The skin acts as a protective barrier, guarding the body against microorganisms, chemicals, and s... more The skin acts as a protective barrier, guarding the body against microorganisms, chemicals, and several environmental factors. Accordingly, this all-important organ must be kept healthy to maintain its optimal functionality. One approach to maintain skin health is the application of multifunction bioactive sunscreens containing antioxidant molecule(s). Rosmarinic acid (RA), a phenolic compound, is known for its antioxidant activity. Herein, the safety and efficacy of a multifunction prototype sunscreen were investigated, aiming to probe putative synergies of this polyphenol with two known and widely used UV filters (bemotrizinol and octyl p-methoxycinnamate). Samples protected the DNA fragmentation compared to UV control, by the comet assay, and showed good skin compatibility in subjects. Formulations F1 and F3 were able to increase skin hydration, and, possibly, the RA interfered with this attribute. An increase in transepidermal water loss was observed for formulations F1, F2 and ...
Skin health is not only significantly affected by ageing, but also by other lifestyle-related fac... more Skin health is not only significantly affected by ageing, but also by other lifestyle-related factors, such as sun exposure, exercise and eating habits, smoking or alcohol intake. It is known that the cutaneous tissue can exhibit visible signs of senescence, in the form of, for example, dull complexion, loss of firmness, or changes in pigmentation. Consumers attempt to improve skin health and appearance not only by cosmetic products, but also with the consumption of food supplements. Recently, there has been an increase in the amount of food supplements with claims that are related to skin and hair health. Nevertheless, the literature is still scarce in evidence of the efficacy of this type of products. Considering this scenario, we aim in this review to assemble studies and methodologies that are directed at the substantiation of the cutaneous health claims of food supplements. For example, we reviewed those that were indicative of antioxidant properties, improvement in pigmentatio...
The use of functional bioactive ingredients and the property of water resistance are differential... more The use of functional bioactive ingredients and the property of water resistance are differentials in the choice of more effective and safer sunscreens. Water-resistance tests are expensive, time-consuming, and usually performed on subjects that expose them to irradiation and long immersion times. Thus, the study of in vitro water resistance using different film/ barrier-forming agents is relevant for obtaining sunscreen resistant to rinsing. We aimed to evaluate the water resistance of a rutin-based bioactive sunscreen containing distinct film/barrier-forming agents by an in vitro method. The in vitro water resistance assessment (% WRR) was carried out in a water bath. In vitro sun protection factor (SPF), critical A, (nm), UVA/UVB ratio, and UVA protection factor (UVA-PF(0)) were evaluated before and after rinsing using a diffuse reflectance spectrophotometer with integration sphere. The formulation with dimethicone showed higher values of SPF after rinsing and achieved the requir...
Several topical products have been developed to avoid the harmful effects from ultraviolet (UV) r... more Several topical products have been developed to avoid the harmful effects from ultraviolet (UV) radiation, such as sunscreens. Research for actives from natural sources is increasing due to the fact that chemical filters could induce adverse events. The microalgae Botryococcus braunii has potential interest in cosmetic applications. Specialized literature reported that B. braunii aqueous extract induced a reduction in skin dehydration and collagen production and promoted antioxidant activity. This research aimed to produce B. braunii biomass and to investigate its contribution regarding photoprotection. Formulations containing B. braunii dry biomass, with or without UV filters into vehicles composed of an emulsifying polymer or a self-emulsifying base, were evaluated in vitro by means of photoprotective activity and photostability. B. braunii dry biomass did not provide adequate photoprotection efficacy; however, it was observed that the self-emulsifying base promoted better sun pro...
Background: The carbamide peroxide is the most commonly active ingredient used for home dental wh... more Background: The carbamide peroxide is the most commonly active ingredient used for home dental whitening products, its quantification in pharmaceutical products is of extreme importance due to the relation with the products potency and the previously related low carbamide peroxide stability. Once, there is only one official carbamide peroxide determination based on iodometric titration, this method is time-consuming and generates a lot of residues. The aim of this study was to carry out development and validation of a simple and fast ultraviolet spectrophotometer assay to quantify an innovative dental whitening gel. Methods: The proposed method was validated according international conference on harmonization guideline. Procedure is based on the iodide/iodine redox chemistry; iodine released through the action of hydrogen peroxide of carbamide peroxide with ultraviolet detection at 350 nm. Results: The procedure was linear in the concentration range of 1.0-4.0 µg/mL, specific to the...
