Terpenes and derivatives as a new perspective for pain treatment: a patent review

Guimarães, Adriana Gibara; Serafini, Mairim Russo; Quintans‐Júnior, Lucindo José

doi:10.1517/13543776.2014.870154

Cited by 107 publications

(69 citation statements)

References 26 publications

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“…In the pharmaceutical field, terpenes are used as excipients to enhance skin penetration, active principles of drugs, and components of non-prescription drugs [5]. In 2002, the sales on terpene-based pharmaceuticals were approximately US $12 billion [5].…”

Section: Introductionmentioning

confidence: 99%

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Terpenes solubility in water and their environmental distribution

Martins

Silva

Ferreira

et al. 2017

Journal of Molecular Liquids

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Terpenes and terpenoids belong to the largest and most diverse class of natural products. Due to the increasing importance of their applications and the emerging perception of their impact on the environment, the available physico-chemical characterization is insufficient. In this work the water solubility of geraniol, linalool, DL-citronellol, thymol, eugenol, carvacrol and p-cymene, in the temperature range from (298.15 to 323.15) K, and at atmospheric pressure, is studied. Due to the low solubility of these compounds a novel technique was adopted for their measurements and validated using the aqueous solubility data for sparingly soluble aromatic compounds. The thermodynamic properties of solution were derived from the experimental data at infinite dilution. It is shown that the solubility of terpenes in water is an endothermic process confirming the existence of UCST phase diagrams, and only for carvacrol and eugenol is entropically driven. The experimental information is shown in a two-dimensional chemical space diagram providing indications to their probable distribution in the environment once released.

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Section: Introductionmentioning

confidence: 99%

“…In 2002, the sales on terpene-based pharmaceuticals were approximately US $12 billion [5]. Examples are the antimalarial drug Artemisinin and the anticancer drug Taxol®, two of the better known terpene-based drugs [6][7][8].…”

Section: Introductionmentioning

confidence: 99%

Terpenes solubility in water and their environmental distribution

Martins

Silva

Ferreira

et al. 2017

Journal of Molecular Liquids

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“…Los monoterpenos despiertan gran interés debido a su baja toxicidad, bajo precio y su amplio rango de propiedades farmacológicas (32)(33)(34)(35). Estudios recientes indican que el linalool presenta una potente actividad antitumoral y las evidencias obtenidas a partir de experimentos in vitro e in vivo sugieren que la inducción de estrés oxidativo puede ser el responsable de su actividad anticancerígena (36).…”

Section: Discussionunclassified

Linalool effect on mitochondrial bioenergetics rat liver

Bueno-Duarte

Méndez‐Sánchez

2015

Vitae

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RESUMENAntecedentes: El linalool (2,6-dimetil-2,7-octadien-6-ol) es un monoterpeno presente en más de 200 tipos de plantas, y constituye el componente mayoritario de varios aceites esenciales. El linalool posee una amplia variedad de potenciales propiedades farmacológicas; que van desde propiedades antisépticas, ansiolíticas, anti-inflamatorias, antifúngicas, antimicrobianas y proapotóticas en diferentes líneas de cé-lulas tumorales. Sin embargo, su principal uso está relacionado como una molécula odorante o fragancia en productos de uso tópico en productos cosméticos y en la industria del perfume. Objetivo: En este estudio se evaluó el efecto del linalool sobre la bioenergética de mitocondrias aisladas de hígado de rata. Métodos: El linalool en concentraciones entre (5-100μg/mL) fue evaluado en mitocondrias aisladas de ratas machos albinas raza Wistar, de acuerdo al método descrito por Voss et al (1961). Inicialmente, se determinó el consumo de oxígeno en mitocondrias intactas mediante un método polarográfico por medio de un oxígrafo. Posteriormente, se determinó el efecto del compuesto sobre las enzimas de la cadena respiratoria mitocondrial usando métodos polarográficos y espectrofotométricos. Resultados: Los resultados obtenidos indican que el linalool en las concentraciones de 5, 10, 50 y 100μg/mL, afecta la velocidad de consumo de oxígeno en el estado 3 y 4 de mitocondrias energizadas con glutamato-malato y succinato. Sin embargo, el efecto inhibitorio es mayor al usar glutamato-malato como sustrato. Por su parte, el análisis de la actividad de las enzimas de la cadena respiratoria mitocondrial mostró que el linalool (50μg/mL) inhibe los complejos I, III y la actividad ATPasa. Conclusiones: El linalool inhibe el complejo I, complejo III y la ATPasa, esta inhibición podría aumentar la generación de especies reactivas de oxígeno.Palabras clave: Linalool, mitocondria, enzimas, consumo de oxígeno. ABSTRACTBacground: The linalool (2,6-dimethyl-2 ,7-octadiene-6-ol) is a monoterpene present in more than 200 types of plants, and it is the major component of several essential oils. The linalool has a wide range of potential pharmacological properties, such as antiseptic, anxiolytic, anti-inflammatory, antifungal, antimicrobial and proapoptotic in different tumor cell lines. However, its primary use is associated as

