关键词： scalarane sesterterpenoids   synthesis   natural terpenoids   X-ray analysis  

摘要： Scalarane sesterterpenoids emerged as interesting bioactive natural products which were isolated extensively from marine sponges and shell-less mollusks. Some representatives were also reported recently from superior plants. Many scalarane sesterterpenoids displayed a wide spectrum of valuable properties, such as antifeedant, antimicrobial, antifungal, antitubercular, antitumor, anti-HIV properties, cytotoxicity and stimulation of nerve growth factor synthesis, as well as anti-inflammatory activity. Due to their important biological properties, many efforts have been undertaken towards the chemical synthesis of natural scalaranes. The main synthetic challenges are connected to their complex polycyclic framework, chiral centers and different functional groups, in particular the oxygenated functional groups at the C-12 position, which are prerequisites of the biological activity of many investigated scalaranes. The current work addresses this problem and the synthesis of 17-oxo-20-norscalaran-12 alpha,19-O-lactone is described. It was performed via the 12 alpha-hydroxy-ent-isocopal-13(14)-en-15-al obtained from (-)-sclareol as an accessible starting material. The tetracyclic lactone framework was built following an addition strategy, which includes the intramolecular Michael addition of a diterpenic acetoacetic ester and an intramolecular aldol condensation reaction as key synthetic steps. The structure and stereochemistry of the target compound have been proven by X-Ray diffraction method.

关键词： COVID-19   Multisystem inflammatory syndrome in children (MIS-C)   Cardiac   Myocarditis   Coronary artery aneurysms   Arrhythmia  

摘要： Purpose of Review To review the spectrum of cardiac manifestations and treatments of multisystem inflammatory syndrome in children (MIS-C) associated with coronavirus disease 2019 (COVID-19). Recent Findings Studies demonstrate that up to 80% of children with MIS-C may have cardiac involvement on a spectrum of severity. Cardiac manifestations include myocarditis, coronary artery aneurysms, conduction abnormalities, and arrhythmias. Current treatments, including inotropic support, immunomodulatory therapy, and anti-coagulation, have been effective at resolving these cardiac findings in the majority of patients. COVID-19 can also cause myocarditis in the acute stage of illness and recent descriptions of COVID-19 vaccine myocarditis have occurred. Cardiac manifestations are common in MIS-C and should be assessed for at presentation and during the clinical course as indicated.

关键词： Cannabis sativa L   alternative splicing   non-coding RNAs   gene expression and regulation  

摘要： It is of significance to mine the structural genes related to the biosynthetic pathway of fatty acid (FA) and cellulose as well as explore the regulatory mechanism of alternative splicing (AS), microRNAs (miRNAs) and long non-coding RNAs (lncRNAs) in the biosynthesis of cannabinoids, FA and cellulose, which would enhance the knowledge of gene expression and regulation at post-transcriptional level in Cannabis sativa L. In this study, transcriptome, small RNA and degradome libraries of hemp 'Yunma No.1' were established, and comprehensive analysis was performed. As a result, a total of 154, 32 and 331 transcripts encoding key enzymes involved in the biosynthesis of cannabinoids, FA and cellulose were predicted, respectively, among which AS occurred in 368 transcripts. Moreover, 183 conserved miRNAs, 380 C. sativa-specific miRNAs and 7783 lncRNAs were predicted. Among them, 70 miRNAs and 17 lncRNAs potentially targeted 13 and 17 transcripts, respectively, encoding key enzymes or transporters involved in the biosynthesis of cannabinoids, cellulose or FA. Finally, the crosstalk between AS and miRNAs or lncRNAs involved in cannabinoids and cellulose was also predicted. In summary, all these results provided insights into the complicated network of gene expression and regulation in C. sativa.

关键词： Medicine/Public Health   general   Pediatrics   Pediatric Surgery  

关键词： Hepatocellular carcinoma   Hepatic arterial infusion chemotherapy   Transarterial chemoembolization   treatment failure   unsuitability  

摘要： Objective: This study aimed to assess the efficacy and safety of hepatic arterial infusion chemotherapy (HAIC) with modified FOLFOX (5fluorouracil, leucovorin, and oxaliplatin) as an alternative treatment option in advanced hepatocellular carcinoma (HCC) patients with failed or unsuitability for transarterial chemoembolization (TACE). Materials and Methods: From September 2018 to January 2020, 87 advanced HCC patients who progressed on TACE or were not eligible for TACE received HAIC treatment with modified FOLFOX. The primary endpoint was overall survival (OS) and secondary endpoints included progression-free survival (PFS), tumor response assessed by Response Evaluation Criteria in Solid Tumors 1.1, and adverse events graded according to CTCAE 5.0. Based on prognostic factors determined by multivariate analysis, a nomogram was developed to predict patient survival. Results: The median OS and PFS were 9.0 months (95%CI 7.6-10.4) and 3.7 months (95%CI 3.1-4.3), respectively. The objective response rate was 13.8%, with a disease control rate of 48.3%. Grade 3 adverse events were observed, such as infection (9.2%), thrombocytopenia (5.7%), hyperbilirubinemia (3.4%), abdominal pain (2.3%) and alanine aminotransferase increase (2.3%). Albumin, AST, and extrahepatic metastasis were incorporated to construct a new nomogram that could stratify patients into three prognostic subgroups, including low-, intermediate-, and high-risk groups, with significant differences in 9-month OS rates (71%, 42% and 6%, respectively;p< 0.001). The nomogram was better than the Okuda, AJCC, and CLIP staging systems for OS prediction. Conclusion: These findings support the feasibility of HAIC with modified FOLFOX as an alternative treatment strategy for advanced HCC when TACE is ineffective or unsuitable.

