Chlorogenic acid in green bean coffee on body weight: a systematic review and meta-analysis of randomized controlled trials.

BACKGROUND: Supplemental green bean coffee extract (GBCE) with caffeine has been shown to prevent weight gain. There are different dosages of GBCE that contain chlorogenic acid (CGA), and the data for their effectiveness in preventing weight gain (500 mg/day) is currently out of date. To better understand the effects of GBCE containing CGA on body weight, the present study sets out to perform a systematic review and meta-analysis of these studies. METHODS: Using electronic databases, including Scopus, Embase, PubMed, and Cochrane Library databases, literature was searched up to October 13, 2022. For the meta-analysis examining the impact of GBCE containing CGA (500 mg/day) on body weight with a random-effects model, the randomized controlled trials (RCTs) were considered. We calculated weighted mean differences and 95% confidence intervals (CIs). To gauge study heterogeneity, the Cochran Q statistic and I-squared tests (I2) were employed. RESULTS: The meta-analysis includes three RCTs with 103 individuals (case = 51, control = 52). The combined findings of GBCE with CGA at least 500 mg/day result in body weight reduction (WMD: - 1.30 and 95% CI: - 2.07 to - 0.52, p = 0.001) without study heterogeneity (I2 = 0%, p = 0.904) and without publication bias estimated using Egger's and Begger's test (p = 0.752 and p = 0.602, respectively). CONCLUSIONS: According to the meta-analysis, GBCE with CGA 500 mg/day lowers body weight. Nevertheless, despite its limited sample size and short-term study, this study was successful. Long-term research on the effectiveness and safety of GBCE and CGA on body weight require more clinical trials. SYSTEMATIC REVIEW REGISTRATION: PROSPERO CRD42021254916.

Synthesis and potential antidiabetic and lipid-lowering activities of putative asperidine B and its desmethyl analogue.

Putative asperidine B is an unnatural 2,6-disubstituted piperidin-3-ol and a structural isomer of (+)-preussin, a well-known pyrrolidin-3-ol alkaloid. This work reports the first enantioselective synthesis of putative asperidine B and its desmethyl analogue via a chiron approach starting from d-isoascorbic acid as well as evaluation of their free-radical scavenging, antidiabetic, and anti-hyperlipidemic activities. Both putative asperidine B and its desmethyl analogue markedly reduced the total reactive oxygen species (ROS) without cytotoxicity in hepatocellular carcinoma (HepG2) cells. The desmethyl analogue was a potent inducer for two antioxidant gene expression, glutathione peroxidase and superoxide dismutase, whereas putative asperidine B only induced superoxide dismutase. In addition, putative asperidine B exerted potent antidiabetic activity via α-glucosidase inhibition (IC50 = 0.143 ± 0.001 mg/mL) comparable to that of acarbose, an antidiabetic drug. Consistent with the parent asperidine B (preussin), both putative asperidine B and its desmethyl analogue inhibited cholesterol absorption in the intestinal Caco-2 cells. These novel and promising antioxidant, antidiabetic, and lipid-lowering effects of piperidin-3-ols could offer a starting point for this class of compounds for obesity and diabetic drug discovery.

Restoring Ampicillin Sensitivity in Multidrug-Resistant Escherichia coli Following Treatment in Combination with Coffee Pulp Extracts.

