The pandemic of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has caused a serious impact on global public health and the economy. SARS-CoV-2 infiltrates host cells via its surface spike protein, which binds to angiotensin-converting enzyme 2 on the host cell membrane. As a result, small molecules targeting spike protein have emerged as a hotspot in anti-SARS-CoV-2 drug research. Activity screening is an important step in seeking small molecule drugs. Therefore, this article aims to review the biological activity evaluation methods of small molecule inhibitors targeting SARS-CoV-2 spike protein, with the goal of laying the foundation for the discovery of new anti-SARS-CoV-2 drugs.

Objective To investigate the effect of omega-3 polyunsaturated fatty acids(ω-3 PUFA)on chronic atrophic gastritis of rats.Methods A rat model of chronic atrophic gastritis was established by synthetic method.The rats successfully modeled were randomly divided into model group,experimental-L group,experimental-M group,experimental-H group,positive control group.Normal rats were selected as the normal group.There were 9 rats in each group.Experimental-L,-M,-H groups were given 3,6 and 12 mL·kg-1ω-3 PUFA daily,respectively.The positive control group was given 0.24 g·kg-1 vitacoenzyme suspension daily.Normal group and model group were given the same amount of 0.9％NaCl.Each group was given the drug for 12 weeks.Enzyme-linked immunosorbent assay(ELISA)was used to detect serum interleukin-1 β(IL-1β)level.In situ end labeling staining(TUNEL)was used to detecte the apoptosis of gastric mucosa.Relevant kits were used to detect the level of superoxide dismutase(SOD)and malonaldehyde(MDA).Results IL-1 β levels in normal group,model group,experimental-L,-M,-H groups and positive control group were(58.96±8.23),(140.02±19.65),(109.81±14.35),(98.72±12.64),(85.31±11.42)and(77.64±10.23)pg·mL-1,respectively;apoptotic indices were(7.89±1.36)％,(77.12±10.05)％,(42.33±6.87)％,(31.05±5.29)％,(22.76±4.16)％and(16.89±3.05)％,respectively;SOD levels were(398.71±58.24),(170.25±29.81),(249.81±34.26),(268.04±34.11),(322.15±46.36)and(276.42±29.81)U·mg-1,respectively;MDA levels were(3.55±0.87),(11.02±2.15),(8.02±1.50),(6.92±1.23),(5.98±1.27)and(6.67±1.32)U·mg-1,respectively.Compared with normal group,the above indexes were significantly different in model group(all P＜0.01);compared with model group,the above indexes were significantly different in experimental-L,experimental-M,experimental-H groups and positive control group(all P＜0.01).Conclusionω-3 PUFA can ameliorate chronic atrophic gastritis of rats,and the mechanism may be related to the anti-inflammatory,anti-apoptosis and anti-oxidative stress effects of to-3 PUFA.

Objective To study the bioequivalence of test and reference olmesartan tablet in Chinese healthy subjects after single dose under fasting and fed conditions.Methods A single-center,random,open,single-dose,two-preparations,double-period,crossover study was adopted.A total of 48 healthy adult male and female subjects(24 cases of fasting test and 24 cases of fed test)were included in the random crossover administration.Single oral dose 20 mg of test and reference were taken under fasting and postprandial conditions,respectively.Plasma concentration of olmesartan in plasma were determined by liquid chromatography tandem mass spectrometry.The main pharmacokinetic parameters were calculated by Phoenix WinNonlin 8.0 software.Results The main pharmacokinetic parameters of the test and reference preparations of olmesartan tablets in the fasting group were as follows:Cmax were(653.06±133.53)and(617.37±151.16)ng·mL-1,AUC0-t were(4 201.18±1 035.21)and(4 087.38±889.99)ng·mL-1·h,AUC0-∞ were(4 254.30±1 058.90)and(4 135.69±905.29)ng·mL-1·h.The main pharmacokinetic parameters of the test and reference preparations of olmesartan tablets in the postprandial group were as follows:Cmax were(574.78±177.05)and(579.98±107.74)ng·mL-1,AUC0-t were(3 288.37±866.06)and(3 181.51±801.06)ng·mL-1·h,AUC0-∞ were(3 326.11±874.26)and(3 242.01±823.09)ng·mL-1·h.Under fasting and postprandial conditions,the 90％confidence intervals of the main pharmacokinetic parameters of the test and reference preparations are both 80.00％-125.00％.Conclusion Under fasting and postprandial conditions,a single oral dose of test and reference preparations olmesartan tablets in Chinese healthy adult volunteers showed bioequivalence.

