Background: One of the therapeutic strategies for type 2 diabetes mellitus involves suppressing postprandial hyperglycemia by inhibiting key enzymes in carbohydrate digestion, α-glucosidase and α-amylase. While such inhibitors are commercially available, some researchers have turned to plants for potentially cheaper and safer alternatives. Objectives: The study aimed to investigate the in vitro α-glucosidase and α-amylase inhibitory activities of the leaf methanolic extracts of two native Philippine plants Ficus nota Blanco Merr. and Ficus septica Burm F, as well as their effects on postprandial blood glucose levels in a mouse model. Methodology: The in vitro activities of the leaf methanolic extracts were evaluated against porcine pancreatic α-amylase and yeast αglucosidase. The most active extract was partially purified into fractions by sequential solvent partitioning and subjected to in vitro testing. Postprandial antihyperglycemic activity was then assessed in normoglycemic ICR mice. Phytochemical analysis was also performed Results: The most active extract and fraction in vitro were FS-crude and FS-HexF, respectively, having significantly more potent αglucosidase inhibitory activity than the commercial drug acarbose. FS-crude and FS-HexF exhibited strong inhibition of αglucosidase and weak inhibition of α-amylase, which is considered favorable for novel inhibitors as it is hypothesized to reduce gastrointestinal adverse effects. However, FS-crude and FS-HexF did not significantly attenuate postprandial blood glucose levels in the oral starch tolerance test. Phytochemical analysis of FS-HexF putatively identified 6-gingerol as one of the possible bioactive components. Conclusion F. septica could be a potential source of glycoside inhibitors as it showed promising in vitro inhibition of α-amylase and α-glucosidase. While it did not exhibit significant postprandial antihyperglycemic activity in this study, more robust testing is recommended to make a definitive conclusion.
Amylases ; Glucosidases ; Hypoglycemic Agents

OBJECTIVE: To explore the clinical features, lysosomal enzymatic [acid α-glucosidase (GAA)] activities and genetic variants in a child with late-onset Pompe disease (LOPD). METHODS: Clinical data of a child who had presented at the Genetic Counseling Clinic of West China Second University Hospital in August 2020 was retrospectively analyzed. Blood samples were collected from the patient and her parents for the isolation of leukocytes and lymphocytes as well as DNA extraction. The activity of lysosomal enzyme GAA in leukocytes and lymphocytes was analyzed with or without addition of inhibitor of GAA isozyme. Potential variants in genes associated with neuromuscular disorders were analyzed, in addition with conservation of the variant sites and protein structure. The remaining samples from 20 individuals undergoing peripheral blood lymphocyte chromosomal karyotyping were mixed and used as the normal reference for the enzymatic activities. RESULTS: The child, a 9-year-old female, had featured delayed language and motor development from 2 years and 11 months. Physical examination revealed unstable walking, difficulty in going upstairs and obvious scoliosis. Her serum creatine kinase was significantly increased, along with abnormal electromyography, whilst no abnormality was found by cardiac ultrasound. Genetic testing revealed that she has harbored compound heterozygous variants of the GAA gene, namely c.1996dupG (p.A666Gfs*71) (maternal) and c.701C>T (p.T234M) (paternal). Based on the guidelines from the American College of Medical Genetics and Genomics, the c.1996dupG (p.A666Gfs*71) was rated as pathogenic (PVS1+PM2_Supporting+PM3), whilst the c.701C>T (p.T234M) was rated as likely pathogenic (PM1+PM2_Supporting+PM3+PM5+PP3). The GAA in the leukocytes from the patient, her father and mother were respectively 76.1%, 91.3% and 95.6% of the normal value without the inhibitor, and 70.8%, 112.9% and 128.2% of the normal value with the inhibitor, whilst the activity of GAA in their leukocytes had decreased by 6 ~ 9 times after adding the inhibitor. GAA in lymphocytes of the patient, her father and mother were 68.3%, 59.0% and 59.5% of the normal value without the inhibitor, and 41.0%, 89.5% and 57.7% of the normal value with the inhibitor, the activity of GAA in lymphocytes has decreased by 2 ~ 5 times after adding the inhibitor. CONCLUSION The child was diagnosed with LOPD due to the c.1996dupG and c.701C>T compound heterozygous variants of the GAA gene. The residual activity of GAA among LOPD patients can range widely and the changes may be atypical. The diagnosis of LOPD should not be based solely on the results of enzymatic activity but combined clinical manifestation, genetic testing and measurement of enzymatic activity.
Humans ; Child ; Male ; Female ; Glycogen Storage Disease Type II/pathology* ; Retrospective Studies ; alpha-Glucosidases/genetics* ; Mothers ; Lysosomes/pathology* ; Mutation

