Effects of diisononyl phthalate on lipid metabolism in HepG2 cells / 环境与职业医学

Background Exposure to diisononyl phthalate (DINP), an endocrine disruptor associated with metabolic diseases and widely used in plastic products, has been linked to the development of several adverse health outcomes in the liver, including non-alcoholic fatty liver disease (NAFLD). Objective To investigate the effects and the possible molecular mechanisms of DINP exposure on lipid metabolism in human hepatocellular carcinoma cells (HepG2 cells). Methods First, HepG2 cells were treated with DINP at three time spots (24, 48, and 72 h) and eleven doses (0, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30, and 100 mmol·L−1). Cell viability were detected using cell counting kit 8 (CCK8). Intracellular lipid deposition was determined by oil red O staining and lipid content detection, and triglyceride (TG) and cholesterol (TC) were further detected. Finally, the mRNA expression levels were detected by fluorescence quantitative PCR, including fatty acid synthesis related genes [acetyl-CoA carboxylase alpha (Accα), fatty acid synthase (Fasn), malonyl-CoA decarboxylase (Mlycd), and sterol regulatory element binding protein 1 (Srebp1)] and β-oxidation related genes [peroxisome proliferator activated receptor alpha (Pparα), AMP-activated protein kinase (Ampk), carnitine palmitoyltransferase 1A (Cpt-1a), transcription factor A, mitochondrial (Tfam), nuclear respiratory factor 1 (Nrf1), and peroxisome proliferator-activated receptor gamma and coactivator 1 alpha (Pgc1-α)]. Results Compared with the control group (0 mmol·L−1), the no observed adverse effect levels (NOAEL) of HepG2 cell viability were 0.3, 0.1, and 0.1 mmol·L−1 after 24, 48, and 72 h exposure to DINP, respectively, and the corresponding lowest observed adverse effect levels (LOAEL) were 1, 0.3, and 0.3 mmol·L−1, respectively (P<0.05). After exposure to 30 mmol·L−1 and 100 mmol·L−1 DINP for 24 h, the intracellular lipid content, lipid deposition, TG, and TC levels were increased significantly compared with the control group (P<0.01). Compared with the control group, the mRNA expression levels of genes related to fatty acid synthesis, such as Mlycd, Srebp1, Fasn, and Accα, were down-regulated after the 100 mmol·L−1 DINP exposure for 24 h, while the mRNA expression level of Mlycd was up-regulated in the 30 mmol·L−1 group. The β-oxidation related genes such as Ampk, Pparα, and Tfam were up-regulated significantly after the 100 mmol·L−1 DINP exposure, while Cpt-1a mRNA expression level was down-regulated (P<0.05). Conclusion Exposure to DINP at 30 mmol·L−1 and 100 mmol·L−1 can interfere with fatty acid synthesis and β-oxidation in lipid metabolism of HepG2 cells, resulting in lipid deposition.

Synthesis and antibacterial activities of phosphonate derivatives containing aminothiazoloxime fragment / 药学学报

Based on the principle of molecular hybridization, fifteen compounds were designed and synthesized through the combination of aminothiazoloxime and phosphonate fragment. The results showed that these compounds had better inhibitory effects on the tested bacteria. In particular, the activities of compounds Ⅲf and Ⅲi against S. aureus, E. coli, methicillin-resistant S. aureus (MRSA) and fluoroquinolone-resistant E. coli (FREC) were the most significant, the minimal inhibitory concentration (MIC) of Ⅲf was 1, 8, 4, 16 μg·mL-1 respectively, and the MIC of Ⅲi was 4, 4, 16, 8 μg·mL-1 respectively, which were slightly lower than that of the control drug oxacillin, and their anti-E. coli, MRSA and FREC activities were superior to that of the control drug oxacillin. Their activities to S. aureus were close to that of oxacillin, and to E. coli, MRSA and FREC were superior to that of oxacillin, which is worthy of further study.