Objective To explore the influence of Buqi Qingchang Decoction(composed of Buzhong Yiqi Decoction plus Baitouweng Decoction with Curcumae Radix and Curcumae Longae Rhizoma added)combined with XELOX chemotherapy and Bevacizumab targeted therapy on the clinical efficacy,quality of life and survival period of patients with metastatic colorectal cancer of qi deficiency and damp-heat syndrome.Methods A retrospective study was conducted in 70 patients with metastatic colorectal cancer of qi deficiency and damp-heat syndrome who were admitted to the Department of Oncology,Chongqing Hospital of the First Affiliated Hospital of Guangzhou University of Chinese Medicine(Chongqing Beibei District Hospital of Traditional Chinese Medicine)from December 2020 to December 2023.The patients were divided into an observation group and a control group according to the therapy,with 35 cases in each group.The control group was treated with XELOX chemotherapy combined with Bevacizumab targeted therapy,while the observation group was given oral administration of Buqi Qingchang Decoction together with chemotherapy and targeted therapy.The changes in the serum levels of tumor markers such as carcinoembryonic antigen(CEA)and carbohydrate antigen 199(CA199),and Karnofsky Performance Status(KPS)scores for quality of life in the two groups were observed before and after treatment.Moreover,the clinical efficacy,progression-free survival(PFS)and overall survival(OS)were compared between the two groups.Results(1)After treatment,the objective response rate(ORR)and disease control rate(DCR)in the observation group were 51.42％(18/35)and 85.71％(30/35),respectively,which were significantly higher than those in the control group[25.71％(9/35)and 54.29％(19/35),respectively],and the differences between the two groups were statistically significant(P＜0.05 or P＜0.01).(2)The PFS of the observation group was 16.7 months and that of the control group was 12.9 months,and the OS of the observation group was 23.3 months and that of the control group was 17.7 months.The PFS and OS of the observation group were significantly longer than those of the control group,and the differences were statistically significant(P＜0.05 or P＜0.01).(3)After treatment,the levels of serum CEA and CA199 in the two groups were significantly decreased compared with those before treatment(P＜0.05),and the KPS scores were significantly increased compared with those before treatment(P＜0.05).The decrease of serum CEA and CA1 99 levels and the increase of KPS scores in the observation group were superior to those in the control group,and the differences were statistically significant(P＜0.05).Conclusion XELOX chemotherapy and Bevacizumab regimen combined with Buqi Qingchang Decoction exerts certain effect in treating metastatic colorectal cancer.The combined therapy is effective on enhancing the efficacy to a certain extent,prolonging the survival period of patients,reducing the risk of disease progression,decreasing the levels of serum tumor markers,and improving the quality of life of patients.

