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The current research is focused on the discovery and optimization of an effective cosmetic carrier of alpha-bisabolol as a first step in the development of a cosmetic product with cleansing and antimicrobial action for facial skin hygiene. A micellar solution of Poloxamer 407 was selected as a cosmetic base because of the good washing ability, easy application, and high tolerability of this polymeric surfactant. The solubilization capacity of a 5% micellar solution with respect to α-bisabolol was investigated by applying varying solubilization techniques and increasing concentrations of the oily active substance. The test samples were subjected to an accelerated physical stability test, viscosimetry, dynamic light scattering (DLS), electrophoretic light scattering (ELS), foamability test, and antimicrobial screening. Over the course of this research, the advantage of the film-hydration method over direct solubilization was demonstrated by the narrower size distribution and smaller hydrodynamic size of the micellar nano-carriers (ranging from 29.02 to 116.5 nm) and the respective higher physical stability of the dispersions. The optimized composition was found to be suitable for application on large skin areas in terms of viscosity in the temperature range from 20 °C to 40 °C (3.4–2.3 mPa.s). Preservation of the washing capacity of the micellar solution in the presence of solubilized α-bisabolol was established. The active composition demonstrated inhibitory activity against Staphylococcus aureus and Escherichia coli and fungicidal activity against Candida albicans. This study concludes that the optimal concentration of α-bisabolol to be solubilized in a 5% Poloxamer 407 micellar solution by the film-hydration technique is 1%, considering the desirable physical endurance and antimicrobial activity. [ABSTRACT FROM AUTHOR]

Introduction. Despite the proven clinical efficacy of antifungal and anti-inflammatory drugs for the prevention and treatment of seborrheic dermatitis, the search for new targets and the development of new substances with a beneficial effect on the scalp microflora, with a low risk of antimicrobial resistance and adverse effects, are relevant.Aim. Development of the antimicrobial multicomponent pharmaceutical substance of plant origin in stages: from a literature search for promising substances, analysis of their composition by GC-MS, in silico evaluation of the affinity of individual components to pathogenetic targets, selection of the optimal composition of a multicomponent substance based on the results of in vitro research of antimicrobial action and the making of a medical dosage form based on it – a medicinal shampoo for the treatment of seborrheic dermatitis.Materials and methods. Objects of research: tea tree essential oil, 1,8-cineole, α-(-)-bisabolol and the multicomponent substance based on them. Methods: molecular docking (AutoDock version 4.2), prediction of pharmacological activity (Phyto4Health), TLC, GC-MS, study of antimicrobial activity in vitro.Results and discussion. Based on the results of a literature search, 3 promising substances were selected for the development of a multicomponent plant-based substance: tea tree essential oil, 1,8-cineole and α-(-)-bisabolol. Molecular docking predicted the targeted activity of the phytochemicals of tea tree essential oil, 1,8-cineole and α-(-)-bisabolol on the domains of ABC-transporters of microorganisms involved in the pathogenesis of seborrheic dermatitis and justified the possibility of use for therapy. The multicomponent substance has been developed based on tea tree essential oil, 1,8-cineole and α-(-)-bisabolol in a mass ratio of 1 : 1 : 1. The qualitative composition of the substance was assessed by TLC and GC-MS methods, and 15 terpenes were quantitatively identified in its composition with a predominance of terpinen-4-ol (16.98 %), 1,8-cineole (25.63 %) and α-(-)-bisabolol (27.67 %). The synergistic antimicrobial activity of the substance has been established against S. epidermidis, S. aureus, C. albicans and M. furfur in comparison with benzalkonium chloride, ketoconazole and climbazole. The composition of a new medical shampoo based on the investigated substance has been developed, which has a pronounced antifungal effect (more than 99.0 %) against M. furfur without visible suppression of normal microflora. For the novel substance of plant origin and medical shampoo, quality parameters were assessed in accordance with the Russian Pharmacopoeia of XIV edition.Conclusion. A substance of plant origin with synergistic and targeted antimicrobial activity has been developed. It has an interest for further study as a drug and API for new products for the treatment of seborrheic dermatitis.

Background: Cheilitis is a chronic inflammatory condition of the lips, and frequent or prolonged use of topical corticosteroids may lead to various adverse events. Therefore, alternative therapies with fewer side effects are beneficial for the treatment of this condition. Aim: To evaluate the efficacy of a lip care formulation containing both panthenol and bisabolol as a monotherapy for mild‐to‐moderate cheilitis. Methods: This single‐centre prospective pilot open‐label study included 20 patients with mild‐to‐moderate cheilitis who were treated with the tested lip care for 8 weeks and evaluated by physician and patient assessments before the final efficacy was determined using the Visioscan score. Results: Of the 20 patients, 13 (65.0%) presented with moderate cheilitis with dry and chapped lips. All parameters, including physician and patient clinical scores and bioengineering measurements, showed significant improvements as early as week 2 and sustained until week 8 following the application of the tested lip care. The frequency of cheilitis flareups also decreased significantly. The tested product was well tolerated without any adverse effects. Conclusions: Lip care with panthenol and bisabolol was safe and effective. It can be used as monotherapy for the treatment of mild‐to‐moderate cheilitis. [ABSTRACT FROM AUTHOR]

