Tryptanthrin inhibits MDR1 and reverses doxorubicin resistance in breast cancer cells

Yu, Sung-Tsai; Chen, Tzer-Ming; Tseng, Sheng-Hong; Chen, Yen‐Hui

doi:10.1016/j.bbrc.2007.04.107

Cited by 101 publications

(66 citation statements)

References 18 publications

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“…It inhibits the production of IFN-␥ and IL-2 after the stimulation of Peyer's patch lymphocytes with staphylococcal enterotoxin B (SEB) (309). Tryptanthrin was also found to inhibit P-glycoprotein (Pgp) through MDR1 gene suppression (346). It was also reported to act as a moderate AhR inducer (281).…”

Section: Malassezia-produced Ahr Ligands and Significance Of Ahr Actimentioning

confidence: 99%

The Malassezia Genus in Skin and Systemic Diseases

et al. 2012

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SUMMARY In the last 15 years, the genus Malassezia has been a topic of intense basic research on taxonomy, physiology, biochemistry, ecology, immunology, and metabolomics. Currently, the genus encompasses 14 species. The 1996 revision of the genus resulted in seven accepted taxa: M. furfur , M. pachydermatis , M. sympodialis , M. globosa , M. obtusa , M. restricta , and M. slooffiae. In the last decade, seven new taxa isolated from healthy and lesional human and animal skin have been accepted: M. dermatis , M. japonica , M. yamatoensis , M. nana , M. caprae , M. equina , and M. cuniculi. However, forthcoming multidisciplinary research is expected to show the etiopathological relationships between these new species and skin diseases. Hitherto, basic and clinical research has established etiological links between Malassezia yeasts, pityriasis versicolor, and sepsis of neonates and immunocompromised individuals. Their role in aggravating seborrheic dermatitis, dandruff, folliculitis, and onychomycosis, though often supported by histopathological evidence and favorable antifungal therapeutic outcomes, remains under investigation. A close association between skin and Malassezia IgE binding allergens in atopic eczema has been shown, while laboratory data support a role in psoriasis exacerbations. Finally, metabolomic research resulted in the proposal of a hypothesis on the contribution of Malassezia -synthesized aryl hydrocarbon receptor (AhR) ligands to basal cell carcinoma through UV radiation-induced carcinogenesis.

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Section: Malassezia-produced Ahr Ligands and Significance Of Ahr Actimentioning

confidence: 99%

The Malassezia Genus in Skin and Systemic Diseases

et al. 2012

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“…Tryptanthrin with chemical name indolo [2,1-b] quinazolin-6,12-dione was reported to carry anti-microbial activity against a variety of microorganisms including bacteria, yeasts, dermatophytes and phytopathogens [10,11] . Recently, tryptanthrin has been paid much attention as an aryl hydrocarbon receptor agonist [12] , anti-inflammatory agent [13] , inducer of caspase-3/Fas mediated apoptosis [14] , cytostatic agent [15] and drug resistance reversal agent [16] . In this study, a series of tryptanthrin derivatives were synthesized and designated as compounds 1-7.…”

Section: Introductionmentioning

confidence: 99%

Cytotoxicity and reversal of multidrug resistance by tryptanthrin-derived indoloquinazolines

Yu¹,

Chern²,

Chen

et al. 2010

Acta Pharmacol Sin

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Aim: To evaluate the effects and elucidate the mechanisms of a series of indoloquinazolines as novel anticancer agents. Methods: Condensation of the substituted isatoic anhydride with the substituted isatin was performed to prepare compounds 1-4, followed by adding malononitrile to prepare compounds 5-7. Cytotoxicity was measured by MTT assays. Apoptosis induction was evaluated using DNA fragmentation, cell cycle assay, caspase 3/7 activity and Western blot. Results: Compounds 3, 4, and 5 display cytotoxicity against MCF-7, HeLa, SKOV3, and A498 cancer cells. DNA ladders appear in cells treated with compounds 3, 4, and 5. Within those, compound 4 exhibits the greatest activity in regards to sub-G 1 accumulations in the cell cycle and the activation of caspase-3/7. Furthermore, Fas and Fas ligand levels are elevated by compound 4, implying that the apoptosis is in part mediated through the signals. On the other hand, compounds 1 and 7 display chemosensitizing activity since cytotoxicity of doxorubicine and etoposide is enhanced in combination with compound 1 and 7, respectively, in MCF-7/adr (doxorubicinresistant) and MCF-7/vp (etoposide-resistant). Conclusion: The cytotoxicity of indoloquinazolines is structure-dependent rather than cell type-dependent due to the similar degree of cytotoxicity induced by the individual compounds in all four cell lines. Further modification of the tryptanthrin skeleton is important to develop novel anticancer agents bearing either cytotoxicity against MCF-7 cells or drug resistance reversal in MCF-7/adr and MCF-7/ vp.

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“…Tryptanthrin is a phytochemical found in the medicinal indigo plants such as Polygonum tinctorium and Isatis tinctoria. It was found to possess a wide spectrum of biological and pharmacological activities, including anti-microbial (7-9), immunomodulatory (11-13), antiinflammatory (13-15) and anti-tumor (16)(17)(18)(19) activities. A previous report has shown that tryptanthrin is able to induce both apoptosis and differentiation in the human leukemia HL-60 cells and U-937 cells in vitro (16), however, the underlying action mechanisms remain unclear.…”

Section: Discussionmentioning

confidence: 99%

“…Reaction mixture containing 40 units of RN ASE OUT TM recombinant ribonuclease inhibitor, 1 M-MLV first strand buffer, 0.5 mM of each dNTP, 10 mM DTT, 0.1g oligo (dT) [12][13][14][15][16][17][18] and 200 units of M-MLV reverse transcriptase was prepared, and 2 g RNA sample was added into 20 l reaction mixture. A negative control using DEPCtreated water instead of RNA sample was used to check if there was any contamination.…”

Section: Reverse Transcriptionmentioning

confidence: 99%

“…It was first isolated from Strobilanthes cusia as an anti-fungal agent against dermatophytes (7). Tryptanthrin is a weakly basic alkaloid and has been reported to have various biological and pharmacological activities, such as inhibitory activities against a variety of microorganisms and parasites (7)(8)(9)(10), immunomodulatory (11)(12)(13) and anti-inflammatory activities (13)(14)(15), and anti-tumor activity towards human leukemia and breast cancer cell lines in vitro (16)(17)(18). Moreover, the crude ethyl acetate extract and tryptanthrin extracted from the indigo plant Polygonum tinctorium have cancer chemopreventive activity by prevention of azoxymethane-induced intestinal tumor formation in F344 rats (19).…”

Section: Introductionmentioning

confidence: 99%

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