Objective To investigate the clinical efficacy of Shen Jiang Zhouche Powder(composed of modified Lizhong Pill,Erchen Decoction,and Zhouche Pill)in the treatment of malignant pleural effusion(MPE)patients with fluid retention in the chest and hypochondrium syndrome.Methods Eighty MPE patients with fluid retention in the chest and hypochondrium syndrome were randomly divided into the treatment group and the control group,with 40 cases in each group.Both groups were given conventional western medical treatment,and additionally the control group was treated with Spironolactone and Furosemide Tablets orally while the treatment group was treated with Shen Jiang Zhouche Powder orally.A total of 21 days constituted one course of treatment,and both groups were treated for two courses and then were followed up for one month.The changes of traditional Chinese medicine(TCM)syndrome scores,scores of Karnofsky Performance Status(KPS)established by Eastern Cooperative Oncology Group(ECOG),and scores of self-rating scale of sleep(SRSS)in the two groups were observed before and after treatment.After treatment,the clinical efficacy,TCM syndrome efficacy and clinical safety of the two groups were evaluated.Results(1)After treatment and one-month follow-up,the total clinical effective rate in the treatment group was 67.5%(27/40)and that in the control group was 45.0%(18/40),and the intergroup comparison(by chi-square test)showed that the clinical efficacy of the treatment group was significantly superior to that in the control group(P＜0.05).(2)After two courses of treatment,the total effective rate of TCM syndrome improvement in the treatment group was 92.5%(37/40)and that of the control group was 50.0%(20/40),and the intergroup comparison(by chi-square test)showed that the TCM syndrome efficacy in the treatment group was significantly superior to that in the control group(P＜0.01).(3)After treatment,except for the score of dyspnea in the control group,the scores of each of the main symptoms(including dry cough,chest tightness,chest pain,tightness of breath,dyspnea)and accompanied symptoms as well as the total TCM syndrome scores in the two groups were significantly decreased compared with those before treatment(P＜0.05 or P＜0.01),and the decrease of the scores of each of the main symptoms and accompanied symptoms as well as the total TCM syndrome scores were significantly superior to those in the control group(P＜0.05 or P＜0.01).(4)After treatment,the scores of KPS and SRSS in the two groups were significantly improved compared with those before treatment(P＜0.01),and the improvement in the treatment group was significantly superior to that in the control group(P＜0.05 or P＜0.01).(5)There were no obvious adverse reactions occurring in both groups,while only mild symptoms of the adverse reactions were presented.The incidence of adverse reactions in the treatment group was 7.5%(3/40)and that in the control group was 12.5%(5/40),and the difference was not statistically significant between the two groups(P＞0.05).Conclusion Shen Jiang Zhouche Powder exerts certain clinical efficacy in the treatment of MPE patients with fluid retention in the chest and hypochondrium syndrome,which is effective on alleviating the clinical symptoms of TCM,and improving the quality of life of patients,without obvious toxicity or side effects.

Objective: To establish reference values for carotid intima-media thickness (CIMT) of adult dwellers in Shenzhen City. Methods: The study was conducted based on the Shenzhen heart failure epidemiological survey from 2021 to 2022. In this survey, residents aged 18 years and above in Shenzhen were selected by using a multi-stage stratified random sampling method. General information, cardiovascular disease (CVD) related behavior and carotid ultrasound examination and etc. were collected from the participants. People with CVD factors, a history of atherosclerotic cardiovascular disease, carotid plaque or having no carotid ultrasound examination results were excluded. The parameter regression model based on fractional polynomial was used to establish the reference values of CIMT by age and sex. Results: A total of 2 163 healthy individuals were enrolled in the final analysis, including 576 males (26.6%) and 1 587 females (73.4%). The fractional polynomial regression of the CIMT mean and standard deviation was obtained. For men, the regression was mean_CIMT=0.324 7+0.006 9×age and SD_CIMT=0.076 9+0.001 2×age. For women, the regression was mean_CIMT=0.354 9+0.005 4×age and SD_CIMT=0.041 6+0.002 0×age. Conclusion: The age and sex reference values for CIMT of adult people in Shenzhen established in this study could provide the latest reference standards for early screening of subclinical CVD.
Male ; Humans ; Adult ; Female ; Carotid Intima-Media Thickness ; Cardiovascular Diseases ; Reference Values ; Carotid Arteries/diagnostic imaging* ; Ultrasonography, Carotid Arteries ; Risk Factors ; Carotid Artery Diseases

