Simultaneous Determination of Seven Sesquiterpene Lactone Glucosides in Ixeris dentata by High-Performance Liquid Chromatography Coupled with Tandem Mass Spectrometry and their Antiviral Activities

Ixeris dentata (Thunb. ex Thunb.) Nakai (Asteraceae), a well-known edible vegetable in Asia, contains various bioactive secondary metabolites, including sesquiterpene lactones. In this study, a high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method has been developed and validated for simultaneous determination of seven sesquiterpene lactone glucosides isolated from the roots of I. dentata. In addition, these compounds were evaluated in terms of their antiviral activities against coxsackievirus B3 (CVB3) and human enterovirus 71 (EV71). The developed method was validated in terms of linearity (R-2 > 0.9996), precision (RSD < 2.24%), accuracy (96.30-102.77%), and stability (RSD < 1.94%) and successfully applied to the quantitation of the I. dentata root samples collected from six different regions of Korea. The content of sesquiterpene lactone glucosides varied significantly based on the region. For the antiviral activities, guaianolides with an ester group at C-8 (compounds 6 and 7) showed the most potent activities against CBV3, while germacranolide (compound 5) showed the most consistent antiviral activity against both CVB3 and EV71. The method was validated to be simple and reliable to simultaneously determine seven putative bioactive sesquiterpene lactone glucosides, the substantial chemotaxonomic markers, in I. dentata root samples.1

Proposing a Value-Based Digital Government Model: Toward Broadening Sustainability and Public Participation

It has generally been well-established, by a number of studies, that the rapid advance and global diffusion of information and communication technology (ICT) is impacting the milieu of governance along with a socio-technical transformation of society at all levels. With a growing interest in digital government, the inquiry concerning a common digital model has been raised. To assist public administrators in thinking about new digital government for their organizations, a new developmental model framework is proposed in this article. This model is drawn from value-based analysis contained in developmental policies, and a subsequent policy development process is also proposed. In doing so, the new model would represent accelerated socio-technical transformation with intelligent technologies, escalating wicked problems appearing despite technological advances. The limitations of the current finite state model are also discussed

Two major modes of East Asian marine heatwaves

We show two major modes of East Asian marine heatwaves (MHWs) associated with two contrasting sea surface temperature patterns over the subtropical western North Pacific (WNP). In the first MHW mode, ocean warming over East Asia occurs along with the subtropical WNP from the earlier winter by an El Niño-Southern Oscillation. The basin-wide ocean warming is finally intensified to an extreme warming state around East Asia, where a high-pressure region in zonal waves across the Eurasian continent passes. In contrast, at the early stage, the second MHW mode is unfavorable with ocean cooling. However, MHWs over East Asia occur due to a significant intensification of a zonally elongated high-pressure zone in response to anomalous subtropical convection in addition to mid-latitude zonal waves. Due to the importance of persistent ocean warming as well as immediate atmospheric forcing, MHW inducible oceanic and atmospheric interactions are clearly distinguishable from those of atmospheric heatwaves

In Vitro Estrogenic and Breast Cancer Inhibitory Activities of Chemical Constituents Isolated from Rheum undulatum L.

We investigated the estrogenic and breast cancer inhibitory activities of chemical constituents isolated from Rhei undulati Rhizoma (roots of Rheum undulatum L.), which is used as a laxative, an anti-inflammatory, and an anti-blood stagnation agent. Estrogen-like activity was studied using the well characterized E-screen assay in estrogen receptor (ER)-positive MCF-7 cells. The mechanism underlying the breast cancer inhibitory activity of the compounds was studied using human ER-negative MDA-MB-231 and ER-positive MCF-7 cells. The activation of apoptosis pathway-related proteins was investigated by western blotting, using extracts of R. undulatum prepared in three solvent conditions (EX1, EX2, and EX3). The R. undulatum chemical constituents (compounds 1–3) showed estrogen-like activity in the concentration range of 10 to 50 μM, by increasing the proliferation of human ER-positive MCF-7 cells. These effects were attenuated by co-treatment with 100 nM fulvestrant, an ER antagonist. Compounds 1–3 decreased the viability of MCF-7 cells in a concentration-dependent manner. Compounds 1 (aloe emodin) and 2 (rhapontigenin) induced mitochondria-independent apoptosis by activating the caspase-8 pathway, whereas the cytotoxic effect of compound 3 (chrysophanol 1-O-β-d-glucopyranoside) was mediated through the mitochondria-dependent apoptotic pathway

The Chemical Constituents from Fruits of Catalpa bignonioides Walt. and Their α-Glucosidase Inhibitory Activity and Insulin Secretion Effect

