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Taheebo

Scientific Name(s): Tabebuia avellanedae Lorentz ex Griseb.
Common Name(s): Ipé Roxo, Lapacho colorado, Lapacho morado, Pau d'Arco, Red lapacho, Taheebo

Clinical Overview

Use

Taheebo has traditionally been used to treat a wide range of conditions, including bacterial infections, blood coagulation, cancer, and inflammatory diseases. However, there are no well-controlled clinical trials to support use of taheebo in these conditions.

Dosing

Clinical information is lacking to provide dosing recommendations for taheebo. In phase 1 and 2 clinical trials, the active component beta-lapachone (ARQ 501) was administered weekly at doses up to 450 mg/m2, either as monotherapy or in combination with various antineoplastic agents. Contraindications: Contraindications have not been identified.

Contraindications

Contraindications have not been identified.

Pregnancy/Lactation

Avoid use. Information regarding safety and efficacy in pregnancy and lactation is lacking.

Interactions

None well documented.

Adverse Reactions

Generally Recognized as Safe (GRAS) by the US Food and Drug Administration (FDA).

Toxicology

No data.

Botany

The Tabebuia spp., such as the Pau d’Arco tree, belongs to the Bignoniaceae plant family. It is an evergreen canopy tree native to the Amazon rainforest and adjacent areas (equatorial and tropical forests) of Central and South America, where it is popularly referred to as "Ipê Roxo." Taheebo is obtained from the bark and hardwood of the tree.1, 2, 3 This species is synonymous with Tabebuia impetiginosa (Mart. ex DC.) Standl, Tabebuia serratifolia (Vahl) Nichols, Handroanthus impetiginosus (Mart, ex DC.) Mattos, Tabebuia heptaphylla Vell. Toledo, and Tabebuia ipé Mart. ex Schum. The distinct related species Tecoma curialis Solhanha da Gama is sometimes marketed under the same names.

History

The inner bark and hardwood of T. avellanedae have been used medicinally by native South American populations for centuries.1 Taheebo is obtained from the purple-colored bark of the tree and has been used in folk medicine to treat bacterial infections, blood coagulation, cancer, and inflammatory diseases.1, 2 Its use may predate the Incas; for more than 1,000 years, taheebo was one of the primary medicines used by the Callawaya tribe. It was used topically as a poultice and concentrated tea to treat a variety of skin conditions, including fungal infections and skin cancers.2 A decoction prepared from the inner bark has been used internally to treat bacterial and fungal infections, fever, syphilis, malaria, trypanosomiasis, and stomach and bladder disorders.3 In 1967, a Brazilian news magazine reported "miraculous" cures in cancer patients using red lapacho. Between 1960 and 1990, the US National Cancer Institute (NCI) conducted research on the use of natural products, including lapachol and beta-lapachone (active components of taheebo), for the treatment of cancer.3 Studies using lapachol were discontinued due to toxicity (not specified).4 Research evaluating the anticancer activity of beta-lapachone have continued.5, 6, 7 In 1999, the FDA listed red lapacho tea as a dietary supplement and an "herb used to alleviate conditions and symptoms of cancer."3

Chemistry

The major active compounds in the hot water extract of T. avellanedae inner bark are naphthoquinones, furanonaphthoquinones, anthraquinones, benzoic acid derivatives, benzaldehyde derivatives, iridoids, coumarins, and flavonoids.2

The 2 main bioactive components of Tabebuia spp. bark responsible for its pharmacologic activity are lapachol and beta-lapachone. The chemical name for lapachol is 2-hydroxy-3-(3-methyl-2 buthenyl)-1,4-naphthoquinone. The chemical name for beta-lapachone, an isomer of lapachol, is 3,4-dihydro-2,2-dimethyl-2H-naphtol[1,2-b]pyran-5,6-dione.3

Uses and Pharmacology

Commercially available botanical drug material is of varying quality and composition,3 making assessments of product clinical efficacy challenging; the bioscientific evidence for products derived from T. impetiginosa is insufficient. When pharmacologic actions of the whole plant extract were compared with those of its isolated constituents, potency appeared to decline with purification.3

Taheebo has astringent, anti-inflammatory, antibacterial, antifungal, diuretic, anticoagulant, laxative, and anticancer properties, among others.2 However, no clinical studies of preparations derived from taheebo have been conducted.