Escherichia coli, particularly multidrug-resistant (MDR) strains, is a serious cause of healthcare-associated infections. Development of novel antimicrobial agents or restoration of drug efficiency is required to treat MDR bacteria, and the use of natural products to solve this problem is promising. We investigated the antimicrobial activity of dried green coffee (DGC) beans, coffee pulp (CP), and arabica leaf (AL) crude extracts against 28 isolated MDR E. coli strains and restoration of ampicillin (AMP) efficiency with a combination test. DGC, CP, and AL extracts were effective against all 28 strains, with a minimum inhibitory concentration (MIC) of 12.5-50 mg/ml and minimum bactericidal concentration of 25-100 mg/ml. The CP-AMP combination was more effective than CP or AMP alone, with a fractional inhibitory concentration index value of 0.01. In the combination, the MIC of CP was 0.2 mg/ml (compared to 25 mg/ml of CP alone) and that of AMP was 0.1 mg/ml (compared to 50 mg/ml of AMP alone), or a 125-fold and 500-fold reduction, respectively, against 13-drug resistant MDR E. coli strains. Time-kill kinetics showed that the bactericidal effect of the CP-AMP combination occurred within 3 h through disruption of membrane permeability and biofilm eradication, as verified by scanning electron microscopy. This is the first report indicating that CP-AMP combination therapy could be employed to treat MDR E. coli by repurposing AMP.

Chlorogenic acid rich in coffee pulp extract suppresses inflammatory status by inhibiting the p38, MAPK, and NF-κB pathways.

Coffee pulp (CP) is a coffee byproduct that contains various active ingredients, namely, chlorogenic acid (CGA) and caffeine. These active compounds show several benefits, including antihyperlipidemia, antioxidants, and anti-inflammation. However, the anti-inflammatory properties of Coffea pulp extract (CPE) are unknown. This work determined the impact of CPE on lipopolysaccharide (LPS)-activated murine macrophage cells and the molecular mechanism behind this action. RAW 264.7 cells were exposed to varying doses of CPE with or without LPS. Inflammatory markers and their mechanism were studied. CPE therapy has been shown to suppress the synthesis of inflammatory cytokines and mediators, namely, tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), IL-1ß, cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and nitric oxide (NO), as well as prostaglandin E2 (PGE2). Finally, CPE inactivated the nuclear factor-kappa B (NF-κB) and MAPK signaling pathways. Consequently, CPE might be used as a nutraceutical to treat inflammation and its related disorders.

Dinactin: A New Antitumor Antibiotic with Cell Cycle Progression and Cancer Stemness Inhibiting Activities in Lung Cancer.

Lung cancer, especially non-small cell lung cancer (NSCLC), is one of the most complex diseases, despite the existence of effective treatments such as chemotherapy and immunotherapy. Since cancer stem cells (CSCs) are responsible for chemo- and radio-resistance, metastasis, and cancer recurrence, finding new therapeutic targets for CSCs is critical. Dinactin is a natural secondary metabolite produced by microorganisms. Recently, dinactin has been revealed as a promising antitumor antibiotic via various mechanisms. However, the evidence relating to cell cycle progression regulation is constrained, and effects on cancer stemness have not been elucidated. Therefore, the aim of this study is to evaluate the new function of dinactin in anti-NSCLC proliferation, focusing on cell cycle progression and cancer stemness properties in Lu99 and A549 cells. Flow cytometry and immunoblotting analyses revealed that 0.1-1 µM of dinactin suppresses cell growth through induction of the G0/G1 phase associated with down-regulation of cyclins A, B, and D3, and cdk2 protein expression. The tumor-sphere forming capacity was used to assess the effect of dinactin on the cancer stemness potential in NSCLC cells. At a concentration of 1 nM, dinactin reduced both the number and size of the tumor-spheres. The quantitative RT-PCR analyses indicated that dinactin suppressed sphere formation by significantly reducing expression of CSC markers (i.e., ALDH1A1, Nanog, Oct4, and Sox2) in Lu99 cells. Consequently, dinactin could be a promising strategy for NSCLC therapy targeting CSCs.

Botanical aspects, phytochemicals, and toxicity of Tamarindus indica leaf and a systematic review of antioxidant capacities of T. indica leaf extracts.

Oxidative stress is a condition occurs when there is the imbalance between prooxidants and free radicals. It involves in cellular metabolism, aging, and immune response. Recently oxidative stress has been proved about its beneficial roles in human body. However, long term oxidative stress and high concentration of free radicals can lead to negative effects on organs, systems, and physiological conditions. Prooxidant or antioxidant, therefore, is one of the most important choices for the prevention of these anomaly. Tamarindus indica is a medicinal plant that has been reported as a source of antioxidants. The plants' leaves possess antioxidant effects according to many studies. However, these results have not yet been systematically summarized. The present systematic review summarizes and discusses about the in vitro antioxidant capacities of T. indica leaves. The plants' description and morphology, elements and phytochemical constituents, total phenolic and flavonoids contents and toxicity are also summarized and discussed here.