The current research is focused on the discovery and optimization of an effective cosmetic carrier of alpha-bisabolol as a first step in the development of a cosmetic product with cleansing and antimicrobial action for facial skin hygiene. A micellar solution of Poloxamer 407 was selected as a cosmetic base because of the good washing ability, easy application, and high tolerability of this polymeric surfactant. The solubilization capacity of a 5% micellar solution with respect to α-bisabolol was investigated by applying varying solubilization techniques and increasing concentrations of the oily active substance. The test samples were subjected to an accelerated physical stability test, viscosimetry, dynamic light scattering (DLS), electrophoretic light scattering (ELS), foamability test, and antimicrobial screening. Over the course of this research, the advantage of the film-hydration method over direct solubilization was demonstrated by the narrower size distribution and smaller hydrodynamic size of the micellar nano-carriers (ranging from 29.02 to 116.5 nm) and the respective higher physical stability of the dispersions. The optimized composition was found to be suitable for application on large skin areas in terms of viscosity in the temperature range from 20 °C to 40 °C (3.4–2.3 mPa.s). Preservation of the washing capacity of the micellar solution in the presence of solubilized α-bisabolol was established. The active composition demonstrated inhibitory activity against Staphylococcus aureus and Escherichia coli and fungicidal activity against Candida albicans. This study concludes that the optimal concentration of α-bisabolol to be solubilized in a 5% Poloxamer 407 micellar solution by the film-hydration technique is 1%, considering the desirable physical endurance and antimicrobial activity.

Centella asiatica is widely used for its antimicrobial, antioxidant, anti-inflammatory, neuroprotective and wound-healing properties. Bisabolol is an unsaturated sesquiterpene found in increased amounts in chamomile and clary sage oil known for its multiple skin-repairing and soothing virtues. The aim of the present research was to histologically evaluate the efficacy of ointment with Centella asiatica extract and bisabolol. 14 mice from the balb/c line were included in the study, which were divided into 2 groups (experimental, control) and each animal included in the study was clipped before applying the mechanical burn. The duration of the experiment was 14 days with collections of biological material at 3.7 and 14 days. Following the study, we found that, in thermal burns, the use of ointment in which Centella asiatica 2% and bisabolol 1% were incorporated speeds up the skin healing process, compared to the untreated injury, and prevents bacterial superinfections from setting in.

The research into new pharmaceutical substances based on essential oils, individual biologically active phytochemicals, and plant extracts is a priority in field of pharmaceutical sciences. A novel multicomponent substance based on Melaleuca alternifolia (M. alternifolia) leaf oil (TTO), 1,8-cineole (eucalyptol), and (-)-α-bisabolol with potent synergetic antimicrobial activity was investigated and suggested for the treatment of seborrheic dermatitis (SD) and dandruff. The objective of this research was to establish and validate a specific, accurate, and precise gas chromatography–mass spectrometry (GC–MS) method for further quantitative and qualitative analysis in order to ensure quality control. The main parameters of validation were suitability, specificity, linearity, accuracy, and intermediate precision according to the European Pharmacopoeia (XI edition), Russian Pharmacopoeia (XIV edition), and some parameters of ICH requirements. The peaks of fifteen chemical phytoconstituents were identified in the test sample solution with the prevalence of (−)-α-bisabolol (27.67%), 1,8-cineole (25.63%), and terpinen-4-ol (16.98%). These phytochemicals in the novel substance were chosen for standardization and validation of the GC–MS method. The chosen chromatographic conditions were confirmed for testing of the plant-based substance in a suitability test. It was established that the GC–MS method provides a significant separation, symmetry of peaks and resolution between phytochemicals. The calibration curves of each phytochemical had good linearity (R2 > 0.999) in five concentrations. In the same concertation range, the accuracy of terpinen-4-ol, 1,8-cineol, and (−)-α-bisabolol determination using the method of additives was 98.3–101.60%; the relative standard deviation (RSD) ranged from 0.89% to 1.51% and corresponded to requirements. The intraday and interday precision was ≤2.56%. Thus, the GC–MS method was validated to be specific, sensitive, linear, accurate, and precise. This GC–MS method could be recommended as a routine analytic technique for multicomponent plant-based substances-enriched terpenes. [ABSTRACT FROM AUTHOR]

Gymnosperma glutinosum is a plant popularly known as "popote", "tatalencho", "tezozotla" or "pegajosa", and it is used in traditional medicine in the region of Tehuacán, Puebla (Mexico), for the treatment of jiotes and acne and to cure diarrhea using the aerial parts in infusions. To analyze the phytochemical composition, we have developed a rapid protocol for the extraction and separation of the components of the aerial parts of G. glutinosum. After a maceration process, chloroformic and methanolic extracts were obtained and analyzed. Extracts were evaluated by GC-MS (gas chromatography-mass spectrometry), and their composition revealed the presence of (−)-α-bisabolol (BIS) as the main component in the chloroformic extract, which was isolated and analyzed by 1H NMR to confirm its presence in the plant. The analysis of methanolic extracts by UPLC-MS (ultra-performance liquid chromatography-mass spectrometry) revealed the occurrence of six methoxylated flavones with m/z 405.08 (C19H18O10), m/z 419.09 (C20H20O10) and m/z 433.11 (C21H22O10), and a group of C20-, C18-hydroxy-fatty acids, which give the plant its sticky characteristic. The presence of BIS, an important sesquiterpene with therapeutic skin effects, as well as some antioxidant compounds such as methoxylated flavones and their oils, could play an important role in cosmetology and dermatology formulations. [ABSTRACT FROM AUTHOR]

