Efficacy and safety of same-day versus next-day administration of PEG-rhG-CSF for the prophylaxis of chemotherapy-induced neutropenia and febrile neutropenia in patients with breast cancer: a retrospective cohort study.

OBJECTIVES: Polyethylene glycol recombinant human granulocyte colony-stimulating factors (PEG-rhG-CSFs) are used to prevent or treat chemotherapy-induced neutropenia (CIN) and febrile neutropenia (FN). This study aimed to compare the efficacy and safety of same-day versus next-day PEG-rhG-CSF administration following chemotherapy and the effects of 3 mg versus 6 mg dosages. METHODS: We retrospectively analyzed cohort data of patients with breast cancer who underwent chemotherapy and received PEG-rhG-CSF either within 24 h (same-day group) or 24 h (next-day group) after chemotherapy. The incidences of CIN and FN were assessed in each chemotherapy cycle between the two groups. The primary endpoint was the incidence of FN in the first cycle and throughout all cycles. The secondary endpoints included the incidences of various grades of CIN (CIN1-CIN4), antibiotic use, chemotherapy regimen modifications, and overall safety. RESULTS: Among the 2385 chemotherapy cycles with prophylactic PEG-rhG-CSF in 620 patients, 798 and 1587 cycleswere in the same-day and next-day group, respectively. No statistically significant differences were observed in the incidence of FN in the first cycle or across all cycles, CIN1-4, or adverse reactions between the two groups. However, the same-day group exhibited significantly higher rates of antibiotic use (2.88% vs. 0.42%, P = 0.03) and chemotherapy regimen modification (4.68% vs. 1.45%, P < 0.001). Subgroup analysis indicated no differences in outcomes for the 6 mg dosage, but a significantly lower incidence of CIN was observed in the same-day group receiving 3 mg (P = 0.025). CONCLUSIONS: These findings suggest that same-day administration of PEG-rhG-CSF is as effective and safe as next-day administration in preventing FN and CIN during chemotherapy.

Comparison of Recurrence and Survival Between Patients with Pathological Stage I Epithelial Ovarian Cancer After Laparoscopic or Laparotomic Surgery: Retrospective Analysis of a Propensity-Matched Cohort.

OBJECTIVE: To compare oncologic outcomes after laparoscopic or laparotomic surgery to treat epithelial ovarian carcinoma in FIGO Stage I. DESIGN: Retrospective cohort study. SETTING: Gynecological cancer ward in a tertiary hospital. PARTICIPANTS: A total of 85 patients with FIGO Stage I epithelial ovarian carcinoma who underwent laparoscopic staging surgery and 206 who underwent laparotomic staging surgery at West China Second Hospital, Sichuan University (Chengdu, China) between January 1, 2013 and December 31, 2019. INTERVENTIONS: Laparoscopic surgery or laparotomic staging surgery. RESULTS: Before propensity score-based matching, the laparotomy group showed higher prevalence of preoperative elevated CA125 level (48.5% vs 35.3%, p = .045) and tumors >15 cm (27.2% vs 5.9%, p <.001). Multivariate analysis associated higher body mass index with better overall survival (adjusted HR 0.83, 95% CI 0.70-0.99, p = .043). Among propensity score-matched patients (82 per group) who were matched to each other according to propensity scoring based on age, body mass index, CA125 level, largest tumor diameter, FIGO stage, history of abdominal surgery, and American Society of Anesthesiologists grade, the rate of progression-free survival at 5 years was similar between the laparoscopy group (87.1%, 95% CI 79.3-95.7%) and the laparotomy group (90.9%, 95% CI 84.7-97.6%, p = .524), as was the rate of overall survival at 5 years (93.9%, 95% CI 88.0-100.0% vs 94.7%, 95% CI 89.8-99.9%, p = .900). Regardless of whether patients were matched, the two groups showed similar rates of recurrence of 9-11% during follow-up lasting a median of 54.9 months. CONCLUSIONS: Rates of recurrence and survival may be similar between laparoscopy or laparotomy to treat Stage I epithelial ovarian cancer. Since laparoscopy is associated with less bleeding and faster recovery, it may be a safe, effective alternative to laparotomy for appropriate patients.

Neoseiulus mites as biological control agents against Megalurothrips usitatus (Thysanoptera: Thripidae) and Frankliniella intonsa (Thysanoptera: Thripidae) on cowpea crop: laboratory to field.

