We designed and synthesized eighteen lycorine derivatives with five different structural types, and evaluated their antiviral activities on a HCoV-OC43-infected H460 cell model. Structure-activity relationships suggested that the introduction of appropriate substituents on the 6N atom of lycorine was beneficial to activity. Compound 6a gave a good activity with the half effective concentration (EC₅₀) and selectivity index (SI) values of 2.36 μmol·L^-1 and 16.52, respectively. Surface plasmon resonance (SPR) result indicated that 6a might target the non-structural protein 12 (NSP12) subunit in RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2 with the dissociation constant (K_D) value of 1.36 μmol·L^-1. Molecular docking indicated that 6a might act on nidovirus RdRp-associated nucleotidyltransferase (NiRAN) catalytic center of NSP12, distinct from the mechanism of nucleoside-like drugs such as remdesivir. This study provides scientific data for the development of lycorine derivatives into a new class of anti-SARS-CoV-2 small molecule inhibitors.

BACKGROUND:Bone transplantation is the only method for the repair of bone defects. However, traditional bone transplantation has some disadvantages. Bone tissue engineering, as a new treatment strategy, can achieve the desire therapeutic outcomes. OBJECTIVE:To fabricate a new tissue-engineered scaffold for improving bone repair effectively. METHODS:Hydroxyapatites (HA) with different Ca/P (1.50/1.67) ratios were synthesized by chemical precipitation method and microwave radiation method. Composite scaffolds of palygorskite (APC)/HA/polycaprolactone (PCL)/col agen (COL), APC/calcium deficiency HA (CDHA)/PCL/COL, and APC/PCL/COL (control group) were prepared by solution perfusion-solvent evaporation and ion leaching method. The material characterization, active ingredients, hydrophilic property, and mechanical properties were evaluated by scanning electron microscope, infrared spectrometer, surface contact measuring instrument and universal mechanics, respectively. The histocompatibility of the implant with the host was assessed through animal experiments. RESULTS AND CONCLUSION:By precise control of pH range, HA with different Ca/P ratios could be synthesized. The mechanical properties, air permeability, hydrophilic property of the APC/HA/PCL/COL and APC/CDHA/PCL/COL composite materials were significantly increased compared with the APC/PCL/COL composite material (P<0.05), while the porosity, water absorption expansion rate were significantly decreased (P<0.05). Results from our animal experiments showed that no immune inflammatory reaction was observed suggesting that the composite materials hold good histocompatibility. To conclude, the APC/HA (1.50/1.67)/PCL/COL composite materials are promising bone substitutes in bone tissue repair.

ObjectiveTo compare differences in life satisfaction, quality of life and mood between UK and Chinese tetraplegia patients after rehabilitation.MethodsThe sample consisted of 44 tetraplegics, 22 from UK and 22 from China, the survey about life satisfaction, quality of life, anxiety and depression was made and analyzed.ResultsPatients of UK group were significantly more satisfied with their situations of vocational and financial, and family life than that in Chinese group, and more active with their value of life, meaning of life and mood than that in Chinese group. No significant differences were identified between two groups in life as a whole, self care, leisure situation, sexual life, partnership relations, contact with friends and ratings of overall quality of life.ConclusionIt is very important to enhance the psychological adaptation of disability so as to improve the quality of life of the tetraplegics in China.

OBJECTIVETo observe the effect of vagal stimulation of different frequencies on heart rate and heart rate variability in the toads.

METHODSThe animals were prepared to be models of isolated heart with right vagosympathetic trunks, then the nerves stimulated by different frequencies. Collected the electrocardiogram of isolated hearts and analyzed the data with HRV software.

RESULTSSince the effect of sympathetic nerve had been diminished, vagal stimulation resulted in HR being markedly attenuated (P < 0.01), SDNN and RMSSD being significantly increased (P < 0.01). There was no significant difference in different levels of frequency. Contrast to group control, HR,SDNN and RMSSD each changed clearly. At the frequency of 0.2 Hz, HF increased markedly (P < 0.01), and LF/HF decreased obviously (P < 0.05) in group P + P. While at the frequency of 0.8 Hz, HF and LF/HF were both around the level of pre-stimulation.

CONCLUSIONThese findings suggest that in the certain electrical stimulation frequency range, the effect of vagal on HR increases along with the frequency. Without the effect of sympathetic nerve, the modulation of vagal to HR and HRV may have different ways.