Journal of Pharmacology and Experimental Therapeutics, 2005
The mixture of the two pentacyclic triterpenes alpha-amyrin and beta-amyrin, isolated from the re... more The mixture of the two pentacyclic triterpenes alpha-amyrin and beta-amyrin, isolated from the resin of Protium kleinii and given by intraperitoneal (i.p.) or oral (p.o.) routes, caused dose-related and significant antinociception against the visceral pain in mice produced by i.p. injection of acetic acid. Moreover, i.p., p.o., intracerebroventricular (i.c.v.), or intrathecal (i.t.) administration of alpha,beta-amyrin inhibited both neurogenic and inflammatory phases of the overt nociception caused by intraplantar (i.pl.) injection of formalin. Likewise, alpha,beta-amyrin given by i.p., p.o., i.t., or i.c.v. routes inhibits the neurogenic nociception induced by capsaicin. Moreover, i.p. treatment with alpha,beta-amyrin was able to reduce the nociception produced by 8-bromo-cAMP (8-Br-cAMP) and by 12-O-tetradecanoylphorbol-13-acetate (TPA) or the hyperalgesia caused by glutamate. On the other hand, in contrast to morphine, alpha,beta-amyrin failed to cause analgesia in thermal models of pain. The antinociception caused by the mixture of compounds seems to involve mechanisms independent of opioid, alpha-adrenergic, serotoninergic, and nitrergic system mediation, since it was not affected by naloxone, prazosin, yohimbine, DL-p-chlorophenylalanine methyl ester, or L-arginine. Interestingly, the i.p. administration of alpha,beta-amyrin reduced the mechanical hyperalgesia produced by i.pl. injection of carrageenan, capsaicin, bradykinin, substance P, prostaglandin E2, 8-Br-cAMP, and TPA in rats. However, the mixture of compounds failed to alter the binding sites of [3H]bradykinin, [3H]resiniferatoxin, or [3H]glutamate in vitro. It is concluded that the mixture of triterpene alpha-amyrin and beta-amyrin produced consistent peripheral, spinal, and supraspinal antinociception in rodents, especially when assessed in inflammatory models of pain. The mechanisms involved in their action are not completely understood but seem to involve the inhibition of protein kinase A- and protein kinase C-sensitive pathways.
This study investigates the antinociception caused by i.p. and p.o. administration of ether fract... more This study investigates the antinociception caused by i.p. and p.o. administration of ether fraction and the triterpene identified as urs-12-ene-3beta-16beta-diol, known as Brein, isolated from Protium kleinii in several models of nociception in mice. The systemic administration of ether fraction (0.3 to 10 mg/kg, i.p. or 3 to 60 mg/kg, p.o.) caused a dose-related antinociception when assessed against acetic acid-induced writhing, with mean ID50 values of 1.2 and 16.4 mg/kg, respectively. The ether fraction (5 to 60 mg/kg, i.p. or 30 to 300 mg/kg, p.o.) also produced dose-related inhibition of both phases of formalin induced licking. The mean ID50s values for the early phase were > 60.0 and 62.1 mg/kg, while for the late phase they were 15.4 and 60.0 mg/kg, respectively, given by i.p. and p.o. routes. The ether fraction (3 to 30 mg/kg, i.p. or 10 to 100 mg/kg, p.o.) produced significant inhibition of the neurogenic nociception caused by topical injection of capsaicin, with mean ID50 values of 6.2 and 16.0 mg/kg, respectively. Given orally (1 to 30 mg/kg) the ether fraction produced graded and pronounced inhibition of glutamate-induced hyperalgesia in mice with a mean ID50 value of 15.2 mg/kg. In contrast, the ether fraction failed to produce antinociception when assessed in the thermal model of pain, the tail flick and hot plate tests. The antinociception caused by the ether fraction, in contrast to that of morphine, was not reversed by naloxone when assessed in the formalin-induced licking. The ether fraction did not affect motor coordination or the core body temperature in mices. The triterpene Brein isolated from P. kleinii, given by i.p. route (10 to 100 mg/kg) produced dose-related inhibition of both phases of formalin induced-licking, with mean ID50s values of 15.3 and 20.6 for the early and the late phases, respectively. These data show that the active principle(s) present in the ether fraction from the resin of P. kleinii elicited pronounced antinociception when assessed by i.p. or p.o routes, against both inflammatory and neurogenic nociception. Such effects seem, at least in part, to be related to the presence of the triterpene Brein in the extract. The mechanisms responsible for the antinociceptive action are at this moment not completely understood, but the involvement of the opioid pathway seems unlikely.