Megalurothrips usitatus (Bagnall) (Thysanoptera: Thripidae) and Frankliniella intonsa (Trybom) (Thysanoptera: Thripidae) have been detrimental to cowpea production in many countries. Laboratory experiments were conducted to determine the prey stage preference and functional response of 2 predatory mites species, Neoseiulus barkeri (Hughes) (Acari: Phytoseiidae), and Neoseiulus californicus (McGregor) (Acari: Phytoseiidae), towards 2 thrips species (TS), M. usitatus, and F. intonsa, at varying densities and life stages on cowpea. Results shown that Neoseiulus species had a preference for different life stages of prey. Neoseiulus barkeri consumed more M. usitatus nymphs, while N. californicus consumed more F. intonsa (second-instar nymphs). The functional response of the 2 Neoseiulus spp. to nymphs of 2 TS was Type II on cowpea. The higher attack rate coefficient (a') and shorter handling time (Th) values were found on N. barkeri against M. usitatus, and a similar trend was found for those in N. californicus against F. intonsa. Field-caged trials were conducted to evaluate the effectiveness of Neoseiulus spp. in controlling 2 TS. The results have shown that Neoseiulus spp. was effective in controlling the 2 TS, with varying control efficacies at high or low release rates. The study provided valuable information on using Neoseiulus spp. as biological control agents against M. usitatus and F. intonsa in cowpea crops.

Role of prostaglandin E2 and its receptors in chronic liver disease.

Chronic liver disease (CLD) is a major global health burden in terms of growing morbidity and mortality. Although many conditions can cause CLD, leading to cirrhosis and hepatocellular carcinoma (HCC), viral hepatitis, drug-induced liver injury (DILI), alcoholic liver disease (ALD) and non-alcoholic fatty liver disease (NAFLD) are the most common culprits. Prostaglandin E2 (PGE2), produced in the liver, is an important lipid mediator derived from the ω-6 polyunsaturated fatty acid, arachidonic acid, and plays a critical role in hepatic homeostasis. The physiological effects of PGE2 are mediated through four classes of E-type prostaglandin (EP) receptors, namely EP1, EP2, EP3 and EP4. In recent years, an increasing number of studies has been done to clarify the effects of PGE2 and EP receptors in regulating liver function and the pathogenesis of CLD to create a new potential clinical impact. In this review, we overview the biosynthesis and regulation of PGE2 and discuss the role of its synthesizing enzymes and receptors in the maintenance of normal liver function and the development and progress of CLD. We also discuss the potential of the PGE2-EP receptors system in treating CLD with various etiologies.

[Distribution Characteristics, Source Analysis and Potential Ecological Risk Assessment of Soil Heavy Metals in Typical River Source Areas of Northeastern Hunan Province].

Soil environmental quality in water source areas related to the residents' life, health and safety, has been the hotspot issues in science of ecological environment protection. A total of 87 surface soil samples were collected from typical river source areas in northeastern Hunan Province, using GIS technique and potential ecological risk assessment index to study the spatial distribution characteristics and Potential ecological risk of soil heavy metals (Cd, Pb, Cr, Hg and As), and the means of multivariate statistical analysis and positive definite matrix factor analysis models (PMF) were used to explain the possible sources and its contribution rates of heavy metals. The results show that:① The soil located in the typical river source area of northeastern Hunan Province was acidic, and the meant of ω(Cd), ω(Pb), ω(Cr), ω(Hg), and ω(As) in soil was 0.20, 41.07, 130.51, 0.29, and 11.63mg·kg-1, respectively. And except As, all of them had enrichment tendency. ② The comprehensive potential ecological risk of soil heavy metals was at a medium level, among which Cr, Pb and As were at a slight level of potential ecological risk, and Cd and Hg all reached a strong level of risk. ③ Cd and Pb of soil had significant homology, which were derived from agricultural activity, Cr and As of soil were affected by both domestic waste discharge and natural parent material, and Hg of soil was mainly derived from fossil combustion and transportation. ④ There were four pollution sources which included household waste discharge source, natural parent material source, Fossil burning and transportation sources, as well as sources of agricultural activities in typical river source area in northeastern Hunan Province, which contributed the rates of heavy metals were 21.36%, 35.92%, 19.30% and 23.42%, respectively, and the contribution rate of man-made sources was higher than that of natural sources. To sum up, this study has reference value for pollution prevention, ecological restoration and beautiful village construction in river source area of northeastern Hunan Province.

Efficacy of Oral Medications or Intrauterine Device-Delivered Progestin in Patients with Endometrial Hyperplasia with or without Atypia: A Network Meta-Analysis.