关键词： Acetonitrile  

摘要： Background: Eprinomectin is used as an active pharmaceutical ingredient (API) in various drug products by the animal health industry. Several major related impurities of eprinomectin API are not separated and coelute by the current United States Pharmacopeia (USP) method for eprinomectin. Objective: The aim was to develop and validate a true and reliable stability-indicating reversed-phase (RP) HPLC method for assay and determination of related substances of eprinomectin in bulk batches of eprinomectin API. Method: HPLC analysis is carried out using a Kinetex C8 column (100mm x 4.6mm i.d. , 2.6 mu m particle size) maintained at 30 degrees C with water-acetonitrile-isopropanol (48+42+10, v/v/v) as mobile phase A and 100% acetonitrile as mobile phase B. Analytes are separated by gradient elution at a flow rate of 0.7mL/min and detected by UV at 252nm. The total run time of the method is 30min. Eprinomectin assay and estimation of all eprinomectin-related substances are obtained in a single HPLC run. Results: The HPLC method was able to separate all analytes of interest by gradient elution. The new method was successfully validated according to current The Internal Council for Hamonisation of Technical Requirements for Pharmaceuticals for Human Use (ICH) and International Cooperation on Hamonisation of Technical Requirements for Registration of Veterinary Medicinal Products (VICH) guidelines and was found to be specific, linear, accurate, precise, robust, and sensitive. Conclusions: An HPLC method for assay of eprinomectin and estimation of its related substances was successfully developed, validated, and demonstrated to be accurate, robust, specific, and stability-indicating. Highlights: The HPLC method presented in this paper is more desirable as compared to USP and suitable for routine analysis of bulk batches of eprinomectin API and stability samples in QC laboratories.

摘要： Background: Cocoa butter (CB), an expensive product containing a specific triacylglycerol (TAG)composition, is often the object of economic adulteration. Objective: The present study investigates the detection and quantification of cocoa butter substitutes (CBS) using differential scanning calorimetry. Method: CBS was mixed with CB (from 0 to 100%) as standard samples and analyzed using differential scanning calorimetry and gas chromatography to evaluate the thermal characteristics and fatty acid composition respectively. Results: Increasing the ratio of CBS/CB changed the thermal parameters and fatty acid profiles significantly. For quantification of CBS in commercial samples, medium melting fraction temperature (T(MMF)via r(2) = 0.922) and melting enthalpy (Delta H(f)via r(2) = 0.972) were successfully used to quantify the value of CBS in the samples suspected of being fraudulent. According to the results, all of the thermal parameters increased significantly (P<0.05) with increasing ratio of CBS/CB. It can be attributed to the presence of saturated fatty acids (C12-C22) in CBS which increases T-LMF. Conclusions: The promising results of the present study could be used as a tool for the fast identification of adulteration and quantification of CBS in chocolate compositions. Highlights: Differential scanning calorimetry methods has been developed for identification of CB adulteration. CBS adulteration was detected in CB and also in commercial chocolate samples.

关键词： TWDP fading channel   MGF   M-ary PSK   ASEP  

摘要： Two-wave with diffuse power (TWDP) is one of the most promising models for the description of small-scale fading effects in 5G networks, which employs mmWave band, and in wireless sensor networks deployed in different cavity environments. However, its current statistical characterization has several fundamental issues. Primarily, conventional TWDP parameterization is not in accordance with the model's underlying physical mechanisms. In addition, available TWDP expressions for PDF, CDF, and MGF are given either in integral or approximate forms, or as mathematically untractable closed-form expressions. Consequently, the existing TWDP statistical characterization does not allow accurate evaluation of system performance in all fading conditions for most modulation and diversity techniques. In this regard, physically justified TWDP parameterization is proposed and used for further calculations. Additionally, exact infinite-series PDF and CDF are introduced. Based on these expressions, the exact MGF of the SNR is derived in a form suitable for mathematical manipulations. The applicability of the proposed MGF for derivation of the exact average symbol error probability (ASEP) is demonstrated with the example of M-ary PSK modulation. The derived M-ary PSK ASEP expression is further simplified for large SNR values in order to obtain a closed-form asymptotic ASEP, which is shown to be applicable for SNR > 20 dB. All proposed expressions are verified by Monte Carlo simulation in a variety of TWDP fading conditions.

关键词： Child discomfort   Parental acceptability   Dental caries   SDF   ART  

摘要： Objectives: To compare pain perception of young children treated with SDF and ART, as well as their parents' acceptability of both modalities. Methods: Eighty, 3 to 8-years old children, having at least one deciduous asymptomatic tooth with active caries, as defined by the ICDAS II scores 4, 5, 6 were randomly assigned into two groups;SDF for caries arresting in the test group, and ART for caries removal in the control group. Pain perception was assessed using Sound, Eye, Motor scale (SEM), whereas parental acceptability was assessed using a self-administered questionnaire. Results: Patients treated with SDF reported significantly less discomfort and pain compared to the ART group, with a mean SEM of 3.70 +/- 1.47 and 6.18 +/- 3.06, respectively (p < 0.001). A significantly higher mean parental acceptability score was detected for SDF treatment (31.85 +/- 2.30) than ART treatment (26.75 +/- 3.60), p < 0.001, with regard to the treatment duration, child comfortability and quality of treatment (p < 0.001). The only dimension showing more satisfaction for the ART treatment was esthetics of anterior teeth (p= 0.01). Conclusions: Parental acceptability was higher for the SDF caries treatment of primary teeth compared to ART treatment, especially in relation to the shorter intervention time, child comfortability and acceptance as well as quality of treatment. Clinical Significance: The shorter average time needed and the ease of application of SDF on cavitated primary lesions, in addition to parental acceptability, place SDF in an advantageous position over the ART on clinical level.