Heukharang lettuce (Lactuca sativa L.) leaf extract displays sleep-promoting effects through GABAA receptor.

ETHNOPHARMACOLOGICAL RELEVANCE: Although lettuce is traditionally known to have hypnotic and sedative effects, to date, only a few studies have documented its sleep-promoting effects and elucidated the related mechanisms. AIM OF THE STUDY: We aimed to investigate the sleep-promoting activity of Heukharang lettuce leaf extract (HLE) with increased lactucin content, known as a sleep-promoting substance in lettuce, in animal models. MATERIALS AND METHODS: To evaluate the effect of HLE on sleep behavior, analysis of electroencephalogram (EEG), gene expression of brain receptors, and activation mechanisms using antagonists were investigated in rodent models. RESULTS: High-performance liquid chromatography analysis showed that HLE contained lactucin (0.78 mg/g of extract) and quercetin-3-glucuronide (1.3 mg/g of extract). In the pentobarbital-induced sleep model, the group administered 150 mg/kg of HLE showed a 47.3% increase in sleep duration time as compared to the normal group (NOR). The EEG analysis showed that the HLE significantly increased non-rapid eye movement (NREM), where delta waves were improved by 59.5% when compared to the NOR, resulting in increased sleep time. In the caffeine-induced arousal model, HLE significantly decreased the awake time increased by caffeine administration (35.5%) and showed a similar level to NOR. In addition, HLE increased the gene and protein expression of gamma-aminobutyric acid receptor type A (GABAA), GABA type B, and 5-hydroxytryptamine (serotonin) receptor 1A. In particular, in comparison to the NOR, the group administered 150 mg/kg HLE showed an increase in expression levels of GABAA and protein by 2.3 and 2.5 times, respectively. When the expression levels were checked using GABAA receptor antagonists, HLE showed similar levels to NOR, as the sleep duration was reduced by flumazenil (45.1%), a benzodiazepine antagonist. CONCLUSIONS: HLE increased NREM sleep and significantly improved sleep behavior due to its action on the GABAA receptors. The collective findings suggest that HLE can be used as a novel sleep-enhancing agent in the pharmaceutical and food industries.

The Effects of Antioxidants on the Changes in Volatile Compounds in Heated Welsh Onions (Allium fistulosum L.) during Storage.

Welsh onion (Allium fistulosum L.) is usually used to enhance the flavor characteristics of various foods. Volatile compounds in Welsh onions, including sulfur-containing compounds, may vary during heat process and storage. Accordingly, the changes in the volatile compounds in Welsh onions, subjected to heat and antioxidant (ascorbic acid and glutathione) treatments during storage, are investigated in the present study. The majority of sulfur-containing compounds in Welsh onions showed significant differences between the untreated Welsh onions and heated Welsh onions. During the heating of the Welsh onions, some sulfur-containing compounds, such as 2-methylthiirane, 1-(methyldisulfanyl)prop-1-ene, 1-[[(E)-prop-1-enyl]disulfanyl]propane, 1-(propyltrisulfanyl)propane, 1-[[(E)-prop-1-enyl]trisulfanyl]propane, and (methyltetrasulfanyl)methane, showed significant differences between the untreated and heated Welsh onions (p < 0.05). In addition, partial least square discriminant analysis (PLS-DA) was applied to discriminate the heated Welsh onion samples added with different antioxidants. The heated Welsh onion samples added with ascorbic acid was mainly associated with 2-phenylacetaldehyde, acetic acid, methylsulfanylmethane, prop-2-ene-1-thiol, undecan-2-one, and (2E,4E)-deca-2,4-dienal. Moreover, the key volatile compounds in the heated Welsh onion samples added with glutathione were 3-ethylthiophene, 1-(methyldisulfanyl)-1-methylsulfanylpropane, 1-methylsulfanylpentane, 2-prop-2-enylsulfanylpropane, and 1-propan-2-ylsulfanylbutane.

Evaluation of Caspase-3 and Ki-67 expression in squamous cell hyperplasia of the stomach induced by Platycodi radix water extract in Sprague-Dawley rats.