The aim of this systematic review was to evaluate the efficacy of oral medication or intrauterine device-delivered progestins in patients with endometrial hyperplasia (EH) with or without atypia. We systematically examined PubMed, EMBASE, the Cochrane Library, and clinicaltrials.gov to identify studies reporting the regression rate of patients with EH who received progestins or non-progestins. The regression rates after different treatments were compared using a network meta-analysis in terms of the relative ratios (RRs) and 95% confidence intervals (CIs). Begg-Mazumdar rank correlation and funnel plots were performed to evaluate the publication bias. Five non-randomized studies and 21 randomized controlled trials involving 2268 patients were included in the network meta-analysis. The levonorgestrel-releasing intrauterine system (LNG-IUS) was associated with a higher regression rate than medroxyprogesterone acetate (MPA) (RR 1.30, 95% CI 1.16-1.46) in patients with EH. Among those without atypia, the LNG-IUS was associated with a higher regression rate than any of the three types of oral medications (MPA, norethisterone, or dydrogesterone (DGT)) (RR 1.35, 95% CI 1.18-1.55). According to the network meta-analysis, combining the LNG-IUS with MPA or metformin increased regression rate, while DGT was associated with the highest regression rate among all oral medications. The LNG-IUS may be the best choice for patients with EH, and combining it with MPA or metformin may further improve its efficacy. DGT may be the preferred choice for patients who are unwilling to use the LNG-IUS or who cannot tolerate its side effects.

Exosome-mediated inhibition of microRNA-449a promotes the amplification of mouse retinal progenitor cells and enhances their transplantation in retinal degeneration mouse models.

Inherited and age-related retinal degenerations are the commonest causes of blindness without effective treatments. Retinal progenitor cells (RPCs), which have the multipotency to differentiate into various retinal cell types, are regarded as a promising source of cell transplantation therapy for retinal degenerative diseases. However, the self-limited expansion of RPCs causes difficulty in cell source supply and restrict its clinical treatment. In this work, we found that inhibition of microRNA-449a (miR-449a) in RPCs can promote proliferation and inhibit apoptosis of RPCs, partially through upregulating Notch signaling. Further optimization of transduction miR-449a inhibitor into RPCs by endothelial cell-derived exosomes can promote the survival of RPCs transplanted in vivo and reduce cell apoptosis in retinal degeneration mouse models. In summary, these studies have shown that exosome-miR-449a inhibitor can effectively promote the expansion of RPCs in vitro and enhance transplanted RPCs survival in vivo, which might provide a novel intervention strategy for retinal degenerations in the future.

[Osteoporosis Screening Values of Osteoporosis Self-Assessment Tool for Asians Index and Body Mass Index in Middle-Aged and Elderly Tibetan Population in Tibet].

Objective: To analyze the screening value of osteoporosis self-screening tool for Asia (OSTA) and body mass index (BMI) for osteoporosis (OP) in middle-aged and elderly Tibetan population in the Tibetan region. Methods: Data on demographic information, bone mineral density (BMD), and other information of 627 middle-aged and elderly people were collected. Analysis of the correlation between OSTA index, BMI and BMD, and receiver operating characteristic (ROC) curve was performed to evaluate the OP screening effects. Results: OSTA index and BMI were correlated with BMD in both female and male populations ( P<0.05). In both male and female populations, OSTA index screening results for OP yielded higher area under the curve ( AUC) than BMI did, with the AUC for female OSTA index being 0.886 and that for female BMI being 0.785, while that for male OSTA index being 0.957 and that for male BMI being 0.834. When comparing the different age groups, the AUC of OSTA index and BMI of the middle-age group was higher than those of the quasi-elderly group and the elderly group, with the AUC of OSTA index and BMI of the middle-age being 0.939 and 0.858, those of the quasi-elderly group being 0.860 and 0.813, and those of the elderly group being 0.750 and 0.650, respectively. When the optimal cut-off value of diagnosis with OSTA index was －2.20, the sensitivity and specificity were both 100%. When the optimal cut-off value for diagnosis with BMI was 17.512 kg/m2, the sensitivity and specificity were both 100%. Conclusion: OSTA index and BMI have different OP screening effects in different middle-aged and elderly Tibetan populations, and OSTA index shows better effects for OP screening than BMI does.

[Clinical study on core decompression in treating osteonecrosis of the femoral head of the necrotic bone-in different site].