The paper explores the evolution of "bone-approaching" acupuncture, its effect target and mechanism. The concrete operation procedure of "bone-approaching" method is recorded originally in Huangdi Neijing (Inner Canon of Yellow Emperor) as short needling and Shu needling (referring to the category of the five needling technique). The periosteum is the most effective stimulation target of "bone-approaching" acupuncture for analgesia, regaining consciousness and regulating spirit. The "bone-approaching" acupuncture is not only prominently effective on bone bi syndrome, but also has the unique effect on painful, encephalogenic and emotional diseases. The paper summarizes and improves "bone-approaching" acupuncture, i.e. "touching bone surface" with needle tip by slow insertion, "touching bone surface" without pain by swift insertion and "touching bone" with needle body by oblique insertion. It contributes to the inheritance, development and supplementation to the bone needling techniques in Huangdi Neijing and is significant for broadening the clinical application range of acupuncture.
Humans ; Acupuncture Therapy ; Periosteum ; Analgesia ; Pain Management ; Consciousness ; Pain

Objective: To explore the effects of expanded frontal-parietal pedicled flap in reconstructing cervical scar contracture deformity in children after burns. Methods: A retrospective observational study was conducted. From January 2015 to December 2020, 18 male children with cervical scar contracture deformity after burns who met the inclusion criteria were admitted to Zhengzhou First People's Hospital, aged 4 to 12 years, including 10 cases with degree Ⅱ cervical scar contracture deformity and 8 cases with degree Ⅲ scar contracture deformity, and were all reconstructed with expanded frontal-parietal pedicled flap. The surgery was performed in 3 stages. In the first stage, a cylindrical skin and soft tissue expander (hereinafter referred to as expander) with rated capacity of 300 to 500 mL was placed in the frontal-parietal region. The expansion time was 4 to 6 months with the total normal saline injection volume being 2.1 to 3.0 times of the rated capacity of expander. In the second stage, expander removal, scar excision, contracture release, and flap transfer were performed, with the flap areas of 18 cm×9 cm to 23 cm×13 cm and the secondary wound areas of 16 cm×8 cm to 21 cm×11 cm after scar excision and contracture release. After 3 to 4 weeks, in the third stage, the flap pedicle was cut off and restored. The rated volume of placed expander, total normal saline injection volume, type of vascular pedicle of flap, survival of flap and reconstruction of scar after the second stage surgery were recorded. The neck range of motion and cervico-mental angle were measured before surgery and one-year after surgery. The appearance of neck, occurrence of common complications in the donor and recipient sites of children, and satisfaction of children's families for treatment effects were followed up. Data were statistically analyzed with paired sample t test. Results: All the patients successfully completed the three stages of operation. The rated volume of implanted expander was 300 mL in 6 children, 400 mL in 9 children, and 500 mL in 3 children, with the volume of normal saline injection being 630 to 1 500 mL. The type of vascular pedicle of flap was double pedicle in 13 cases and was single pedicle in 5 cases. All the flaps in 17 children survived well, and the secondary wounds after neck scar excision and contracture release were all reconstructed in one procedure. In one case, the distal blood supply of the single pedicled flap was poor after the second stage surgery, with necrosis of about 2.5 cm in length. The distal necrotic tissue was removed on 10 days after the operation, and the wound was completely closed after the flap was repositioned. In the follow-up of 6 months to 3 years post operation, the cervical scar contracture deformity in 18 children was corrected without recurrence. The flap was not bloated, the texture was soft, and the appearances of chin and neck were good. The range of motion of cervical pre-buckling, extension, left flexion, and right flexion, and cervico-mental angle in one year after operation were improved compared with those before operation (with t values of 43.10, 22.64, 27.96, 20.59, and 88.42, respectively, P<0.01). The incision in the frontal donor site was located in the hairline, the scar was slight and concealed. No complication such as cranial depression was observed in expander placement site, and the children's families were satisfied with the result of reconstruction. Conclusions: Application of expanded frontal-parietal pedicled flap in reconstructing the cervical scar contracture deformity in children after burns can obviously improve the appearance and function of neck, with unlikely recurrence of postoperative scar contractures, thus it is an ideal method of reconstruction.
Burns/surgery* ; Child ; Cicatrix/surgery* ; Contracture/surgery* ; Humans ; Male ; Perforator Flap ; Reconstructive Surgical Procedures/methods* ; Saline Solution ; Skin Transplantation ; Treatment Outcome

