E93 is indispensable for reproduction in ametabolous and hemimetabolous insects.

Ecdysone-induced protein 93 (E93), known as the "adult-specifier" transcription factor in insects, triggers metamorphosis in both hemimetabolous and holometabolous insects. While E93 is conserved in ametabolous insects, its spatiotemporal expression and physiological function remain poorly understood. In this study, we first discovered that in the ametabolous firebrat Thermobia domestica, the previtellogenic ovary exhibits cyclically high E93 expression, and E93 mRNAs are broadly distributed in previtellogenic ovarioles. E93 homozygous mutant females of T. domestica exhibit severe fecundity deficiency due to impaired previtellogenic development of the ovarian follicles, likely because E93 induces the expression of genes involved in ECM (extracellular matrix)-receptor interactions during previtellogenesis. Moreover, we revealed that in the hemimetabolous cockroach Blattella germanica, E93 similarly promotes previtellogenic ovarian development. In addition, E93 is also essential for vitellogenesis to guarantee ovarian maturation and promotes the vitellogenesis-previtellogenesis switch in the fat body of adult female cockroaches. Our findings deepen the understanding of the roles of E93 in controlling reproduction in insects and of E93 expression and functional evolution, which are proposed to have made crucial contributions to the origin of insect metamorphosis.

Patient satisfaction and follow-up adherence to glaucoma case management clinic in China.

AIM: To assess glaucoma patient satisfaction and follow-up adherence in case management and identify associated predictors to improve healthcare quality and patient outcomes. METHODS: In this cross-sectional study, a total of 119 patients completed a Patient Satisfaction Questionnaire-18 and a sociodemographic questionnaire. Clinical data was obtained from the case management system. Follow-up adherence was defined as completing each follow-up within ±30d of the scheduled time set by ophthalmologists during the study period. RESULTS: Average satisfaction scored 78.65±7, with an average of 4.39±0.58 across the seven dimensions. Age negatively correlated with satisfaction (P=0.008), whilst patients with follow-up duration of 2 or more years reported higher satisfaction (P=0.045). Multivariate logistics regression analysis revealed that longer follow-up durations were associated with lower follow-up adherence (OR=0.97, 95%CI, 0.95-1.00, P=0.044). Additionally, patients with suspected glaucoma (OR=2.72, 95%CI, 1.03-7.20, P=0.044) and those with an annual income over 100 000 Chinese yuan demonstrated higher adherence (OR=5.57, 95%CI, 1.00-30.89, P=0.049). CONCLUSION: The case management model proves effective for glaucoma patients, with positive adherence rates. The implementation of this model can be optimized in the future based on the identified factors and extended to glaucoma patients in more hospitals.

Effects of different storage containers on the flavor characteristics of Jiangxiangxing baijiu.

Storage is a key factor controlling the quality of Jiangxiangxing baijiu, and storage time and the type of storage container play crucial roles in shaping the baijiu's distinct flavor. To investigate the influence of storage containers on the flavor characteristics of Jiangxiangxing baijiu, the sensory qualities, flavor components, and metal ions of Jiangxiangxing baijiu were measured during 24 months of storage in a pottery jar or a stainless steel tank. The results showed that Jiangxiangxing baijiu preserved in a pottery jar was superior to that stored in a stainless steel tank. A total of 96 flavor substances were detected, and 17 key flavor characteristic substances were screened by combining the results of odor activity values (OAV) and orthogonal partial least squares-discriminant analysis (OPLS-DA). A correlation heat map and redundancy analysis (RDA) showed that aluminum, cadmium, iron, cobalt, magnesium, potassium, and copper ions promoted the formation of key characteristic substances including diethoxymethane, lactic acid, 2,3-dimethyl-5-ethylpyrazine, 1-hexanol, and 2-methyl-1-propanol. Overall, the results show that 24-month pottery jar storage can promote the flavor quality of Jiangxiangxing baijiu. This study established a theoretical foundation to select the appropriate storage conditions and control the flavor quality of Jiangxiangxing baijiu.

