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1.
Int J Mol Sci ; 25(9)2024 Apr 27.
Article in English | MEDLINE | ID: mdl-38731983

ABSTRACT

Acne vulgaris is a prevalent skin disorder affecting many young individuals, marked by keratinization, inflammation, seborrhea, and colonization by Cutibacterium acnes (C. acnes). Ellagitannins, known for their antibacterial and anti-inflammatory properties, have not been widely studied for their anti-acne effects. Chestnut (Castanea sativa Mill., C. sativa), a rich ellagitannin source, including castalagin whose acne-related bioactivity was previously unexplored, was investigated in this study. The research assessed the effect of C. sativa leaf extract and castalagin on human keratinocytes (HaCaT) infected with C. acnes, finding that both inhibited IL-8 and IL-6 release at concentrations below 25 µg/mL. The action mechanism was linked to NF-κB inhibition, without AP-1 involvement. Furthermore, the extract displayed anti-biofilm properties and reduced CK-10 expression, indicating a potential role in mitigating inflammation, bacterial colonization, and keratosis. Castalagin's bioactivity mirrored the extract's effects, notably in IL-8 inhibition, NF-κB inhibition, and biofilm formation at low µM levels. Other polyphenols, such as flavonol glycosides identified via LC-MS, might also contribute to the extract's biological activities. This study is the first to explore ellagitannins' potential in treating acne, offering insights for developing chestnut-based anti-acne treatments pending future in vivo studies.


Subject(s)
Acne Vulgaris , Fagaceae , Hydrolyzable Tannins , Plant Extracts , Plant Leaves , Humans , Hydrolyzable Tannins/pharmacology , Fagaceae/chemistry , Acne Vulgaris/microbiology , Acne Vulgaris/drug therapy , Plant Extracts/pharmacology , Plant Extracts/chemistry , Plant Leaves/chemistry , Keratinocytes/drug effects , Keratinocytes/metabolism , NF-kappa B/metabolism , HaCaT Cells , Propionibacterium acnes/drug effects , Anti-Bacterial Agents/pharmacology , Biofilms/drug effects , Interleukin-8/metabolism
2.
ACS Appl Mater Interfaces ; 16(17): 21595-21609, 2024 May 01.
Article in English | MEDLINE | ID: mdl-38635857

ABSTRACT

A microneedle transdermal drug delivery system simultaneously avoids systemic toxicity of oral administration and low efficiency of traditional transdermal administration, which is of great significance for acne vulgaris therapy. Herein, eugenol-loaded hyaluronic acid-based dissolving microneedles (E@P-EO-HA MNs) with antibacterial and anti-inflammatory activities are developed for acne vulgaris therapy via eugenol transdermal delivery integrated with photothermal therapy. E@P-EO-HA MNs are pyramid-shaped with a sharp tip and a hollow cavity structure, which possess sufficient mechanical strength to penetrate the stratum corneum of the skin and achieve transdermal delivery, in addition to excellent in vivo biocompatibility. Significantly, E@P-EO-HA MNs show effective photothermal therapy to destroy sebaceous glands and achieve antibacterial activity against deep-seated Propionibacterium acnes (P. acnes) under near-infrared-light irradiation. Moreover, cavity-loaded eugenol is released from rapidly dissolved microneedle bodies to play a sustained antibacterial and anti-inflammatory therapy on the P. acnes infectious wound. E@P-EO-HA MNs based on a synergistic therapeutic strategy combining photothermal therapy and eugenol transdermal administration can significantly alleviate inflammatory response and ultimately facilitate the repair of acne vulgaris. Overall, E@P-EO-HA MNs are expected to be clinically applied as a functional minimally invasive transdermal delivery strategy for superficial skin diseases therapy in skin tissue engineering.


Subject(s)
Acne Vulgaris , Administration, Cutaneous , Anti-Bacterial Agents , Eugenol , Hyaluronic Acid , Needles , Photothermal Therapy , Propionibacterium acnes , Acne Vulgaris/therapy , Acne Vulgaris/drug therapy , Eugenol/chemistry , Eugenol/pharmacology , Hyaluronic Acid/chemistry , Animals , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Propionibacterium acnes/drug effects , Mice , Drug Delivery Systems , Humans , Skin
3.
J Cosmet Dermatol ; 23(6): 2156-2169, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38406887