Platycodi radix is widely used in traditional herbal medicine for the treatment of bronchitis, asthma, pulmonary tuberculosis, hypertension, hyperlipidemia, and diabetes. This study aimed to investigate cell proliferation (Ki-67) and apoptosis (Caspase-3) potential in squamous cell hyperplasia of the stomach induced by a Platycodi radix water extract in a subchronic toxicity study. One hundred formalin-fixed, paraffin-embedded stomach tissues of rats treated with Platycodi radix at doses of 0, 500, 1,000, and 3,000 mg/kg body weight/day were used for the analysis. They were conventionally stained using hematoxylin and eosin (H&E) and immunohistochemically (IHC) stained using caspase-3 and Ki-67 antibodies. The incidence of squamous cell hyperplasia was significantly increased in the 3,000 mg/kg b.w./day treatment group in both sexes (p<0.01). However, the hyperplastic change was completely repaired after 4 weeks of recovery period. Ki-67 expression was similar in all groups, with no statistically significant differences among the groups. Caspase-3 expression was significantly increased in both sexes in the 3,000 mg/kg b.w./day treatment group (p<0.01), compared with the vehicle control groups, and then reduced to normal levels in the recovery groups in both sexes. In conclusion, this study showed that squamous cell hyperplasia induced by the Platycodi radix water extract in the limiting ridge of the stomach is not considered to be abnormal proliferative change; as a result, squamous cell hyperplasia is considered to be a non-adverse effect when induced by the oral administration of the Platycodi radix water extract once daily for 13 weeks in rats.

Integrated digital pathology at scale: A solution for clinical diagnostics and cancer research at a large academic medical center.

OBJECTIVE: Broad adoption of digital pathology (DP) is still lacking, and examples for DP connecting diagnostic, research, and educational use cases are missing. We blueprint a holistic DP solution at a large academic medical center ubiquitously integrated into clinical workflows; researchapplications including molecular, genetic, and tissue databases; and educational processes. MATERIALS AND METHODS: We built a vendor-agnostic, integrated viewer for reviewing, annotating, sharing, and quality assurance of digital slides in a clinical or research context. It is the first homegrown viewer cleared by New York State provisional approval in 2020 for primary diagnosis and remote sign-out during the COVID-19 (coronavirus disease 2019) pandemic. We further introduce an interconnected Honest Broker for BioInformatics Technology (HoBBIT) to systematically compile and share large-scale DP research datasets including anonymized images, redacted pathology reports, and clinical data of patients with consent. RESULTS: The solution has been operationally used over 3 years by 926 pathologists and researchers evaluating 288 903 digital slides. A total of 51% of these were reviewed within 1 month after scanning. Seamless integration of the viewer into 4 hospital systems clearly increases the adoption of DP. HoBBIT directly impacts the translation of knowledge in pathology into effective new health measures, including artificial intelligence-driven detection models for prostate cancer, basal cell carcinoma, and breast cancer metastases, developed and validated on thousands of cases. CONCLUSIONS: We highlight major challenges and lessons learned when going digital to provide orientation for other pathologists. Building interconnected solutions will not only increase adoption of DP, but also facilitate next-generation computational pathology at scale for enhanced cancer research.

A dietary anthocyanin cyanidin-3-O-glucoside binds to PPARs to regulate glucose metabolism and insulin sensitivity in mice.

We demonstrate the mechanism by which C3G, a major dietary anthocyanin, regulates energy metabolism and insulin sensitivity. Oral administration of C3G reduced hepatic and plasma triglyceride levels, adiposity, and improved glucose tolerance in mice fed high-fat diet. Hepatic metabolomic analysis revealed that C3G shifted metabolite profiles towards fatty acid oxidation and ketogenesis. C3G increased glucose uptake in HepG2 cells and C2C12 myotubes and induced the rate of hepatic fatty acid oxidation. C3G directly interacted with and activated PPARs, with the highest affinity for PPARα. The ability of C3G to reduce plasma and hepatic triglycerides, glucose tolerance, and adiposity and to induce oxygen consumption and energy expenditure was abrogated in PPARα-deficient mice, suggesting that PPARα is the major target for C3G. These findings demonstrate that the dietary anthocyanin C3G activates PPARs, a master regulators of energy metabolism. C3G is an agonistic ligand of PPARs and stimulates fuel preference to fat.