Cholesterol-Lowering Effects of Asperidine B, a Pyrrolidine Derivative from the Soil-Derived Fungus Aspergillus sclerotiorum PSU-RSPG178: A Potential Cholesterol Absorption Inhibitor.

Isolated secondary metabolites asperidine B (preussin) and asperidine C, produced by the soil-derived fungus Aspergillus sclerotiorum PSU-RSPG178, were found to exhibit inhibitory effects against 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase and oxidative stress in an in vitro assay. Whether or not the known pyrrolidine asperidine B and the recently isolated piperidine asperidine C have lipid-lowering effects remains unknown. Thus, this study aimed to investigate the hypocholesterolemic effects of asperidines B and C and identify the mechanisms involved in using in vitro, ex vivo, and in vivo models. The results show that both compounds interfered with cholesterol micelle formation by increasing bile acid binding capacity, similar to the action of the bile acid sequestrant drug cholestyramine. However, only asperidine B, but not asperidine C, was found to inhibit cholesterol uptake in Caco-2 cells by up-regulating LXRα without changing cholesterol transporter NPC1L1 protein expression. Likewise, reduced cholesterol absorption via asperidine-B-mediated activation of LXRα was also observed in isolated rat jejunal loops. Asperidine B consistently decreases plasma cholesterol absorption, similar to the effect of ezetimibe in rats. Therefore, asperidine B, the pyrrolidine derivative, has therapeutic potential to be developed into a type of cholesterol absorption inhibitor for the treatment of hypercholesterolemia.

Antibacterial Activity of Coffea robusta Leaf Extract against Foodborne Pathogens.

The purpose of this study was to examine the phytochemical compounds and antibacterial activity of Coffea robusta leaf extract (RLE). The results indicated that chlorogenic acid (CGA) is a major component of RLE. The minimum inhibitory concentrations (MICs) of RLE against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Salmonella Typhimurium were 6.25, 12.5, 12.5, and 12.5 mg/ml, respectively. RLE effectively damages the bacterial cell membrane integrity, as indicated by the high amounts of proteins and nucleic acids released from the bacteria, and disrupts bacterial cell membrane potential and permeability, as revealed via fluorescence analysis. Cytotoxicity testing showed that RLE is slightly toxic toward HepG2 cells at high concentration but exhibited no toxicity toward Caco2 cells. The results from the present study suggest that RLE has excellent potential applicability as an antimicrobial in the food industry.

Anticancer Activities of Polygonum odoratum Lour.: A Systematic Review.