Anti-inflammatory activity

In vitro and animal data

In an in vitro experimental study, a total of 5 novel compounds isolated from the water extract of T. avellanedae were found to have antimicrobial properties.8 The water extract of T. avellanedae blocks inflammatory mediators in vitro and in vivo. It suppresses the production of prostaglandin E2 and nitric oxide and blocks the mRNA expression of their catalyzing enzymes.2, 9 In an in vivo study in mice, a 200 mg/kg dose of taheebo ethanolic extract had anti-inflammatory effects.10

Clinical data

Research reveals no clinical data to support use of taheebo as an anti-inflammatory agent.

Antiparasitic activity

In vitro and animal data

In an in vitro study, lapachol and antimony, bismuth, and tin complexes of lapachol demonstrated antiparasitic activity.11, 12 Tabebuia extracts inhibit interleukin-2 (IL-2)–dependent T-lymphocyte activation and proliferation, but have no effect on cytokine expression (IL-2 and tumor necrosis factor-alpha). Immune inhibitory effects of Tabebuia were not mediated by beta-lapachone and were observed in aqueous but not ethanol extracts.13 When antileishmanial activity of lapachol, isolapachol, and dihydrolapachol, as well as various soluble derivatives, was tested in vitro and in vivo, all lapachol compounds demonstrated significant activity against Leishmania in vitro; in vivo, a difference between treated and untreated mice was observed with only 1 of the 5 tested compounds 5 weeks after parasite injection. No toxicity was evident at concentrations similar to the 50% inhibitory concentration.14 Lapachol, beta-lapachone, and their derivatives demonstrated anthelmintic activity against Toxocara canis larvae both in vitro and in vivo in mice.15

Clinical data

Research reveals no clinical data to support use of taheebo as an anti-inflammatory agent.

Antimicrobial activity

In vitro and animal data

In studies evaluating the antimicrobial activity of T. impetiginosa, methanol extracts of the inner bark showed weak to moderate activity against Bifidobacterium longum, Lactobacillus acidophilus, Lactobacillus casei, and Escherichia coli, and strong activity against Clostridium paraputrificum, Clostridium perfringes, and Helicobacter pylori.The 2 compounds thought to be responsible for the antibacterial activity were identified as lapachol and anthraquinone-2-carboxyl acid. In a study evaluating the activity of taheebo against H. pylori, lapachol was more effective than metronidazole, but far less effective than amoxicillin and tetracycline.3, 16, 17 When tested in vitro against methicillin-resistant Staphylococcus aureus, beta-lapachone demonstrated synergistic activity with conventional agents (eg, beta-lactams, fluoroquinolones, carbapenems).18 Lapachol has demonstrated activity against mycobacteria. In cell culture, lapachol was more effective intracellularly than extracellularly and demonstrated immunomodulatory effects (inhibition of the surface expression of the costimulatory molecule cluster of differentiation 86 [CD86]), which may enhance the capability of the host cell to control mycobacterial invasion.19

Clinical data

Research reveals no clinical data to support use of taheebo as an anti-inflammatory agent.

Anticancer activity

In vitro and animal data

Lapachol is purported to have anticancer properties. While the mechanism of action is unknown, lapachol is involved in the inhibition of oxidative phosphorylation, activation of cytochrome P450 reductase, and enhancement of peroxidation of lipids in sarcoma cells.1, 20 Studies in cell cultures show that lapachol causes alterations in the protein profile and inhibits cellular invasiveness in HeLa cells (a human cancer cell line), suggesting antimetastatic activity.1 In a series of studies, T. impetiginosa was shown to have activity against a wide range of cancer cell lines, including Walker 256 carcinoma, prostate cancer, human promyelocytic leukemia, breast cancer, ovarian cancer, epidermoid laryngeal cancer, esophageal cancer, radioresistant human malignant melanoma, lung adenocarcinoma, cervical cancer, and osteosarcoma cells.3, 21, 22, 23, 24, 25, 26, 27

