Hot Natural Products & Bioactive Compounds

Theaflavin is a suitable natural inhibitor against influenza A (H1N1) neuraminidase, which has anti-inflammatory, antioxidative, anti-mutagenic, anti-HSV-1, and anti-carcinogenic properties. Theaflavin is active in the prevention of fatty liver and obesity, it can significantly reduce lipid accumulation, suppress fatty acid synthesis, and stimulate fatty acid oxidation. Theaflavin inhibits LPS-Induced IL-6, MCP-1, and ICAM-1 expression in bone marrow-derived macrophages through the blockade of NF-κB and MAPK signaling pathways; it also protects nigral dopaminergic neurons against chronic MPTP/probenecid induced Parkinson's disease.

1. Theaflavin-3,3'-digallate is an inducer of oxidative stress and apoptosis.
2. A combination microbicide containing theaflavin-3,3'-digallate and lactic acid can reduce herpes simplex virus (HSV) transmission.
3. Theaflavin-3,3'-digallate may be useful chemoprevention agents for prostate cancer through suppressing the function of androgen and its receptor.
4. Theaflavin-3, 3'-digallate has strong antioxidant and antiangiogenic activities, it inhibits the tube formation of endothelial cells via decreased both MMP-2 and MMP-9 activities in vitro.
5. Theaflavin-3,3'-digallate may exert its anti-inflammatory and cancer chemopreventive actions by suppressing the activation of NFkappaB through inhibition of IkappaB kinase (IKK) activity.
6. Theaflavin-3,3'-digallate is a potent AMP-activated protein kinase (AMPK) activator with anti-adiposity activity in adipocytes, suggesting its potential application in functional foods and nutraceuticals for obesity management.
7. Theaflavin-3,3'-digallate can repress osteoclastogenesis and prevent wear debris-induced osteolysis via suppression of ERK pathway, it is a promising candidate for the treatment of osteoclast-related osteolytic diseases, such as wear debris-induced peri-implant osteolysis (PIO).

Theaflavin-3'-gallate, acts as prooxidants and induces oxidative stress, with carcinoma cells more sensitive than normal fibroblasts.

1. Semialactone shows inhibitory activities on human acyl-CoA:cholesterol acyltransferase(hACAT)1 with IC50 values of 79.1 uM and on human hACAT2 with IC50 values of 76.9 uM, it may be effective in the prevention and treatment of hypercholesterolemia or atherosclerosis via inhibitory effect on hACAT.

Vitexin, an HIF-1alpha inhibitor, which has anticonvulsant, anti-depressant, anti-glycation, spasmolytic, anti-metastatic, antitumor, anti-inflammatory and antinociceptive activities. Vitexin can be effectively used for the prevention of UV-induced adverse skin reactions such as free radical production and skin cell damage; it non-competitively inhibits Ach but not the Ca(2+) influx.

Standard reference

1. Naringenin triacetate exhibits a better binding affinity with multiple crystal structures of first bromodomain BRD4 (BRD4 BD1) when compared with the known inhibitors.

1. Murrangatin and murracarpin show chondroprotective activity by downregulation of
interleukin-1β, tumor necrosis factorα, prostaglandins E2,and matrix metalloproteinases
-13, and both of them may be a new backbone for developing inhibitors of cyclooxygenase 2.
2. Murrangatin can significantly inhibit Epstein–Barr virus early antigen (EBV–EA) activation, and preserve the high viability of Raji cells, suggests that it may be a valuable anti-tumor-promoting agent.
3. Murrangatin exhibits cytotoxicity against cholangiocarcinoma cell line, KKU-100.
4. Murrangatin exhibits antibacterial activity against P. gingivalis (ATCC 33277).
5. Murrangatin shows soluble epoxide hydrolase inhibitory activity with IC50 values 13.9±6.5uM.