Centella asiatica is widely used for its antimicrobial, antioxidant, anti-inflammatory, neuroprotective and wound-healing properties. Bisabolol is an unsaturated sesquiterpene found in increased amounts in chamomile and clary sage oil known for its multiple skin-repairing and soothing virtues. The aim of the present research was to histologically evaluate the efficacy of ointment with Centella asiatica extract and bisabolol. 14 mice from the balb/c line were included in the study, which were divided into 2 groups (experimental, control) and each animal included in the study was clipped before applying the mechanical burn. The duration of the experiment was 14 days with collections of biological material at 3.7 and 14 days. Following the study, we found that, in thermal burns, the use of ointment in which Centella asiatica 2% and bisabolol 1% were incorporated speeds up the skin healing process, compared to the untreated injury, and prevents bacterial superinfections from setting in. [ABSTRACT FROM AUTHOR]

Hydroxyapatite, Ca5(PO4)3(OH), is a biomimetic active ingredient, which is used in commercial oral care products such as toothpastes and mouthwashes worldwide. Clinical studies (in vivo) as well as in situ and in vitro studies have shown the preventive effects of hydroxyapatite in various field of oral care. In some products, hydroxyapatite is combined with other active ingredients, to achieve an additional antibacterial effect or to promote gum health. This review analyzes the efficacy of six selected natural and nature-inspired ingredients that are commonly used together with hydroxyapatite. These additional actives are either antibacterial (lactoferrin, xylitol, and zinc) or promote gum health (allantoin, bisabolol, and hyaluronic acid). A systematic literature search was performed, and all studies found on each ingredient were analyzed. In summary, all analyzed ingredients mentioned in this review are well described in scientific studies on their beneficial effect for oral health and can be used to expand the preventive effect of hydroxyapatite in oral care products. [ABSTRACT FROM AUTHOR]

German chamomile otherwise known as Matricaria chamomilla L. syn Chamomilla recutita (L.) Rauschert is widely used in herbal teas and cosmetics given its outstanding antioxidant properties. Two released cultivars of German chamomile viz. 'CIM-Sammohak' and 'CIM-Ujjwala' were chemically profiled to investigate the constitutional makeup of their aerial parts, flowers, leaves, and roots collected during the flowering season. The whole aerial part and then the aerial part inclusive of flowers harvested 50 cm above ground level were investigated separately to note the differences in the chemical composition due to the flowers. The oils from the flowers of CIM-Sammohak were also chemically distinguished using hydro distillation and steam distillation methods. α-bisabolone oxide A, α-bisabolol oxide A, and α-bisabolol oxide B were higher in the flowers using hydro distillation method while the concentrations of α-(E, E)-farnesene, germacrene D, and (E)-β-farnesene increased on using steam distillation technique for flowers essential oil extraction. α-bisabolol oxide A (0.1 %-41.9 %), α-bisabolone oxide A (2.1%-28.3%), (E)-β-farnesene (1.0%-39.6%), and α-bisabolol oxide B (1.5 %-16.6 %) were identified to be the major compounds in all the oils of CIM-Sammohak whereas the oils of CIM-Ujjwala revealed entirely different composition dominant of acetylenic molecules viz. (2Z,8Z)-matricaria ester (60.1%-81.9%) and (2E,8Z)-matricaria ester (1.5%-7.2%). The flower yield of CIM- Sammohak was higher compared to CIM-Ujjwala; and it is highly demanded in the market for its dry flower and essential oils. However, the CIM-Ujjwala is suitable as source of bioactive (2Z,8Z)-matricaria ester useful in cosmetic and pharmaceutical industries. [ABSTRACT FROM AUTHOR]

Irritated and itchy skin is a common skin condition. Consumers tend to opt for natural ingredients for irritated skin (e.g., after insect bites or sun exposure). We tested a cosmetic product with 94% of its ingredients being of natural origin, each with its beneficial properties, e.g., nourishing shea butter, cooling menthol, and soothing bisabolol. Skin discomfort was induced either by a chemical irritant (capsaicin) or UV radiation by a solar simulator. In this clinical, prospective, and controlled experimental study, we investigated the soothing effect of the tested product. We observed a soothing effect on the capsaicin-induced itching and stinging sensation with a statistically significant decrease in the discomfort sensations one minute after a single application. The tested product also showed a significant reduction in the UV-induced skin erythema (UVA+B exposure). In a real-world study, these results can be correlated with a decrease of itching and irritation after sunburn or after insect bites. [ABSTRACT FROM AUTHOR]