Several potential anticancer mechanisms have been proposed, including the inhibition of topoisomerase I. Lapachol also induces oxidative stress via generation of reactive oxygen species, which leads to apoptosis and cell cycle arrest.23 In other research, beta-lapachone was found to initiate apoptosis only in transformed cells without causing DNA damage.3 Furthermore, it increased activation of pro-apoptotic factor JNK and decreased activation of P13K, AKT, and ERK, which are considered cell survival/proliferation factors.28 Beta-lapachone reportedly induces apoptosis via the novel mechanism of modulating E2F-1 expression, which activates the G1/S-phase checkpoint.5 An aqueous extract of Pau d’Arco stimulated the mitogen-activated protein kinase (MEK)/extracellular signal-regulated kinase 1/2 (ERK 1/2) pathway, leading to stimulation of Nrf2-dependent gene expression.29 In vitro research using an aqueous extract of taheebo in estrogen receptor–positive breast cancer cells demonstrated upregulation of apoptosis-specific and xenobiotic metabolism–specific genes and down-regulation of cell cycle regulatory and estrogen-responsive genes.24 In the presence of probiotics, lapachol can be converted to a more active cytotoxic compound against breast cancer cell lines than lapachol alone.30

It is generally understood that NAD(P)H:quinone oxidoreductase (NQ01) activity is an important determinant of beta-lapachone cytotoxicity and that NQ01 is overexpressed in most common types of cancer. NQ01 catalyzes the redox cycling of beta-lapachone via production of an unstable hydroquinone. Under aerobic conditions, this unstable quinone is quickly oxidized back to the parent quinine, resulting in futile cycling between the 2 forms of beta-lapachone and a rapid increase in intracellular calcium, mitochondrial membrane depolarization, loss of adenosine triphosphate, DNA fragmentation, and, finally, apoptosis. Beta-lapachone acts, in part, through upregulation of NQ01.31 In leukemia cells, beta-lapachone is directly cytotoxic. It decreases cell viability and telomerase activity, resulting from down-regulation of telomerase reverse transcriptase.32

Clinical data

The NCI studied the anticancer effects of the lapachol component of taheebo in the 1960s and 1970s. Phase 1 clinical trials at oral doses up to 4,000 mg/day had no therapeutic effect and it was determined that inadequate serum concentrations were achieved with oral administration. In contrast to lapachol, beta-lapachone demonstrated activity against several tumor cell lines, including leukemia, lung, prostate, and breast cancers, as well as several multidrug-resistant cell lines.3, 28

A series of phase 1 and 2 clinical trials have been conducted with beta-lapachone (ARQ 501) in patients with cancer. Early signs of clinical activity were demonstrated.5, 6, 7

Other uses

Taheebo is capable of inhibiting platelet aggregation and vascular smooth muscle proliferation. While the mechanism of action is unclear, its antiplatelet effects may be due to suppression of arachidonic acid and collagen liberation, and its inhibition of vascular smooth muscle proliferation may be due to suppression of phosphorylated MEK/ERK activation.33

There is in vitro and in vivo evidence that a seminatural, naphthoquinone derivative of lapachol, 3-hydroxy-4-(hydroxyimino)-2-(3-methybut-2-enylnaphtalen-2[4H])-one, can induce hypotension.34

In vitro, beta-lapachone has been shown to have antipsoriatic activity.3

Mice with either scrape or burn wounds treated with beta-lapachone ointment healed faster than those treated with a control ointment. In cell cultures, beta-lapachone induced macrophage proliferation and increased vascular endothelial growth factor release from macrophages.35, 36

When an ethanolic extract of taheebo (150 mg/kg body weight daily by gavage) was administered to mice fed a high-fat diet, it interfered with obesity and fat accumulation by regulation of gene expression related to lipid metabolism.37

Dosing

Taheebo has been used for centuries in native South American medicine for a wide range of conditions, and more recently as an alternative cancer therapy. However, clinical information is lacking to provide dosing recommendations.