OBJECTIVE: To analyze the clinical effect of decompression and bone grafting on osteonecrosis of the femoral head(ONFH) at different sites of necrotic lesions. METHODS: A total of 105 patients with ARCOⅡstage ONFH admitted from January 2017 to December 2018 were retrospectively analyzed. There were 71 males and 34 females, with an average age of (55.20±10.98) years old. The mean course of all patients was(15.91±9.85) months. According to Japanese Inveatigation Committee (JIC) classification, all patients were divided into 4 types:17 cases of type A, 26 cases of type B, 33 cases of type C1 and 29 cases of type C2. All four groups were treated with decompression of the pulp core and bone grafting. Visual analogue scale(VAS) and Harris hip joint score were used before and at 3, 6, 12, and 24 months after the operation, and the collapse of the femoral head was observed by X-ray examination within 2 years. RESULTS: All 105 patients were successful on operation without complications, and the mean follow-up duration was (24.45±2.75) months. Harris score showed that there was no statistical difference among four groups before surgery and 3, 6 months after surgery (P>0.05);at 12 and 24 months after surgery, there were significant differences among all groups (P<0.01). There were significant differences in intragroup Harris scores at preoperative and postoperative time points among four groups (P<0.01). VAS showed that there was no statistical difference among four groups before and 3, 6 months after surgery (P>0.05);at 12 and 24 months after surgery, there were significant differences among all groups (P<0.01). There were significant differences in VAS at preoperative and postoperative time points among four groups (P<0.01). None of the patients in four groups had femoral head collapse before and 3, 6 months after surgery. At 12 months after operation, there were 3 cases of femoral head collapse in group C and 4 cases in group C2(P>0.05);At 24 months after operation, 1 case of femoral head collapse occurred in group B, 6 cases in group C1 and 8 cases in group C2(P<0.05). CONCLUSION: Core decompression and bone grafting can improve the effect of ONFH and hip preservation. The effect of hip preservation for ONFH is closely related to the location of the osteonecrosis lesion, so the influence of the location of lesion on the effect of hip preservation should be considered in clinical treatment, so as to make better preoperative hip preservation plan.

Bitter-RF: A random forest machine model for recognizing bitter peptides.

Introduction: Bitter peptides are short peptides with potential medical applications. The huge potential behind its bitter taste remains to be tapped. To better explore the value of bitter peptides in practice, we need a more effective classification method for identifying bitter peptides. Methods: In this study, we developed a Random forest (RF)-based model, called Bitter-RF, using sequence information of the bitter peptide. Bitter-RF covers more comprehensive and extensive information by integrating 10 features extracted from the bitter peptides and achieves better results than the latest generation model on independent validation set. Results: The proposed model can improve the accurate classification of bitter peptides (AUROC = 0.98 on independent set test) and enrich the practical application of RF method in protein classification tasks which has not been used to build a prediction model for bitter peptides. Discussion: We hope the Bitter-RF could provide more conveniences to scholars for bitter peptide research.

Recurrence and survival of patients with stage III endometrial cancer after radical surgery followed by adjuvant chemo- or chemoradiotherapy: a systematic review and meta-analysis.

OBJECTIVE: To compare recurrence and survival in patients with stage III endometrial cancer after radical surgery, followed by either adjuvant chemoradiotherapy (ACR) or adjuvant chemotherapy (AC). METHODS: We searched for relevant studies in PubMed Central, Embase and the Cochrane Central Register of Controlled Trials. Data were pooled on rates of recurrence as well as rates of progression-free, disease-free and overall survival. Heterogeneity was evaluated using the I2 test. Subgroup and sensitivity analyses were performed to identify potential sources of heterogeneity. RESULTS: Data from 18,375 patients in 15 retrospective studies and one randomized controlled trial were meta-analyzed. Compared to the AC group, the ACR showed significantly lower risk of local recurrence (OR 0.43, 95%CI 0.32-0.59) and total recurrence (OR 0.72, 95%CI 0.58-0.89). ACR was also associated with significantly better overall survival (HR 0.66, 95%CI 0.57-0.76), progression-free survival (HR 0.56, 95%CI 0.39-0.81) and disease-free survival (HR 0.66, 95%CI 0.53-0.83). CONCLUSIONS: Adding adjuvant radiotherapy to adjuvant chemotherapy after radical surgery may significantly reduce risk of local and overall recurrence, while significantly improving survival of patients with stage III endometrial cancer.

A high-performance liquid chromatography-tandem mass spectrometry method for quantification of perampanel in human plasma: Effect of concomitant anti-seizure medications on perampanel concentration in patients with epilepsy.

