Genistein sodium dihydrate(Axcentua Pharmaceuticals AB)

This study investigated the hypoglycaemic activity of lotus seed epicarp phenolic extract (LSEPE) by inhibiting starch hydrolytic enzyme activity and slowing down carbohydrate digestion. Total phenolic and flavonoid contents in LSEPE were 620.37 ± 10.45 mg GAE/g DW and 422.69 ± 23.57 mg RE/g DW, respectively. A total of 57 phenolic compounds were first identified in LSEPE. The IC₅₀ of LSEPE for inhibiting α-amylase and α-glucosidase were 124.44 ± 2.89 μg/mL and 0.99 ± 0.02 μg/mL, approximately 3.28 to 1.61 times that of acarbose. LSEPE acted as a mixed-type inhibitor of α-amylase and an anti-competitive-type inhibitor of α-glucosidase. UV spectroscopy, fluorescence quenching, and CD analysis showed that LSEPE could change the enzymes' microenvironment and hydrophobicity. Moreover, LSEPE slowed the starch hydrolysis rate in vitro and increased the proportions of slowly digestible starch (SDS) and resistant starch (RS) by 60.51% and 19.98%. Therefore, the lotus seed epicarppolyphenols could be the potential natural ingredients for developing anti-hyperglycemic functional foods.

Seventeen compounds were isolated from the aerial parts of Ceratocarpus arenarius L., including 1 previously undescribed xanthone and 6 firstly isolated compounds. The structures of compounds were identified by Mass spectrometry and NMR spectroscopy. In addition, the in vitro cytotoxicity of the isolates against human oesophageal squamous carcinoma KYSE-150 and KYSE-70 cell were investigated by MTT to identify Genistein (8) and 1,4-dihydroxy-2-naphthoic acid (9) as the most effective compounds, which could exhibit anti-proliferation activity with IC₅₀ values of 39.11 μg/mL and 5.71 μg/mL against KYSE-150, 34.07 μg/mL and 4.51 μg/mL KYSE-70, respectively. Swiss target prediction and Molecular docking were applied to reveal the action mechanism of the effective compounds and provide guidance for the potential use of the C. arenarius L. in antitumor treatment.