The research into new pharmaceutical substances based on essential oils, individual biologically active phytochemicals, and plant extracts is a priority in field of pharmaceutical sciences. A novel multicomponent substance based on Melaleuca alternifolia (M. alternifolia) leaf oil (TTO), 1,8-cineole (eucalyptol), and (-)-α-bisabolol with potent synergetic antimicrobial activity was investigated and suggested for the treatment of seborrheic dermatitis (SD) and dandruff. The objective of this research was to establish and validate a specific, accurate, and precise gas chromatography–mass spectrometry (GC–MS) method for further quantitative and qualitative analysis in order to ensure quality control. The main parameters of validation were suitability, specificity, linearity, accuracy, and intermediate precision according to the European Pharmacopoeia (XI edition), Russian Pharmacopoeia (XIV edition), and some parameters of ICH requirements. The peaks of fifteen chemical phytoconstituents were identified in the test sample solution with the prevalence of (−)-α-bisabolol (27.67%), 1,8-cineole (25.63%), and terpinen-4-ol (16.98%). These phytochemicals in the novel substance were chosen for standardization and validation of the GC–MS method. The chosen chromatographic conditions were confirmed for testing of the plant-based substance in a suitability test. It was established that the GC–MS method provides a significant separation, symmetry of peaks and resolution between phytochemicals. The calibration curves of each phytochemical had good linearity (R2 > 0.999) in five concentrations. In the same concertation range, the accuracy of terpinen-4-ol, 1,8-cineol, and (−)-α-bisabolol determination using the method of additives was 98.3–101.60%; the relative standard deviation (RSD) ranged from 0.89% to 1.51% and corresponded to requirements. The intraday and interday precision was ≤2.56%. Thus, the GC–MS method was validated to be specific, sensitive, linear, accurate, and precise. This GC–MS method could be recommended as a routine analytic technique for multicomponent plant-based substances-enriched terpenes.

Abstract T-type calcium channels are known molecular targets of certain phytocannabinoids and endocannabinoids. Here we explored the modulation of Cav3.2 T-type calcium channels by terpenes derived from cannabis plants. A screen of eight commercially available terpenes revealed that camphene and alpha-bisabolol mediated partial, but significant inhibition of Cav3.2 channels expressed in tsA-201 cells, as well as native T-type channels in mouse dorsal root ganglion neurons. Both compounds inhibited peak current amplitude with IC50s in the low micromolar range, and mediated an additional small hyperpolarizing shift in half-inactivation voltage. When delivered intrathecally, both terpenes inhibited nocifensive responses in mice that had received an intraplantar injection of formalin, with alpha-bisabolol showing greater efficacy. Both terpenes reduced thermal hyperalgesia in mice injected with Complete Freund’s adjuvant. This effect was independent of sex, and absent in Cav3.2 null mice, indicating that these compounds mediate their analgesic properties by acting on Cav3.2 channels. Both compounds also inhibited mechanical hypersensitivity in a mouse model of neuropathic pain. Hence, camphene and alpha-bisabolol have a wide spectrum of analgesic action by virtue of inhibiting Cav3.2 T-type calcium channels.

Gymnosperma glutinosum is a plant popularly known as “popote”, “tatalencho”, “tezozotla” or “pegajosa”, and it is used in traditional medicine in the region of Tehuacán, Puebla (Mexico), for the treatment of jiotes and acne and to cure diarrhea using the aerial parts in infusions. To analyze the phytochemical composition, we have developed a rapid protocol for the extraction and separation of the components of the aerial parts of G. glutinosum. After a maceration process, chloroformic and methanolic extracts were obtained and analyzed. Extracts were evaluated by GC-MS (gas chromatography-mass spectrometry), and their composition revealed the presence of (−)-α-bisabolol (BIS) as the main component in the chloroformic extract, which was isolated and analyzed by 1H NMR to confirm its presence in the plant. The analysis of methanolic extracts by UPLC-MS (ultra-performance liquid chromatography-mass spectrometry) revealed the occurrence of six methoxylated flavones with m/z 405.08 (C19H18O10), m/z 419.09 (C20H20O10) and m/z 433.11 (C21H22O10), and a group of C20-, C18-hydroxy-fatty acids, which give the plant its sticky characteristic. The presence of BIS, an important sesquiterpene with therapeutic skin effects, as well as some antioxidant compounds such as methoxylated flavones and their oils, could play an important role in cosmetology and dermatology formulations.

Cisplatin (CP) treatment has been long associated with the development of acute kidney injury (AKI) through mechanisms involving inflammation and oxidative stress. α-Bisabolol (BIS), a sesquiterpene alcohol isolated from the essential oil of various plants, including chamomile, has garnered popularity lately due to its antioxidant, anti-inflammatory, and anticancer properties. Therefore, we investigated the nephroprotective effects of BIS in the murine model of CP-induced AKI and the underlying mechanism of action. BALB/c mice were given BIS orally at 25 mg/kg for 7 days. On day 7, they were given a single dose of CP at 20 mg/kg intraperitoneally. BIS treatment continued for 3 more days. The animals were sacrificed at the end of the experiment (day 11). Kidneys, plasma, and urine were collected, and subsequently, various physiological, biochemical, and histological parameters were assessed. BIS has significantly normalized the alterations of water intake, urine volume, relative kidney weight, and the concentrations of urea and creatinine, as well as the creatinine clearance induced by CP treatment. BIS significantly mitigated the effects of CP-induced kidney injury by reducing kidney injury molecule-1, neutrophil gelatinase-associated lipocalin, adiponectin, and cystatin C. Likewise, the renal concentrations of proinflammatory cytokines, tumor necrosis factor α, interleukin (IL)-6 and IL-1β that were elevated in CP group were significantly reduced in mice treated with BIS and CP. A similar significant reduction was also observed in the CP-induced augmented levels of markers of oxidative stress, as well as the metabolite pteridine. Moreover, BIS significantly reduced the CP–induced renal DNA damage, and markedly lessened the acute tubular necrosis observed in kidney histology. Additionally, BIS significantly reduced the CP-induced increase in the phosphorylated nuclear factor κB (NFκB) in the kidney. These data strongly suggest that BIS exerts a protective action against CP-induced nephrotoxicity by mitigating inflammation and oxidative stress through the inhibition of NFκB activation. No overt adverse effects were noted with BIS treatment. Additional investigations should be done to consider BIS as an efficacious nephroprotective agent against CP. [ABSTRACT FROM AUTHOR]

