Discovery of two new long chain fatty acid esters of flavonol glycoside from Pollen Typhae Carbonisatus and their protective effects on HBMECs.

ABATRACTTwo new compounds, namely, isorhamnenin-3--neohesperidin-6''-linoleic acid ester () and isorhamnenin-3--neohesperidin-6''-palmitate (), along with 17 known compounds, were isolated from Pollen Typhae Carbonisatus (PTC). Their structures were elucidated on the basis of one-dimensional (1D)-, two-dimensional (2D)-nuclear magnetic resonance (NMR), and high-resolution electrospray ionization mass spectrometry (HRESIMS) spectroscopic data analyses. The two new compounds ( and ) exhibited a protective effect in a dose-dependent manner and promoted tube generation in the oxygen-glucose deprivation/reoxygenation (OGD/R)-induced human brain microvascular endothelial cells (HBMECs).

Fortuneicyclidins A and B, Pyrrolizidine Alkaloids with a 7-Azatetracyclo[5.4.3.0.0]tridecane Core, from .

Fortuneicyclidins A () and B (), a pair of epimeric pyrrolizidine alkaloids containing an unprecedented 7-azatetracyclo[5.4.3.

Discovery and optimization of withangulatin A derivatives as novel glutaminase 1 inhibitors for the treatment of triple-negative breast cancer.

To develop novel GLS1 inhibitors as effective therapeutic agents for triple-negative breast cancer (TNBC), 25 derivatives were synthesized from the natural inhibitor withangulatin A (IC = 18.2 μM). Bioassay optimization identified a novel and selective GLS1 inhibitor 7 (IC = 1.

Water-soluble derivatives of 25-OCH-PPD and their anti-proliferative activities.

(20R)-25-Methoxyl-dammarane-3β,12β,20-triol (25-OCH-PPD, AD-1) is a dammarane-type sapogenin showing anti-tumor potential. In the search for new anti-tumor agents with higher potency than our previously identified compound 25-OCH-PPD, 11 novel sulfamic acid and diacid derivatives that could improve water solubility and contribute to good drug potency and pharmacokinetic profiles were designed and synthesized. Their in vitro anti-tumor activities in MCF-7, A-549, HCT-116, and BGC-823 cell lines and one normal cell line were tested by standard MTT assay.

Sulfamic and succinic acid derivatives of 25-OH-PPD and their activities to MCF-7, A-549, HCT-116, and BGC-823 cell lines.

In the search for new anti-tumor agents with higher potency than our previously identified compound 1 (25-OH-PPD, 25-hydroxyprotopanaxadiol), 12 novel sulfamic and succinic acid derivatives that could improve water solubility and contribute to good drug potency and pharmacokinetic profiles were designed and synthesized. Their in vitro anti-tumor activities in MCF-7, A-549, HCT-116, and BGC-823 cell lines and one normal cell line were tested by standard MTT assay. Results showed that compared with compound 1, compounds 2, 3, and 7 exhibited higher cytotoxic activity on A-549 and BGC-823 cell lines, together with lower toxicity in the normal cell.