β-caryophyllene, a dietary cannabinoid, complexed with β-cyclodextrin produced anti-hyperalgesic effect involving the inhibition of Fos expression in superficial dorsal horn

Quintans‐Júnior, Lucindo J.; Araújo, Adriano A. S.; Brito, Renan Guedes de; Santos, Priscila L.; Quintans, Jullyana S.S.; Serafini, Mairim Russo; Silva, Gabriel Francisco da; Carvalho, Flavio M. S.; Brogden, Nicole K.; Sluka, Kathleen A.

doi:10.1016/j.lfs.2016.02.049

Cited by 52 publications

(36 citation statements)

References 49 publications

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“…Hădărugă et al (2009) demonstrated using molecular modeling and docking studies that the rate of complex formation between BCP and βCD is relatively low, but the stability of the BCP-βCD complex seems to be higher when compared with other terpenes-βCD-complexes, such as caryophyllene-oxide or α-bisabolol. In fact, βCD has an intrinsic ability to form inclusion complexes with terpenes, which was strongly demonstrated in several studies with BCP Quintans-Júnior et al, 2016;Hădărugă, Hădărugă, Riviş & Pârvu, 2009), and to enhance pharmacological aspects, mainly bioavailability and efficacy to produce a lasting therapeutic effect (as can see in Figure 3, B and C) . Several pre-clinical and clinical studies show that the analgesic effect produced by terpenes can be improved by CDs (Brito, Araujo, Quintans, Sluka & Quintans-Junior, 2015;Oliveira, Guimaraes, Araujo, Quintans, Santos & Quintans-Junior, 2015).…”

Section: Pharmacological Improvementmentioning

confidence: 80%

“…These characteristics of CDs are interesting in relation to complex compounds, such as terpenes, that present many limitations due to their low solubility in an aqueous medium (Quintans-Júnior et al, 2016;Siqueira-Lima et al, 2014). CDs are usually able to enhance the bioavailability of insoluble compounds by increasing their drug solubility, their dissolution, and their drug permeability (Rasheed & Kumar, 2008).…”

Section: Inclusion Methods and Complexation Efficiencymentioning

confidence: 99%

“…Importantly, the complexation of β-caryophyllene and β-caryophyllene/CD improved the pharmacological aspects when compared with terpene alone. This effect seems to be related to an increased bioavailability of the active compound (Quintans-Júnior et al, 2016). Lu et al (2009) found that the relative bioavailability of the inclusion complex of genipin/β-CD compared to free genipin was 305.3%.…”

Section: Pharmacokineticsmentioning

confidence: 99%

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Inclusion of terpenes in cyclodextrins: Preparation, characterization and pharmacological approaches

Lima

Lucchese

Araújo-Filho

et al. 2016

Carbohydrate Polymers

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124

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Section: Pharmacological Improvementmentioning

confidence: 80%

Section: Inclusion Methods and Complexation Efficiencymentioning

confidence: 99%

Section: Pharmacokineticsmentioning

confidence: 99%

See 1 more Smart Citation

Inclusion of terpenes in cyclodextrins: Preparation, characterization and pharmacological approaches

Lima

Lucchese

Araújo-Filho

et al. 2016

Carbohydrate Polymers

Self Cite

124

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“…In an experimental study conducted in an FM model in mice, this compound, complexed in β-CD, reduced primary and secondary hyperalgesia as well as inhibited the superficial dorsal horn of the spinal cord, possibly by activation of descending pain pathway [32]. Antagonism studies, in a capsaicin-induced nociception test, showed that the antinociceptive effect of β-caryophyllene was reversed by naloxone, β-funaltrexamine (a μ-opioid receptor antagonist), and AM630 (a CB2 receptor antagonist) [83].…”

