Anti-bacterial effects of components from <i>Sanguisorba officinalis</i> L. on <i>Vibrio vulnificus</i> and their soluble epoxide hydrolase inhibitory activity

<p><i>Sanguisorba officinalis</i> L. is a traditional herbal medicine, which is prevailingly applied to cure hemorrhoids, wounds and ulcers in Eastern Asian countries. The purpose of this study was to investigate the antibacterial and soluble epoxide hydrolase (sEH) inhibitory effects of the extracts and components from <i>S. officinalis</i>. The methanol extract was divided into ethyl acetate (EtOAc), <i>n</i>-butanol (<i>n</i>-BuOH), and water layers. In our screening procedure, the EtOAc and <i>n</i>-BuOH extracts and compounds (<b>1</b>–<b>2</b>) remarkably suppressed the growth of <i>V. vulnificus</i> in a dose-dependent manner. In addition, the EtOAc extract and compound <b>1</b> exhibited significant inhibitory effect on the <i>V</i>. <i>vulnificus</i> induced cytotoxicity on HeLa cells. Furthermore, compound <b>4</b> displayed an inhibition against sEH with an IC₅₀ value of 7.0 ± 0.5 μM. A kinetic analysis demonstrated that the inhibitory effect of compound <b>4</b> was a mixed type, with an inhibitory constant (<i>K</i>_<i>i</i>) 0.22 ± 0.0 μM.</p

Lipolytic effect of compounds isolated from leaves of mulberry (<i>Morus alba</i> L.) in 3T3-L1 adipocytes

<p>In this study, 19 known compounds were isolated from mulberry (<i>Morus alba</i> L.) leaves. The lipid accumulation inhibitory activity of the isolated compounds was investigated. Compounds <b>4</b> and <b>12</b> showed good anti-adipogenic activity based on 3T3-L1 adipocytes with values of 36.6 ± 9.0 and 34.7 ± 4.0%, respectively. In addition, compounds <b>3</b>, <b>6</b> and <b>15</b> showed significant inhibitory activity with values from 15.4 to 21.2% and compounds <b>2</b>, <b>8</b>–<b>9</b> and <b>17</b>–<b>18</b> exhibited weak activity with values ranging from 2.1 to 10.7% at a concentration of 40.0 μM. These results show the potentiality that mulberry leaf is an excellent inhibitory phytochemical source against lipid accumulation.</p

NF-κB Inhibitory Activity of Sucrose Fatty Acid Esters and Related Constituents from Astragalus membranaceus

Twelve compounds, including six sucrose fatty acid esters (<b>1</b>–<b>6</b>), four galactosyl acylglycerols (<b>7</b>–<b>10</b>), and two sphingolipids (<b>11</b> and <b>12</b>), were isolated from the roots of Astragalus membranaceus. Their structures were identified on the basis of spectroscopic analysis. Among the isolated sucrose fatty acid esters, 6′-<i>O</i>-linoleyl sucrose (<b>1</b>) was identified as a new compound, and 6′-<i>O</i>-palmitoyl sucrose (<b>2</b>) and 6-<i>O</i>-palmitoyl sucrose (<b>3</b>) were isolated from nature for the first time. This is the first report on sucrose fatty acid ester components from <i>A. membranaceus</i>. The nuclear factor-κB (NF-κB) inhibitory activity of isolated compounds was measured in HepG2 cells stimulated with TNF-α using a luciferase reporter system. Among them, compounds <b>1</b>–<b>6</b> exhibited significant inhibition of NF-κB activation in a dose-dependent manner, with IC₅₀ values ranging from 4.4 to 24.7 μM. Compounds <b>1</b>–<b>6</b> also exhibited inhibition of TNF-α-induced expression of iNOS and ICAM-1 mRNA and dose-dependent inhibition of iNOS promoter activity, with IC₅₀ values ranging from 3.3 to 5.0 μM. These data demonstrate the potential of sucrose fatty acid esters from <i>A. membranaceus</i> to prevent and treat inflammatory diseases

Coumarins and Lignans from Zanthoxylum schinifolium and Their Anticancer Activities