Interpretable thoracic pathologic prediction via learning group-disentangled representation.

Deep learning has brought a significant progress in medical image analysis. However, their lack of interpretability might bring high risk for wrong diagnosis with limited clinical knowledge embedding. In other words, we believe it's crucial for humans to interpret how deep learning work for medical analysis, thus appropriately adding knowledge constraints to correct the bias of wrong results. With such purpose, we propose Representation Group-Disentangling Network (RGD-Net) to explain the process of feature extraction and decision making inside deep learning framework, where we completely disentangle feature space of input X-ray images into independent feature groups, and each group would contribute to diagnose of a specific disease. Specifically, we first state problem definition for interpretable prediction with auto-encoder structure. Then, group-disentangled representations are extracted from input X-ray images with the proposed Group-Disentangle Module, which constructs semantic latent space by enforcing semantic consistency of attributes. Afterwards, adversarial constricts on mapping from features to diseases are proposed to prevent model collapse during training. Finally, a novel design of local tuning medical application is proposed based on RGB-Net, which is capable to aid clinicians for reasonable diagnosis. By conducting quantity of experiments on public datasets, RGD-Net have been superior to comparative studies by leveraging potential factors contributing to different diseases. We believe our work could bring interpretability in digging inherent patterns of deep learning on medical image analysis.

Effects of biochar on plant growth and hydro-chemical properties of recycled concrete aggregate.

Biochar has been used as a sustainable amendment to mitigate environmental risks, improve plant growth and soil properties. This study conducted laboratory column tests to investigate the effects of plant-biochar interactions on shrub growth, hydraulic properties and nutrient contents of recycled concrete aggregates (RCAs). In total, three test conditions, namely, vegetated RCA without biochar (R), with 5 % biochar (R5) and 10 % biochar (R10) were subject to drying. With biochar application, total N, P and K of RCA increased by >100 %, 200 % and 31 %, respectively, while pH reduced to 8.3. With shrub growth, the lowest RCA pH was reduced to 7.8. The leaf area index (LAI) of shrub increased by 51 % due to biochar amendment, while the differences in shoot height were insignificant. The water retention capacity of RCA was enhanced by improving the saturated water content and air-entry value by 27 % and 100 %. The slope of the soil suction-LAI correlation for biochar amend cases was 1.6 times lower than R. This indicates that biochar may limit the increase of matric suction and prevent excessive water loss during drying. However, the differences between R5 and R10 were not significant. Therefore, 5 % biochar amendment is highly suggested as it can substantially improve plant growth and soil hydraulic properties during drying.

Case report: Clinical characteristics of two cases of pneumonia caused with different strains of Chlamydia psittaci.

Background: With the development of metagenomic sequencing technologies, more and more cases of pneumonia caused with Chlamydia psittaci (C. psittaci) have been reported. However, it remains unknown about the characteristics of patients with pneumonia caused by different strains of C. psittaci. Here, we shared the clinical characteristics of two cases of pneumonia caused with C. psittaci strains SZ18-2 and SZ15 which were rarely identified in humans. Case presentation: Case 1: A 69-year-old male farmer who fed ducks presented to hospital for cough, diarrhea and lethargy with the temperature of 39.8°C. Case 2: A 48-year-old male worker who slaughtered ducks was transferred to hospital for high fever, cough, myalgia, diarrhea and loss of appetite. Both patients did not take any protective measures (wearing face masks or gloves) while processing ducks. C. psittaci pneumonia was diagnosed by metagenomic next-generation sequencing and polymerase chain reaction. After treatment with doxycycline and azithromycin individually, they recovered well and discharged from hospital. Through OmpA sequencing, two different strains of SZ18-2 and SZ15 were identified in case 1 and case 2, respectively. Conclusions: Patients infected with different strains of C. psittaci may own different clinical manifestations. C. psittaci infection should be suspected when pneumonia appears, accompanied by digestive symptoms and multiple organ dysfunction, especially under the exposure of specific birds.