Anti-microbial and anti-inflammatory effects of Cheonwangbosim-dan against Helicobacter pylori-induced gastritis.

BACKGROUND: There are various Helicobacter species colonizing the stomachs of animals. Although Helicobacter species usually cause asymptomatic infection in the hosts, clinical signs can occur due to gastritis associated with Helicobacter in animals. Among them, Helicobacter pylori is strongly associated with chronic gastritis, gastric ulcers, and gastric cancers. As the standard therapies used to treat H. pylori have proven insufficient, alternative options are needed to prevent and eradicate the diseases associated with this bacterium. Cheonwangbosim-dan (CBD), a traditional herbal formula that is popular in East Asia, has been commonly used for arterial or auricular flutter, neurosis, insomnia, and cardiac malfunction-induced disease. OBJECTIVES: The present study investigated the antimicrobial effect of CBD on H. pylori-infected human gastric carcinoma AGS cells and model mice. METHODS: AGS cells were infected with H. pylori and treated with a variety of concentrations of CBD or antibiotics. Mice were given 3 oral inoculations with H. pylori and then dosed with CBD (100 or 500 mg/kg) for 4 weeks or with standard antibiotics for 1 week. One week after the last treatment, gastric samples were collected and examined by histopathological analysis, real-time quantitative polymerase chain reaction, and immunoblotting. RESULTS: Our results showed that CBD treatment of AGS cells significantly reduced the H. pylori-induced elevations of interleukin-8, inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2). In the animal model, CBD treatment inhibited the colonization of H. pylori and the levels of malondialdehyde, inflammation, proinflammatory cytokines, iNOS, and COX-2 in gastric tissues. CBD also decreased the phosphorylation levels of p38 mitogen-activated protein kinase family. CONCLUSIONS: This study suggests that CBD might be a prospective candidate for treating H. pylori-induced gastric injury.

Effects of hydroxycinnamic acids on the reduction of furan and α-dicarbonyl compounds.

The effects of hydroxycinnamic acids such as cinnamic acid (CNA), p-coumaric acid(CMA), caffeic acid (CFA), and chlorogenic acid (CGA) on the reduction of furan in canned-coffee model systems (CCMS) containing α-dicarbonyls [glyoxal (GO) or methylglyoxal (MGO)] were investigated. The concentration of furan in CCMS containing GO, which was 59.76 µg/L, was reduced by the addition of CFA and CGA to 48.31 µg/L and 41.38 µg/L, respectively; similarly, the furan concentration in model system containing MGO was 45.79 µg/L, and this decreased to 35.41 µg/L (by CFA) and 32.65 µg/L (by CGA), respectively. In addition, the effects of hydroxycinnamic acids on the trapping of GO and MGO were determined. CFA and CGA greatly reduced the concentration of GO to 303.51 µg/L and 267.80 µg/L, respectively (compared to 515.79 µg/L in the control), whereas that of MGO was decreased to 207.01 µg/L and 219.14 µg/L (compared to 417.14 µg/L in the control). The trapping of α-dicarbonyls such as GO and MGO by CFA and CGA could be closely related to furan reduction in CCMS.

A Double-Blind, Randomized Controlled 12-Week Follow-Up Trial to Evaluate the Efficacy and Safety of Polycan in Combination with Glucosamine for the Treatment of Knee Osteoarthritis.

AIM: The aim of the present study was to examine the efficacy and safety of Polycan, a ß-glucan produced from the black yeast Aureobasidium pullulans SM-2001, in combination with glucosamine in reducing knee osteoarthritis-associated symptoms. METHODS: This was a double-blind, randomized controlled trial of a formulated product composed of 16.7 mg of Polycan and 250 mg of glucosamine (Group A), 16.7 mg of Polycan and 500 mg of glucosamine (Group B), or 500 mg of glucosamine (control group) per capsule, administered as three capsules once per day over a period of 12 weeks, conducted with 100 osteoarthritis patients, aged 35-80 years. The primary outcome measure was osteoarthritis symptoms assessed by the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) questionnaire. The secondary outcome measures included rescue medication use (according to data from a patient-reported diary) and other safety indices (body weight, blood pressure, hematological, and biochemistry markers). RESULTS: Compared with the control group, Group B demonstrated a statistically significant reduction in the total WOMAC score after 12 weeks of treatment (p < 0.05). There was a significant reduction in the frequency of rescue medication used in Groups A and B compared with the control group (p < 0.05). There were no significant changes in hematology and biochemistry parameters or health indices between the active and the control group. CONCLUSION: Among patients with mild or moderate osteoarthritis, a daily oral dose of Polycan (50 mg) in combination with glucosamine (750 mg or 1500 mg; Group A or B, respectively) resulted in a better treatment outcome than treatment with glucosamine (1500 mg) alone.