Zanthoxylum schinifolium is an aromatic shrub, and its pericarp and leaves are widely used in culinary applications in East Asian countries. It has also long been used in traditional Oriental medicine for treating the common cold, stomach ache, diarrhea, and jaundice. In this study, we identified two new compounds, zanthoxyloside (<b>1</b>) and schinifolisatin A (<b>13</b>), along with 23 known coumarins (<b>2</b>–<b>12</b>) and lignans (<b>14</b>–<b>25</b>), from a methanol extract of the stems of Z. schinifolium. The chemical structures of the compounds were determined by mass, 1D-, and 2D NMR spectroscopy. The anticancer effects of the isolated compounds were examined in three human cancer cell lines. Compounds <b>10</b>–<b>12</b> significantly reduced the proliferation of HL-60 human acute promyelocytic leukemia cells with IC₅₀ values of 4.62–5.12 μM. Treatment of PC-3 prostate cancer cells and SNU-C5 colorectal cancer cells with compound <b>10</b> resulted in potent antiproliferative activity, with IC₅₀ values of 4.39 and 6.26 μM, respectively. Also, compounds <b>10</b>–<b>12</b> induced the apoptosis of three cancer cells. Furthermore, the induction of apoptosis was accompanied by down-regulation of p-ERK1/2 MAPK, p-AKT, and c-myc levels, in a time-dependent manner. These data suggested that compounds <b>10</b>–<b>12</b> from Z. schinifolium have potential in cancer treatment

Tyrosinase inhibitory components from <i>Aloe vera</i> and their antiviral activity

<p>A new compound, 9-dihydroxyl-2'-<i>O</i>-(<i>Z</i>)-cinnamoyl-7-methoxy-aloesin (<b>1</b>), and eight known compounds (<b>2</b>–<b>9</b>) were isolated from <i>Aloe vera.</i> Their structures were elucidated using 1D/2D nuclear magnetic resonance and mass spectra. Compound <b>9</b> exhibited reversible competitive inhibitory activity against the enzyme tyrosinase, with an IC₅₀ value of 9.8 ± 0.9 µM. A molecular simulation revealed that compound <b>9</b> interacts via hydrogen bonding with residues His244, Thr261, and Val283 of tyrosinase. Additionally, compounds <b>3</b> and <b>7</b> were shown by half-leaf assays to exhibit inhibitory activity towards <i>Pepper mild mottle virus</i>.</p

Cytotoxic triterpene saponins from the mangrove <i>Aegiceras corniculatum</i>

<p>Using various chromatographic separations, sixteen compounds, including one new triterpene saponin named aegicoroside A (<b>1</b>), were isolated from the leaves of the Vietnamese mangrove <i>Aegiceras corniculatum</i>. Their structures were determined by spectroscopic methods such as 1D and 2D NMR and HR-ESI-MS. The cytotoxic activities of the isolated compounds against MCF7 (breast), HCT116 (colon), B16F10 (melanoma), and A549 (adenocarcinoma) cancer cell lines were also evaluated. Strong cytotoxicity was observed for sakurasosaponin (<b>2</b>) against all four cancer cell lines and for sakurasosaponin methyl ester (<b>3</b>) against MCF7, A549, and HCT116 cell lines with IC₅₀ values ranging from 2.89 ± 0.02 to 9.86 ± 0.21 μM.</p

A new rearranged abietane diterpene from <i>Clerodendrum inerme</i> with antioxidant and cytotoxic activities

<p>Eight compounds were isolated from the leaves of <i>Clerodendrum inerme</i>, including one new rearranged abietane diterpene, crolerodendrum B (<b>1</b>). Their structures were determined by means of spectroscopic methods including one-dimensional and two-dimensional nuclear magnetic resonance (1-D and 2-DNMR), high-resolution electrospray ionisation mass spectrometry (HR-ESI-MS) and circular dichroism (CD). The DPPH radical scavenging and cytotoxic activities of isolated compounds against MCF7 (breast), HCT116 (colon) and B16F10 (melanoma) cancer cell lines were evaluated. Compounds <b>1</b>, <b>3</b> and <b>4</b> exhibited strong DPPH radical-scavenging effects (ED₅₀ values of 17.6 ± 2.1, 10.1 ± 0.8 and 11.3 ± 0.3 μM, respectively) and <b>4</b> showed strong cytotoxicity against the HCT116 cell line (IC₅₀ = 3.46 ± 0.01 μM).</p