Kinase modulators approved by FDA in 2022 / 药学学报

The FDA approved a total of 37 new drugs in 2022, including 22 new molecular entities and 15 new biological products. This is the year with the lowest number of new drugs approved by the FDA since 2017. Among these approved drugs, 21 new drugs belong to the "first-in-class" category, accounting for 56% of the total approved drugs, which is the highest ratio in the past 10 years. Among the drugs approved in 2022, there are 5 small molecule kinase modulators, including the tyrosine kinase 2 (TYK2) allosteric inhibitor deucravacitinib, the first oral pyruvate kinase (PK) activator mitapivat, the Janus kinase 1 (JAK1) selective inhibitor abcrocitinib, the JAK2 selective inhibitor pacritinib and the broad-spectrum fibroblast growth factor receptor (FGFR) inhibitor futibatinib. This review briefly describes the discovery background, research and development process, synthesis routes and clinical efficacy and safety of small molecule kinase modulators approved by the FDA in 2022, hoping to provide ideas and methods for further research on kinase modulators.

Synthesis and biological activities of chlorin e6-based conjugate of fluorouracil as dual-mode antitumor photosensitizer / 药学实践杂志

Objective To design and synthesize the conjugate (compound 1) of chlorin e6 (compound 3) with fluorouracil (5-Fu) as novel pH-responsive dual-mode antitumor photosensitizer by acyl hydrazone bond coupling, based on literature reports that combination of 5-Fu and photosensitizer possess synergistic anti-tumor effect, and investigate its photodynamic antitumor activity and mechanism. Methods Lead compound 3 was obtained by alkali degradation with 25% KOH-CH3OH on pheophorbide a (compound 4) which was prepared through acid hydrolysis of chlorophyll a in crude chlorophyll extracts from silkworm excrement. Reflux reaction of 5-Fu with P2S5 in pyridine formed crude 4-thio-5-fluorouracil which was followed to react with hydrazine hydrate (N2H4·H2O) in CH3OH to give 5-fluorouracil-4-hydrazone (compound 2). Then, treatment of compound 3 i.e. acid alkali degradation product of chlorophyll a in silkworm excrement with EDC·HCl generated its 171- and 152 cyclic anhydride which was followed to directly react with intermediate compound 2 to successfully get title compound 1. In addition, its pH-responsive 5-Fu release and photodynamic antitumor activity and their mechanisms in vitro were investigated. Results Compound 1 could responsively release 5-Fu at pH 5.0, with a cumulative release rate of 60.3% within 24 h. It exhibited much higher phototoxicity against melanoma B16-F10 and liver cancer HepG2 cells than talaporfin and its precursor compound 3, with IC50 value being 0.73 μmol/L for B16-F10 cells and 0.90 μmol/L for HepG2 cells, respectively. Upon light irradiation, it also could significantly induce cell apoptosis and intracellular ROS level and block cell cycle in S phase. Its structure was confirmed by UV, 1H-NMR, ESI-MS and elemental analysis data. Conclusion The conjugate compound 1 of compound 3 and 5-Fu has the advantages of strong PDT anticancer activity, high therapeutic index (i.e. dark toxicity/phototoxicity ratio) and responsively release 5-Fu at pH 5.0 etc. which shows “unimolecular” dual antitumor effects of PDT and chemotherapy and is worthy of further research and development.

Methodology for the Development of Clinical Practice Guidelines for Chinese Patent Medicine（Part 4）： Evidence Retrieval and Evaluation / 中医杂志

The retrieval and evaluation of evidence is the basis for the development of clinical practice guidelines for Chinese patent medicine. As traditional Chinese medicine has a different development trajectory and utilization characteristics from modern medicine， there is certain differences in terms of evidence composition， retrieval and integration.This paper discussed multi-source body of evidence on Chinese patent medicine based on modern evidence-based medicine and ancient medical literature， and summarized the retrieval strategy as well as the possible problems and solving methods. For different types of evidence on Chinese patent medicine， the corresponding evaluation tools have been recommended， and the order to integrate the evidence based on the quality of the evidence from high to low is suggested. Finally， a multi-source based evidence retrieval-evaluation-integration scheme for Chinese patent medicine has been formed， which will provide a methodological reference for practitioners in the development of clinical practice guidelines for Chinese patent medicine.