Cancers are a potential cause of death worldwide and represent a massive burden for healthcare systems. Treating cancers requires substantial resources, including skilled personnel, medications, instruments, and funds. Thus, developing cancer prevention and treatment measures is necessary for healthcare personnel and patients alike. P. odoratum (Polygonaceae family) is a plant used as a culinary ingredient. It exhibits several pharmacological activities, such as antibacterial, antifungal, antioxidant, anti-inflammatory, and anticancer. Several classes of phytochemical constituents of P. odoratum have been reported. The important ones might be polyphenol and flavonoid derivatives. In this systematic review, the activities of P. odoratum against cancerous cells were determined and summarized. Data were obtained through a systematic search of electronic databases (EMBASE, PubMed, Scopus, Thai Thesis Database, Science Direct and Clinical Key). Eight studies met the eligibility criteria. The cancerous cell lines used in the studies were lymphoma, leukemia, oral, lung, breast, colon, and liver cancer cells. Based on this review, P. odoratum extracts significantly affected Epstein-Barr virus (EBV) genome-carrying human lymphoblastoid (Raji), mouse lymphocytic leukemia (P388), human acute lymphocytic leukemia (Jurkat), breast adenocarcinoma (MCF-7), human colon adenocarcinoma (HT-29), human T lymphoblast (MOLT-4), human promyelocytic leukemia cell line (HL-60), human hepatocellular carcinoma (HepG2), and oral squamous cell carcinoma (SAS, SCC-9, HSC-3) through induction of cell apoptosis, arrest of the cell cycle, inhibition of cell proliferation, migration, and colonization. The molecular mechanism of P. odoratum against cancers was reported to involve suppressing essential proteins required for cell proliferation, colonization, migration, apoptosis, and angiogenesis. They were survivin, cyclin-D, cyclooxygenase 2 (COX-2), matrix metalloproteinase-9 (MMP-9), and vascular endothelial growth factor A (VEGF-A). The extract of P. odoratum was also involved in the protein kinase B (Akt)/mammalian target of rapamycin (mTOR) pathway by inhibiting the expression of Akt, phosphorylated Akt, mTOR, and phosphorylated mTOR. From the key results of this review, P. odoratum is a promising chemotherapy and chemopreventive agent. Further investigation of its pharmacological activity and mechanism of action should be conducted using standardized extracts. In vivo experiments and clinical trials are required to confirm the anticancer activity.

Potential Antimicrobial Properties of Coffee Beans and Coffee By-Products Against Drug-Resistant Vibrio cholerae.

Vibrio cholerae is the causative organism of the cholera epidemic, and it remains a serious global health problem, particularly the multidrug-resistant strain, despite the development of several generic drugs and vaccines over time. Natural products have long been exploited for the treatment of various diseases, and this study aimed to evaluate the in vitro antibacterial activity of coffee beans and coffee by-products against V. cholerae antimicrobial resistant strains. A total of 9 aqueous extracts were investigated, including light coffee (LC), medium coffee (MC), dark coffee (DC), dried green coffee (DGC), dried red coffee (DRC), fresh red coffee (FRC), Arabica leaf (AL), Robusta leaf (RL), and coffee pulp (CP). The influential coffee phytochemicals, i.e., chlorogenic acid (CGA), caffeic acid (CA), and caffeine, were determined using HPLC. The antibacterial properties were tested by agar well-diffusion techniques, and the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were further determined against 20 V. cholerae isolates. The results revealed that all tested strains were sensitive to coffee extracts, with MIC and MBC values in the range of 3.125-25.0 mg/mL and 12.5-50.0 mg/mL, respectively. With a MIC of 6.25 mg/mL, DGC, DRC, and CP appeared to be the most effective compounds against 65, 60, and 55% of clinical strains, respectively. The checkerboard assay revealed that the combination of coffee extract and tetracycline was greater than either treatment alone, with the fractional inhibitory concentration index (FICI) ranging from 0.005 to 0.258. It is important to note that CP had the lowest FICI (0.005) when combined with tetracycline at 60 ng/mL, which is the most effective dose against V. cholerae six-drug resistance strains (azithromycin, colistin, nalidixic acid, sulfamethoxazole, tetracycline, and trimethoprim), with a MIC of 47.5 µg/mL (MIC alone = 12.5 mg/mL). Time killing kinetics analysis suggested that CA might be the most effective treatment for drug-resistant V. cholerae as it reduced bacterial growth by 3 log10 CFU/mL at a concentration of 8 mg/mL within 1 h, via disrupting membrane permeability, as confirmed by scanning electron microscopy (SEM). This is the first report showing that coffee beans and coffee by-product extracts are an alternative for multidrug-resistant V. cholerae treatment.

Antimicrobial Activity of the Green Tea Polyphenol (-)-Epigallocatechin-3-Gallate (EGCG) against Clinical Isolates of Multidrug-Resistant Vibrio cholerae.

