Amentoflavone and its derivatives as novel natural inhibitors of human Cathepsin B

Pan, Xulin; Tan, Ning‐Hua; Zeng, Guang‐Zhi; Zhang, Yumei; Jia, Rui-Rui

doi:10.1016/j.bmc.2005.05.071

Cited by 62 publications

(34 citation statements)

References 23 publications

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“…Amentoflavone inhibits lens aldose reductase (Shimizu et al, 1984;Iwu et al, 1990;Felicio et al, 1995). It is noteworthy that amentoflavone and several of its derivatives are potent inhibitors of human cathepsin B (Pan et al, 2005). Cathepsin B is a protease involved in several inflammation-related disorders.…”

Section: General Biochemical Pharmacology Of Naturally Occurring Biflmentioning

confidence: 99%

Biochemical pharmacology of biflavonoids: Implications for anti-inflammatory action

et al. 2008

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Biflavonoids belong to a subclass of the plant flavonoid family. Distribution of biflavonoids in the plant kingdom is limited to several species. Previously, some pharmacological activities of biflavonoids were described such as inhibition of histamine release from mast cells and inhibition of lymphocyte proliferation, suggesting the anti-inflammatory/antiallergic potential of the biflavonoids. Furthermore, several natural biflavonoids including ochnaflavone and ginkgetin inhibit phospholipase A2. Most importantly, certain biflavonoids exhibit anti-inflammatory activity through the regulation of proinflammatory gene expression in vitro and in vivo. Recently, several synthetic approaches yielded new biflavonoid molecules with anti-inflammatory potential. These molecules also exhibit phospholipase A2 and cyclooxygenase-2 inhibitory activity. Although the bioavailability needs be improved, certain biflavonoids may have potential as new anti-inflammatory agents. This is the first review of biflavonoid pharmacology to date.

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Section: General Biochemical Pharmacology Of Naturally Occurring Biflmentioning

confidence: 99%

Biochemical pharmacology of biflavonoids: Implications for anti-inflammatory action

et al. 2008

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“…15,16 Amentoflavone is an inhibitor of cathepsin B, a member of the papain superfamily of cysteine proteases involved in the pathology of numerous diseases, including cancer. 17 Experiments in A549 cells showed that amentoflavone could inhibit the degradation of inhibitory α subunit of NF-αB and NF-κB translocation into the nucleus. 18 Amentoflavone suppressed prostaglandin E 2 biosynthesis by down-regulating cyclooxygenase (COX)-2/inducible nitric oxide synthase expression.…”

mentioning

confidence: 99%

Effect of Amentoflavone on the Inhibition of Pulmonary Metastasis Induced by B16F-10 Melanoma Cells in C57BL/6 Mice

Guruvayoorappan

Kuttan

2007

Integr Cancer Ther

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This study was an investigation of the antimetastatic activity of amentoflavone using B16F-10 melanoma-induced experimental lung metastasis in C57BL/6 mice. Amentoflavone treatment significantly reduced tumor nodule formation accompanied by reduced lung collagen hydroxyproline, hexosamine, and uronic acid levels. Serum sialic acid and γ γ-glutamyl transpeptidase levels were also significantly inhibited after amentoflavone treatment. Amentoflavone treatment up-regulated the lung tissue inhibitor of metalloprotease-1 and tissue inhibitor of metalloprotease-2 expression. The cytokine profile and growth factors such as interleukin-1β β, interleukin-6, tumor necrosis factor-α α, granulocyte monocytecolony stimulating factor, vascular endothelial growth factor, interleukin-2, and tissue inhibitor of metalloprotease-1 in the serum of these animals were markedly altered after amentoflavone treatment. This altered level of cytokines after amentoflavone treatment was also accompanied by enhanced natural killer cell antibody-dependent cellular cytotoxicity. The study reveals that amentoflavone treatment could alter proinflammatory cytokine production and could inhibit the activation and nuclear translocation of p65, p50, c-Rel subunits of nuclear factor-κ κB, and other transcription factors such as c-fos, activated transcription factor-2, and cyclic adenosine monophosphate response element-binding protein in B16F-10 melanoma cells.

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“…Ferruginol (2) showed effects on gastric secretion, endogenous prostaglandins and non-protein sulfhydryls, and its mechanism of assessment of action was elevated in vitro models in mice and rats [60,61]. Some of natural biflavones inhibit cathepsin B and cathepsin K, especially HIF with IC 50 of 0.58 mM against cathepsin B [62,63]. In addition, taxodione (10) also showed HIV-1 PR inhibitory activity in 0.1 mM concentraction [32].…”

Section: Cytotoxicitiesmentioning

confidence: 99%

Ethnobotany, Phytochemistry, and Biological Activities of Taxodium Rich.

Li¹

2013

TOPHARMCJ

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Taxodium Rich. is a genus of the family Cupressaceae. The trees are especially prized for their rot and termite resistant wood. Taxodium leaves and cones, which are particularly rich in essential oils were used as folk medicine to treat skin, gastro-intestinal, respiratory, inflammation, and infections. Preliminary bioactivity assays reported antimicrobial, antitumor, antitermitic, antispasmodic and bronchodilator activities of the extracts or isolates from Taxodium but further pharmacological investigations of bioactive compounds are not available. To data, at least 130 compounds have been identified from extant or fossil Taxodium. Fifty-seven compounds have been isolated primarily from the cones, leaves, and branches of extant Taxodium, with diterpenoids and flavonoids as the major components. At least three major abietane diterpenoids (sugiol (1), ferruginol (2), and 6,7-dehydroferruginol (3)) are also identified in the fossil Taxodium by GC/MS. The diterpenoids may be important marker compounds for understanding the evolution of the genus Taxodium. However, the taxonomy and evolutionary pattern of Taxodium remains elusive until a full understanding of the chemical constituents of all Taxodium taxa is determined.

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Amentoflavone and its derivatives as novel natural inhibitors of human Cathepsin B

Cited by 62 publications

References 23 publications

Biochemical pharmacology of biflavonoids: Implications for anti-inflammatory action

Biochemical pharmacology of biflavonoids: Implications for anti-inflammatory action

Effect of Amentoflavone on the Inhibition of Pulmonary Metastasis Induced by B16F-10 Melanoma Cells in C57BL/6 Mice

Ethnobotany, Phytochemistry, and Biological Activities of Taxodium Rich.

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