L'huile essentielle de Matricaire, remarquable par sa couleur bleu encre, est connue pour ses propriétés antiallergiques et apaisantes au niveau cutané, mais elle a également une action anti-infectieuse, notamment contre Helicobacter pylori. Elle a comme défaut d'être chère et de pouvoir teinter un soin aromatique ou un vêtement. [ABSTRACT FROM AUTHOR]

T-type calcium channels are known molecular targets of certain phytocannabinoids and endocannabinoids. Here we explored the modulation of Cav3.2 T-type calcium channels by terpenes derived from cannabis plants. A screen of eight commercially available terpenes revealed that camphene and alpha-bisabolol mediated partial, but significant inhibition of Cav3.2 channels expressed in tsA-201 cells, as well as native T-type channels in mouse dorsal root ganglion neurons. Both compounds inhibited peak current amplitude with IC50s in the low micromolar range, and mediated an additional small hyperpolarizing shift in half-inactivation voltage. When delivered intrathecally, both terpenes inhibited nocifensive responses in mice that had received an intraplantar injection of formalin, with alpha-bisabolol showing greater efficacy. Both terpenes reduced thermal hyperalgesia in mice injected with Complete Freund's adjuvant. This effect was independent of sex, and absent in Cav3.2 null mice, indicating that these compounds mediate their analgesic properties by acting on Cav3.2 channels. Both compounds also inhibited mechanical hypersensitivity in a mouse model of neuropathic pain. Hence, camphene and alpha-bisabolol have a wide spectrum of analgesic action by virtue of inhibiting Cav3.2 T-type calcium channels. [ABSTRACT FROM AUTHOR]

Bisabolol is one of the bioactive constituents of chamomile. It was aimed to biotransform (-)-α-bisabolol by different fungi for the production of new bioactive metabolites, which was converted to α-bisabolol oxide A and B by Thamnidium elegans. Additionally, the biotransformation by Penicillium neocrassum yielded a new metabolite, which was characterized as 2-(5-methyl-5-(6-methyl-7-oxabicyclo[4.1.0]heptan-3-yl)tetrahydrofuran-2-yl)propan-2-ol = bisafuranol. The substrate and its metabolite mixtures were tested using antioxidant DPPH• scavenging assay. Antimicrobial activity was evaluated by an in vitro microdilution assay against a panel of human pathogenic bacteria and yeasts resulting in the lowest MIC and MFC values of 150 µg/mL. (-)-α-Bisabolol was effective against Propionibacterium acnes and Staphylococcus epidermidis (75, 37.5 µg/mL, respectively). The antioxidant activity of the metabolites was found to be more effective in scavenging free radicals. [ABSTRACT FROM AUTHOR]

This study aimed to assess the benefits of the solvent-free microwave extraction (SFME) on chamomile (Matricaria recutita L.) essential oil quality and yield compared to the extraction by steam distillation (SD). The oil obtained by SFME and SD presented a blue color, a solubility in 70% ethanol (v/v) of four, a relative density of 0.929–0.925 g/mL, a refractive index of 1.5013–1.4790, and an acidity value of 6.23 and 3.43, respectively. The yields were significantly different between extraction methods, being the highest (0.5 mL (0.083% v/w)) for SFME and 0.2 mL (0.03%) for SD. The GC-MS analysis showed a marked difference in sesquiterpenes, such as Chamazulene, α-bisabolol, α-bisabolol oxide A, and α-bisabolol oxide B. The SFME had 97% and 20% more content of chamazulene and α-bisabolol respectively, whilst SD had 88% and 12% more content of α-bisabolol oxide A and B, respectively. The results suggest that SME is an outstanding alternative for essential oil extraction due to much higher yield and quality compared to the steam distillation.

Premature ejaculation (PE) has been defined as the inability to control or delay ejaculation, resulting in dissatisfaction or distress of the patient. Although PE is the most frequent sexual dysfunction, it is still underdiagnosed. An accurate clinical history is the best diagnostic approach that, in the majority of cases, is enough to differentiate between primary and acquired PE. Nowadays, treatment is not curative but is effective in increasing the intravaginal ejaculatory latency time (IELT), improving the sexual satisfaction of the couple [...].

