An Overview of the Pharmacological Properties and Potential Applications of Natural Monoterpenes

Kozioł, Agata; Stryjewska, Agnieszka; Librowski, Tadeusz; Sałat, Kinga; Gaweł, Magdalena; Moniczewski, Andrzej; Lochyński, Stanisław

doi:10.2174/1389557514666141127145820

Cited by 162 publications

(119 citation statements)

References 66 publications

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“…AT ratio of trial participants at baseline and after treatment was determined through inspection of hair follicles using a standard method 31. In the study cohort, most of the individuals had low baseline anagen ratios, with the majority below 50% anagen (0.5 AT ratio; Figure 5A–C, baseline).…”

Section: Resultsmentioning

confidence: 99%

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Promotion of anagen, increased hair density and reduction of hair fall in a clinical setting following identification of FGF5-inhibiting compounds via a novel 2-stage process

Burg¹,

Yamamoto²,

Namekata³

et al. 2017

CCID

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BackgroundThere are very few effective, scientifically validated treatments with known mechanisms of action for treatment of hair loss in both men and women. Fibroblast growth factor 5 (FGF5) is an important factor in the irreversible transition from anagen to catagen, and inhibition of FGF5 prolongs anagen phase and reduces hair loss.ObjectiveWe aimed to screen botanically derived molecules for FGF5 inhibitory activity in vitro and assess efficacy in a clinical setting.MethodsWe screened for FGF5 inhibitory efficacy via a novel 2-step in vitro pipeline consisting of an engineered FGF5 responsive cell line, followed by an activated dermal papillae (DP) cell method. Efficacy in a clinical setting was assessed in a randomized, single-blind, placebo-controlled trial against early- to mid-stage pattern hair loss in men and women.ResultsWe observed FGF5 inhibitory activity for a number of compounds from the monoterpenoid family, many showing greater inhibitory efficacy than our previously reported crude plant extracts. Evaluation of a lead candidate in a clinical study over 112 days showed a significant improvement in anagen:telogen (AT) ratio (p = 0.002), reduced hair fall (p = 0.007) and improved visual grading (p = 0.004). Scientifically matched photography on a subgroup of randomly chosen participants highlighted significant improvement in hair density, with increases evident in all tested participants compared to baseline.ConclusionIsolates from the monoterpenoid family displayed efficacy in FGF5 inhibition in vitro. A topical formulation containing a leading isolate significantly improved AT ratio, reduced hair fall and increased apparent hair density in the tested population of men and women.

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Section: Resultsmentioning

confidence: 99%

“…Monoterpenes are C10 compounds that may be cyclic or acyclic with the generalized cyclic structure illustrated in Figure 1. Numerous monoterpenoid compounds of botanical origin are known to have pharmacological properties, including anti-inflammatory and anti-microbial activities, growth modulation and anti-tumor actions 29,31…”

Section: Introductionmentioning

confidence: 99%

Promotion of anagen, increased hair density and reduction of hair fall in a clinical setting following identification of FGF5-inhibiting compounds via a novel 2-stage process

Burg¹,

Yamamoto²,

Namekata³

et al. 2017

CCID

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“…The reaction product was ethyl (4-tert-butyl-1-ethenylcyclohexyl)acetate (4). The resulting ethyl (4-tert-butylcyclohexylidene)acetate (2) was reduced using lithium aluminum hydride.…”

Section: Resultsmentioning

confidence: 99%

“…[1] It was also examined by testing its ability to produce seizures or to inhibit seizures induced by pentylenetetrazol and maximal electroshock in CF-1 mice. [4] Previously, derivatives with cyclohexane unit were used as a substrate for active compounds with high local anesthetic activity. Due to its interactions with the inhibitory neurotransmitter γ-aminobutyric acid, picrotoxin acts as a stimulant and convulsant and mainly impacts the central nervous system, causing seizures and respiratory paralysis when administered at high doses.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Activity of New 4‐tert‐Butylcyclohexanone Derivatives

Kozioł

Jasnowski

Grela

et al. 2019

Chemistry & Biodiversity

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In the synthesis performed in this study, derivatives of 4-tert-butylcyclohexanone 1 were obtained using typical reactions of organic synthesis. The bioactivity of the selected compounds was evaluated. 1-(Bromomethyl)-8-tert-butyl-2-oxaspiro[4.5]decan-3-one (5) was characterized by attractant properties against larvae and a weak feeding deterrent activity against adults of Alphitobius diaperinus PANZER. This bromolactone was a moderate antifeedant towards Myzus persicae SULZER. In addition, ethyl (4-tert-butylcyclohexylidene)acetate (2) and bromolactone 5 displayed antibacterial activity. The strongest bacteriostatic effect was observed against Gram-positive strains: Bacillus subtilis and Staphylococcus aureus. The bromolactone 5 also limited the growth of Escherichia coli strain.