The role of adjuvant external beam radiation therapy for papillary thyroid carcinoma invading the trachea.

PURPOSE: To evaluate the effect of adjuvant external beam radiation therapy (EBRT) on local failure-free survival rate (LFFS) for papillary thyroid cancer (PTC) invading the trachea. MATERIALS AND METHODS: Fifty-six patients with locally advanced PTC invading the trachea were treated with surgical resection. After surgery, 21 patients received adjuvant EBRT and radioactive iodine therapy (EBRT group) and 35 patients were treated with radioactive iodine therapy (control group). RESULTS: The age range was 26-87 years (median, 56 years). The median follow-up period was 43 months (range, 4 to 145 months). EBRT doses ranged from 50.4 to 66 Gy (median, 60 Gy). Esophagus invasion and gross residual disease was more frequent in the EBRT group. In the control group, local recurrence developed in 9 (9/35, 26%) and new distant metastasis in 2 (2/35, 6%) patients, occurring 4 to 68 months (median, 37 months) and 53 to 68 months (median, 60 months) after surgery, respectively. Two patients had simultaneous local recurrence and new distant metastasis. There was one local failure in the EBRT group at 18 months after surgery (1/21, 5%). The 5-year LFFS was 95% in the EBRT group and 63% in the control group (p = 0.103). In the EBRT group, one late grade 2 xerostomia was developed. CONCLUSION: Although, EBRT group had a higher incidence of esophagus invasion and gross residual disease, EBRT group showed a better 5-year LFFS. Adjuvant EBRT may have contributed to the better LFFS in these patients.

Dietary galacto-oligosaccharides improve skin health: a randomized double blind clinical trial.

BACKGROUND AND OBJECTIVES: To study the effects of galacto-oligosaccharides (GOS) on the skin, we investigated skin-related parameters in healthy adults who received GOS for 12 weeks. METHODS AND STUDY DESIGN: This double-blind, randomized, placebo-controlled study included subjects divided into two groups (control and GOS) by stratified block randomization. The GOS group received 1.0 g of GOS twice a day, whereas the control group received only vehicle. RESULTS: The results showed that the increase in corneometer values from baseline to week 12 was significantly greater in the GOS group than in the control group (6.91 vs 2.88 arbitrary units, p<0.05). The transepidermal water loss (TEWL) in the GOS group was reduced significantly after 12 weeks of GOS treatment (20.1 g/h/m2 at baseline vs 17.5 g/h/m2 at week 12, p<0.05). The differences in total and percentage of wrinkle areas between the two groups were statistically significant after 12 weeks of GOS treatment (p<0.05). CONCLUSION: Our findings support that oral treatment with GOS is beneficial to the skin and present the possibility of new nutritional strategies for skin care.

Antiproliferative and Apoptotic Activity of Chamaecyparis obtusa Leaf Extract against the HCT116 Human Colorectal Cancer Cell Line and Investigation of the Bioactive Compound by Gas Chromatography-Mass Spectrometry-Based Metabolomics.

Chamaecyparis obtusa (CO) belongs to the Cupressaceae family, and it is found widely distributed in Japan and Korea. In this study, the anti-proliferative activities of the methanol and water extracts of CO leaves against a human colorectal cancer cell line (HCT116) were investigated. The methanol extract of CO leaves, at a concentration of 1.25 µg/mL, exhibited anti-proliferative activity against HCT116 cells, while displaying no cytotoxicity against Chang liver cells. Comparative global metabolite profiling was performed using gas chromatography-mass spectrometry coupled with multivariate statistical analysis, and it was revealed that anthricin was the major compound contributing to the anti-proliferative activity. The activation of c-Jun N-terminal kinases played a key role in the apoptotic effect of the methanol extract of CO leaves in HCT116 human colon cancer cells. These results suggest that the methanol extract and anthricin derived from CO leaves might be useful in the development of medicines with anti-colorectal cancer activity.