Animals ; Bufonidae ; physiology ; Electric Stimulation ; Female ; Heart Rate ; physiology ; In Vitro Techniques ; Male ; Vagus Nerve ; physiology

Angiotensin II ; pharmacology ; Animals ; Heart Rate ; drug effects ; physiology ; Rabbits

Objective To evaluate the clinical efficacy of periradicular compound betamethasone injections into the periganglionic space in the treatment of radicular pain.Methods Periganglionic compound betamethasone infiltrations were performed in 76 patients with lumbar radicular pain under MSCT guidance.All patients were divided into two groups including group 1(31 cases of lumbar disc herniation)and group 2(45 cases of lumbar degenerative disorders).The total and two groups scores of VAS were compared after the therapeutic procedure with evaluation of the efficacy.Results 88%(69/76)of patients showed significant pain reduction,with the score of VAS 6.5?2.0(before therapy)dropping to 3.4?1.8(after 1 week)and 3.8?1.9(after 3 month).Differences in improvements before and after the therapy were statistically significant.Differences between one-week and three-month follow-up were not statistically significant.Differences between the two groups demonstrated no statistical significance.Conclusion Periradicular compound betamethasone injection under CT guidance is safe and useful in the treatment of lumbar radicular pain.

Five new megastigmanes (1-5) were isolated from a decoction of Uncaria rhynchophylla by separation techniques of column chromatography using a combination of multiple stationary phases, including macroporous adsorbent resin, MCI resin, silica gel, Sephadex LH-20, and Toyopearl HW-40F, and reversed phase HPLC. Their structures were characterized by spectroscopic data analysis of HR-ESI-MS, NMR, and CD, in combination with Mosher's mothed as well as ECD and NMR calculations. The new compounds were named uncarphyllonone A (1), uncarphyllonols A (2) and B (3), and uncarphabscisic acids A (4) and B (5). Although the structures of 3 and 4 were previously reported, the reported NMR spectroscopic data were incorrect or do not support the assigned structures in literatures. This is also the first report of discovery of new megastigmane natural products from the Uncaria genus.

OBJECTIVETo optimize the formulation of an emollient for treatment of atopic dermatitis prepared using ceramide, sodium hyaluronate, paeonol, and camellia-seed oil.

METHODSThe emollients with different ratios of the 4 components were designed according to the L9(34)orthogonal table with 4 factors and 3 levels. The efficacy of the prepared emollients was tested in 4-6 week-old BALB/c mouse models of atopic dermatitis to determine the optimal formulation of the emollient by evaluating skin water content, transepidermal water loss (TEWL), pharmacodynamics and skin irritation.

RESULTSRange analysis of the orthogonal table and analysis of variance showed that ceramide and camellia seed oil contents had the greatest impact on the skin water content and TEWL, respectively, and the optimal composition of the emollient contained the 4 components at the ratios of D1E1F1G1. Pharmacodynamic experiments showed that at high, medium and low doses, the emollient with the optimal formulation significantly improved the skin water content, pH and TEWL in the mice (P<0.05) with similar effects in the positive control group (P>0.05) and a skin irritation test score of 0.

CONCLUSIONThe emollient we prepared can significantly improve skin water content, pH and TEWL in the mouse model of atopic dermatitis without skin irritations.

OBJECTIVEThis study aimed to establish the reference value range of healthy teeth mobility in Chinese youth.

METHODS200 right side teeth of Han nationality of Chinese youths were measured so as to get the range of the parameters.

RESULTSAll parameters of 14 teeth were achieved. The parameter of TM in mandibular incisor was the highest and in mandibular first molar lowest.

CONCLUSIONIt is very significant to get and quantify the healthy teeth's parameter range. Because they can be served as the healthy contrast when dentists diagnose the mobility. It also reflects the fact that lower the TM parameter is, firmer the tooth will be.

Adult ; Asian Continental Ancestry Group ; statistics & numerical data ; Female ; Humans ; Incisor ; physiology ; Male ; Molar ; physiology ; Reference Values ; Tooth Mobility ; diagnosis

China ; epidemiology ; Cost of Illness ; Diabetes Mellitus ; economics ; mortality ; Humans ; Life Expectancy ; Quality of Life ; Quality-Adjusted Life Years