A new butenolide cinnamate and other biological active chemical constituents from <i>Polygonum glabrum</i>

<div><p>Phytochemical investigation of the methanol extract of the aerial parts of <i>Polygonum glabrum</i> afforded one new natural product ( − )-2-methoxy-2-butenolide-3-cinnamate (<b>1</b>) along with six known compounds, β-hydroxyfriedalanol (<b>2</b>), 3-hydroxy-5-methoxystilbene (<b>3</b>), ( − ) pinocembrin (<b>4</b>), sitosterol-(6′-<i>O</i>-palmitoyl)-3-<i>O</i>-β-d-glucopyranoside (<b>5</b>), ( − ) pinocembrin-5-methyl ether (<b>6</b>) and sitosterol-3-<i>O</i>-β-d-glucopyranoside (<b>7</b>). Compound <b>1</b> showed promising <i>in vitro</i> anti-HIV-1 activity against primary isolates HIV-1<sub>UG070</sub> (X4, subtype D) and HIV-1<sub>VB59</sub> (R5, subtype C) assayed using TZM-bl cell line with IC<sub>50</sub> in the range of 15.68–22.43 μg/mL. The extract showed TI in the range of 19.19–27.37 with IC<sub>50</sub> in the range of 10.90–15.55 μg/mL. Compounds <b>1</b>, <b>3</b> and <b>4</b> exhibited <i>in vitro</i> anti-mycobacterium activity against <i>Mycobacterium tuberculosis</i> H37Ra with IC<sub>50</sub> values of 1.43, 3.33 and 1.11 μg/mL in dormant phase and 2.27, 3.33 and 1.21 μg/mL in active phase, respectively. Compound <b>4</b> was found to be the most active antiproliferative with IC<sub>50</sub> values of 1.88–11.00 μg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines.</p></div>