Pompe disease, also known as glycogen storage disease type Ⅱ, is a rare autosomal recessive disease. With the application of enzyme replacement therapy, more and more patients with Pompe disease can survive to adulthood, and nervous system-related clinical manifestations gradually emerge. Nervous system involvement seriously affects the quality of life of patients with Pompe disease, and a systematic understanding of the clinical manifestations, imaging features and pathological changes of nervous system injury in Pompe disease is of great significance for the early identification and intervention of Pompe disease. This article reviews the research progress of neurological damage in Pompe disease.
Humans ; Glycogen Storage Disease Type II/drug therapy* ; alpha-Glucosidases ; Quality of Life ; Enzyme Replacement Therapy

This study employed the α-glucosidase inhibitory activity model as an anti-diabetic assay and implemented a bioactivity-guided isolation strategy to identify novel natural compounds with potential therapeutic properties. Hypericum sampsoniiwas investigated, leading to the isolation of two highly modified seco-polycyclic polyprenylated acylphloroglucinols (PPAPs) (1 and 2), eight phenolic derivatives (3-10), and four terpene derivatives (11-14). The structures of compounds 1 and 2, featuring an unprecedented octahydro-2H-chromen-2-one ring system, were fully characterized using extensive spectroscopic data and quantum chemistry calculations. Six compounds (1, 5-7, 9, and 14) exhibited potential inhibitory effects against α-glucosidase, with IC₅₀ values ranging from 0.050 ± 0.0016 to 366.70 ± 11.08 μg·mL^-1. Notably, compound 5 (0.050 ± 0.0016 μg·mL^-1) was identified as the most potential α-glucosidase inhibitor, with an inhibitory effect about 6900 times stronger than the positive control, acarbose (IC₅₀ = 346.63 ± 15.65 μg·mL^-1). A docking study was conducted to predict molecular interactions between two compounds (1 and 5) and α-glucosidase, and the hypothetical biosynthetic pathways of the two unprecedented seco-PPAPs were proposed.
Molecular Structure ; Hypericum/chemistry* ; alpha-Glucosidases ; Magnetic Resonance Spectroscopy ; Glycoside Hydrolase Inhibitors/pharmacology*

Nine compounds were isolated from the 90% ethanol extract of Salacia polysperma by silica gel, Sephadex LH-20 column chromatography, together with preparative HPLC methods. Based on HR-ESI-MS, MS, 1D and 2D NMR spectral analyses, the structures of the nine compounds were identified as 28-hydroxy wilforlide B(1), wilforlide A(2), 1β,3β-dihydroxyurs-9(11),12-diene(3),(-)-epicatechin(4),(+)-catechin(5),(-)-4'-O-methyl-ent-galloepicatechin(6), 3-hydroxy-1-(4-hydroxy-3-methoxy-phenyl)propan-1-one(7),(-)-(7S,8R)-4-hydroxy-3,3',5'-trimethoxy-8',9'-dinor-8,4'-oxyneoligna-7,9-diol-7'-aldehyde(8), and vanillic acid(9). Compound 1 is a new oleanane-type triterpene lactone. Compounds 1, 3, 4, 7-9 were isolated from the Salacia genus for the first time. All compounds were assayed for their α-glucosidase inhibitory activity. The results suggested that compound 8 exhibited moderate α-glucosidase inhibitory activity, with an IC_(50) value of 37.2 μmol·L~(-1), and the other compounds showed no α-glucosidase inhibitory activity.
Salacia/chemistry* ; alpha-Glucosidases ; Triterpenes/pharmacology* ; Magnetic Resonance Spectroscopy ; Ethanol ; Molecular Structure