Effects of acupuncture at GB20 on CO2 reactivity in the basilar and middle cerebral arteries during hypocapnia in healthy participants.

OBJECTIVES: The acupoint GB20 is known to affect vertebrobasilar blood flow regulation. However, no previous study has used transcranial Doppler imaging to examine whether acupuncture at GB20 has a selective effect on blood flow in various cerebral arteries, such as the basilar artery (BA) and the middle cerebral arteries (MCAs). Therefore, this study sought to determine the specific effects of GB20 acupuncture on cerebral blood flow (CBF). MATERIALS AND METHODS: Blood flow velocity and CO(2) reactivity were measured by transcranial Doppler imaging with a 2-MHz pulsed Doppler probe observed through both temporal windows for the MCAs and through the suboccipital window for the BA before and after GB20 acupuncture treatment in 15 healthy young male volunteers. The changes in hyperventilation-induced CO(2) reactivity and corrected blood flow velocities at 40 mmHg (CV40) were assessed for the BA and both MCAs. Blood pressure and heart rate were measured before and after the acupuncture treatment. RESULTS: CO(2) reactivity in the BA increased significantly after GB20 acupuncture treatment compared with baseline (p=0.041). In contrast, CO(2) reactivity in both MCAs remained unchanged. The CV40 in the BA and the MCAs showed no change after the GB20 acupuncture treatment. The mean heart rate decreased significantly after the GB20 acupuncture, whereas the mean blood pressure showed no change. CONCLUSIONS: This study demonstrated that acupuncture treatment on GB20 increases CO(2) reactivity specifically in the BA, with no effect in the MCAs. These results clinically support the use of GB20 to treat disorders of posterior cerebral circulation and support the idea that particular acupoints affect specific brain regions and cerebral arteries.

Metabolite profiling of red and white pitayas (Hylocereus polyrhizus and Hylocereus undatus) for comparing betalain biosynthesis and antioxidant activity.

Metabolite profiling of red and white pitayas (Hylocereus polyrhizus and Hylocereus undatus) was performed using gas chromatography-time-of-flight-mass spectrometry and ultraperformance liquid chromatography-quadrupole-time-of-flight-mass spectrometry with multivariate analysis. Different species and parts of pitayas (red peel, RP; white peel, WP; red flesh, RF; and white flesh, WF) were clearly separated by partial least-squares discriminate analysis. Furthermore, betalain-related metabolites, such as betacyanins and betaxanthins, or their precursors were described on the basis of their metabolites. The results of antioxidant activity tests [1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS), and ferric reducing ability of plasma (FRAP)], total phenolic contents (TPC), total flavonoid contents (TFC), and total betacyanin contents (TBC) showed the following: RP ≥ WP > RF > WF. TPC, TFC, TBC, and betalain-related metabolites were higher in the peel than in the flesh and suggested to be the main contributors to antioxidant activity in pitayas. Therefore, peels as well as pulp of pitaya could beneficially help in the food industry.

Effect of ST36 Acupuncture on Hyperventilation-Induced CO 2 Reactivity of the Basilar and Middle Cerebral Arteries and Heart Rate Variability in Normal Subjects.