Computationally guided discovery of novel non-steroidal AR-GR dual antagonists demonstrating potency against antiandrogen resistance.

As a major class of medicine for treating the lethal type of castration-resistant prostate cancer (PCa), long-term use of androgen receptor (AR) antagonists commonly leads to antiandrogen resistance. When AR signaling pathway is blocked by AR-targeted therapy, glucocorticoid receptor (GR) could compensate for AR function especially at the late stage of PCa. AR-GR dual antagonist is expected to be a good solution for this situation. Nevertheless, no effective non-steroidal AR-GR dual antagonist has been reported so far. In this study, an AR-GR dual binder H18 was first discovered by combining structure-based virtual screening and biological evaluation. Then with the aid of computationally guided design, the AR-GR dual antagonist HD57 was finally identified with antagonistic activity towards both AR (IC50 = 0.394 µM) and GR (IC50 = 17.81 µM). Moreover, HD57 could effectively antagonize various clinically relevant AR mutants. Further molecular dynamics simulation provided more atomic insights into the mode of action of HD57. Our research presents an efficient and rational strategy for discovering novel AR-GR dual antagonists, and the new scaffold provides important clues for the development of novel therapeutics for castration-resistant PCa.

Two Path Gland Segmentation Algorithm of Colon Pathological Image Based on Local Semantic Guidance.

Colonic adenocarcinoma is a disease severely endangering human life caused by mucosal epidermal carcinogenesis. The segmentation of potentially cancerous glands is the key in the detection and diagnosis of colonic adenocarcinoma. The appearance of cancerous tissue is different in gland segmentation in colon pathological images, and it is impossible to accurately segment the changes of glands from benign to malignant using a single network. Given these issues, a two-path gland segmentation algorithm of colon pathological image based on local semantic guidance is proposed in this paper. The improved candidate region search algorithm is adopted to expand the original image data set and generate sub-datasets sensitive to specific features. Then, the semantic feature-guided model is employed to extract the local adenocarcinoma features and acts on the backbone network together with context feature extraction based on the attention mechanism. In this way, a larger receptive field and more local feature information are obtained, the learning ability of the network to the morphological features of glands is enhanced, and the performance of automatic gland segmentation is finally improved. The algorithm is verified on Warwick Qu-Dataset. Compared with the current popular segmentation algorithms, our algorithm has good performance in Dice coefficient, F1 score, and Hausdorff distance on different types of test sets.

Value of different scoring models in predicting the survival of patients with liver cirrhosis after transjugular intrahepatic portosystemic shunt / 临床肝胆病杂志