Perampanel is a first-in-class α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist and a novel anti-seizure medication. It is currently used as adjunctive treatment for partial seizures in patients over 12 years of age. With the increasing clinical application of perampanel, monitoring its concentration under certain clinical conditions is important. This study developed a rapid and sensitive high-performance liquid chromatography-tandem mass spectrometry method to quantify perampanel in human plasma. Protein precipitation with acetonitrile was performed for sample preparation. Perampanel and perampanel-d5 (internal standard) were analyzed under gradient conditions using a C18 column. The mobile phase was composed of 0.1% (v/v) formic acid in water (solvent A) and 0.1% (v/v) formic acid in acetonitrile (solvent B) at a flow rate of 0.4 mL/min. Mass detection was performed using multiple reaction monitoring in the positive ionization mode. The proposed method was validated over a range of 0.5-500 ng/mL for perampanel. The linearity (r2 value) was higher than 0.999, and the linear equation was y = 0.00116x + 0.0116. The accuracy of the low-, middle-, and high-quality control samples was between 103% and 113%, and the intra- and inter-day precisions were below 6.81%. The quality of the proposed method was evaluated in accordance with the US Food and Drug Administration Bioanalytical Method Validation Guidance for Industry. The plasma concentrations of perampanel in 25 patients were successfully determined to be 38.7-577.7 ng/mL using the validated method.

[Case-control study on robot-assisted core decompression and conventional core decompression for early necrosis of femoral head].

OBJECTIVE: To compare clinical effect of robot-assisted core decompression and conventional core decompression in treating ARCO Ⅰ stage necrosis of femoral head. METHODS: A retrospective analysis was performed on 60(unilateral operation) patients who underwent core decompression for femoral head necrosis from February 2018 to February 2020. Among them, 30 patients(30 hips) were underwent robot-assisted core decompression (RCD group), including 19 males and 11 females, aged from 17 to 58 years old with an average of(38.50±10.61) years old;30 patients(30 hips) were underwent traditional core decompression surgery (CCD group), including 20 males and 10 females, aged from 20 to 55 years old with an average of (40.63±10.63) years old. Intraoperative fluoroscopy times, intraoperative blood loss and operation time between two groups, and Harris score, visual analogue scale (VAS) before opertaion and 24 months after operation were compared. RESULTS: All patients were followed up, RCD group followed up from 21 to 26 months with an average of(23.40±1.65) months, CCD group followed up from 21 to 26 months with an average of (23.30±1.66) months, and had no difference between two groups(P>0.05). The number of intraoperative X-ray fluoroscopy, intraoperative blood loss and operative time in RCD group were (9.43±1.14) times, (153.80±22.04) ml, (33.40±1.87) min, respectively;while(19.67±1.32) times, (165.04±20.41) ml and (54.75±3.46) min in CCD group respectively;and there were statistical difference between two groups(P<0.05). In addition, there were no statistical difference between two groups in Harris score and VAS at 24 months after operation(P>0.05). CONCLUSION: Compared with conventional core decompression, robot-assisted core decompression could reduce the number of intraoperative fluoroscopy, shorten operation time, and reduce risk of surgery.

Identification of adaptor proteins using the ANOVA feature selection technique.

The adaptor proteins play a crucially important role in regulating lymphocyte activation. Rapid and efficient identification of adaptor proteins is essential for understanding their functions. However, biochemical methods require not only expensive experimental costs, but also long experiment cycles and more personnel. Therefore, a computational method that could accurately identify adaptor proteins is urgently needed. To solve this issue, we developed a classifier that combined the support vector machine (SVM) with the composition of k-Spaced Amino Acid Pairs (CKSAAP) and the amino acid composition (AAC) to identify adaptor proteins. Analysis of variance (ANOVA) was used to select the optimized features which could generate the maximum prediction performance. By examining the proposed model on independent data, we found that the 447 optimized features could achieve an accuracy of 92.39% with an AUC of 0.9766, demonstrating the powerful capabilities of our model. We hope that the proposed model could provide more clues for studying adaptor proteins.

[Biblio-metrology analysis on clinical application of Chengshan (BL57) in ancient Chinese medical literature].