The spread of multidrug-resistant (MDR) Vibrio cholerae necessitates the development of novel prevention and treatment strategies. This study aims to evaluate the in vitro antibacterial activity of green tea polyphenol (-)-epigallocatechin-3-gallate (EGCG) against MDR V. cholerae. First, MIC and MBC values were evaluated by broth microdilution techniques against 45 V. cholerae strains. The checkerboard assay was then used to determine the synergistic effect of EGCG and tetracycline. The pharmaceutical mode of action of EGCG was clarified by time-killing kinetics and membrane disruption assay. Our results revealed that all of the 45 clinical isolates were susceptible to EGCG, with MIC and MBC values in the range of 62.5-250 µg/mL and 125-500 µg/mL, respectively. Furthermore, the combination of EGCG and tetracycline was greater than either treatment alone, with a fractional inhibitory concentration index (FICI) of 0.009 and 0.018 in the O1 and O139 representative serotypes, respectively. Time-killing kinetics analysis suggested that EGCG had bactericidal activity for MDR V. cholerae after exposure to at least 62.5 µg/mL EGCG within 1 h. The mode of action of EGCG might be associated with membrane disrupting permeability, as confirmed by scanning electron microscopy. This is the first indication that EGCG is a viable anti-MDR V. cholerae treatment.

Impact of Pharmacist-Led Diabetes Self-Care Education on Patients With Type 2 Diabetes in Pakistan: A Randomized Controlled Trial.

Introduction: There is a little evidence on efficacy of pharmacy-based interventions on clinical outcomes of type 2 diabetes mellitus (T2DM) patients in Pakistan. Objective: To appraise the impact of pharmacist-led self-care education on glycemic control, self-care practices and disease knowledge of T2DM patients with poor glycemic control (HbA1c ≥ 7%). Methods: In this 6-months, randomized controlled trial (RCT), n = 75, T2DM patients seeking care at a diabetes clinic were randomized in to two groups. Intervention group (n = 38) received two face-to-face educational sessions (at enrollment and on week 12), whereas control group (n = 37) received usual care. Outcome measures such as glycemic control, self-care practices and disease knowledge were assessed at the time of enrollment and after 6-months in both groups. Results: Thirty-three intervention and thirty-three participants from the control group completed the study. Mean glycated hemoglobin (% HbA1c) significantly reduced in the intervention group from 9.00 ± 1.43 to 8.09 ± 1.16 (p < .01). However, no significant change was observed in the control group (9.20 ± 1.24 to 8.93 ± .97; p = .06). Cohen's d effect size of the intervention on HbA1c was .78. Percentage of participants achieving glycemic control (HbA1c < 7%) were significantly higher (p < .05) in the intervention group as compared to the control group (twenty-four vs. six), after 6 months of the trial. A significant (p < .01) improvement in mean scores for disease knowledge and self-care activities was also observed in the intervention group participants, whereas no significant improvements (p > .05) were observed in the control group. Conclusion: The study demonstrated an improvement in glycemic control, disease knowledge and self-care activities of T2DM patients who received pharmacist-led educational intervention. The study findings support clinical significance of integrating pharmacy-based interventions in diabetes management.

Novel Clinical Risk Scoring Model for Predicting Amputation in Patients With Necrotizing Fasciitis: The ANF Risk Scoring System.

