From traditional Chinese medicine to rational cancer therapy

Efferth, Thomas; Li, Paul C. H.; Konkimalla, V. Badireenath; Kaina, Bernd

doi:10.1016/j.molmed.2007.07.001

Cited by 480 publications

(333 citation statements)

References 55 publications

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“…Small molecules have been shown to have a wide range of biological activities and this has been confirmed in clinical trials (27). In the present study, we showed that aspirin decreased rWnt-3A-induced luciferase activity, in agreement with Cho et al (19).…”

Section: Discussionsupporting

confidence: 92%

Evaluation of anti-Wnt/β-catenin signaling agents by pGL4-TOP transfected stable cells with a luciferase reporter system

Chuang

Lieu

Tsai

et al. 2010

Braz J Med Biol Res

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Section: Discussionsupporting

confidence: 92%

Evaluation of anti-Wnt/β-catenin signaling agents by pGL4-TOP transfected stable cells with a luciferase reporter system

Chuang

Lieu

Tsai

et al. 2010

Braz J Med Biol Res

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“…Mercury content found in traditional medicines justifiably alarms the public (4-7), and many mercury-containing traditional medicines have been banned. However, some are still in use today (1)(2).…”

Section: Introductionmentioning

confidence: 99%

Mercury in Traditional Medicines: Is Cinnabar Toxicologically Similar to Common Mercurials?

Liu

Shi²,

Yu³

et al. 2008

Exp Biol Med (Maywood)

195

153

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Mercury is a major toxic metal ranking top in the Toxic Substances List. Cinnabar (contains mercury sulfide) has been used in traditional medicines for thousands years as an ingredient in various remedies, and 40 cinnabar-containing traditional medicines are still used today. Little is known about toxicology profiles or toxicokinetics of cinnabar and cinnabar-containing traditional medicines, and the high mercury content in these Chinese medicines raises justifiably escalations of public concern. This minireview searched the available database of cinnabar, compared cinnabar with common mercurials, such as mercury vapor, inorganic mercury, and organic mercury, and discusses differences in their bioavailability, disposition, and toxicity. The analysis showed that cinnabar is insoluble and poorly absorbed from the gastrointestinal tract. Absorbed mercury from cinnabar is mainly accumulated in kidney, resembling the disposition pattern of inorganic mercury. Heating cinnabar results in release of mercury vapor, which in turn can produce toxicity similar to inhalation of these vapors. The doses of cinnabar required to produce neurotoxicity are thousands 1000 times higher than methyl mercury. Following long-term use of cinnabar, renal dysfunction may occur. Dimercaprol and succimer are effective chelation therapies for general mercury intoxication including cinnabar. Pharmacology studies of cinnabar suggest sedative and hypnotic effects, but the therapeutic basis of cinnabar is still not clear. In summary, cinnabar is chemically inert with a relatively low toxic potential when taken orally. In risk assessment, cinnabar is less toxic than many other forms of mercury, but the rationale for its inclusion in traditional Chinese medicines remains to be fully justified.

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“…A relevant concern is the detection of effects present in these infusions that may interfere with cell division. In this context, plants have been a source of clinically relevant anticancer compounds and nowadays many natural products and derivatives belong to the standard repertoire of cancer chemotherapy (Efferth et al, 2007). As an example, the compound homoharringtonine, isolated from Cephalotaxus species, has recently been reported to be among the most potent members of the antileukemia alkaloids (Quintás-Cardama, Cortes, 2008).…”

Section: Discussionmentioning

confidence: 99%

“…A considerable portion of anti-tumor agents currently used in the clinic are of natural origin. In fact, half of all anti-cancer drugs approved internationally between the 1940s and 2006 were either natural products or their derivatives and were developed on the basis of knowledge gained from small molecules or macromolecules that exist in nature (Efferth et al, 2007).…”

Section: Introductionmentioning

confidence: 99%

Alkaloid-rich fraction of Himatanthus lancifolius contains anti-tumor agents against leukemic cells

Lima

Hilst

Mattana

et al. 2010

Braz. J. Pharm. Sci.

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The effects of the alkaloid-rich fraction of Himatanthus lancifolius (Müll. Arg) Woodson on normal marrow cells and leukemic cell lines were investigated. After 48 h exposure, the proliferation assay showed significant cell growth inhibition for Daudi (0.1-10 µg/mL), K-562 (1-10 µg/mL), and REH cells (10-100 µg/mL), yet was inert for normal marrow cells. A similar inhibition profile was observed in clonogenic assays. This alkaloid-rich fraction, in which uleine is the main compound, showed no signs of toxicity to any cells up to 10 µg/mL. Cell feature analyses after induction of differentiation showed maintenance of the initial phenotype. Flow cytometric expression of Annexin-V and 7-AAD in K-562 and Daudi cells has indicated that the cells were not undergoing apoptosis or necrosis, suggesting cytostatic activity for tumor cells. Os efeitos da fração rica em alcalóides indólicos de Himatanthus lancifolius (Müll. Arg) Woodson sobre células normais de medula óssea e linhagens celulares leucêmicas foram investigados. Após 48 horas de exposição, os ensaios de proliferação demonstraram efeitos inibitórios significativos para as linhagens Daudi (0,1-10 µg/mL), K-562 (1-10 µg/mL) e REH (10-100 µg/mL), enquanto mostrou-se inerte sobre células normais de medula óssea. Os perfis de inibição se repetiram nos ensaios clonogênicos. A fração rica em alcalóides, na qual a uleína é a substância majoritária, não demonstrou toxicidade até a dose de 10 µg/mL para nenhuma das células incluídas no estudo. Da mesma forma, não se observou influência dessa fração sobre a diferenciação celular dessas linhagens, mas manutenção de seu estado maturacional inicial. O conjunto de dados descritos associado à baixa co-expressão de anexina-V e 7-AAD sugerem que esta fração exerce atividade citostática para células tumorais.

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From traditional Chinese medicine to rational cancer therapy

Cited by 480 publications

References 55 publications

Evaluation of anti-Wnt/β-catenin signaling agents by pGL4-TOP transfected stable cells with a luciferase reporter system

Evaluation of anti-Wnt/β-catenin signaling agents by pGL4-TOP transfected stable cells with a luciferase reporter system

Mercury in Traditional Medicines: Is Cinnabar Toxicologically Similar to Common Mercurials?

Alkaloid-rich fraction of Himatanthus lancifolius contains anti-tumor agents against leukemic cells

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