ABSTRACT

BACKGROUND: Acne is a common skin issue that typically occurs during adolescence. It causes long-lasting redness and swelling in the skin. An alternative approach to treating acne could involve using a cosmetic facial mask containing herbal ingredients such as Curcumin and Rosa Damascena extract for its antibacterial properties. AIMS: This study aims to create and try out a peel-off mask gel made from Curcumin and R. Damascena extract. This gel is intended to have the ability to kill bacteria such as Staphylococcus aureus, Escherichia coli, and Propionibacterium acnes and remove dead cells from the skin surface. METHODS: The peel-off mask was made using polyvinyl alcohol (PVA) in 8% and 10% as solidifier. The evaluation of peel-off masks comprises the examination of physiochemical and mechanical aspects. Furthermore, their longevity, effectiveness, and antibacterial properties are also considered. RESULTS: The white color, pleasant smell, and soft texture were the defining features of the peel-off gel mask. The changes in PVA affect the pH level, thickness, and how quickly the peel-off mask dries. The stability test found that the peel-off mask had no significant physical changes when exposed to freezing and thawing. However, there were some differences in color and separation when using the real-time method. A prepared peel-off mask containing 10% PVA and curcumin works best against P. acne. The amount of PVA in the formula affected the physical and chemical qualities, but it did not impact on the antibacterial abilities of the peel-off mask gel. The best formula that gives the best results uses 10% PVA + curcumin. CONCLUSIONS: Using the Curcumin and R. Damascena extract in the creation of the peel-off mask gel ensures its efficacy and safety for skin application.


Subject(s)
Acne Vulgaris , Anti-Bacterial Agents , Antioxidants , Curcumin , Plant Extracts , Rosa , Staphylococcus aureus , Curcumin/pharmacology , Curcumin/administration & dosage , Plant Extracts/pharmacology , Plant Extracts/administration & dosage , Plant Extracts/chemistry , Rosa/chemistry , Humans , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/administration & dosage , Antioxidants/pharmacology , Antioxidants/administration & dosage , Acne Vulgaris/drug therapy , Acne Vulgaris/microbiology , Staphylococcus aureus/drug effects , Propionibacterium acnes/drug effects , Polyvinyl Alcohol/chemistry , Escherichia coli/drug effects , Skin Cream/administration & dosage , Skin/drug effects , Skin/microbiology , Microbial Sensitivity Tests
4.
Nucleic Acids Res ; 51(6): 2915-2930, 2023 04 11.
Article in English | MEDLINE | ID: mdl-36864821

ABSTRACT

Acne vulgaris is a chronic disfiguring skin disease affecting ∼1 billion people worldwide, often having persistent negative effects on physical and mental health. The Gram-positive anaerobe, Cutibacterium acnes is implicated in acne pathogenesis and is, therefore, a main target for antibiotic-based acne therapy. We determined a 2.8-Šresolution structure of the 70S ribosome of Cutibacterium acnes by cryogenic electron microscopy and discovered that sarecycline, a narrow-spectrum antibiotic against Cutibacterium acnes, may inhibit two active sites of this bacterium's ribosome in contrast to the one site detected previously on the model ribosome of Thermus thermophilus. Apart from the canonical binding site at the mRNA decoding center, the second binding site for sarecycline exists at the nascent peptide exit tunnel, reminiscent of the macrolides class of antibiotics. The structure also revealed Cutibacterium acnes-specific features of the ribosomal RNA and proteins. Unlike the ribosome of the Gram-negative bacterium Escherichia coli, Cutibacterium acnes ribosome has two additional proteins, bS22 and bL37, which are also present in the ribosomes of Mycobacterium smegmatis and Mycobacterium tuberculosis. We show that bS22 and bL37 have antimicrobial properties and may be involved in maintaining the healthy homeostasis of the human skin microbiome.


Subject(s)
Acne Vulgaris , Anti-Bacterial Agents , Propionibacterium acnes , Ribosomes , Tetracyclines , Humans , Acne Vulgaris/drug therapy , Acne Vulgaris/microbiology , Anti-Bacterial Agents/chemistry , Propionibacterium acnes/drug effects , Protein Biosynthesis , Ribosomes/drug effects , Tetracyclines/pharmacology
5.
J Ethnopharmacol ; 287: 114935, 2022 Apr 06.
Article in English | MEDLINE | ID: mdl-34954264