Ecological and biological patterns of stream fish studies from the Piracicaba-CapivariJundiaí Basin (PCJ Basin, SP) assessed through a systematic review / Padrões ecológicos e biológicos de estudos de peixes de riachos da Bacia PiracicabaCapivari-Jundiaí (Bacia PCJ, SP) avaliados por meio de uma revisão sistemática

Tropical streams are among the most threatened ecosystems in the world. As such, studies carried out and compiled over spatial and temporal scales can provide useful information to examine patterns of species diversity and threats to their survival. Here we conducted a systematic review of published research on biological and ecological aspects of stream fish fauna found in the Piracicaba-Capivari-Jundiaí Basin, an industrial watershed of São Paulo State. We aimed to detect main patterns, trends and gaps in studies related to species composition, distribution, spatial and temporal scales, as well as in the covered topics. Results were related to main land uses, biomes and Conservation Units. A constant increase in published articles occurred from 2003 until 2016 with an average of 1.8 articles/year. Twenty-six publications were considered for the present study, reporting on fish samples obtained in 67 sites and resulting in 89 species. A high proportion of studies were concentrated in the Corumbataí sub-basin, and rarefaction curves indicated that stream fish richness in the PCJ Basin may be considerably higher than that shown by the actual numbers. Basin studies were unevenly distributed and did do not include such highly preserved areas as the Camanducaia, Jaguari and Jundiaí sub-basins. We emphasize the importance of further surveys in these regions, as well as in high priority conservation areas, which may lead to new insights for developing appropriate conservation strategies for this basin.

Riachos tropicais estão entre os ecossistemas mais ameaçados do mundo e a compilação de estudos temporais e espaciais pode fornecer informações úteis para examinar padrões de diversidade de espécies e ameaças nesses sistemas. Realizamos uma revisão sistemática das pesquisas publicadas sobre aspectos biológicos e ecológicos da ictiofauna de riachos da bacia do Piracicaba-Capivari-Jundiaí, uma bacia industrial do Estado de São Paulo. O objetivo foi detectar os principais padrões, tendências e lacunas em estudos relacionados à composição, distribuição de espécies, escalas espaciais, temporais e temas abordados. Os resultados foram relacionados aos principais usos do solo, biomas e Unidades de Conservação. Foi verificado um aumento constante de artigos entre 2003 e 2016, com média de 1,8 artigos/ano. Vinte e seis publicações foram consideradas para o estudo, que indicaram 67 locais amostrados, e o registro de 89 espécies. Uma alta proporção deles concentrou-se na sub-bacia de Corumbataí e curvas de rarefação indicaram que a riqueza de peixes de riacho na bacia do PCJ deve ser consideravelmente maior do que os números atuais. A distribuição desigual de estudos na bacia, que não inclui áreas altamente preservadas como as sub-bacias de Camanducaia, Jaguari e Jundiaí, enfatiza a necessidade de se obter mais informações nessas regiões, bem como em áreas de conservação de alta prioridade. Novas abordagens relacionadas a conceitos e teorias ecológicas em estudos futuros poderão fornecer informações que ajudem a desenvolver estratégias de conservação adequadas para esta bacia.

Keratinase mediated fabrication and partial characterization of gold nanoparticles and its antibacterial potential

Keratinase is mainly involved in recycling of keratin waste. Of late, researchers extended its application to nanotechnology. In the present study, we have made an attempt to fabricate and characterize gold nanoparticles using crude keratinase enzyme from Serratia ficaria and also study their biological application, particularly antibacterial activity. The formation of gold nanoparticles (AuNPs) was first verified by UV-Visible Spectroscopy. FTIR spectra confirmed the presence of responsible secondary metabolites for stabilization of nanoparticles. The morphological characteristics and particle size of synthesized nanoparticles were analyzed. The AuNPs showed significant antibacterial activity against Klebsiella pneumonia, Bacillus cereus and Staphylococcus aureus. The highest radical scavenging activity, 60.62% for AuNPs was observed at 500 µg/mL. Results of this study reveals significance of keratinase application in nano-based biological applications.

