; genetics ; Male ; Middle Aged ; Sequence Deletion ; Smoking ; genetics

Background and purpose: Malignant tumors often relapsed or metastasized after first-line chemotherapy and needed second-line or above treatment. We conducted this study to deifne the maximum-tolerated dose (MTD) of lobaplatin with ifxed docetaxel for Chinese patients in previously treated solid tumors. Methods:Escalating doses of lobaplatin with fixed docetaxel were administered in a modified Fibonacci sequence. The initial doses were lobapla-tin 30 mg/m2 and docetaxel 60 mg/m2, respectively. Escalating doses was 5 mg/m2. The regimen was repeated every 21 days. If no dose-limiting toxicity (DLT) was observed, the next dose level was applied. The procedures were repeated until DLT appeared. The MTD was declared to be one dose level below the level at which DLT appeared. Results:Seventeen patients received fifty-eight cycles chemotherapy at lobaplatin of levelⅠ(30mg/m2), levelⅡ(35 mg/m2)and levelⅢ(40 mg/m2). Cases of complete response (CR), partial response (PR), stable disease (SD) and progression disease (PD) for the whole group were 0, 1, 10 and 3, respectively. Response rate (RR, CR+PR) and disease control rate (DCR, CR+PR+SD) were 7.1%(1/14) and 78.6%(11/14), respectively. The most common toxicity was leukopenia. Three DLTs occurred in 3 patients in the whole group, including 2 DLTs in dose levelⅢ. We declared thus levelⅡwas MTD. Conclusion:MTD of lobaplatin in our re-search was 35 mg/m2 combined with fixed dose of docetaxel. This combination regimen was well tolerated.

Objective To report a 33-year-old man with post-headache stroke-like episodes,with whom ischemic changes were found in basal ganglia and occipital-temporal lobe and muscle biopsy revealed abnormal mitochondrial structure and function without regular mutations detected in mtDNA.Methods Gene chip technique was used to detect the mutation of whole sequence of mtDNA,and direct sequencing technique was used to confirm the mutations.Results Three mutations were found.A new mutation in the mitochondrial cytochrome C oxidase subunit 1 (MTCO1),a T→C transition at nucleotide position 6253 resulted in conservative methionine transferring to threonine.His mother also held the mutation,which was not found in 98 control samples.So T6253C was considered the nosogenetic mutation.Conclusion This is the first time to report a mutation in MTCO1 responsible of MELAS.

3 cm)and small lesions(diameter≤3 cm)were 80.6%(79/98)and 67.2% (45/67),respectively(P