Section: Discussion Of Unusual Topics In Fibromyalgiamentioning

confidence: 98%

“…In relation to FM, some classes of bioactive compounds extracted from medicinal plants have presented analgesic activity described in the literature, such as essential oils [24][25][26], extracts [27,28], monoterpenes [29][30][31], sesquiterpenes [32], saponins [33], and alkaloids ( Figure 1 and Table 2) [34]. * All preclinical studies used the chronic muscle pain model induced by acid saline.…”

Section: Introductionmentioning

confidence: 99%

Natural Products as Promising Pharmacological Tools for the Management of Fibromyalgia Symptoms – A Review

Brito¹,

Santos²,

AlmeidaOliveira³

et al. 2018

Discussions of Unusual Topics in Fibromyalgia

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Fibromyalgia (FM) is the second most common rheumatologic disorder, affecting 5% of the world population, and has a serious effect on the quality of life of patients, as well as an economic impact through lost workdays. This pain syndrome is a common cause of chronic widespread pain and is characterized by reduced pressure pain thresholds with hyperalgesia and allodynia, nonrestorative sleep, fatigue, cognitive dysfunction, and mood disturbances. The pharmacological treatment strategies for FM include the use of antidepressants, calcium channel modulators, muscle relaxants, and analgesics but have shown limited efficacy and therapeutic adherence. Thus, researchers have been seeking potential substances (new chemical entities or through drug repositioning) that could be used for FM treatment. In this context, natural products (NPs) have been shown to be promising pharmacological tools due to the variety of their pharmacological activity and the number of molecular sites available as possible active targets. Recent clinical and preclinical studies have been conducted to verify the possible applicability of NPs such as essential oils (EOs), plants extracts, terpenes, sapogenins, and alkaloids in the treatment of FM. The results have shown that natural products have an analgesic effect in different animal models of FM, probably by activation of inhibitory descending pathways, such as the periaqueductal gray and rostroventromedial medulla. Natural products and their secondary metabolites could therefore be a promising source for FM management. However, translational studies that seek to validate the preclinical studies are scarce, incipient, and lacking an approach focused on the traditional pharmaceutical market.

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A systematic review on the neuroprotective perspectives of beta‐caryophyllene

Machado

Islam

Ali

et al. 2018

Phytotherapy Research

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Beta (β)-caryophyllene (BCAR) is a major sesquiterpene of various plant essential oils reported for several important pharmacological activities, including antioxidant, anti-inflammatory, anticancer, cardioprotective, hepatoprotective, gastroprotective, nephroprotective, antimicrobial, and immune-modulatory activity. Recent studies suggest that it also possesses neuroprotective effect. This study reviews published reports pertaining to the neuropharmacological activities of BCAR. Databases such as PubMed, Scopus, MedLine Plus, and Google Scholar with keywords "beta (β)-caryophyllene" and other neurological keywords were searched. Data were extracted by referring to articles with information about the dose or concentration/route of administration, test system, results and discussion, and proposed mechanism of action. A total of 545 research articles were recorded, and 41 experimental studies were included in this review, after application of exclusion criterion. Search results suggest that BCAR exhibits a protective role in a number of nervous system-related disorders including pain, anxiety, spasm, convulsion, depression, alcoholism, and Alzheimer's disease.Additionally, BCAR has local anesthetic-like activity, which could protect the nervous system from oxidative stress and inflammation and can act as an immunomodulatory agent. Most neurological activities of this natural product have been linked with the cannabinoid receptors (CBRs), especially the CB2R. This review suggests a possible application of BCAR as a neuroprotective agent.

show abstract

β-caryophyllene, a dietary cannabinoid, complexed with β-cyclodextrin produced anti-hyperalgesic effect involving the inhibition of Fos expression in superficial dorsal horn

Cited by 52 publications

References 49 publications

Inclusion of terpenes in cyclodextrins: Preparation, characterization and pharmacological approaches

Inclusion of terpenes in cyclodextrins: Preparation, characterization and pharmacological approaches

Natural Products as Promising Pharmacological Tools for the Management of Fibromyalgia Symptoms – A Review

A systematic review on the neuroprotective perspectives of beta‐caryophyllene

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