Solriamfetol impurities:Synthesis,characterization,and analytical method(UPLC-UV)validation / 药物分析学报

Given that impurities may affect the quality and safety of drug products,impurity identification and profiling is an integral part of drug quality control and is particularly important for newly developed medications such as solriamfetol,which is used to treat excessive daytime sleepiness.Although the high-performance liquid chromatography analysis of commercial solriamfetol has revealed the presence of several impurities,their synthesis,structure elucidation,and chromatographic determination have not been reported yet.To bridge this gap,we herein identified,synthesized,and isolated eight process-related solriamfetol impurities,characterized them using spectroscopic and chromatographic tech-niques,and proposed plausible mechanisms of their formation.Moreover,we developed and validated a prompt impurity analysis method based on ultrahigh-performance liquid chromatography with UV detection,revealing that its selectivity,linearity,accuracy,precision,and quantitation limit meet the acceptance criteria of method validation stipulated by the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use.Thus,the developed method was concluded to be suitable for the routine analysis of solriamfetol substances.

Design, synthesis and antidiabetic activity studies of purine derivatives / 药学学报

Based our previous work, twelve purine derivatives were designed and synthesized as dual modulators of GPR119 and DPP-4by conjugating the GPR119 activating and DPP-4 inhibiting fragments with the position 6 and 9 of purine core via an approach of merged pharmacophores. Compound 11, bearing 2-fluoro-4-methylsulphonyl anilide and cyanopyrrolidine moieties, exhibited the most potent GPR119 agonistic activities (EC50 = 0.33 μmol·L-1, IA = 71.1%) and DPP-4 inhibitory (58.4% inhibition at 10 μmol·L-1, 21.2% inhibition at 1 μmol·L-1) activities in the in vitro antidiabetic study. Subsequently, we performed studies on structure activity relationships and molecular docking to guide the further drug design.

Nurses′ experience and reality dilemma in advance care planning:a qualitative meta-synthesis / 中国实用护理杂志

Objective:To systematically evaluate and integrate the qualitative research of the practical experience and practical difficulties of advance care planning (ACP), so as to provide a reference for subsequent clinical nurses to better carry out ACP.Methods:PubMed, Web of Science, Embase, Cochrane Library, CINAHL, CNKI, Wanfang, VIP, Chinese Biomedical Literature Database were collected the qualitative research on the practical experience and practical difficulties of nurses′advance care planing, and the search time was the database establishment until August 1, 2022. Literature quality evaluation was conducted by the Joanna Briggs Institute (JBI) (2016), and the results were summarized using Meta integration method.Results:A total of 13 studies were included, and 39 studies were summarized into 11 new categories, forming 4 integrated results: nurses′ cognition of ACP practice, emotional experience of nurses′ ACP practice, personal factors that hinder ACP practice, and external environmental factors that hinder ACP practice.Conclusions:In ACP practice, nurses should be actively guided to have positive cognitive and emotional experience to improve their competence in ACP practice. At the same time, government departments should be united to support, integrate hospitals, society and other forces to formulate coping strategies against obstacles, so as to promote the development and practice of ACP.

Meta synthesis of qualitative research on male participation in traumatic childbirth experience / 中国实用护理杂志

Objective:To systematically review the qualitative research on male participation in traumatic childbirth experience, and to provide reference for promoting and improving the physical and mental health and paternity experience of expectant fathers.Methods:Qualitative research on male participation in traumatic childbirth experience published in databases of PubMed, Embase, Web of Science, Spring Link, the Cochrane Library, China National Knowledge Infrastructure (CNKI), China Biomedical Literature Database (CBM) and Wanfang Database were searched from the establishment of the database to June 2022. The quality of literature was evaluated by the quality evaluation standard of Australian JBI Evidence-based Health Care Center, and the pooled integration method in Meta integration was used to integrate the results.Results:A total of 12 articles were included, and 51 main research results were extracted, which were further summarized into 10 categories, and 4 integrated results were formed: men had prominent negative emotional experience; men lack decision-making participation and communication with medical staff during traumatic childbirth; the impact of traumatic childbirth experience on men; perception and coping after traumatic childbirth.Conclusions:Medical staff should pay attention to the emotional experience of men participating in traumatic childbirth, meet their decision-making information needs in the process of accompanying delivery, identify negative emotions in time after delivery and provide help and support, strengthen the family-centered perinatal health service model, promote the physical and mental health of expectant fathers, and improve the family well-being.