Objective To compare the value of Child-Pugh score, Model for End-Stage Liver Disease (MELD) score, MELD combined with serum sodium concentration (MELD-Na) score, CLIF Consortium Acute Decompensation (CLIF-C AD) score, and Freiburg index of post-transjugular intrahepatic portosystemic shunt (TIPS) survival (FIPS) score in predicting the survival of patients undergoing TIPS. Methods A retrospective analysis was performed for the clinical data of 447 patients with liver cirrhosis who underwent TIPS in several hospitals in southwest China, among whom there were 306 patients in the survival group and 62 in the death group. The scores of the above five models were calculated, and a survival analysis was performed based on these models. The independent samples t -test was used for comparison of normally distributed continuous data between groups, and the non-parametric Mann-Whitney U test was used for comparison of non-normally distributed continuous data between groups; the Pearson chi-square test was used for comparison of categorical data between groups; a multivariate Cox regression analysis was used for correction analysis of known influencing factors with statistical significance which were not included in the scoring models; the Kaplan-Meier method was used to evaluate the discriminatory ability of each model in identifying risks in the surgical population, and the log-rank test was used for analysis. The area under the receiver operating characteristic curve (AUC), C-index at different time points, and calibration curve were used to evaluate the predictive ability of each scoring model. Results Compared with the death group, the survival group had significantly lower age ( Z =2.884, P < 0.05), higher albumin ( t =3.577, P < 0.05), and Na + ( Z =-3.756, P < 0.05) and significantly lower proportion of patients with alcoholic cirrhosis ( χ 2 =22.674, P < 0.05), aspartate aminotransferase ( Z =2.141, P < 0.05), prothrombin time ( Z =2.486, P < 0.05), international normalized ratio ( Z =2.429, P < 0.05), total bilirubin ( Z =3.754, P < 0.05), severity of ascites ( χ 2 =14.186, P < 0.05), and scores of the five models (all P < 0.05). Survival analysis showed that all scoring models effectively stratified the prognostic risk of the patients undergoing TIPS. Comparison of the C-index of each scoring model at different time points showed that Child-Pugh score had the strongest ability in predicting postoperative survival, followed by MELD-Na score, MELD score, and CLIF-C AD score, and FIPS score had a relatively poor predictive ability; in addition, the prediction efficiency of each score gradually decreased over time. Child-Pugh score had the largest AUC of 0.832 in predicting 1-year survival rate after surgery, and MELD-Na score had the largest AUC of 0.726 in predicting 3-year survival rate after surgery, but FIPS score had a poor ability in predicting 1- and 3-year survival rates. Conclusion All five scoring models can predict the survival of patients with liver cirrhosis after TIPS and can provide effective stratification of prognostic risk for such patients. Child-Pugh score has a better ability in predicting short-term survival, while MELD-Na score has a better ability in predicting long-term survival, but FIPS score has a relatively poor predictive ability in predicting both short-term and long-term survival.

Advances in application of regulatory T cells in transplant immune tolerance: from basic to clinical research / 器官移植

Regulatory T cells (Treg) are important inhibitory immune cells to establish immune tolerance, which play a pivotal role in regulating excessive immune response and autoimmune diseases of the host. Previous studies related to transplant immune tolerance have confirmed that increasing the number of Treg in vivo or enhancing the function of Treg serve as a therapeutic strategy to induce transplant immune tolerance. At present, Treg-based induction methods for transplant immune tolerance include adoptive infusion of Treg, in vivo amplification of Treg and utilization of antigen-specific Treg. In this article, the characteristics and mechanism of Treg, the latest research progress on basic experiments and clinical practice of Treg related to transplant immune tolerance at home and abroad were reviewed, and future challenges and development of Treg therapy were prospected, aiming to unravel the significance and application prospect of Treg in transplant immune tolerance, explore the advantages and limitations of Treg therapeutic strategies, and provide reference and evidence for subsequent research in this field.

Review of traditional Chinese medicines in ameliorating neuropsychiatric diseases by improving the levels of monoamine neurotransmitters via gut microbiota regulation / 中国中药杂志

The degeneration of monoaminergic system and the reduction of monoamine neurotransmitters(MNTs) are associated with the occurrence of a variety of neuropsychiatric diseases, becoming the key indicators for clinical diagnosis and treatment. Recent studies suggested gut microbiota could influence the occurrence, development, and treatment of neuropsychiatric diseases by directly or indirectly regulating the synthesis and metabolism of MNTs. Rich clinical experience has been accumulated in the amelioration and treatment of neuropsychiatric diseases by traditional Chinese medicines. The traditional oral administration method demonstrates obvious advantages in regulating gut microbiota. It provides a new idea for explaining the pharmacodynamic material basis and mechanism of traditional Chinese medicines in ameliorating neuropsychiatric disease by improving the levels of MNTs via gut microbiota regulation. Focusing on three common neuropsychiatric diseases including Alzheimer's disease, Parkinson's disease, and major depression, we summarized the pathways of gut microbiota in regulating the levels of MNTs and the paradigms of traditional Chinese medicines in ameliorating neuropsychiatric diseases via the "bacteria-gut-brain axis", aiming to provide ideas for the development of drugs and treatment schemes.