This study was conducted to verify the effect of acupuncture on cerebral haemodynamics to provide evidence for the use of acupuncture treatment as a complementary therapy for the high-risk stroke population. The effect of ST36 acupuncture treatment on the hyperventilation-induced CO2 reactivity of the basilar and middle cerebral arteries was studied in 10 healthy male volunteers (mean age, 25.2 ± 1.5 years) using a transcranial Doppler sonography with an interval of 1 week between measurements, and a portable ECG monitoring system was used to obtain ECG data simultaneously. The CO2 reactivity of the basilar and middle cerebral arteries increased significantly after ST36 acupuncture treatment, whereas the mean arterial blood pressure and pulse rate did not change significantly. The high-frequency power significantly increased after ST36 acupuncture treatment, and the percentage increase of high-frequency power correlated significantly with the percentage increase in the CO2 reactivity of the contralateral middle cerebral artery. These data suggest that ST36 acupuncture treatment increases CO2 reactivity, indicating improvement of vasodilatory potential of the cerebral vasculature to compensate for fluctuations caused by changes in external conditions. The increase in parasympathetic tone by ST36 acupuncture treatment is responsible for this therapeutic effect.

Molecular structural differences between low methoxy pectins induced by pectin methyl esterase II: effects on texture, release and perception of aroma in gels of similar modulus of elasticity.

Six low-methoxy pectins with different degrees of methylesterification and amidation, and molecular weights were used to prepare gels with similar moduli of elasticity by varying the concentrations of pectin and calcium phosphate. Five aroma compounds were added to the gels and their sensory textural properties, release and perception of aromas were investigated. Sensory firmness, springiness, adhesiveness, chewiness and cohesiveness differed according to the gel type, even though the moduli of elasticity were not significantly different (p<0.05). Release and perception of aromas also displayed significant difference according to the gel type (p<0.05). Low-methoxy amidated pectin exhibited the lowest release and perception for all the aroma compounds, while pectin-methylesterase-treated pectin gels exhibited relatively higher aroma release and perception. These results showed that the structural properties of pectins and gelling factors that increase the non-polar character of the gel matrices could decrease the release and perception of aromas in pectin gel systems.

Prevention of inflammation-mediated neurotoxicity by butylidenephthalide and its role in microglial activation.

Microglial cells are the prime effectors in immune and inflammatory responses of the central nervous system (CNS). During pathological conditions, the activation of these cells helps restore CNS homeostasis. However, chronic microglial activation endangers neuronal survival through the release of various proinflammatory molecules and neurotoxins. Thus, negative regulators of microglial activation have been considered as potential therapeutic candidates to target neurodegeneration, such as that in Alzheimer's and Parkinson's diseases. The rhizome of Ligusticum chuanxiong Hort. (Ligusticum wallichii Franch) has been widely used for the treatment of vascular diseases in traditional oriental medicine. Butylidenephthalide (BP), a major bioactive component from L. chuanxiong, has been reported to have a variety of pharmacological activities, including vasorelaxant, anti-anginal, anti-platelet and anti-cancer effects. The aim of this study was to examine whether BP represses microglial activation. In rat brain microglia, BP significantly inhibited the lipopolysaccharide (LPS)-induced production of nitric oxide (NO), tumour necrosis factor-α and interleukin-1ß. In organotypic hippocampal slice cultures, BP clearly blocked the effect of LPS on hippocampal cell death and inhibited LPS-induced NO production in culture medium. These results newly suggest that BP provide neuroprotection by reducing the release of various proinflammatory molecules from activated microglia.

Differences in the volatile compositions of ginseng species (Panax sp.).

The volatile compositions in dried white ginseng according to species (Panax ginseng, Panax notoginseng, and Panax quinquefolius) were analyzed and compared by applying multivariate statistical techniques to gas chromatography-mass spectrometry data sets. Main volatile compounds of ginseng species in the present study were sesquiterpenes, such as bicyclogermacrene, (E)-ß-farnesene, ß-panasinsene, calarene, α-humulene, ß-elemene, etc. In particular, α-selinene, α-terpinolene, ß-bisabolene, ß-phellandrene, ß-sesquiphellandrene, zingiberene, germacrene D, limonene, α-gurjunene, (E)-caryophyllene, δ-cadinene, (E)-ß-farnesene, α-humulene, bicyclogermacrene, longiborn-8-ene, ß-neoclovene, and (+)-spathulenol were mainly associated with the difference between P. ginseng and P. notoginseng versus P. quinquefolius species. On the other hand, the discrimination between P. ginseng and P. notoginseng could be constructed by hexanal, 2-pyrrolidinone, (E)-2-heptenal, (E)-2-octenal, heptanal, isospathulenol, (E,E)-2,4-decadienal, 3-octen-2-one, benzaldehyde, 2-pentylfuran, and (E)-2-nonenal.