Qualitative research on home-based hospice care experiences of nurses: a Meta-synthesis / 中国实用护理杂志

Objective:To systematically review the experience of nurses′ in providing home-based hospice care, so as to provide a basis for improving the quality of home-based hospice care and the nursing service system.Methods:Qualitative researches on nurses′ experience of providing home-based hospice care were retrieved from the Cochrane Library, PubMed,Web of Science, EBSCO, Medline, China National Knowledge Internet, China Biomedical Literature Database, Wanfang Database, VIP Database from inception to April 1, 2022. Adopting Joanna Briggs Institute Critical Appraisal Tool (2016) to evaluate the quality of included studies, the Meta-synthesis was used to explain and integrate the research results.Results:A total of 9 articles were included. This study extracted 23 clear results, 8 new categories, and 3 integrated results, including the significance of nurses′ acceptance of home-based hospice care; positive and negative emotions coexist when nurses provide home-based hospice care; challenges in implementing home-based hospice care.Conclusions:The development of home-based hospice care service is helpful to provide continuous care for the terminally ill patients and improve their quality of life, but at the same time, the ability of home-based hospice care of nurses should be further improved and the related policy guarantee should be perfected to promote the steady development of home-based hospice care in China.

Evidence summary of oral hygiene management in patients with periodontitis / 中国实用护理杂志

Objective:To summarize oral hygiene management approaches applicable to patients with periodontitis, thus provide a basis for decision making by clinical staffs.Methods:Computerized decision systems, various guideline websites, dental association websites, evidence summary databases and journal databases for evidence involving oral hygiene management in patients with periodontitis were searched, including clinical decision making, guidelines, expert consensus, evidence summaries and systematic reviews/Meta-analyses. The search time was from January 2015 to November 2021, and the updated search was carried out in June 2022. Then performed pooled analyses, methodological quality evaluations, and evidence level evaluations.Results:Finally 12 studies, including three guidelines, an expert consensus and eight systematic reviews, and summarized 18 pieces of evidence in three aspects, risk assessment and control, oral hygiene guidance, and clinical practice promotion were included.Conclusions:The evidence from this study is generally scientific and practical, and it should be adapted to local conditions and patient preferences in order to maximize the transfer of evidence into clinical practice.

Attitudes and experiences of medical staff regarding the presence of family members during the administration of CPR: a Meta synthesis / 中国实用护理杂志

Objective:To systematically integrate the attitudes and experiences of medical staffs towards the family presence during resuscitation and provide a reference for the development of family presence during resuscitation clinical practice in China.Methods:To search PubMed, Embase, Web of Science, The Cochrane Library, CINAHL, CNKI, CBM and Wanfang database for qualitative studies on medical staff's attitudes and experiences of family presence during resuscitation since its inception to August 2022. The quality of the literature was evaluated using the Australian JBI Centre for Evidence-Based Health Care (2017) quality assessment criteria for qualitative studies, which were integrated using a pooled integration approach.Results:A total of 12 papers were included to distil the findings of 74 studies, which were summarized to form 10 new categories and 4 consolidated findings including medical staffs′ attitudes towards and reasons for family presence during resuscitation, the impact of family presence during resuscitation on the resuscitation team, the impact of family presence during resuscitation on patients and families, and the real-life dilemmas and recommendations for medical staffs to allow family presence during resuscitation.Conclusions:We should pay attention to the difficulties and needs of family presence during resuscitation by medical staff, take into account the medical context in China, and improve the humanistic care system in our hospitals by considering hospital management, clinical practice, and the demands of patients and their families, in order to improve the accessibility of family presence during resuscitation by the medical staff.

Experience of caesarean section women participating in skin-to-skin contact: Meta-integration qualitative study / 中国实用护理杂志