Genomic epidemiology of Vibrio parahaemolyticus from acute diarrheal patients in Shenzhen City from 2013 to 2021 / 中华预防医学杂志

Objective: To characterize the prevalence and genomic epidemiology of Vibrio parahaemolyticus from acute diarrheal patients in Shenzhen City from 2013 to 2021. Methods: Based on the Shenzhen Infectious Diarrhea Surveillance System, acute diarrheal patients were actively monitored in sentinel hospitals from 2013 to 2021. Whole-genome sequencing (WGS) of Vibrio parahaemolyticus isolates was performed, and the genomic population structure, serotypes, virulence genes and multilocus sequence typing were analyzed. Outbreak clusters from 2019 to 2021 were explored based on single-nucleotide polymorphism analysis. Results: A total of 48 623 acute diarrhea cases were monitored in 15 sentinel hospitals from 2013 to 2021, and 1 135 Vibrio parahaemolyticus strains were isolated, with a positive isolation rate of 2.3%. Qualified whole-genome sequencing data of 852 isolates were obtained. Eighty-nine serotypes, 21 known ST types and 5 new ST types were identified by sequence analysis, and 93.2% of strains were detected with toxin profile of tdh+trh-. 8 clonal groups (CGs) were captured, with CG3 as the absolute predominance, followed by CG189. The CG3 group was dominated by O3:K6 serotype and ST3 sequence type, while CG189 group was mainly O4:KUT, O4:K8 serotypes and ST189a and ST189 type. A total of 13 clusters were identified, containing 154 cases. About 30 outbreak clusters with 29 outbreak clusters caused by CG3 strains from 2019 to 2021. Conclusion: Vibrio parahaemolyticus is a major pathogen of acute infectious diarrhea in Shenzhen City, with diverse population structures. CG3 and CG189 have been prevalent and predominant in Shenzhen City for a long time. Scattered outbreaks and persistent sources of contamination ignored by traditional methods could be captured by WGS analysis. Tracing the source of epidemic clone groups and taking precise prevention and control measures are expected to significantly reduce the burden of diarrhea diseases caused by Vibrio parahaemolyticus infection in Shenzhen City.

Experimental Investigation on the Influencing Factors of Compressive Strength of Foamed Lightweight Material Utilizing Completely Decomposed Granite.

The utilization of construction waste soil to produce foamed concrete together with cement and a foaming agent is a promising method for waste recycling. Completely decomposed granite (CDG), which is widely available in southern China, was selected as a typical construction waste soil in foamed material production. The Taguchi method was applied to study the influence of various parameters on compressive strength, including cement dosage, CDG dosage, water to solid materials ratio (W/M), fine particles content, and gravel particles content. Analysis of variance (ANOVA) on a CDG-based sample showed that all factors have significant effects on compressive strength and the most effective parameter was cement dosage, followed in sequence by CDG dosage, W/M, gravel particles content, and fine particles content. However, only cement dosage and W/M influence the internal structure significantly during water/vacuum-immersion tests. The relationship between micro-pore structure and compressive strength suggested that with the decrease of open porosity, the compressive strength showed an increasing trend. This study reveals the possibility of CDG as a raw material for foamed lightweight soil and provides a technical reference of production procedure.

Discovery of novel antagonists targeting the DNA binding domain of androgen receptor by integrated docking-based virtual screening and bioassays.

