Hot Natural Products & Bioactive Compounds

Vaccarin exhibits extensive biological activities including vascular endothelial cell protective effects, it can significantly promote neovascularization by enhancing protein expression of p-Akt , p‑Erk, and CD31, and selectively protect vascular endothelium from dysfunction induced by H2O2.

1. 6'-O-Cinnamoylharpagide has anti-inflammatory activity.

1. Saponarin, which isolated from Gypsophila trichotoma Wend, shows in vitro and in vivo hepatoprotective and antioxidant activity against CCl4-induced liver damage.
2. Saponarin has antioxidant activity against cocaine-induced oxidative stress and hepatotoxicity.
3. Saponarin exerts anti-inflammatory effects in LPS-induced RAW 264.7 macrophages via inhibition of NF-κB, ERK and p38 signaling.
4. Saponarin shows hypoglycemic activity in the range of 20-80 mg/kg compared to 100-200 mg/kg for acarbose as reported.
5. Saponarin is characterized as α-glucosidase inhibitor present in Tinospora cordifolia, it also has hypoglycemic activity.
6. Saponarin exerts slight antihypertensive activity in non-diabetic spontaneously hypertensive rats (SHR), however, such effect is not observed in streptozotocin-induced diabetic SHR (SHR-D), indicates that diabetes and hypertension in combination are more difficult to be modulated by saponarin.

Protosappanin B possesses antitumor, anti-inflammation and anti-oxidation properties, it protects PC12 cells against oxygen–glucose deprivation-induced neuronal death by maintaining mitochondrial homeostasis via induction of ubiquitin-dependent p53 protein degradation.

Demethylzeylasteral exhibits strong inhibition towards UDP-glucuronosyltransferase (UGT) 1A6 and 2B7, and the inhibition kinetic parameters (Ki) are calculated to be 0.6 uM and 17.3 uM for UGT1A6 and UGT2B7, respectively. Demethylzeylasteral has antimicrobial, strong immunosuppressive, and antifertility activities; it concentration-dependently and in a partially reversible manner can inhibit the Ca(2+) current in spermatogenic cells with an IC(50) of 8.8 microg/ml, and it also can inhibit significantly the sperm acrosome reaction initiated by progesterone.

Cinobufotalin is a main cardiac toxin in toad, it is a novel anti-HCC agent, it induces growth inhibition and apoptosis in cultured HCC cells through ceramide production. Cinobufotalin is also an effective reversal agent for the multidrug resistance of tumors, it can reverse the adriamycin-resistance in Raji/ADR cells and the expression of P-gp and MRP-1 proteins. Cinobufotalin can promote the dendritic cells(DCs) derived from peripheral blood of patients with chronic hepatitis B to mature and effectively enhance its(the DCs') capabilities, therefore the treatment of cinobufotalin may potentiate the antiviral immunity of the patients with chronic hepatitis B(CHB).

1. Ikarisoside F and epimedin A can bind to AdoHcy hydrolase, inhibit the activity of AdoHcy hydrolase, thus regulating the cellular biomethylation as well as reducing cellular Hcy level.

Sagittatoside A selectively activates estrogen response element (ERE)-luciferase activity via ERα, and sagittatoside A and icariin induces ERα phosphorylation at serine 118 residue.