Cisplatin (CP) treatment has been long associated with the development of acute kidney injury (AKI) through mechanisms involving inflammation and oxidative stress. α-Bisabolol (BIS), a sesquiterpene alcohol isolated from the essential oil of various plants, including chamomile, has garnered popularity lately due to its antioxidant, anti-inflammatory, and anticancer properties. Therefore, we investigated the nephroprotective effects of BIS in the murine model of CP-induced AKI and the underlying mechanism of action. BALB/c mice were given BIS orally at 25 mg/kg for 7 days. On day 7, they were given a single dose of CP at 20 mg/kg intraperitoneally. BIS treatment continued for 3 more days. The animals were sacrificed at the end of the experiment (day 11). Kidneys, plasma, and urine were collected, and subsequently, various physiological, biochemical, and histological parameters were assessed. BIS has significantly normalized the alterations of water intake, urine volume, relative kidney weight, and the concentrations of urea and creatinine, as well as the creatinine clearance induced by CP treatment. BIS significantly mitigated the effects of CP-induced kidney injury by reducing kidney injury molecule-1, neutrophil gelatinase-associated lipocalin, adiponectin, and cystatin C. Likewise, the renal concentrations of proinflammatory cytokines, tumor necrosis factor α, interleukin (IL)-6 and IL-1β that were elevated in CP group were significantly reduced in mice treated with BIS and CP. A similar significant reduction was also observed in the CP-induced augmented levels of markers of oxidative stress, as well as the metabolite pteridine. Moreover, BIS significantly reduced the CP–induced renal DNA damage, and markedly lessened the acute tubular necrosis observed in kidney histology. Additionally, BIS significantly reduced the CP-induced increase in the phosphorylated nuclear factor κB (NFκB) in the kidney. These data strongly suggest that BIS exerts a protective action against CP-induced nephrotoxicity by mitigating inflammation and oxidative stress through the inhibition of NFκB activation. No overt adverse effects were noted with BIS treatment. Additional investigations should be done to consider BIS as an efficacious nephroprotective agent against CP.

Abstract Background Chamomile (Matricaria recutita L.) has a long history of use in herbal medicine with various applications, and the flower heads contain numerous secondary metabolites which are medicinally active. In the major crop plants, next generation sequencing (NGS) approaches are intensely applied to exploit genetic resources, to develop genomic resources and to enhance breeding. Here, genotyping-by-sequencing (GBS) has been used in the non-model medicinal plant chamomile to evaluate the genetic structure of the cultivated varieties/populations, and to perform genome wide association study (GWAS) focusing on genes with large effect on flowering time and the medicinally important alpha-bisabolol content. Results GBS analysis allowed the identification of 6495 high-quality SNP-markers in our panel of 91 M. recutita plants from 33 origins (2–4 genotypes each) and 4 M. discoidea plants as outgroup, grown in the greenhouse in Gatersleben, Germany. M. recutita proved to be clearly distinct from the outgroup, as was demonstrated by different cluster and principal coordinate analyses using the SNP-markers. Chamomile genotypes from the same origin were mostly genetically similar. Model-based cluster analysis revealed one large group of tetraploid genotypes with low genetic differentiation including 39 plants from 14 origins. Tetraploids tended to display lower genetic diversity than diploids, probably reflecting their origin by artificial polyploidisation from only a limited set of genetic backgrounds. Analyses of flowering time demonstrated that diploids generally flowered earlier than tetraploids, and the analysis of alpha-bisabolol identified several tetraploid genotypes with a high content. GWAS identified highly significant (P

Acute Kidney Injury (AKI) is associated with high morbidity and mortality. Ischemia and reperfusion (I/R) are events that lead to AKI through hypoxia, reactive oxygen species (ROS) production, oxidative stress and apoptosis. We aimed to evaluate the mechanism of nephroprotection mediated by Bisabolol in human tubular kidney cells after injury by I/R in vitro. HK2 cells were exposed to I/R and treated with Bisabolol. Cell viability was accessed by MTT assay. Cells were submitted to flow cytometry to evaluate necrotic/apoptotic cells, reactive oxygen species production and mitochondrial transmembrane depolarization. TBARS and GSH were used as parameters of redox balance. Also, KIM-1 supernatant levels were measured. In order to identify an interaction between bisabolol and NOX4, molecular docking and enzymatic assays were performed. Expression of isoform NOX4 on treated cells was examined by western-blot. Finally, cells were visualized by scanning electron microscopy. Bisabolol improved cell viability and prevented cell death by apoptosis, indicated also by the decreased levels of KIM-1. It was observed a decrease on reactive oxygen species production and mitochondrial depolarization, with antioxidant regulation by increased GSH and decreased lipid peroxidation. It was also demonstrated that bisabolol treatment can inhibit NOX4. Finally, SEM images showed that bisabolol reduced I/R-induced cell damage. Bisabolol treatment protects HK2 cells against oxidative damage occasioned by I/R. This effect is related to inhibition of apoptosis, decrease on KIM-1 release, reactive oxygen species accumulation and mitochondrial dysfunction. Bisabolol inhibited NOX4 activity in the tubular cells, impairing reactive oxygen species synthesis. Image 1 [ABSTRACT FROM AUTHOR]

Background: On account of emergence of multi- and extensively drug-resistant Mycobacterium tuberculosis (Mtb) strains, combinations of drugs with natural compounds were tested to search for antibiotic activity enhancers. In this work we studied terpenes (α-pinene, bisabolol, βelemene, (R)-limonene, (S)-limonene, myrcene, sabinene), which are the main constituents of essential oil obtained from Mutellina purpurea L., a plant with described antitubercular activity, to investigate their interactions with antibiotics against reference Mtb strains and multidrug-resistant clinical isolates. Methods: The serial dilution method was used to evaluate the minimal inhibitory concentration (MIC) of tested compounds, while the fractional inhibitory concentration index (FICI) was calculated for characterization of interactions. Moreover, IC50 values of tested compounds were determined using monkey kidney epithelial cell line (GMK). Results: The combinations of all studied terpenes with ethambutol or rifampicin resulted in a synergistic interaction. Bisabolol and (R)-limonene decreased the MIC for rifampicin at least two-fold for all tested strains, however no synergistic action was observed against virulent strains. The tested terpenes showed slight (bisabolol) or no cytotoxic effect against normal eukaryotic cells in vitro. Conclusions: The obtained enhanced activity (FICI < 0.5) of ethambutol and rifampicin against H37Ra strain under the influence of the studied terpenes may be correlated to the capability of essential oil constituents to modify bacterial resistance mechanisms in general. The observed differences in avirulent and virulent bacteria susceptibility to terpenes tested separately and in combinations with antibiotics can be correlated with the differences in the cell wall structure between H37Ra mutant and all virulent strains. [ABSTRACT FROM AUTHOR]