Androgen receptor (AR), a ligand-activated transcription factor, is a master regulator in the development and progress of prostate cancer (PCa). A major challenge for the clinically used AR antagonists is the rapid emergence of resistance induced by the mutations at AR ligand binding domain (LBD), and therefore the discovery of novel anti-AR therapeutics that can combat mutation-induced resistance is quite demanding. Therein, blocking the interaction between AR and DNA represents an innovative strategy. However, the hits confirmed targeting on it so far are all structurally based on a sole chemical scaffold. In this study, an integrated docking-based virtual screening (VS) strategy based on the crystal structure of the DNA binding domain (DBD) of AR was conducted to search for novel AR antagonists with new scaffolds and 2-(2-butyl-1,3-dioxoisoindoline-5-carboxamido)-4,5-dimethoxybenzoicacid (Cpd39) was identified as a potential hit, which was competent to block the binding of AR DBD to DNA and showed decent potency against AR transcriptional activity. Furthermore, Cpd39 was safe and capable of effectively inhibiting the proliferation of PCa cell lines (i.e., LNCaP, PC3, DU145, and 22RV1) and reducing the expression of the genes regulated by not only the full-length AR but also the splice variant AR-V7. The novel AR DBD-ARE blocker Cpd39 could serve as a starting point for the development of new therapeutics for castration-resistant PCa.

The repellent effect of tea tree oil emulsion on leeches / 药学学报

Leech bites usually lead to more bleeding, and dermal tissue is damaged to form lifelong scars. If leeches enter the body cavity, it will be more dangerous. Therefore, there is an urgent need to develop effective repellents. In this study, oil in water (O/W) emulsion of tea tree oil was prepared with tea tree oil as the main ingredient, and konjac glucomannan (KGM), ethyl cellulose (EC) as the main excipients. The filter-paper ring method and repellent test in water were used to evaluate the repellent effects on leeches. The animal experiments were approved by the Ethics Committee of Academy of Military Medical Sciences and were conducted in accordance with relevant guidelines and regulations. The activities of acetylcholinesterase (AchE), glutathione S-transferase (GST) and carboxylesterase (CarE) in vivo were measured to clarify the repellent mechanisms. The results showed that a uniform and stable tea tree oil emulsion was successfully prepared, which has excellent hydrophilicity and can effectively repel leeches. The tea tree oil emulsion has a good repellent effect on leeches, which can avoid the volatilization of tea tree oil and prolong the effective repelling time. The novel formulation of tea tree oil provides a new idea for repelling effects with long time and high efficiency based on similar essential oil.

Deep multi-kernel auto-encoder network for clustering brain functional connectivity data.

In this study, we propose a deep-learning network model called the deep multi-kernel auto-encoder clustering network (DMACN) for clustering functional connectivity data for brain diseases. This model is an end-to-end clustering algorithm that can learn potentially advanced features and cluster disease categories. Unlike other auto-encoders, DMACN has an added self-expression layer and standard back-propagation is used to learn the features that are beneficial for clustering brain functional connectivity data. In the self-expression layer, the kernel matrix is constructed to extract effective features and a new loss function is proposed to constrain the clustering portion, which enables the training of a deep neural learning network that tends to cluster. To test the performance of the proposed algorithm, we applied the end-to-end deep unsupervised clustering algorithm to brain connectivity data. We then conducted experiments based on four public brain functional connectivity data sets and our own functional connectivity data set. The DMACN algorithm yielded good results in various evaluations compared with the existing clustering algorithm for brain functional connectivity data, the deep auto-encoder clustering algorithm, and several other relevant clustering algorithms. The deep-learning-based clustering algorithm has great potential for use in the unsupervised recognition of brain diseases.

Cytotoxic benzopyranone and xanthone derivatives from a coral symbiotic fungus Cladosporium halotolerans GXIMD 02502.