α-Glucosidase inhibition and antihyperglycemic activity of prenylated xanthones from Garcinia mangostana.

An ethanol extract of the fruit case of Garcinia mangostan, whose most abundant chemical species are xanthones, showed potent α-glucosidase inhibitory activity (IC(50)=3.2 µg/ml). A series of isolated xanthones (1-16) demonstrated modest to high inhibition of α-glucosidase with IC(50) values of 1.5-63.5 µM. In particular, one hitherto unknown xanthone 16 has a very rare 2-oxoethyl group on C-8. Kinetic enzymatic assays with a p-nitrophenyl glucopyranoside indicated that one of them, compound (9) exhibited the highest activity (K(i)=1.4 µM) and mixed inhibition. Using, a physiologically relevant substrate, maltose, as substrate, many compounds (6, 9, 14, and 15) also showed potent inhibition which ranged between 17.5 and 53.5 µM and thus compared favorably with deoxynojirimycin (IC(50)=68.8 µM). Finally, the actual pharmacological potential of the ethanol extract was demonstrated by showing that it could elicit reduction of postprandial blood glucose levels. Furthermore, the most active α-glucosidase inhibitors (6, 9, and 14) were proven to be present in high quantities in the native seedcase by a HPLC chromatogram.

The compositions of volatiles and aroma-active compounds in dried omija fruits (Schisandra chinensis Baillon) according to the cultivation areas.

Differences in the compositions of volatiles from dried omija fruits (Schisandra chinensis Baillon) cultivated in different areas (Mungyeong, Jangsu, Jechon, and Hoengseong) in South Korea were determined by applying principal component analysis to gas chromatography-mass spectrometry data sets. Quantitative assessments revealed that terpene hydrocarbons, such as germacrene D, ß-selinene, α-ylangene, ß-elemene, α-selinene, and (E)-ß-farnesene, were the main volatiles in all omija fruit samples. On the other hand, (E)-ß-ocimene, calarene, (E)-ß-farnesene, ß-selinene, nonanal, 2-methylbutanoic acid, benzoic acid, 2,3-butanediol, and phenethyl alcohol were the major volatile components that contributed to the discrimination between omija fruit samples from the four cultivation areas. In addition, aroma-active compounds in four dried omija fruits were investigated and compared by gas chromatography-olfactometry using aroma extract dilution analysis. (E)-ß-Ocimene (floral and herbaceous), α-pinene (pine-like and woody), hexanal (cut grass-like), 5-methylfurfural (burnt sugar-like and sweet), and α-terpinene (minty, green, and fresh) were important aroma-active compounds in all omija samples. Interestingly, the flavor dilution factors of most aroma-active compounds were lower for omija sample cultivated in Hoengseong than for those cultivated in Mungyeong, Jangsu, and Jechon.

Metabolic profiling and predicting the free radical scavenging activity of guava (Psidium guajava L.) leaves according to harvest time by 1H-nuclear magnetic resonance spectroscopy.

Guava leaves were classified and the free radical scavenging activity (FRSA) evaluated according to different harvest times by using the (1)H-NMR-based metabolomic technique. A principal component analysis (PCA) of (1)H-NMR data from the guava leaves provided clear clusters according to the harvesting time. A partial least squares (PLS) analysis indicated a correlation between the metabolic profile and FRSA. FRSA levels of the guava leaves harvested during May and August were high, and those leaves contained higher amounts of 3-hydroxybutyric acid, acetic acid, glutamic acid, asparagine, citric acid, malonic acid, trans-aconitic acid, ascorbic acid, maleic acid, cis-aconitic acid, epicatechin, protocatechuic acid, and xanthine than the leaves harvested during October and December. Epicatechin and protocatechuic acid among those compounds seem to have enhanced FRSA of the guava leaf samples harvested in May and August. A PLS regression model was established to predict guava leaf FRSA at different harvesting times by using a (1)H-NMR data set. The predictability of the PLS model was then tested by internal and external validation. The results of this study indicate that (1)H-NMR-based metabolomic data could usefully characterize guava leaves according to their time of harvesting.