Background: Today, the sun protection factor (SPF) value of sunscreen products is determined in vivo with a standardized protocol (EN ISO 24444: 2010), and the measured SPF biological end point is the visible skin erythema. However, many of the sunscreen products currently available on the market have antiphlogistic ingredients, which may potentially result in an overestimated SPF of the sunscreen. Aims: To investigate the potential influence of the antiphlogistic ingredients panthenol and bisabolol in sunscreens on the determined SPF value in vivo. Methods: Formulations with different concentrations of the antiphlogistic ingredients bisabolol or panthenol were tested. As a reference, a base formulation (vehicle) without antiphlogistic ingredients was used. First, the SPF of the sunscreen formulas with and without antiphlogistic ingredients was analyzed in vitro. To investigate whether the antiphlogistic ingredient may suppress the inflammatory response to ultraviolet (UV) irradiation, the SPF was determined in vivo. Finally, selected formulations were also analyzed in an erythema model for testing formulations on UV-induced inflammation. Results: It could be confirmed that no differences between the formula with and that without the active antiphlogistic ingredients bisabolol or panthenol exist when measured in vitro. However, there was also no statistically significant difference in the erythemal response between the vehicle (without an antiphlogistic active ingredient) and the test formulations with different concentrations of the antiphlogistic active ingredients in the in vivo determination of the SPF. Evidence of anti-inflammatory activity of the sunscreen antiphlogistics bisabolol and panthenol was also not apparent in the UV model over a time course of 48 h. Conlusion: The antiphlogistic ingredients panthenol and bisabolol incorporated in the tested sunscreen formula do not interfere with erythema reddening and thus do not affect the SPF value in vivo. [ABSTRACT FROM AUTHOR]

Tick-borne diseases raise serious health concerns for both humans and animals. Tick control and disease prevention largely depend on synthetic acaricides and repellents, often incriminated for high toxicity. To find alternative, safe, and efficient agents against ticks, research on plant-based volatile terpenes constitutes a promising direction. This study aimed to separate and identify hemp flower compounds with repellent properties against Hyalomma marginatum (Acari: Ixodidae). Produced by supercritical CO 2 extraction under different pressure (100–110 bar) and temperature (40–60 °C) conditions, the hemp extracts were tested in a moving object bioassay. The extract with the highest repellent power was further subjected to batch liquid-liquid chromatography (LLC). The biphasic solvent system (n -heptane/methanol/acetonitrile 10/5/10, v/v/v) for separating the major hemp terpenes was selected by combining the COSMO-RS-based distribution coefficient screening with experimental validation. Bisabolol (>99%), caryophyllene oxide (>98%), and caryophyllene/humulene (3.5/1, w/w, >95% purity) were thus isolated and assessed in the H. marginatum bioassay. The activity of bisabolol (20% w/w in hexane) was comparable to the synthetic repellent DEET at the same concentration. For the large-scale purification of bisabolol, trapping multiple dual mode, a semi-continuous flow-reversal LLC operating mode, was proposed and evaluated. Bisabolol was obtained with a solvent consumption 2.6-times lower and productivity 2.7-times higher than the batch process. In conclusion, using a multi-methodological computer-aided approach, bisabolol was efficiently identified and isolated as a good tick repellent agent from hemp flowers. • Terpene-rich hemp flower extracts were obtained with supercritical CO2 technology. • The Hyalomma marginatum repellency was evaluated in a moving object bioassay. • Hemp terpenes were separated by liquid-liquid chromatography (LLC). • Bisabolol was isolated and identified as the most potent tick repellent compound. • The large-scale purification of bisabolol was achieved by trapping multiple dual mode LLC. [ABSTRACT FROM AUTHOR]

Bisabolol (α-(−)-bisabolol) is a sesquiterpene which is a part of the essential oil of a variety of plants, but its common source is German chamomile. Several bioactivities including anti-inflammatory, anti-nociceptive, and anti-tumor effects were attributed to bisabolol. However, the neuropharmacological properties of bisabolol have not yet been reported. The present study evaluated behavioral effects of bisabolol using elevated plus maze (EPM), open field test (OFT), and rotarod test. Moreover, this study also examined whether the 5-HT and GABA-benzodiazepine receptor systems are involved in the anxiolytic-like effects of bisabolol. After acute intraperitoneal treatment with bisabolol at the doses of 0.5, 1, 2, 5, and 10 mg/kg, OFT, EPM, and rotarod were utilized for investigating behavioral effects. Flumazenil, a benzodiazepine receptor antagonist, and WAY-100635, a 5-HT receptor antagonist, were used to determine the action mechanism in the EPM. Bisabolol especially at the dose of 1 mg/kg was effective in increasing the total number of entries and time spent in the open arms of EPM while number of rearing and grooming in OFT was decreased in comparison to the control. In the rotarod, permanence time was decreased in the mice treated with the high doses of bisabolol. Pretreatment with flumazenil, but not WAY-100635, was able to reverse the effect of bisabolol 1 mg/kg in the EPM, indicating that the anxiolytic-like activity of bisabolol occurs via the GABAergic but not serotonergic transmission. The present study supports the idea that bisabolol may mediate its anxiolytic-like and sedative mechanisms involving GABA receptors. [ABSTRACT FROM AUTHOR]