Background: Necrotizing fasciitis (NF) is a life-threatening infection of the skin and soft tissue that spreads quickly and requires immediate surgery and medical treatment. Amputation or radical debridement of necrotic tissue is generally always required. The risks and benefits of both the surgical options are weighed before deciding whether to amputate or debride. This study set forth to create an easy-to-use risk scoring system for predicting the risk scoring system for amputation in patients with NF (ANF). Methods: This retrospective study included 1,506 patients diagnosed with surgically confirmed NF at three general hospitals in Thailand from January 2009 to December 2012. All diagnoses were made by surgeons who strictly observed the guidelines for skin and soft tissue infections produced by the Infectious Diseases Society of America. Patients were randomly allocated to either the derivation (n = 1,193) or validation (n = 313) cohort. Clinical risk factors assessed at the time of recruitment were used to create the risk score, which was then developed using logistic regression. The regression coefficients were converted into item scores, and the total score was calculated. Results: The following four clinical predictors were used to create the model: female gender, diabetes mellitus, wound appearance stage 3 (skin necrosis and gangrene), and creatinine ≥1.6 mg/dL. Using the area under the receiver operating characteristic curve (AuROC), the ANF system showed moderate power (78.68%) to predict amputation in patients with NF with excellent calibration (Hosmer-Lemeshow χ2 = 2.59; p = 0.8586). The positive likelihood ratio of amputation in low-risk (score ≤ 4) and high-risk (score ≥ 7) patients was 2.17 (95%CI: 1.66-2.82) and 6.18 (95%CI: 4.08-9.36), respectively. The ANF system showed good performance (AuROC 76.82%) when applied in the validation cohort. Conclusion: The developed ANF risk scoring system, which includes four easy to obtain predictors, provides physicians with prediction indices for amputation in patients with NF. This model will assist clinicians with surgical decision-making in this time-sensitive clinical setting.

Coffee Consumption and Non-alcoholic Fatty Liver Disease: An Umbrella Review and a Systematic Review and Meta-analysis.

Background: The effects of coffee consumption on hepatic outcomes are controversial. This study investigated the associations between coffee consumption and the incidence of non-alcoholic fatty liver disease (NAFLD) in the general population and the reduction of liver fibrosis among patients with NAFLD. Methods: The study consisted of two parts: an umbrella review and a systematic review and meta-analysis (SRMA). The searches for each part were performed separately using PubMed, EMBASE, Cochrane, Scopus, and CINAHL databases. All articles published up to September 2021 were reviewed. To be eligible, studies for the umbrella review were required to report outcomes that compared the risks of NAFLD in the general population and/or liver fibrosis in patients with NAFLD who did and did not drink coffee. Our SRMA included primary studies reporting the effects of coffee consumption on NAFLD-related outcomes. The outcomes were pooled using a random-effects model and reported in both qualitative and quantitative terms (pooled risk ratio, odds ratio, and weighted mean difference). Results: We identified four published SRMAs during the umbrella review. Most studies showed that individuals in the general population who regularly drank coffee were significantly associated with a lower NAFLD incidence than those who did not. Our SRMA included nine studies on the effects of coffee consumption on NAFLD incidence. Pooled data from 147,875 subjects showed that coffee consumption was not associated with a lower NAFLD incidence in the general population. The between-study heterogeneity was high (I 2, 72-85%). Interestingly, among patients with NAFLD (5 studies; n = 3,752), coffee consumption was significantly associated with a reduction in liver fibrosis (odds ratio, 0.67; 95% CI, 0.55 to 0.80; I 2, 3%). There were no differences in the coffee consumption of the general population and of those with NAFLD (4 studies; n = 19,482) or by patients with no/mild liver fibrosis and those with significant fibrosis (4 studies; n = 3,331). Conclusions: There are contrasting results on the effects of coffee on NAFLD prevention in the general population. Benefits of coffee consumption on liver fibrosis were seen among patients with NAFLD. Systematic Review Registration: https://www.crd.york.ac.uk/prospero/display_record.php?ID=CRD42021226607, identifier CRD42021226607.

Novel clinical risk scoring model for predicting mortality in patients with necrotizing fasciitis: The MNF scoring system.