In phase 1 and 2 clinical trials, beta-lapachone (ARQ 501) was administered at weekly doses up to 450 mg/m2, either as monotherapy or in combination with various antineoplastic agents.5, 6, 7

Pregnancy / Lactation

Avoid use. Information regarding safety and efficacy in pregnancy and lactation is lacking.

Interactions

None well documented. Avoid use of taheebo with anticoagulants.

Adverse Reactions

Taheebo is generally considered safe and has been granted GRAS status by the FDA.3

Interference with the biological cycle of vitamin K is associated with the isolated compound lapachol. When consumed as red lapacho tea, which contains all of the components of taheebo including some pro–vitamin K compounds, the effect appears to be canceled.3

Exposure to wood dust from Tabebuia spp. can lead to asthma.38

Pau d’Arco tea can reportedly cause nausea and vomiting.39

Hemolytic anemia has been reported as a limiting toxicity in animals.14

When administered to patients with cancer, beta-lapachone did not exhibit dose-limiting toxicity. Adverse events were mild and included anemia, hemolysis, hyperbilirubinemia, edema, nausea, constipation, and fatigue.5, 6, 7

Toxicology

No toxicity in humans has been reported for the bark extract or its main constituents.

References

1. Balassiano IT, De Paulo SA, Henriques Silva N, Cabral MC, da Gloria da Costa Carvalho M. Demonstration of the lapachol as a potential drug for reducing cancer metastasis. Oncol Rep. 2005;13(2):329-333.15643520
2. Byeon SE, Chung JY, Lee YG, Kim BH, Kim KH, Cho JY. In vitro and in vivo anti-inflammatory effects of taheebo, a water extract from the inner bark of Tabebuia avellanedae. J Ethnopharmacol. 2008;119(1):145-152.18634864
3. Gómez Castellanos JR, Prieto JM, Heinrich M. Red Lapacho (Tabebuia impetiginosa)--a global ethnopharmacological commodity? J Ethnopharmacol. 2009;121(1):1-13.18992801
4. Lu JJ, Bao JL, Wu GS, et al. Quinones derived from plant secondary metabolites as anti-cancer agents. Anticancer Agents Med Chem. 2013;13:456-463.22931417
5. Shapiro GI, Supko JC, Ryan DP. Phase I trial of ARQ 501, an activated checkpoint therapy (ACT) agent, in patients with advanced solid tumors [abstract]. J Clin Oncol. 2005;23(16S):2042.
6. Khong HT, Dreisbach HL, Kindler DF, et al. A phase 2 study of ARQ501 in combination with gemcitabine in adult patients with treatment naïve, unresectable pancreatic adenocarcinoma [abstract]. J Clin Oncol. 2007;25(18S):2007.
7. Hartner LP, Rosen L, Hensley M, et al. Phase 2 dose multi-center, open-label study of AR! 501, a checkpoint activator, in adult patients with persistent, recurrent or metastatic leiomyosarcoma (LMS). J Clin Oncol. 2007;25(18S):20521.
8. Suo M, Isao H, Kato H, Takano F, Ohta T. Anti-inflammatory constituents from Tabebuia avellanedae. Fitoterapia. 2012;83(8):1484-1488.22955001
9. Zhang L, Hasegawa I, Ohta T. Anti-inflammatory cyclopentene derivatives from the inner bark of Tabebuia avellandedae. Fitoterapia. 2016;109:217-223.26779946
10. Lee MH, Choi HM, Hahm DH, et al. Analgesic and anti-inflammatory effects in animal models of an ethanolic extract of taheebo, the inner bark of Tabebuia avellanedae. Mol Med Rep. 2012;6(4):791-796.22825254
11. Barbosa MI, Corrêa RS, de Oliveira KM, et al. Antiparasitic activities of novel ruthenium/lapachol complexes. J Inorg Biochem. 2014;136:33-39.24727183
12. Rocha MN, Nogueira PM, Demicheli C, et al. Cytotoxicity and in vitro antileishmanial activity of antimony (V), bismuth (V), and tin (IV) complexes of lapachol. Bioinorg Chem Appl. 2013;2013:961783.23781165