The chemical constituents of the seeds of Moringa oleifera were isolated and purified by using Sephadex LH-20, Toyo-pearl HW-40F, silica gel, ODS, and MCI column chromatography. The structures of compounds were identified by high-resolution mass spectrometry, ~1H-NMR, ~(13)C-NMR, HMQC, HMBC, and ~1H-~1H COSY, as well as physicochemical properties of compounds and literature data. Twelve compounds were isolated from 30% ethanol fraction of the seeds of M. oleifera and identified as ethyl-4-O-α-L-rhamnosyl-α-L-rhamnoside(1), ethyl-3-O-α-L-rhamnosyl-α-L-rhamnoside(2),(4-hydroxybenzyl)ethyl carbamate(3),(4-aminophenyl)acetic acid(4), ethyl-α-L-rhamnoside(5), methyl-α-L-rhamnoside(6), moringapyranosyl(7), 2-[4-(α-L-rhamnosyl)phenyl]methyl acetate(8), niaziridin(9), 5-hydroxymethyl furfural(10), 4-hydroxybenzeneacetamide(11), and 4-hydroxybenzoic acid(12). Among them, compounds 1 and 2 are two new compounds, compound 3 is a new natural product, and compounds 4-5 were yielded from Moringa plant for the first time. All compounds were evaluated for α-glucosidase inhibitory activity in vitro. Compound 10 showed excellent inhibitory activity with IC_(50) of 210 μg·mL~(-1).
Moringa oleifera/chemistry* ; alpha-Glucosidases ; Moringa ; Seeds ; Plant Extracts/pharmacology*

Aims: This study aimed to evaluate antidiabetic potential of indigenous Lactobacillus isolates by measuring the ability of α-glucosidase inhibitory (AGI) and antioxidant activity. The mechanism of probiotics as antidiabetic can occur through the AGI and antioxidant activity of LAB, which is able to suppress oxidative stress that causes chronic inflammation and pancreatic β cell apoptosis, and then through the ability to produce exopolysaccharide (EPS) and short chain fatty acids (SCFA). Methodology and results: MRS broth enriched with 10% glucose was selected as the growth medium for Lactobacillus. The growth medium was then centrifuged to obtain CFS and CFE was produced by extracting the medium with 96% ethanol as a solvent. The results showed that Lactobacillus pentosus MK42 had the highest AGI activity of 80.32 ± 2.20%. Antioxidant activity was not significantly different (P>0.05) among the tested Lactobacillus isolates. Lactobacillus paracasei RK41 produced the highest EPS (360.13 ± 50.01 mg/L), which was not significantly different (P>0.05) from Lactobacillus plantarum1 RB210. All Lactobacillus isolates were able to produce acetic acid, but not all were able to produce propionic and butyric acid. The highest propionic acid was produced by L. plantarum1 RB210 at 0.40 ± 0.31 mmol/L and the highest butyric acid was produced by L. plantarum1 MK2 at 0.22 ± 0.08 mmol/L. Conclusion, significance and impact of study The results show definitively that indigenous Lactobacillus isolates have considerable α-glucosidase inhibitor, antioxidant activity and the ability to produce of EPS and SCFA. This preliminary study suggests the use of indigenous Lactobacillus isolates which have the potential as antidiabetic agent, although the responsible compounds are unknown.
alpha-Glucosidases ; Antioxidants ; Lactobacillus--isolation & ; purification ; Hypoglycemic Agents

Aims: The study aimed to investigate the effect of glucose on alpha-amylase and glucoamylase production in some Indonesian indigenous fungi. Methodology and results: Fungi were screened for their ability to produce alpha-amylase and glucoamylase in the presence of glucose. The strains were grown in a medium containing starch and glucose as carbon sources with glucose concentrations varying from 0 to 5% for four days, and the alpha-amylase and glucoamylase were analyzed at the end of the growth period. Most strains showed repression on the amylases production when glucose was added to the medium. However, some strains showed no repression on amylases production when glucose was supplemented to the medium. The addition of glucose repressed glucoamylase production, but no repression on alpha-amylase was noted for strain KKB4, vice versa, there was repression on alpha-amylase production but no repression on glucoamylase production for strain FIG1. Strains FNCC 6151 and MLT1J1 showed no repression on both alpha-amylase and glucoamylase production when glucose was added to the medium up to 5%. The occurrence of repression in the production of alpha-amylase and glucoamylase was strain-specific. Conclusion, significance and impact of study Out of the nine indigenous fungi strains examined, strains FNCC 6151 and MLT1J1 showed no repression on both alpha-amylase and glucoamylase production when glucose was added to the medium up to 5%. Those two strains have the potential to be improved further to produce both alpha-amylase and glucoamylase.
Glucosidases ; alpha-Amylases ; Glucan 1,4-alpha-Glucosidase