Objective:To systematically review qualitative research on maternal participation in skin-to-skin contact experience during cesarean delivery, the promotion of skin-to-skin contact in cesarean section.Methods:We searched databases including the PubMed, Embase, Web of Science, Cochrane Library, Ebsco, SinoMed, Wan Fang, CNKI, VIP. All of the qualitative research on the real experience of skin-to-skin contact from the participation of caesarean section women were collected. The search time limit was from the establishment of the databases to May 2022. The JBI Critical Appraisal Tool for qualitative studies from Australia was used to evaluate the methodology quality of the included research, and the meta-aggregation was used to conduct the synthesis.Results:Totally 11 qualified studies were included and integrated into 49 valuable findings. Similar results were summarized into 12 groups, and 4 integrated results were synthesized, including the needs of cesarean section mothers; positive experience after skin-to-skin contact in caesarean section; skin-to-skin contact practice strengthen the role of mothers and promotes breastfeeding; difficulties and challenges of skin-to-skin contact during cesarean section.Conclusions:Skin-to-skin contact positively affects mother and infant delivered by cesarean section. Medical staff need to pay attention to the feelings and needs of cesarean section women participating in skin-to-skin contact, optimize information, environment, and humanistic support, and improve skin-to-skin contact practices. Medical institutions should rationally allocate obstetric resources to alleviate the difficulties faced by skin-to-skin contact practices.

Green synthesis of gold nanoparticles from Sophora flavescens extract and their antibacterial effect against some pathogenic bacteria

Aims@#The current study was aimed to evaluate the antibacterial activity of biogenic synthesized golden nanoparticles from Sophora flavescens Aiton roots aqueous extract against multidrug-resistant (MDR) clinical bacterial isolates.@*Methodology and results@#The green synthesis of gold nanoparticles (AuNPs) was accomplished using S. flavescens roots aqueous extract and examined using many accepted techniques. The antibacterial activity of S. flavescens extract and the aqueous AuNPs at concentrations (7% and 9%) ppm were investigated against two clinical MDR bacteria, including Gram-positive (Staphylococcus aureus) and Gram-negative bacteria (Pseudomonas aeruginosa). The findings demonstrate inhibitory activity against the selected MDR bacterial isolates for the aqueous extract of S. flavescens and the aqueous AuNPs noted by the significant decrease in the number of bacteria after treatment with highly significant differences (P≤0.01) compared to the untreated control.@*Conclusion, significance and impact of study@#Sophora flavescens root extracts and their biosynthesized AuNPs with antibacterial activity may find broad applications in fighting MDR pathogenic bacteria and therapeutic manufacturing.

Effect of superfine powder and aqueous extract of Polygonati Rhizoma on rats with natural perimenopausal syndrome / 中国中药杂志

This study aims to examine the effect of superfine powder and aqueous extract of Polygonati Rhizomaon on natural perimenopausal syndrome in rats and explore the underlying mechanism. To be specific, a total of 60 female SD rats(14-15 months old) with estrous cycle disorder were screened by the vaginal smear and randomized into model control group, β-estradiol 3-benzoate group(0.1 mg·kg~(-1)), superfine powder of Polygonati Rhizoma group(0.25, 0.5 g·kg~(-1)) and aqueous extract of Polygonati Rhizoma group(0.25, 0.5 g·kg~(-1)), and another 10 female SD rats(14-15 months old) were selected as the youth control group. The administration lasted 6 weeks. Then the perimenopausal syndrome-related indexes such as body temperature, microcirculatory blood flow of face and ear, vertigo period, salivary secretion, grip force, and bone strength were determined and open field test was conducted. The immune system-related indexes such as the wet weight and index of thymus and spleen, percentage of T lymphocytes and subgroups in peripheral blood, and hematological indexes were measured. In addition, the ovary-related indexes such as estrous cycle, the wet weight and index of uterus and ovary, ovarian tissue morphology, and cell apoptosis were determined. Moreover, hypothalamus-pituitary-ovary axis(HPO)-related indexes such as serum sex hormone levels, cytochrome P450 family 11 subfamily A member 1(CYP11A1), cytochrome P450 family 19 subfamily A member 1(CYP19A1), and cytochrome P450 family 17 subfamily A member 1(P450 17A1) in ovarian tissue were measured. The results showed that the superfine powder and aqueous extract of Polygonati Rhizoma significantly decreased body temperature(anal, facial and dorsal temperature), microcirculatory blood flow in the ear, and vertigo period, increased salivary secretion, grip force, bone strength, total distance and total speed in the open field test, wet weight and index of thymus and spleen, lymphocyte ratio, CD3~+ level, and CD4~+/CD8~+ ratio, reduced neutrophil number and ratio, estrous cycle disorder ratio, and number of ovarian apoptotic cells, raised wet weight and index of uterus, wet weight of ovary, levels of inhibin B(INHB), estradiol(E_2), anti-müllerian hormone(AMH), and ovarian CYP11A1 and CYP19A1, decreased follicle-stimulating hormone(FSH) and luteinizing hormone(LH) content, and improved ovarian tissue morphology. It is suggested that the superfine powder and aqueous extract of Polygonati Rhizoma can improve the symptoms associated with natural perimenopausal syndrome in rats and enhance ovarian function and immune function. The mechanism is that they regulate HPO axis function by increasing estrogen synthesis.