Coral-derived microorganisms have been historically proven to be prolific sources of bioactive secondary metabolites. Twelve benzopyranone and/or xanthone derivatives, including a new benzopyranone with an uncommon carboxyl group at C-8, coniochaetone K (1), were obtained from the Beibu Gulf-derived coral symbiotic fungus Cladosporium halotolerans GXIMD 02502. Their structures were determined by extensive spectroscopic data interpretation and comparison with literature values. The absolute configuration of 1 was accomplished by comparison of specific optical rotation as well as quantum chemical ECD calculations. The in vitro cytotoxicity of compounds 1-12 against two human prostatic cancer cell lines, C4-2B and 22RV1, were evaluated. And compounds 1, 3, 6-8, and 10-11 demonstrated significant cytotoxicity with inhibitions ranging from 55.8% to 82.1% at the concentration of 10 µM.

Selection of Reference Genes for Normalization of Gene Expression in Thermobia domestica (Insecta: Zygentoma: Lepismatidae).

Zygentoma occupies a key evolutionary position for understanding the evolution of insect metamorphosis but has received little attention in terms of genetic analysis. To develop functional genomic studies in this insect, we evaluated five candidate internal reference genes for quantitative RT-PCR (qPCR) studies from Thermobia domestica, a representative species of Zygentoma, including Actin 5C (Actin5C), Elongation factor-1 alpha (EF1A), Ribosome protein S26 (RPS26), Ribosome protein L32 (RPL32), and Superoxide dismutase 2 (SOD2), at different developmental stages, in various body parts, and under dsRNA microinjection and starvation stresses, using four algorithms (delta Ct, geNorm, NormFinder and BestKeeper) and a comparative algorithm (RefFinder). Specific suitable reference genes were recommended across specific experimental conditions, and the combination of RPS26 and RPL32 was appropriate for all tested samples. Employing our selected reference gene combination, we investigated the gene expression pattern of Myoglianin (Myo), a crucial gene-regulating insect metamorphosis, in ametabolous T. domestica, and demonstrated the efficiency of RNA interference (RNAi) in firebrat nymphs. This study provides a basis for reliable quantitative studies of genes and greatly benefits evolutionary and functional genomics studies in Zygentoma.

HPLC-DAD-Guided Isolation of Diversified Chaetoglobosins from the Coral-Associated Fungus Chaetomium globosum C2F17.

Cytochalasans have continuously aroused considerable attention among the chemistry and pharmacology communities due to their structural complexities and pharmacological significances. Sixteen structurally diverse chaetoglobosins, 10-(indol-3-yl)-[13]cytochalasans, including a new one, 6-O-methyl-chaetoglobosin Q (1), were isolated from the coral-associated fungus Chaetomium globosum C2F17. Their structures were accomplished by extensive spectroscopic analysis combined with single-crystal X-ray crystallography and ECD calculations. Meanwhile, the structures and absolute configurations of the previously reported compounds 6, 12, and 13 were confirmed by single-crystal X-ray analysis for the first time. Chaetoglobosins E (6) and Fex (11) showed significant cytotoxicity against a panel of cancer cell lines, K562, A549, Huh7, H1975, MCF-7, U937, BGC823, HL60, Hela, and MOLT-4, with the IC50 values ranging from 1.4 µM to 9.2 µM.

Research Progress on Chemical Constituents and Pharmacological Effects of Piperis Fructus / 中国实验方剂学杂志

Piperis Fructus is the dried nearly ripe or ripe fruit of Piperaceae, which is an important spice material and a traditional Chinese medicine (TCM), it is widely used in the world. It is recorded to possess the efficacy of warming spleen and stomach for dispelling cold, depressing Qi and dissolving phlegm. Piperis Fructus mainly contains amide alkaloids with piperine as the main ingredient and volatile oil dominated by monoterpenoids and sesquiterpenoids, which have a wide range of biological activities, such as anti-cancer, anti-oxidation, anti-inflammatory, etc. By referring to relevant papers at home and abroad, the researches on chemical compositions from different parts and pharmacological effects of Piperis Fructus in recent 5 years were summarized and analyzed. It was found that Piperis Fructus has great potential for drug development as a TCM with homology of medicine and food, which can provide a reference for further research and comprehensive utilization of Piperis Fructus.