Steroid saponins are secondary metabolites with multiple medicinal values that are found in large quantities in natural medicines, especially Vernonia amygdalina, a famous nature medicine for the treatment of tonsillitis, diabetes, pneumonia. The current study was designed to combine molecular networking (MN) with diagnostic ions for rapid identification of Δ^7,9(11) stigmastane-type saponins which were the α-glucosidase inhibitory active substances in V. amygdalina. First, the α-glucosidase inhibitory activities of five Δ^7,9(11) stigmastane-type steroid saponins that were previously isolated were screened, which indicated that the Δ^7,9(11) stigmastane-type steroid saponin was one of the active constituents responsible for ameliorating diabetes. Furthermore, a strategy was proposed to identify stigmastane-type steroid saponins and verify the plausibility of derived fragmentation pathways by applying MN, MolNetEnhancer and unsupervised substructure annotation (MS2LDA). Based on this strategy, other seven Δ^7,9(11) stigmastane-type steroid saponins were identified from this plant. Our research provide scientific evidence for the antidiabetic potential of the steroid saponin-rich extract of V. amygdalina leaf.
alpha-Glucosidases/metabolism* ; Vernonia/chemistry* ; Plant Extracts/chemistry* ; Plant Leaves/chemistry* ; Saponins/chemistry* ; Steroids/chemistry* ; Diabetes Mellitus

OBJECTIVE: To explore the clinical effect of warming-needle moxibustion with different lengths of moxa stick for asthenospermia with kidney deficiency and liver depression. METHODS: A total of 240 patients with asthenospermia of kidney deficiency and liver depression were randomly divided into a 4-cm group (moxibustion with 4-cm moxa stick, 60 cases, 3 cases dropped off), a 3-cm group (moxibustion with 3-cm moxa stick, 60 cases, 4 cases dropped off), a 2-cm group (moxibustion with 2-cm moxa stick, 60 cases, 2 cases dropped off) and an acupuncture group (60 cases, 3 cases dropped off). All patients were treated with warming-needle moxibustion with different lengths of moxa stick or conventicnal acupuncture at Zhongwan (CV 12), Guanyuan (CV 4), Zhongji (CV 3), Guilai (ST 29), Yaoyangguan (GV 3), Guanyuanshu (BL 26), etc., once a day, five times a week; 4-week treatment was taken as one course, a total of two courses of treatment were given. The semen routine indexes, seminal plasma biochemical indexes, sex hormone levels and TCM syndrome score were compared before and after treatment among the 4 groups. RESULTS: After treatment, the sperm density, sperm viability, ratio of grade A sperm, ratio of grade A and B sperm, seminal plasma fructose and neutral α-glucosidase were higher than those before treatment (P<0.05, P<0.01), and the sperm deformity rates were lower than those before treatment in the 4-cm group and the 3-cm group (P<0.01, P<0.05). The ratio of grade A sperm, ratio of grade A and B sperm, seminal plasma fructose and neutral α-glucosidase in the 4-cm group were higher than the other three groups (P<0.05, P<0.01), and the sperm deformity rate was lower than the other three groups (P<0.05). After treatment, except for dizziness and tinnitus score, each-domain score and total scores of TCM syndrome scale in the 4-cm group and the 3-cm group were lower than those before treatment (P<0.01, P<0.05). The each-domain score of depression, weak waist and knees, low sexual function and total score in the 4-cm group were lower than those in the other three groups (P<0.05, P<0.01). The total effective rate was 87.7% (50/57) in the 4-cm group, which was higher than 78.6% (44/56) in the 3-cm group, 77.6% (45/58) in the 2-cm group and 70.2% (40/57) in the acupuncture group (P<0.05, P<0.01). CONCLUSION The warming-needle moxibustion with 4-cm moxa stick could effectively improve quality and motility of sperm and clinical symptoms in patients with asthenospermia of kidney deficiency and liver depression, which is superior to moxibustion with 3-cm, 2-cm moxa sticks and conventional acupuncture.
Acupuncture Points ; Acupuncture Therapy ; Depression ; Fructose ; Humans ; Kidney ; Liver ; Male ; Moxibustion ; Semen ; Treatment Outcome ; alpha-Glucosidases