Protium kleinii (Burseraceae), a native Brazilian medicinal plant is claimed to be useful to trea... more Protium kleinii (Burseraceae), a native Brazilian medicinal plant is claimed to be useful to treat some inflammatory states. Now we reported that topical application of either the ether extract or the main active constituent from P. kleinii the pentacyclic triterpene alpha-amyrin, all caused a dose-related inhibition of both ear oedema (ID50 values are 0.55 and 0.31 mg/ear, respectively) and influx of polymorphonuclear cells (ID50 values are 0.72 and 0.45 mg/ear, respectively) in response to topical application of 12-O-tetradecanoylphorbol-acetate (TPA) in the of mice ear. In terms of the efficacy, the maximal obtained inhibition for both ear oedema and neutrophil influx was very similar to that produced by the topical application of the steroidal antiinflammatory drug dexamethasone (DE; with inhibition of 70+/-5%, 66+/-3%, and 87+/-4% for oedema and 83+/-6%, 73+/-5%, and 91+/-3% for neutrophil influx, for the ether extract, alpha-amyrin, and dexamethasone, respectively). Likewise, both the ether extract and alpha-amyrin given topically dose-dependently prevented the increase of the proinflammatory cytokine interleukin-1beta levels in response to topical application of TPA. The calculated mean ID50 values are 1.81 and 0.53 mg/ear, respectively. Again, the efficacy of the extract and alpha-amyrin was very similar to that produced by dexamethasone (63+/-6%, 61+/-5%, and 74+/-5%, respectively). In marked contrast to phenidone, a lipo and cyclooxygenase inhibitor, neither the ether extract nor the alpha-amyrin inhibited arachidonic acid-mediated ear oedema in mice. Collectively, these results indicate that the active constituents present in the ether extract of P. kleinii including the pentacyclic triterpene alpha-amyrin are good candidates to develop a skin permeable antiinflammatory drug.
The skin acts as a protective barrier, guarding the body against microorganisms, chemicals, and s... more The skin acts as a protective barrier, guarding the body against microorganisms, chemicals, and several environmental factors. Accordingly, this all-important organ must be kept healthy to maintain its optimal functionality. One approach to maintain skin health is the application of multifunction bioactive sunscreens containing antioxidant molecule(s). Rosmarinic acid (RA), a phenolic compound, is known for its antioxidant activity. Herein, the safety and efficacy of a multifunction prototype sunscreen were investigated, aiming to probe putative synergies of this polyphenol with two known and widely used UV filters (bemotrizinol and octyl p-methoxycinnamate). Samples protected the DNA fragmentation compared to UV control, by the comet assay, and showed good skin compatibility in subjects. Formulations F1 and F3 were able to increase skin hydration, and, possibly, the RA interfered with this attribute. An increase in transepidermal water loss was observed for formulations F1, F2 and ...
Skin health is not only significantly affected by ageing, but also by other lifestyle-related fac... more Skin health is not only significantly affected by ageing, but also by other lifestyle-related factors, such as sun exposure, exercise and eating habits, smoking or alcohol intake. It is known that the cutaneous tissue can exhibit visible signs of senescence, in the form of, for example, dull complexion, loss of firmness, or changes in pigmentation. Consumers attempt to improve skin health and appearance not only by cosmetic products, but also with the consumption of food supplements. Recently, there has been an increase in the amount of food supplements with claims that are related to skin and hair health. Nevertheless, the literature is still scarce in evidence of the efficacy of this type of products. Considering this scenario, we aim in this review to assemble studies and methodologies that are directed at the substantiation of the cutaneous health claims of food supplements. For example, we reviewed those that were indicative of antioxidant properties, improvement in pigmentatio...
