Berberidaceae

Etoposide (VP-16-213) is a topoisomerase II inhibitor that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50=60.3 μM). Etoposide has antitumor activity and induces apoptosis and autophagy.

Epimedokoreanin B (EKB), an isoprenylated flavonoid isolated from Korean Epimedium, exhibited anticancer activity in human non-small cell lung cancer (NSCLC) A549 and NCI-H292 cells.Epimedokoreanin B also possesses anti-inflammatory and antibacterial activities, and may have scavenging activity against DPPH radicals, inhibiting the proliferation of MCF-7 and HepG2 in a dose-dependent manner. Epimedokoreanin B also exhibits anti-inflammatory and antibacterial activity, with DPPH radical scavenging activity, and inhibits the proliferation of MCF-7 and HepG2 in a dose-dependent manner.Epimedokoreanin B significantly inhibits the formation of N (α)-(carboxymethyl)lysine (CML) and N (Ï)-(carboxymethyl)arginine (CMA), and prevents clinical complications of diabetes mellitus through the inhibition of advanced glycation end-products (AGEs).

Picropodophyllin (Picropodophyllin (PPP)) (PPP) is a specific IGF-1R inhibitor (IC50: 1 nM). Picropodophyllin specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast/stem cell growth factor (KIT).

Baohuoside I (Icariside-II) is a component of Epimedium koreanum, exhibits anti-inflammatory activity and anti-osteoporosis activities.

Epimedin A has anti-osteoporosis activities in vivo.

Icaritin (Anhydroicaritin) has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apoptosis, inhibit ENKL cell proliferation. Icaritin has anti-multiple myeloma activity, mainly mediated by inhibiting IL-6/JAK2/STAT3 signaling. Icaritin at low concentration (4 or 8 μMol/L) can promote rat chondrocyte proliferation and inhibit cell apoptosis, while the effect of Icaritin on rat chondrocyte at high concentration was reversed.

Icariin (Ieariline) belongs to the flavonol glycoside group of natural products, can inhibit PDE5 and PDE4 activity (IC50=432/73.50 μM), is also a PPARα activator. Icariin can increase cardiovascular and cerebrovascular blood flow, promote hematopoiesis, immunity and bone metabolism.

Icariside I (Lcariside I) is isolated from Epimedium herb. It can stimulate osteogenic differentiation of BMSCs and inhibit bone resorption activity of osteoclasts.

Caulophyllogenin is a partial PPARγ agonist (EC50 = 12.6 μM) derived from the stem bark of Kalopanax pictus (Araliaceae). Caulophyllogenin inhibits pro-inflammatory cytokine secretion and can be used in studies about the prevention and treatment of inflammatory diseases, type-2 diabetes, obesity and metabolic syndrome.

Picropodophyllotoxin (AXL 1717) is a cyclolignan alkaloid found in the mayapple plant family (Podophyllum peltatum), and a small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF1R) with potential antineoplastic activity. Picropodophyllotoxin (AXL 1717) specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast/stem cell growth factor (KIT). This agent shows potent activity in the suppression o f tumor cell proliferation and the induction of tumor cell apoptosis. IGF1R, a receptor tyrosine kinase overexpressed in a variety of human cancers, plays a critical role in the growth and survival of many types of cancer cells.

Epimedin A1 (Hexandraside F)(Hexandraside F) is a flavonoid extracted from Herba Epimedii which is one of commonly used Chinese medicines.

Tetradehydropodophyllotoxin (Dehydropodophyllotoxin) has anti-tumor activity.

Deoxypodophyllotoxin shows cytotoxic , antineoplastic, antitumor, insecticidal, anti-angiogenic, vascular disrupting, insecticidal, antiviral, and anti-inflammatory activities.

Oxyberberine (8-Oxoberberine) is isolated from the methanol extract of A. mexicana. It has been used to study the SW480 human colon cancer cell line.

4'-Demethylpodophyllotoxin is isolated from the herb of Dysosma pleiantha (Hance) Woodson with remarkable cytotoxic potential in diverse cancer cell lines.

Isoanhydroicaritin is a naturally occurring flavonoid that inhibits physiological melanin synthesis and recovery and inhibits mushroom tyrosinase.

1. Epimedin B (Epmedin B) has potential activity against osteoporosis by stimulating osteoblasts.

8,2'-Diisoprenylquercetin 3-methyl ether is a natural flavonoid compound extracted from the fruit of Sinopodophyllum hexandrum, exhibiting significant anticancer activity, particularly against breast cancer cell lines such as MDA-231 and T47D.

Dihydropalmatine (2,3,9,10-tetramethoxy-6,8-dihydro-5H-isoquinolino[2,1-b]isoquinoline) is a natural product derived from the roots and stem barks of Berberis aristata.

Epimedoside A has significant antioxidant activity in vitro.

Noricaritin, a flavonoid derived from Epimedium root, induces cell proliferation in lung tissue and inhibits the production of pro-inflammatory cytokines and chemokines in human lung epithelial cells.

1. β-Anhydroicaritin exhibits immunosuppressive effect on the mouse macrophages stimulated by LPS. 2. β-Anhydroicaritin phytosomes can inhibit enhanced bone turnover induced by ovariectomy, improve BMD the biomechanical properties of vertebrae, without any stimulation on uterus. 3. β-Anhydroicaritin possesses significant protective effects on the zymosan-induced peritonitis mice, which might be associated with the regulation of Ca(2+); influx in macrophages and iNOS expression.

Epmedin C (Baohuoside-VI) was metabolized via desugarization, dehydrogenation, hydrogenation, dehydroxylation, hydroxylation, demethylation and glucuronidation pathways in vivo. It has potential activity against osteoporosis by stimulating osteoblasts.

Podofilox ((+)-Shikonin) is a lignan (LIGNANS) found in PODOPHYLLIN resin from the roots of PODOPHYLLUM plants. It is a potent spindle poison, toxic if taken internally, and has been used as a cathartic. It is very irritating to skin and mucous membranes, has keratolytic actions, has been used to treat warts and keratoses, and may have antineoplastic properties, as do some of its congeners and derivatives.