ABSTRACT: Necrotizing fasciitis (NF) is a life-threatening soft tissue infection that rapidly progresses and requires urgent surgery and medical therapy. If treatment is delayed, the likelihood of an unfavorable outcome, including death, is significantly increased. The goal of this study was to develop and validate a novel scoring model for predicting mortality in patients with NF. The proposed system is hereafter referred to as the Mortality in Necrotizing Fasciitis (MNF) scoring system. A total of 1503 patients with NF were recruited from 3 provincial hospitals in Thailand during January 2009 to December 2012. Patients were randomly allocated into either the derivation cohort (n = 1192) or the validation cohort (n = 311). Clinical risk factors used to develop the MNF scoring system were determined by logistic regression. Regression coefficients were transformed into item scores, the sum of which reflected the total MNF score. The following 6 clinical predictors were included: female gender; age > 60 years; white blood cell (WBC) ≤5000/mm3; WBC ≥ 35,000/mm3; creatinine ≥ 1.6 mg/dL, and pulse rate > 130/min. Area under the receiver operating characteristic curve (AuROC) analysis showed the MNF scoring system to have moderate power for predicting mortality in patients with NF (AuROC: 76.18%) with good calibration (Hosmer-Lemeshow χ2: 1.01; P = .798). The positive likelihood ratios of mortality in patients with low-risk scores (≤2.5) and high-risk scores (≥7) were 11.30 (95% confidence interval [CI]: 6.16-20.71) and 14.71 (95%CI: 7.39-29.28), sequentially. When used to the validation cohort, the MNF scoring system presented good performance with an AuROC of 74.25%. The proposed MNF scoring system, which includes 6 commonly available and easy-to-use parameters, was shown to be an effective tool for predicting mortality in patients with NF. This validated instrument will help clinicians identify at-risk patients so that early investigations and interventions can be performed that will reduce the mortality rate among patients with NF.

Effect of Roasting Degree, Extraction Time, and Temperature of Coffee Beans on Anti-Hyperglycaemic and Anti-Hyperlipidaemic Activities Using Ultrasound-Assisted Extraction.

Coffee consumption has been linked to a low risk of metabolic syndrome. However, evidence supporting its anti-hyperglycaemic and anti-hyperlipidaemic activities remain poorly defined. The ultrasound-assisted extraction (UAE) technique has been shown to achieve high yields of bioactive compounds in coffee, with preserved functionality. The goal of the present study was to determine the effect of various coffee roasting extracts using UAE on their anti-hyperglycaemic and anti-hyperlipidaemic properties. We examined α-amylase and α-glucosidase, micelle size, micelle solubility, and pancreatic lipase activities. Coffee roasting degrees were classified as light coffee (LC), medium coffee (MC), and dark coffee (DC). We showed that DC at 80°C for 10 min, 40°C for 20 min, and 20°C for 20 min has a high potency to inhibit α-amylase, α-glucosidase, and pancreatic lipase activities by 33.79±3.25%, 19.68±1.43%, and 36.63±1.58%, respectively. LC enhanced cholesterol micelle size and suppressed cholesterol micelle solubility, which suggests that coffee roasting may enhance anti-hyperglycaemic and anti-hyperlipidaemic activities.

Unraveling the Immunopathogenesis and Genetic Variants in Vasculitis Toward Development of Personalized Medicine.

Leukocytoclastic vasculitis (LCV) is a systemic autoimmune disease characterized by the inflammation of the vascular endothelium. Cutaneous small vessel vasculitis (CSVV) and anti-neutrophil cytoplasmic antibodies (ANCA)-associated vasculitis (AAV) are two examples of LCV. Advancements in genomic technologies have identified risk haplotypes, genetic variants, susceptibility loci and pathways that are associated with vasculitis immunopathogenesis. The discovery of these genetic factors and their corresponding cellular signaling aberrations have enabled the development and use of novel therapeutic strategies for vasculitis. Personalized medicine aims to provide targeted therapies to individuals who show poor response to conventional interventions. For example, monoclonal antibody therapies have shown remarkable efficacy in achieving disease remission. Here, we discuss pathways involved in disease pathogenesis and the underlying genetic associations in different populations worldwide. Understanding the immunopathogenic pathways in vasculitis and identifying associated genetic variations will facilitate the development of novel and targeted personalized therapies for patients.

Antispasmodic Effect of Asperidine B, a Pyrrolidine Derivative, through Inhibition of L-Type Ca2+ Channel in Rat Ileal Smooth Muscle.