The use of functional bioactive ingredients and the property of water resistance are differential... more The use of functional bioactive ingredients and the property of water resistance are differentials in the choice of more effective and safer sunscreens. Water-resistance tests are expensive, time-consuming, and usually performed on subjects that expose them to irradiation and long immersion times. Thus, the study of in vitro water resistance using different film/ barrier-forming agents is relevant for obtaining sunscreen resistant to rinsing. We aimed to evaluate the water resistance of a rutin-based bioactive sunscreen containing distinct film/barrier-forming agents by an in vitro method. The in vitro water resistance assessment (% WRR) was carried out in a water bath. In vitro sun protection factor (SPF), critical A, (nm), UVA/UVB ratio, and UVA protection factor (UVA-PF(0)) were evaluated before and after rinsing using a diffuse reflectance spectrophotometer with integration sphere. The formulation with dimethicone showed higher values of SPF after rinsing and achieved the requir...
Several topical products have been developed to avoid the harmful effects from ultraviolet (UV) r... more Several topical products have been developed to avoid the harmful effects from ultraviolet (UV) radiation, such as sunscreens. Research for actives from natural sources is increasing due to the fact that chemical filters could induce adverse events. The microalgae Botryococcus braunii has potential interest in cosmetic applications. Specialized literature reported that B. braunii aqueous extract induced a reduction in skin dehydration and collagen production and promoted antioxidant activity. This research aimed to produce B. braunii biomass and to investigate its contribution regarding photoprotection. Formulations containing B. braunii dry biomass, with or without UV filters into vehicles composed of an emulsifying polymer or a self-emulsifying base, were evaluated in vitro by means of photoprotective activity and photostability. B. braunii dry biomass did not provide adequate photoprotection efficacy; however, it was observed that the self-emulsifying base promoted better sun pro...
Background: The carbamide peroxide is the most commonly active ingredient used for home dental wh... more Background: The carbamide peroxide is the most commonly active ingredient used for home dental whitening products, its quantification in pharmaceutical products is of extreme importance due to the relation with the products potency and the previously related low carbamide peroxide stability. Once, there is only one official carbamide peroxide determination based on iodometric titration, this method is time-consuming and generates a lot of residues. The aim of this study was to carry out development and validation of a simple and fast ultraviolet spectrophotometer assay to quantify an innovative dental whitening gel. Methods: The proposed method was validated according international conference on harmonization guideline. Procedure is based on the iodide/iodine redox chemistry; iodine released through the action of hydrogen peroxide of carbamide peroxide with ultraviolet detection at 350 nm. Results: The procedure was linear in the concentration range of 1.0-4.0 µg/mL, specific to the...
Journal of Pharmacology and Experimental Therapeutics, 2005
The mixture of the two pentacyclic triterpenes alpha-amyrin and beta-amyrin, isolated from the re... more The mixture of the two pentacyclic triterpenes alpha-amyrin and beta-amyrin, isolated from the resin of Protium kleinii and given by intraperitoneal (i.p.) or oral (p.o.) routes, caused dose-related and significant antinociception against the visceral pain in mice produced by i.p. injection of acetic acid. Moreover, i.p., p.o., intracerebroventricular (i.c.v.), or intrathecal (i.t.) administration of alpha,beta-amyrin inhibited both neurogenic and inflammatory phases of the overt nociception caused by intraplantar (i.pl.) injection of formalin. Likewise, alpha,beta-amyrin given by i.p., p.o., i.t., or i.c.v. routes inhibits the neurogenic nociception induced by capsaicin. Moreover, i.p. treatment with alpha,beta-amyrin was able to reduce the nociception produced by 8-bromo-cAMP (8-Br-cAMP) and by 12-O-tetradecanoylphorbol-13-acetate (TPA) or the hyperalgesia caused by glutamate. On the other hand, in contrast to morphine, alpha,beta-amyrin failed to cause analgesia in thermal models of pain. The antinociception caused by the mixture of compounds seems to involve mechanisms independent of opioid, alpha-adrenergic, serotoninergic, and nitrergic system mediation, since it was not affected by naloxone, prazosin, yohimbine, DL-p-chlorophenylalanine methyl ester, or L-arginine. Interestingly, the i.p. administration of alpha,beta-amyrin reduced the mechanical hyperalgesia produced by i.pl. injection of carrageenan, capsaicin, bradykinin, substance P, prostaglandin E2, 8-Br-cAMP, and TPA in rats. However, the mixture of compounds failed to alter the binding sites of [3H]bradykinin, [3H]resiniferatoxin, or [3H]glutamate in vitro. It is concluded that the mixture of triterpene alpha-amyrin and beta-amyrin produced consistent peripheral, spinal, and supraspinal antinociception in rodents, especially when assessed in inflammatory models of pain. The mechanisms involved in their action are not completely understood but seem to involve the inhibition of protein kinase A- and protein kinase C-sensitive pathways.