OBJECTIVE: To analyze and sum up clinical application regularities of Chengshan (BL57) acupoint in ancient Chinese literature. METHODS: The book Zhonghua Yidian (Collection of Chinese Medical Classic Works, 5th edition) containing 1 156 ancient medical books was used as the retrieved literature source. The key retrieval words used were BL57 acupoint related indications, prescriptions, treatment methods and taboos, followed by sorting out relevant articles and establishing a database. RESULTS: A total of 196 articles meeting our inclusion standards of the present study, involving 61 ancient books which contain 174 related terms covering 56 diseases or syndromes of internal medicine, surgery, pediatrics, ophthalmology and otorhinola-ryngology, etc.. Among them, the most frequently attending disease treated by single BL57 or acupoints combination was limb meridian disorders, and the most frequently used auxiliary acupoint was Kunlun (BL60). The most frequently used auxiliary meridian was the Bladder Meridian of Foot Taiyang. In addition, a total of 71 terms involved the acupuncture and moxibustion techniques of BL57, covering 7 treatment methods. In terms of the treatment methods, the dose of moxibustion was five cones in each session, and the depth of acupuncture needle insertion was about seven fen. CONCLUSION: BL57 is widely used in various clinical departments, especially for limb meridian diseases.

Reproductive and oncological outcomes of fertility-sparing surgery in patients with stage I epithelial ovarian cancer: A systematic review and meta-analysis.

OBJECTIVE: We meta-analyzed available evidence on fertility, survival, and cancer recurrence in patients with stage I epithelial ovarian cancer (EOC) after fertility-sparing surgery (FSS). METHODS: We systematically reviewed PubMed, EMBASE, and the Cochrane Central Register of Controlled Trials to identify studies reporting reproductive and oncological outcomes of patients with stage I EOC who underwent FSS. Random-effects models were used to calculate pooled rates of disease outcomes, along with 95% confidence intervals (CIs). Subgroup and sensitivity analyses were conducted to identify sources of heterogeneity in the data. RESULTS: We included 23 observational retrospective studies involving 1126 patients. The pooled pregnancy rate was 30% (95% CI, 0.26-0.34), while the pooled natural conception rate was 26% (95% CI, 0.20-0.33). The pooled live birth rate was 27% (95% CI, 0.22-0.32). The pooled rate of EOC recurrence was 12% (95% CI, 0.09-0.14), which did not differ significantly from the rate among patients who underwent radical surgery (odds ratio, 0.77; 95% CI, 0.45-1.33). CONCLUSIONS: FSS is associated with good oncological outcomes but less than satisfactory reproductive outcomes. All in all, the procedure appears to be a safe alternative to radical surgery for EOC patients who want to preserve fertility.

Synthesis and Biological Evaluation of 5-Fluoro-2-Oxindole Derivatives as Potential α-Glucosidase Inhibitors.

α-Glucosidase inhibitors are known to prevent the digestion of carbohydrates and reduce the impact of carbohydrates on blood glucose. To develop novel α-glucosidase inhibitors, a series of 5-fluoro-2-oxindole derivatives (3a ∼ 3v) were synthesized, and their α-glucosidase inhibitory activities were investigated. Biological assessment results showed that most synthesized compounds presented potential inhibition on α-glucosidase. Among them, compounds 3d, 3f, and 3i exhibited much better inhibitory activity with IC50 values of 49.89 ± 1.16 µM, 35.83 ± 0.98 µM, and 56.87 ± 0.42 µM, respectively, which were about 10 ∼ 15 folds higher than acarbose (IC50 = 569.43 ± 43.72 µM). A kinetic mechanism study revealed that compounds 3d, 3f, and 3i inhibited the α-glucosidase in a reversible and mixed manner. Molecular docking was carried out to simulate the affinity between the compound and α-glucosidase.

Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors.

Coumarin and chalcone, two important kinds of natural product skeletons, both exhibit α-glucosidase inhibitory activity. In this work, coumarin-chalcone derivatives 3 (a∼v) were synthesized, and their α-glucosidase inhibitory activity was screened. The results showed that all synthetic derivatives (IC50: 24.09 ± 2.36 to 125.26 ± 1.18 µM) presented better α-glucosidase inhibitory activity than the parent compounds 3-acetylcoumarin (IC50: 1.5 × 105 µM) and the positive control acarbose (IC50: 259.90 ± 1.06 µM). Among them, compound 3t displayed the highest α-glucosidase inhibitory activity (IC50: 24.09 ± 2.36 µM), which was approximately 10 times stronger than that of acarbose. The kinetic assay of 3t (K I = 18.82 µM, K IS = 59.99 µM) revealed that these compounds inhibited α-glucosidase in a mixed-type manner. Molecular docking was used to simulate the interaction between α-glucosidase and compound 3t.