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“…Additionally, the use of medicinal plants as an optional treatment has been increasing, especially in developing countries. Hence, chemical and pharmacological studies are essential for the usage to become safe and improve effectiveness (Guimaraes et al 2013(Guimaraes et al , 2014Quintans et al 2014). Chrysobalanus icaco L. (Chrysobalanaceae), popularly kwon as 'abajeru' or 'grageru', is a medicinal plant common in tropical areas.…”

Section: Research Articlementioning

confidence: 99%

“…In addition, previous reports showed the presence of diterpenes in the roots of C. icaco (Gustafson et al 1991) and anthocyanins in its fruits (Brito et al 2007) that may contribute to a better understanding of the pharmacological effects. Terpenes have been promising substances in the study of new chemical entities targeting analgesic and anti-inflammatory drugs (Guimaraes et al 2013(Guimaraes et al , 2014.…”

Section: Research Articlementioning

confidence: 99%

Phytochemical screening and analgesic profile of the lyophilized aqueous extract obtained from Chrysobalanus icaco leaves in experimental protocols

Araújo-Filho

Dias

Quintans‐Júnior

et al. 2016

Pharmaceutical Biology

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Context: Chrysobalanus icaco L. (Chrysobalanaceae) has been used for the treatment of abdominal pain and cramps. Objective: Assess the chemical and pharmacological profile of the lyophilized aqueous extract from C. icaco leaves (AEC). Materials and methods: Chromatographic methods were used to assess compounds from AEC. Mice were treated with vehicle (control group) or AEC (100, 200 or 400 mg/kg, p.o.) (group with 7-8 mice) and the analgesic profile was assessed employing the acetic acid-induced writhing, formalin, hot plate tests and hyperalgesia induced by carrageenan (CG) or tumour necrosis factor-alpha. The animal motor performance was assessed using rota-rod and grip strength tests. Results:The chromatographic profile of AEC demonstrated the presence of terpenoid compounds. The acute pretreatment with AEC, at all doses, produced a significant (p < 0.01) inhibition of painful bahaviour (11.4 ± 3.6; 10.3 ± 2.8; 11.3 ± 2.2) when compared to the control group (24.7 ± 4.7) in acetic acid-induced writhing test. In the formalin test, AEC were effective in the second phase (p < 0.01) (57.2 ± 10.3; 56.3 ± 9.2; 54.7 ± 8.9) when compared to control group (121.9 ± 18.5). No response was observed in the hot plate test. The higher dose of AEC produced a significant (p < 0.01 or p < 0.05) inhibitory effect on the mechanical hyperalgesia test. AEC did not affect the motor performance of the mice. Discussion: The terpenoids from AEC are known for its analgesic and anti-inflammatory properties. So, these results corroborate the experiments using the AEC in inflammatory pain protocols. Conclusion: Our results suggest that AEC act against inflammatory pain. ARTICLE HISTORY

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Terpenes and derivatives as a new perspective for pain treatment: a patent review

Cited by 107 publications

References 26 publications

Terpenes solubility in water and their environmental distribution

Terpenes solubility in water and their environmental distribution

Linalool effect on mitochondrial bioenergetics rat liver

Phytochemical screening and analgesic profile of the lyophilized aqueous extract obtained from Chrysobalanus icaco leaves in experimental protocols

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