This study investigates the antinociception caused by i.p. and p.o. administration of ether fract... more This study investigates the antinociception caused by i.p. and p.o. administration of ether fraction and the triterpene identified as urs-12-ene-3beta-16beta-diol, known as Brein, isolated from Protium kleinii in several models of nociception in mice. The systemic administration of ether fraction (0.3 to 10 mg/kg, i.p. or 3 to 60 mg/kg, p.o.) caused a dose-related antinociception when assessed against acetic acid-induced writhing, with mean ID50 values of 1.2 and 16.4 mg/kg, respectively. The ether fraction (5 to 60 mg/kg, i.p. or 30 to 300 mg/kg, p.o.) also produced dose-related inhibition of both phases of formalin induced licking. The mean ID50s values for the early phase were > 60.0 and 62.1 mg/kg, while for the late phase they were 15.4 and 60.0 mg/kg, respectively, given by i.p. and p.o. routes. The ether fraction (3 to 30 mg/kg, i.p. or 10 to 100 mg/kg, p.o.) produced significant inhibition of the neurogenic nociception caused by topical injection of capsaicin, with mean ID50 values of 6.2 and 16.0 mg/kg, respectively. Given orally (1 to 30 mg/kg) the ether fraction produced graded and pronounced inhibition of glutamate-induced hyperalgesia in mice with a mean ID50 value of 15.2 mg/kg. In contrast, the ether fraction failed to produce antinociception when assessed in the thermal model of pain, the tail flick and hot plate tests. The antinociception caused by the ether fraction, in contrast to that of morphine, was not reversed by naloxone when assessed in the formalin-induced licking. The ether fraction did not affect motor coordination or the core body temperature in mices. The triterpene Brein isolated from P. kleinii, given by i.p. route (10 to 100 mg/kg) produced dose-related inhibition of both phases of formalin induced-licking, with mean ID50s values of 15.3 and 20.6 for the early and the late phases, respectively. These data show that the active principle(s) present in the ether fraction from the resin of P. kleinii elicited pronounced antinociception when assessed by i.p. or p.o routes, against both inflammatory and neurogenic nociception. Such effects seem, at least in part, to be related to the presence of the triterpene Brein in the extract. The mechanisms responsible for the antinociceptive action are at this moment not completely understood, but the involvement of the opioid pathway seems unlikely.
Protium kleinii (Burseraceae), a native Brazilian medicinal plant is claimed to be useful to trea... more Protium kleinii (Burseraceae), a native Brazilian medicinal plant is claimed to be useful to treat some inflammatory states. Now we reported that topical application of either the ether extract or the main active constituent from P. kleinii the pentacyclic triterpene alpha-amyrin, all caused a dose-related inhibition of both ear oedema (ID50 values are 0.55 and 0.31 mg/ear, respectively) and influx of polymorphonuclear cells (ID50 values are 0.72 and 0.45 mg/ear, respectively) in response to topical application of 12-O-tetradecanoylphorbol-acetate (TPA) in the of mice ear. In terms of the efficacy, the maximal obtained inhibition for both ear oedema and neutrophil influx was very similar to that produced by the topical application of the steroidal antiinflammatory drug dexamethasone (DE; with inhibition of 70+/-5%, 66+/-3%, and 87+/-4% for oedema and 83+/-6%, 73+/-5%, and 91+/-3% for neutrophil influx, for the ether extract, alpha-amyrin, and dexamethasone, respectively). Likewise, both the ether extract and alpha-amyrin given topically dose-dependently prevented the increase of the proinflammatory cytokine interleukin-1beta levels in response to topical application of TPA. The calculated mean ID50 values are 1.81 and 0.53 mg/ear, respectively. Again, the efficacy of the extract and alpha-amyrin was very similar to that produced by dexamethasone (63+/-6%, 61+/-5%, and 74+/-5%, respectively). In marked contrast to phenidone, a lipo and cyclooxygenase inhibitor, neither the ether extract nor the alpha-amyrin inhibited arachidonic acid-mediated ear oedema in mice. Collectively, these results indicate that the active constituents present in the ether extract of P. kleinii including the pentacyclic triterpene alpha-amyrin are good candidates to develop a skin permeable antiinflammatory drug.
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