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“…They are known for their aromatic, gastronomic and phytotherapeutic features. Hence, EO extracted from these plants is actively investigated for antimicrobial effect [4], as they could substitute antibiotics in the treatment of infectious diseases caused by multi-resistant bacteria (MRB).…”

Section: Introductionmentioning

confidence: 99%

Antimicrobial activity of essential oils extracted from leaves of native Moroccan plants against clinical bacterial isolates

Malki¹,

Eddaraji²,

Alloudane³

et al. 2018

int. arab. j antimicrob. agents

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Introduction: Medicinal plants possess plentiful of bioactive molecules effective against multi-resistance bacteria. The aim of this study is to assess the in vitro antimicrobial activities of essential oils extracted from three Moroccan aromatic plants. Method:Analysis of essential oils of Origanum compactum, Rosmarinus officinalis and Pelargonium asperum, collected from different localities in Morocco was performed using a GC-MS spectrophotometry. Antibacterial activity by disc diffusion assay was evaluated in vitro against five clinical multi-resistant isolates.Results: Origanum showed strong antibacterial activity against tested strains except Pseudomonas aeruginosa while Rosmarinum showed a bactericidal effect against Acinetobacter baumanii, Escherichia coli and Staphylococcus aureus. Pelargonium presented only slight growth inhibition of Staphylococcus aureus on solid medium. Interestingly, fractions F7 and F8 of Pelargonium which represented only 0.3% and 0.1% respectively of the total mass were found to be bactericidal against Klebsiella pneumoniae and Pseudomonas aeruginosa. Conclusions:Ours results showed that the antimicrobial activities were variables depending on the chemical composition of essential oils, the fraction used and the microorganism tested.Essential oils fractionation allows detection of bioactive substances, especially those owning antimicrobial activity and present in small quantities. IntroductionThe overuse of antibiotics to treat infectious diseases resulted in the emergence of multidrug resistance (MDR) bacteria. Actually, this increased phenomenon is currently considered as a major threat to global public health. This has prompted the World Health Organization (WHO) to direct research into new alternatives and especially to plants that have always constituted a source of ongoing bioactive molecules and current inspiration for new medicines. Delacroix in 1881 showed for the first time the essential oils (Eos) action against bacteria [1]. Since then, numerous studies have been reported the in vitro antimicrobial activities of certain chemical compounds of various plant extracts [2]. The capacity of certain essential oils to neutralize germs is now irrefutable [3].Origanum compactum, Rosmarinus officinalis and Pelargonium asperum are wildly used plants over the world and particularly in Mediterranean countries. They are known for their aromatic, gastronomic and phytotherapeutic features. Hence, EO extracted from these plants is actively investigated for antimicrobial effect [4], as they could substitute antibiotics in the treatment of infectious diseases caused by multi-resistant bacteria (MRB).The mode of action of EOs on bacteria is not clearly elucidated, but for the variety of molecules in these oils, it seems that their effect results from a combination of several modes of action that involve various cell targets [5].This study was carried out aiming to perform qualitative and quantitative analyses and to assess the in vitro antimicrobial activities of EOs extracted fr...

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An Overview of the Pharmacological Properties and Potential Applications of Natural Monoterpenes

Cited by 162 publications

References 66 publications

Promotion of anagen, increased hair density and reduction of hair fall in a clinical setting following identification of FGF5-inhibiting compounds via a novel 2-stage process

Promotion of anagen, increased hair density and reduction of hair fall in a clinical setting following identification of FGF5-inhibiting compounds via a novel 2-stage process

Synthesis and Biological Activity of New 4‐tert‐Butylcyclohexanone Derivatives

Antimicrobial activity of essential oils extracted from leaves of native Moroccan plants against clinical bacterial isolates

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