13. Böhler T, Nolting J, Gurragchaa P, et al. Tabebuia avellanedae extracts inhibit IL-2-independent T-lymphocyte activation and proliferation. Transpl Immunol. 2008;18(4):319-323.18158117
14. Lima NM, Correia CS, Leon LL, et al. Antileishmanial activity of lapachol analogues. Mem Inst Oswaldo Cruz. 2004;99(7):757-761.15654435
15. Mata-Santos T, Pinto NF, Mata-Santos HA, et al. Anthelmintic activity of lapachol, β-lapachone and its derivatives against Toxocara canis larvae. Rev Inst Med Trop Sao Paulo. 2015;57(3):197-204.26200958
16. Park BS, Kim JR, Lee SE, et al. Selective growth-inhibiting effects of compounds identified in Tabebuia impetiginosa inner bark on human intestinal bacteria. J Agric Food Chem. 2005;53(4):1152-1157.15713033
17. Park BS, Lee HK, Lee SE, et al. Antibacterial activity of Tabebuia impetiginosa Martius ex DC (taheebo) against Helicobacter pylori. J Ethnopharmacol. 2006;105(1-2):255-262.16359837
18. Macedo L, Fernandes T, Silveira L, Mesquita A, Franchitti AA, Ximenes EA. β-lapachone activity in synergy with conventional antimicrobials against methicillin resistant Staphylococcus aureus strains. Phytomedicine. 2013;21(1):25-29.24035227
19. Oliveira RA, Azevedo-Ximenes E, Luzzati R, Garcia RC. The hydroxy-naphthoquinone lapachol arrests mycobacterial growth and immunomodulates host macrophages. Int Immunopharmacol. 2010;10(11):1463-1473.20837170
20. Fiorito S, Epifano F, Bruyère C, Mathieu V, Kiss R, Genovese S. Growth inhibitory activity for cancer cell lines of lapachol and its natural and semi-synthetic derivatives. Bioorg Med Chem Lett. 2014;24(2):454-457.24374273
21. Inagaki R, Ninomiya M, Tanaka K, Watanabe K, Koketsu M. Synthesis and cytotoxicity on human leukemia cells of furonaphthoquinones isolated from tabebuia plants. Chem Pharm Bull(Tokyo). 2013;61(6):670-673.23727782
22. Inagaki R, Ninomiya M, Tanaka K, Koketsu M. Synthesis, characterization, and antileukemic properties of naphthoquinone derivatives of lawsone. ChemMedChem. 2015;10(8):1413-1423.26088596
23. Kandioller W, Balsano E, Meier SM, et al. Organometallic anticancer complexes of lapachol: metal centre-dependent formation of reactive oxygen species and correlation with cytotoxicity. Chem Commun (Camb). 2013;49(32):3348-3350.23505633
24. Mukherjee B, Telang N, Wong GY. Growth inhibition of estrogen receptor positive human breast cancer cells by taheebo from the inner bark of Tabebuia avellandae tree. Int J Mol Med. 2009;24(2):253-260.19578798
25. Rao KV, McBride TJ, Oleson JJ. Recognition and evaluation of lapachol as an antitumor agent. Cancer Res. 1968;28:1952-1954.
26. Sunassee SN, Veale CG, Shunmoogam-Gounden N, et al. Cytotoxicity of lapachol, β-lapachone and related synthetic 1,4-naphthoquinones against oesophageal cancer cells. Eur J Med Chem. 2013;62:98-110.23353747
27. Bang W, Jeon YJ, Cho JH, et al. β-lapachone suppresses the proliferation of human malignant melanoma cells by targeting specificity protein 1. Oncol Rep. 2016;35(2):1109-1116.26718788
28. Kung HN, Weng TY, Liu YL, Lu KS, Chau YP. Sulindac compounds facilitate the cytotoxicity of β-lapachone by up-regulation of NAD(P)H quinone oxidoreductase in human lung cancer cells. PLoS One. 2014;9(2):e88122.24505400
29. Richter M, Winkel AF, Schummer D, et al. Pau d'arco activates Nrf2-dependent gene expression via the MEK/ERK-pathway. J Toxicol Sci. 2014;39(2):353-361.24646717