Catalpa pod has been used in traditional medicine for the treatment of diabetes mellitus in South America. Studies on the constituents of Catalpa species have shown that it is rich in iridoids. In the present study, three previously undescribed compounds (2–4), including two secoiridoid derivatives along with twelve known compounds, were isolated from the fruits of Catalpa bignonioides Walt. In addition, fully assigned 13C-NMR of 5,6-dihydroxy-7,4’-dimethoxyflavone-6-O-sophoroside (1) is reported for the first time in the present study. The structures of compounds were determined on the basis of extensive spectroscopic methods, including UV, IR, 1D, and 2D NMR, mass spectroscopy, and CD spectroscopic data. All the isolated compounds were evaluated for α-glucosidase inhibitory activity. Among the tested compounds, compounds 2, 3, and 9 exhibited significant inhibitory activity against α-glucosidase enzyme assay. Meanwhile, the effect of compounds 2, 3, and 9 on glucose-stimulated insulin secretion (GSIS) was measured using pancreatic β-cells. Compounds 2, 3, and 9 exhibited non-cytotoxicity-stimulated insulin secretion in INS-1 cells. The expression levels of proteins associated with β-cell function and insulin secretion such as phosphorylation of total insulin receptor substrate-2 (IRS-2), phosphatidylinositol 3-kinase (PI3K), Akt, activated pancreatic duodenal homeobox-1 (PDX-1), and peroxisome proliferator-activated receptor-γ (PPAR-γ) were increased in INS-1 cells after treatment with compounds 2, 3, and 9. The findings of the present study could provide a scientific warrant for their application as a potential antidiabetic agent

Marine heatwave events strengthen the intensity of tropical cyclones

Abstract Marine heatwaves become more frequent and stronger due to global warming. It is necessary to clarify how and by which process marine heatwaves affect marine weather systems. Here, we examine how marine heatwaves strengthen tropical cyclones. We analyze 128 tropical cyclones that intensified with marine heatwaves and 184 tropical cyclones that intensified without marine heatwaves over the western North Pacific and Atlantic. Marine heatwaves finally lead to a maximum intensity of 35.4% stronger (106.72 kts) tropical cyclone. Notably, satellite data reveal that marine heatwaves are associated with precipitation-richer tropical cyclone conditions despite similar tropical cyclone intensities. Due to the increased latent heat flux during marine heatwaves, intensified precipitation near the tropical cyclone center contributes to the intensification process. This study provides insights into how more frequent marine heatwaves by global warming impact tropical cyclones

The Chemical Constituents from Fruits of <i>Catalpa bignonioides</i> Walt. and Their α-Glucosidase Inhibitory Activity and Insulin Secretion Effect

Catalpa pod has been used in traditional medicine for the treatment of diabetes mellitus in South America. Studies on the constituents of Catalpa species have shown that it is rich in iridoids. In the present study, three previously undescribed compounds (2–4), including two secoiridoid derivatives along with twelve known compounds, were isolated from the fruits of Catalpa bignonioides Walt. In addition, fully assigned 13C-NMR of 5,6-dihydroxy-7,4’-dimethoxyflavone-6-O-sophoroside (1) is reported for the first time in the present study. The structures of compounds were determined on the basis of extensive spectroscopic methods, including UV, IR, 1D, and 2D NMR, mass spectroscopy, and CD spectroscopic data. All the isolated compounds were evaluated for α-glucosidase inhibitory activity. Among the tested compounds, compounds 2, 3, and 9 exhibited significant inhibitory activity against α-glucosidase enzyme assay. Meanwhile, the effect of compounds 2, 3, and 9 on glucose-stimulated insulin secretion (GSIS) was measured using pancreatic β-cells. Compounds 2, 3, and 9 exhibited non-cytotoxicity-stimulated insulin secretion in INS-1 cells. The expression levels of proteins associated with β-cell function and insulin secretion such as phosphorylation of total insulin receptor substrate-2 (IRS-2), phosphatidylinositol 3-kinase (PI3K), Akt, activated pancreatic duodenal homeobox-1 (PDX-1), and peroxisome proliferator-activated receptor-γ (PPAR-γ) were increased in INS-1 cells after treatment with compounds 2, 3, and 9. The findings of the present study could provide a scientific warrant for their application as a potential antidiabetic agent

Phytochemicals in Chinese Chive (<i>Allium tuberosum</i>) Induce the Skeletal Muscle Cell Proliferation via PI3K/Akt/mTOR and Smad Pathways in C2C12 Cells

Chinese chive (Allium tuberosum) is a medicinal food that is cultivated and consumed mainly in Asian countries. Its various phytochemicals and physiological effects have been reported, but only a few phytochemicals are available for skeletal muscle cell proliferation. Herein, we isolated a new compound, kaempferol-3-O-(6″-feruloyl)-sophoroside (1), along with one known flavonoid glycoside (2) and six amino acid (3–8) compounds from the water-soluble fraction of the shoot of the Chinese chive. The isolated compounds were identified using extensive spectroscopic methods, including 1D and 2D NMR, and evaluated for their proliferation activity on skeletal muscle cells. Among the tested compounds, newly isolated flavonoid (1) and 5-aminouridine (7) up-regulated PI3K/Akt/mTOR pathways, which implies a positive effect on skeletal muscle growth and differentiation. In particular, compound 1 down-regulated the Smad pathways, which are negative regulators of skeletal muscle growth. Collectively, we suggest that major constituents of Chinese chive, flavonoids and amino acids, might be used in dietary supplements that aid skeletal muscle growth