Antispasmodic agents are used for modulating gastrointestinal motility. Several compounds isolated from terrestrial plants have antispasmodic properties. This study aimed to explore the inhibitory effect of the pyrrolidine derivative, asperidine B, isolated from the soil-derived fungus Aspergillus sclerotiorum PSU-RSPG178, on spasmodic activity. Isolated rat ileum was set up in an organ bath. The contractile responses of asperidine B (0.3 to 30 µM) on potassium chloride and acetylcholine-induced contractions were recorded. To investigate its antispasmodic mechanism, CaCl2, acetylcholine, Nω-nitro-l-arginine methyl ester (l-NAME), nifedipine, methylene blue and tetraethylammonium chloride (TEA) were tested in the absence or in the presence of asperidine B. Cumulative concentrations of asperidine B reduced the ileal contraction by ~37%. The calcium chloride and acetylcholine-induced ileal contraction was suppressed by asperidine B. The effects of asperidine B combined with nifedipine, atropine or TEA were similar to those treated with nifedipine, atropine or TEA, respectively. In contrast, in the presence of l-NAME and methylene blue, the antispasmodic effect of asperidine B was unaltered. These results suggest that the antispasmodic property of asperidine B is probably due to the blockage of the L-type Ca2+ channel and is associated with K+ channels and muscarinic receptor, possibly by affecting non-selective cation channels and/or releasing intracellular calcium.

Shifting of Physicochemical and Biological Characteristics of Coffee Roasting Under Ultrasound-Assisted Extraction.

Ultrasound-assisted extraction (UAE) is an effective tool for the extraction of natural antioxidants. Thus, differentially roasted Arabica-coffee beans known as light (LC), medium (MC), and dark coffee (DC) were prepared and extracted under the influence of UAE. Following that, they were examined specifically on theirs physicochemical and biological characteristics: nutritional values, pH, °Brix, antioxidant activities, polyphenol content, caffeine, and chlorogenic-acid levels. Various parameters, such as extraction temperatures (20, 40, and 80°C) and extraction time periods (5, 10, and 20 min), were examined. DC extract was less acidic than those on MC and LC extracts. LC showed higher moisture content than the MC and DC (1.56, 1.3, and 0.92%, respectively). MC displayed the highest polyphenol content and potent antioxidant activity. Caffeine and chlorogenic acid contents trend to decrease during roasting. The maximum caffeine level was found in MC at 80°C for 5 min (27.65 mg/g extract). The highest chlorogenic acid content was in LC at 80°C for 10 min (16.67 mg/g extract). The caffeine and chlorogenic acid contents were related to the polyphenol content and depended on the roasting and extraction conditions. These results suggest that the UAE at various temperature and extraction time period may alter the physicochemical and biological characteristics of different coffee roasts.

Coffea arabica bean extract inhibits glucose transport and disaccharidase activity in Caco-2 cells.

The major constituents of Coffea arabica (coffee), including caffeine, chlorogenic acid and caffeic acid, exhibit antihyperglycemic properties in in vitro and in vivo models. However, whether Coffea arabica bean extract (CBE) regulates glucose uptake activity and the underlying mechanisms involved remain unclear. The aim of the present study was to examine the effects of CBE on glucose absorption and identify the mechanisms involved using an in vitro model. The uptake of a fluorescent glucose analog into Caco-2 colorectal adenocarcinoma cells was determined. The expression levels of sodium glucose co-transporter 1 (SGLT1) and glucose transporter 2 (GLUT2) were evaluated. In addition, glycoside hydrolase enzyme activity was investigated. It was observed that CBE inhibited disaccharidase enzyme activity. Furthermore, CBE exerted an inhibitory effect on intestinal glucose absorption by downregulating SGLT1- and GLUT2-mediated 5' AMP-activated protein kinase phosphorylation and suppressing hepatocyte nuclear factor 1α expression. These data suggest that CBE may attenuate glucose absorption and may have potentially beneficial antihyperglycemic effects in the body; however, the mechanisms underlying the effects of CBE must be elucidated through further investigation.