Background: Chamomile (Matricaria recutita L.) has a long history of use in herbal medicine with various applications, and the flower heads contain numerous secondary metabolites which are medicinally active. In the major crop plants, next generation sequencing (NGS) approaches are intensely applied to exploit genetic resources, to develop genomic resources and to enhance breeding. Here, genotyping-by-sequencing (GBS) has been used in the non-model medicinal plant chamomile to evaluate the genetic structure of the cultivated varieties/populations, and to perform genome wide association study (GWAS) focusing on genes with large effect on flowering time and the medicinally important alpha-bisabolol content. Results: GBS analysis allowed the identification of 6495 high-quality SNP-markers in our panel of 91 M. recutita plants from 33 origins (2-4 genotypes each) and 4 M. discoidea plants as outgroup, grown in the greenhouse in Gatersleben, Germany. M. recutita proved to be clearly distinct from the outgroup, as was demonstrated by different cluster and principal coordinate analyses using the SNP-markers. Chamomile genotypes from the same origin were mostly genetically similar. Model-based cluster analysis revealed one large group of tetraploid genotypes with low genetic differentiation including 39 plants from 14 origins. Tetraploids tended to display lower genetic diversity than diploids, probably reflecting their origin by artificial polyploidisation from only a limited set of genetic backgrounds. Analyses of flowering time demonstrated that diploids generally flowered earlier than tetraploids, and the analysis of alpha-bisabolol identified several tetraploid genotypes with a high content. GWAS identified highly significant (P < 0.01) SNPs for flowering time (9) and alpha-bisabolol (71). One sequence harbouring SNPs associated with flowering time was described to play a role in self-pollination in Arabidopsis thaliana, whereas four sequences harbouring SNPs associated with alpha-bisabolol were identified to be involved in plant biotic and abiotic stress response in various plants species. Conclusions: The first genomic resource for future applications to enhance breeding in chamomile was created, andanalyses of diversity will facilitate the exploitation of these genetic resources. The GWAS data pave the way for future research towards the genetics underlying important traits in chamomile, the identification of marker-trait associations, and development of reliable markers for practical breeding [ABSTRACT FROM AUTHOR]

The aim of the current investigation was to design, synthesize and demonstrate the anticancer and apoptotic activity of trifluoromethyl-phenyl-triazolyl derivative of beta-bisabolol (TTB) in ME-180 human cervical cancer cells. MTT and clonogenic assays were used to evaluate the cell viability and colony formation tendencies of the cells respectively. Phase contrast and fluorescence microscopic investigations were used to evaluate the effect of TTB on cellular morphology and apoptosis. Flow cytometric analysis using fluorescent CM-DCFH2-DA were used to study the effect of TTB on reactive oxygen species (ROS) formation. The results revealed that TTB significantly inhibited the proliferation of ME-180 human cervical cancer cells in a time-dependent as well as dose-dependent manner. TTB has the capacity to inhibit both anchorage dependent as well as anchorage independent growth of ME-180 cervical cancer cells. TTB-treated cells revealed chromatin condensation, fragmented nuclei and nuclear shrinkage. A 3-fold increase of ROS production was seen after 72 ?M TTB treatment. Video Clip of Methodology: Phase contrast microscopic study: 2 min Full Screen Alternate

Background: On account of emergence of multi- and extensively drug-resistant Mycobacterium tuberculosis (Mtb) strains, combinations of drugs with natural compounds were tested to search for antibiotic activity enhancers. In this work we studied terpenes (α-pinene, bisabolol, β-elemene, (R)-limonene, (S)-limonene, myrcene, sabinene), which are the main constituents of essential oil obtained from Mutellina purpurea L., a plant with described antitubercular activity, to investigate their interactions with antibiotics against reference Mtb strains and multidrug-resistant clinical isolates. Methods: The serial dilution method was used to evaluate the minimal inhibitory concentration (MIC) of tested compounds, while the fractional inhibitory concentration index (FICI) was calculated for characterization of interactions. Moreover, IC50 values of tested compounds were determined using monkey kidney epithelial cell line (GMK). Results: The combinations of all studied terpenes with ethambutol or rifampicin resulted in a synergistic interaction. Bisabolol and (R)-limonene decreased the MIC for rifampicin at least two-fold for all tested strains, however no synergistic action was observed against virulent strains. The tested terpenes showed slight (bisabolol) or no cytotoxic effect against normal eukaryotic cells in vitro. Conclusions: The obtained enhanced activity (FICI < 0.5) of ethambutol and rifampicin against H37Ra strain under the influence of the studied terpenes may be correlated to the capability of essential oil constituents to modify bacterial resistance mechanisms in general. The observed differences in avirulent and virulent bacteria susceptibility to terpenes tested separately and in combinations with antibiotics can be correlated with the differences in the cell wall structure between H37Ra mutant and all virulent strains.