Ethyl Acetate Fraction of <i>Helianthus tuberosus</i> L. Induces Anti-Diabetic, and Wound-Healing Activities in Insulin-Resistant Human Liver Cancer and Mouse Fibroblast Cells

Traditional, complementary, and integrative medicine are globally accepted alternative methods for the treatment of diabetes mellitus (DM). However, the mechanism of anti-diabetic effects of Helianthus tuberosus L. remains unproven. In the present study, antioxidant and anti-diabetic activity of the tubers of H. tuberosus were studied in detail. Methanolic extracts of H. tuberosus tubers were subjected to solvent fractionation method by increasing the polarity of the solvent using n-hexane, and ethyl acetate. The obtained methanol extracts and its fractions were subjected to free radical scavenging activity (DPPH and ABTS assay) and in vitro enzyme (α-amylase and α-glucosidase) inhibition assay. Moreover, glucose uptake in insulin-resistant HepG2 cell line was analyzed. The preliminary phytochemical analysis confirmed the presence of phenolic and flavonoid compounds in the active fraction. The radical scavenging and in vitro diabetic related enzyme inhibitory activities were found to be dose dependent. The maximum ABTS+ and DPPH scavenging activity was documented in ethyl acetate fraction of the H. tuberosus followed by methanol extract, hexane fraction, and methanol fraction. We also found that H. tuberosus showed a less toxicity in mouse fibroblast cells and enhance the glucose uptake in insulin-resistant HepG2 cells. Besides, the ethyl acetate fraction of the H. tuberosus analyzed by UPLC-QTOF-MS-MS and GC/MS revealed the presence of phenolic compounds such as neochlorogenic acid, chlorogenic acid, caffeic acid, 5-O-(4-coumaroyl)-quinic acid, feruloylquinic acid, caffeoylquinic acid, isoxazolidine, salicylic acid β-D-glucoside, dicaffeoylquinic acid isomers, salvianolic acid derivative isomers, and 1,4 dicaffeoylquinic acid etc. Among the identified phytochemicals, six were chosen for molecular docking study to explore their its inhibitory interactions with α-amylase and α-glucosidase. Taken together, the findings of the present study suggested that phytocompounds of EAF were responsible for the significant in vitro antioxidant, wound-healing, and anti-diabetic activities

Ethyl Acetate Fraction of Helianthus tuberosus L. Induces Anti-Diabetic, and Wound-Healing Activities in Insulin-Resistant Human Liver Cancer and Mouse Fibroblast Cells

Traditional, complementary, and integrative medicine are globally accepted alternative methods for the treatment of diabetes mellitus (DM). However, the mechanism of anti-diabetic effects of Helianthus tuberosus L. remains unproven. In the present study, antioxidant and anti-diabetic activity of the tubers of H. tuberosus were studied in detail. Methanolic extracts of H. tuberosus tubers were subjected to solvent fractionation method by increasing the polarity of the solvent using n-hexane, and ethyl acetate. The obtained methanol extracts and its fractions were subjected to free radical scavenging activity (DPPH and ABTS assay) and in vitro enzyme (&alpha;-amylase and &alpha;-glucosidase) inhibition assay. Moreover, glucose uptake in insulin-resistant HepG2 cell line was analyzed. The preliminary phytochemical analysis confirmed the presence of phenolic and flavonoid compounds in the active fraction. The radical scavenging and in vitro diabetic related enzyme inhibitory activities were found to be dose dependent. The maximum ABTS+ and DPPH scavenging activity was documented in ethyl acetate fraction of the H. tuberosus followed by methanol extract, hexane fraction, and methanol fraction. We also found that H. tuberosus showed a less toxicity in mouse fibroblast cells and enhance the glucose uptake in insulin-resistant HepG2 cells. Besides, the ethyl acetate fraction of the H. tuberosus analyzed by UPLC-QTOF-MS-MS and GC/MS revealed the presence of phenolic compounds such as neochlorogenic acid, chlorogenic acid, caffeic acid, 5-O-(4-coumaroyl)-quinic acid, feruloylquinic acid, caffeoylquinic acid, isoxazolidine, salicylic acid &beta;-D-glucoside, dicaffeoylquinic acid isomers, salvianolic acid derivative isomers, and 1,4 dicaffeoylquinic acid etc. Among the identified phytochemicals, six were chosen for molecular docking study to explore their its inhibitory interactions with &alpha;-amylase and &alpha;-glucosidase. Taken together, the findings of the present study suggested that phytocompounds of EAF were responsible for the significant in vitro antioxidant, wound-healing, and anti-diabetic activities