30. Oliveira Silva E, Cruz de Carvalho T, Parshikov IA, Alves dos Santos R, Silva Emery F, Jacometti Cardoso Furtado NA. Cytotoxicity of lapachol metabolites produced by probiotics. Lett Appl Microbiol. 2014;59(1):108-114.24635204
31. Lamberti MJ, Vittar NB, da Silva Fde C, Ferreira VF, Rivarola VA. Synergistic enhancement of antitumor effect of β-Lapachone by photodynamic induction of quinone oxidoreductase (NQO1). Phytomedicine. 2013;20(11):1007-1112.23746950
32. Moon DO, Kang CH, Kim MO, et al. Beta-lapachone (LAPA) decreases cell viability and telomerase activity in leukemia cells: suppression of telomerase activity by LAPA. J Med Food. 2010;13(3):481-48820438329
33. Son DJ, Lim Y, Park YH, et al. Inhibitory effects of Tabebuia impetiginosa inner bark extract on platelet aggregation and vascular smooth muscle cell proliferation through suppressions of arachidonic acid liberation and ERK1/2 MAPK activation. J Ethnopharmacol. 2006;108(1):148-151.16766151
34. Dantas BP, Ribeiro TP, Assis VL, et al. Vasorelaxation induced by a new naphthoquinone-oxime is mediated by NO-sGC-cGMP pathway. Molecules. 2014;19(7):9773-9785.25006785
35. Fu SC, Chau YP, Lu KS, Kung HN. β-lapachone accelerates the recovery of burn-wound skin. Histol Histopathol. 2011;26(7):905-914.21630220
36. Kung HN, Yang MJ, Chang CF, Chau YP, Lu KS. In vitro and in vivo wound healing-promoting activities of beta-lapachone. Am J Physiol Cell Physiol. 2008;295(4):C931-C943.18650264
37. Choi WH, Um MY, Ahn J, Jung CH, Park MK, Ha TY. Ethanolic extract of taheebo attenuates increase in body weight and fatty liver in mice fed a high-fat diet. Molecules. 2014;19(10):16013-16023.
38. Algranti E, Mendonça EM, Ali SA, Kokron CM, Raile V. Occupational asthma caused by Ipe (Tabebuia spp) dust. J Investig Allergol Clin Immunol. 2005;15(1):81-83.15864889
39. Cheng KC, Li YX, Cheng JT. The use of herbal medicine in cancer-related anorexia/cachexia treatment around the world. Curr Pharm Des.2012;18(31):4819-4826.

Disclaimer

This information relates to an herbal, vitamin, mineral or other dietary supplement. This product has not been reviewed by the FDA to determine whether it is safe or effective and is not subject to the quality standards and safety information collection standards that are applicable to most prescription drugs. This information should not be used to decide whether or not to take this product. This information does not endorse this product as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this product. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this product. This information is not specific medical advice and does not replace information you receive from your health care provider. You should talk with your health care provider for complete information about the risks and benefits of using this product.

This product may adversely interact with certain health and medical conditions, other prescription and over-the-counter drugs, foods, or other dietary supplements. This product may be unsafe when used before surgery or other medical procedures. It is important to fully inform your doctor about the herbal, vitamins, mineral or any other supplements you are taking before any kind of surgery or medical procedure. With the exception of certain products that are generally recognized as safe in normal quantities, including use of folic acid and prenatal vitamins during pregnancy, this product has not been sufficiently studied to determine whether it is safe to use during pregnancy or nursing or by persons younger than 2 years of age.

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