Advances in physiological activities and synthesis of β-nicotinamide mononucleotide / 生物工程学报

Nicotinamide mononucleotide (NMN) is one of the key precursors of coenzyme Ⅰ (NAD+). NMN exists widely in a variety of organisms, and β isomer is its active form. Studies have shown that β-NMN plays a key role in a variety of physiological and metabolic processes. As a potential active substance in anti-aging and improving degenerative and metabolic diseases, the application value of β-NMN has been deeply explored, and it is imminent to achieve large-scale production. Biosynthesis has become the preferred method to synthesize β-NMN because of its high stereoselectivity, mild reaction conditions, and fewer by-products. This paper reviews the physiological activity, chemical synthesis as well as biosynthesis of β-NMN, highlighting the metabolic pathways involved in biosynthesis. This review aims to explore the potential of improving the production strategy of β-NMN by using synthetic biology and provide a theoretical basis for the research of metabolic pathways as well as efficient production of β-NMN.

Research progress of bio-metal organic frameworks in drug delivery system / 中国药科大学学报

@#In recent years, bio-metal organic frameworks (Bio-MOFs) synthesized with biocompatible ligands have been widely investigated as a potential drug delivery carrier due to their large specific surface area and porosity, rich host-guest intermolecular interactions, and good biocompatibility.In this review, we summarized the design methods of Bio-MOFs including structural and toxic factors, as well as a variety of drug loading methods including click chemistry, with particular focus on recent research advances in Bio-MOFs for pulmonary drug delivery systems, improving pharmaceutical properties of drugs, sustained and controlled drug release, stimulation response and targeted drug delivery systems.Finally, we summarized the bottlenecks that constrain the development of Bio-MOFs in clinical studies of actual pharmaceutical formulations and their future directions for approved formulations, aiming to provide some theoretical reference for promoting the application of Bio-MOFs in drug delivery systems.

Cassiae Semen improves non-alcoholic fatty liver disease through autophagy-related pathway / 中草药·英文版

OBJECTIVE@#Cassiae Semen (CS, Juemingzi in Chinese) has been used for thousands of years in ancient Chinese history for relieving constipation, improving liver function as well as preventing myopia. Here we aimed to elucidate the anti-steatosis effect and underlying mechanism of CS against non-alcoholic fatty liver disease (NAFLD).@*METHODS@#High-performance liquid chromatography (HPLC) was used to identify the major components of CS water extract. Mice were fed with a high-fat and sugar-water (HFSW) diet to induce hepatic steatosis and then treated with CS. The anti-NAFLD effect was determined by measuring serum biomarkers and histopathology staining. Additionally, the effects of CS on cell viability and lipid metabolism in oleic acid and palmitic acid (OAPA)-treated HepG2 cells were measured. The expression of essential genes and proteins involved in lipid metabolism and autophagy signalings were measured to uncover the underlying mechanism.@*RESULTS@#Five compounds, including aurantio-obtusin, rubrofusarin gentiobioside, cassiaside C, emodin and rhein were simultaneously identified in CS extract. CS not only improved the diet-induced hepatic steatosis in vivo, as indicated by decreased number and size of lipid droplets, hepatic and serum triglycerides (TG) levels, but also markedly attenuated the OAPA-induced lipid accumulation in hepatocytes. These lipid-lowering effects induced by CS were largely dependent on the inhibition of fatty acid synthase (FASN) and the activation of autophagy-related signaling, including AMP-activated protein kinase (AMPK), light chain 3-II (LC3-II)/ LC3-1 and autophagy-related gene5 (ATG5).@*CONCLUSION@#Our study suggested that CS effectively protected liver steatosis via decreasing FASN-related fatty acid synthesis and activating AMPK-mediated autophagy, which might become a promising therapeutic strategy for relieving NAFLD.