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BCN5494 |
Harmine
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Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase ((DYRK)) inhibitor with neuroprotective, anticancer and anti-inflammatory activities. It regulates PPARγ expression through inhibition of the Wnt signaling pathway, it also selectively binds to MAO-A and reversibly inhibits monoamine oxidase A (MAO-A) but not the variant MAO-B. Harmine is able to induce beta cell proliferation, increase islet mass and improve glycemic control. Harmine induces apoptosis and inhibits proliferation, migration and invasion of human gastric cancer cells, which may be mediated by down-regulation of COX-2 expression. |
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BCN6322 |
Picroside I
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Picroside I is a hepatoprotective agent which is reported to be antimicrobial and used against hepatitis B. It has antioxidant, and anti-inflammatory activities, it may be the valuable anti-invasive drug candidates for cancer therapy by suppressing Collagenases and Gelatinases. Picroside I can enhance basic fibroblast growth factor(bFGF)-, staurosporine- or dbc-mitogen-activated protein (MAP)-induced neurite outgrowth from PC12D cells. |
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BCN6611 |
Torilin
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1. Torilin has anti-inflammatory properties, it inhibits inflammation by limiting TAK1-mediated MAP kinase and NF-κB activation.
2. Torilin can attenuate arthritis severity, modify leukocyte activations in dLNs or joints, and restore serum and splenocyte cytokine imbalances, it may have immunomodulatory and anti-inflammatory properties with the capacity to ameliorate the inflammatory response in collagen-induced-arthritis-(CIA)-mice.
3. Torilin inhibits melanin production in alpha-melanocyte stimulating hormone-activated B16 melanoma cells, with an IC(50) value of 25 microM.
4. Torilin shows excellent antimicrobial activity against Bacillus subtilis ATCC 6633 spores and vegetative cells, it functions as a surfactant with hydrophilic and hydrophobic properties related to denaturalization of various proteins,the distortion of coat proteins due to direct binding polar groups of spore coats with hydrophilic groups of torilin may be responsible for the observed rapid inactivation of bacterial spores.
5. Torilin has a potent anti-angiogenic activity both in vivo and in vitro, and it may have a strong activity to suppress tumorigenesis by inhibition of tumor invasion.
6. Torilin is an inhibitor of testosterone 5 alpha-reductase, it (IC50 = 31.7 +/- 4.23 microM) shows a stronger inhibition of 5 alpha-reductase than alpha-linolenic acid (IC50 = 160.3 +/- 24.62 microM) but is weaker than finasteride (IC50 = 0.38 +/- 0.06 microM).
7. Torilin reverses multidrug-resistance in cancer cells, it can potentiate the cytotoxicities of adriamycin, vinblastine, taxol and colchicine against multidrug-resistant KB-V1 and MCF7/ADR cells.
8. Torilin and torilolone show hepatoprotective effects on tacrine-induced cytotoxicity in human liver-derived Hep G2 cells, the EC50 values are 20.6 +/- 1.86 and 3.6 +/- 0.1 microM, respectively; and silybin as a positive control shows an EC50 value of 69.0 +/- 3.4 microM. |
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BCN6679 |
Licoricidin
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1. The hexane-ethanol extract of Glycyrrhiza uralensis, which contains licoricidin, is a potent anti-metastatic agent, which can markedly inhibit the metastatic and invasive capacity of malignant prostate cancer cells.
2. Licoricidin inhibits lung metastasis of 4T1 mammary carcinoma cells, which may be mediated via inhibition of cancer cell migration, tumor angiogenesis, and lymphangiogenesis.
3. Licoricidin and licorisoflavan A are effective in inhibiting the growth of all three bacterial species(Porphyromonas gingivalis, Prevotella intermedia and Solobacterium moorei), with minimal inhibitory concentrations in the range of 2-80 ug /ml, they have a potential for reducing bacterial volatile sulfur compounds (VSCs) production and therefore for controlling halitosis.
4. Licoricidin blocks UVA-induced photoaging via ROS scavenging,this activity converges to limit the activity of MMP-1, suggests that licoricidin may be considered as an active ingredient in new topically applied anti-ageing formulations.
5. Licoricidin and licorisoflavan A have potential for the development of novel host-modulating strategies for the treatment of cytokine and/or MMP-mediated disorders such as periodontitis. |
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BCN6696 |
Delta-Tocotrienol
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1. Delta-tocotrienol displays significant radioprotective effects, it protects mouse and human hematopoietic progenitors from gamma-irradiation through extracellular signal-regulated kinase/mammalian target of rapamycin signaling.
2. Delta-tocotrienol is a potential angiogenic inhibitor, it (2.5-5 microM) can significantly suppress human colorectal adenocarcinoma cells (DLD-1-CM) -induced tube formation, migration, and adhesion on human umbilical vein endothelial cells.
3.Delta-tocotrienol is a nontoxic activator of mir-34a which can inhibit nonsmall cell lung cancer cells (NSCLC) cell proliferation, induce apoptosis and inhibit invasion, and thus offering a potential starting point for the design of novel anticancer agents.
4.Grape seed polyphenol and delta-tocotrienol may have benefits in reducing non-alcoholic steatohepatitis (NASH, the second phase in liver disease). |