Objective: To evaluate the efficiency of internal carotid artery (ICA) embolization technology in endoscopic salvage surgery for recurrent nasopharyngeal carcinoma (rNPC) invading the ICA. Methods: From January 2016 to March 2021, 83 patients with rNPC who invaded the ICA and underwent endoscopic extended nasopharyngectomy were retrospectively collected from the Eye & ENT Hospital in Fudan University, including 60 males and 23 females. The age of the patients ranged from 27 to 77 years. The standard of ICA invasion was that the distance from the lesion to the ICA on enhanced MRI was ≤ 1.8 mm. The clinical characteristics, ICA management strategy and survival prognosis of patients were analyzed, and the effectiveness of ICA embolization was evaluated. Kaplan-Meier method was used to calculate the survival rate and Log-rank test was used to compare the difference. Results: In 83 patients with rNPC, there were 13 patients with rT2, 38 patients with rT3, 32 patients with rT4, and 16 patients had lymph node metastasis. A total of 37 patients (44.6%) underwent ICA coil embolization before surgery, of which 2 cases underwent external carotid-middle cerebral artery artery bypass grafting and ICA embolization due to positive balloon occlusion test (BOT). Patients with positive surgical margin accounted for 24.1% (20/83). Among them, patients with rT4 and patients without ICA embolization had a higher positive rate of surgical margin (P value was 0.001, 0.043, respectively). The 3-year overall survival (OS) and progression free survival (PFS) rate of all patients was 46.5% and 26.7%, respectively. In addition, the 3-year OS and PFS of patients with ICA embolization was significantly higher than those without ICA embolization, respectively (69.1% vs 27.8%, P=0.003; 33.9% vs 18.9%, P=0.018). Only 2 patients (2/37, 5.4%) had cerebral infarction complications after coil embolization of the affected ICA due to negative BOT. Conclusion: Preoperative ICA embolization can be used to treat patients with rNPC invading the ICA, improve the total removal rate and survival rate of patients, which is an effective salvage treatment.
Humans ; Male ; Female ; Adult ; Middle Aged ; Aged ; Nasopharyngeal Carcinoma ; Salvage Therapy ; Retrospective Studies ; Carotid Artery, Internal ; Neoplasm Recurrence, Local/surgery* ; Nasopharyngeal Neoplasms/pathology*

OBJECTIVE: To investigate the clinical effect of double mini-locking plates in the treatment of ulna olecranon fractures. METHODS: From March 2017 to May 2020, 19 patients with olecranon fractures were treated with double mini locking plates, including 12 males and 7 females, aged from 20 to 75 years old with an average of (40.50±7.62) years old;10 patients had the injuries on the left side and 9 patients on the right side. All the 19 patients were fresh closed fractures without ulnar coronoid process fracture, elbow dislocation and other injuries. The fracture healing time and complications were recorded, and the clinical efficacy was evaluated by Mayo elbow performance score (MEPS) before operation and 12 months after operation. RESULTS: All the 19 patientswas followed up, and the duration ranged from 12 to 17 months with an average of (13.51±3.17) months. Postoperative follow-up showed all fractures healed. Fracture healing time ranged from 2 to 6 months, with an average of(3.77±1.24) months. There was no internal fixation fracture, screw loosening, infection, internal fixation irritation, heterotopic ossification, elbow stiffness and other complications occurred. The MEPS score of affected elbow at 12 months after operation was 91.26±3.87, which was significantly different from that before operation 56.18±9.56 ( CONCLUSION It is a reliable fixation method to treat olecranon fracture with double mini locking plate. The incision lengh is small and the fracture fixation is reliable. Elbow joint function exercise can be performed early after operation. Postoperative internal fixation has less skin irritation and satisfactory elbow joint function recovery.
Adult ; Aged ; Bone Plates ; Elbow Joint ; Female ; Fracture Fixation, Internal ; Humans ; Male ; Middle Aged ; Olecranon Process ; Treatment Outcome ; Ulna Fractures ; Young Adult