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Thymus × citriodorus (Pers.) Schreb. is an interspecific hybrid between Thymus pulegioides and Thymus vulgaris, known for its pharmacological activities as diaphoretic, deodorant, antiseptic and disinfectant, the last mostly related with its antimicrobial activity. The folk use of other extracts, as hydrolates, have also been disseminated, as regulators of oily skin with anti-acne effect. AIM OF THE STUDY: We aimed to evaluate the anti-acne potential of two Thymus x citriodorus (TC) preparations, the essential oil (EO) and the hydrolate, to be used as active ingredients for skin applications. Specifically, we intend to validate their anti-acne potential by describing their activity on acne related bacteria, bacterial virulence, anti-oxidant and anti-inflammatory potential, and biocompatibility on inflammatory cells. Additionally, we aimed to report their ecotoxicity under the Globally Harmonized System of Classification and Labelling of Chemicals (GHS), thus focusing not only on the consumer, but also on environmental safety assessment. MATERIALS AND METHODS: Minimum inhibitory concentration (MIC) against C. acnes, S. aureus and S. epidermidis was evaluated. Minimum lethal concentration (MLC) was also determined. The effect on C. acnes biofilm formation and disruption was evaluated with crystal violet staining. Anti-inflammatory activity was investigated on LPS-stimulated mouse macrophages (RAW 264.7), by studying nitric oxide (NO) production (Griess reagent) and cellular biocompatibility through MTT assay. In-vitro NO and 2,2-Diphenyl-1-picrylhydrazyl (DPPH) scavenging potential were also evaluated. The ecotoxicity was evaluated using Daphnia magna acute toxicity assays. RESULTS: EO presented direct antimicrobial activity, with visual MICs ranging from 0.06% for S. epidermidis and C. acnes to 0.125% for S. aureus. MLCs were higher than the obtained MICs. Hydrolate revealed visual MIC only for C. acnes. TC essential oil was effective in preventing biofilm formation and disrupting preformed biofilms even at sub-inhibitory concentrations. Hydrolate showed a more modest anti-biofilm effect. Regarding anti-inflammatory activity, TC hydrolate has a higher cellular biocompatibility. Still, both plant preparations were able to inhibit at least 50% of NO production at non-cytotoxic concentrations. Both EO and hydrolate have poor anti-oxidant activities. Regarding the ecotoxicity, TC essential oil was classified under acute 3 category, while the hydrolate has proved to be nontoxic, in accordance to the GHS. CONCLUSIONS: These results support the anti-acne value of different TC preparations for different applications. TC hydrolate by presenting higher biocompatibility, anti-inflammatory potential and the ability to modulate C. acnes virulence, can be advantageous in a product for everyday application. On the other hand, EO by presenting a marked antimicrobial, anti-biofilm and anti-inflammatory activities, still with some cytotoxicity, may be better suited for application in acute flare-ups, for short treatment periods.


Subject(s)
Anti-Bacterial Agents/pharmacology , Anti-Inflammatory Agents/pharmacology , Plant Extracts/pharmacology , Thymus Plant/chemistry , Acne Vulgaris/drug therapy , Animals , Anti-Bacterial Agents/isolation & purification , Anti-Inflammatory Agents/isolation & purification , Biofilms/drug effects , Daphnia , Mice , Microbial Sensitivity Tests , Nitric Oxide/metabolism , Oils, Volatile/isolation & purification , Oils, Volatile/pharmacology , Plant Extracts/toxicity , Propionibacterium acnes/drug effects , RAW 264.7 Cells , Staphylococcus aureus/drug effects , Staphylococcus epidermidis/drug effects , Toxicity Tests, Acute
6.
ACS Appl Mater Interfaces ; 13(41): 48433-48448, 2021 Oct 20.
Article in English | MEDLINE | ID: mdl-34613687

ABSTRACT

The excessive colonization of Propionibacterium acnes (P. acnes) is responsible for the genesis of acne vulgaris, a common inflammatory disease of skin. However, the conventional anti-acne therapies are always limited by various side effects, drug resistance, and poor skin permeability. Microneedles (MNs) are emerging topical drug delivery systems capable of noninvasively breaking through the skin stratum corneum barrier to efficiently enhance the transdermal drug penetration. Herein, MNs loaded with intelligent pH-sensitive nanoplatforms were constructed for amplified chemo-photodynamic therapy against acne vulgaris, jointly exerting antimicrobial and anti-inflammatory effects. The photosensitizer indocyanine green (ICG) was loaded into the zeolitic imidazolate framework-8 (ZIF-8) to improve its photostability, which would be triggered by 808 nm laser irradiation to generate cytotoxic reactive oxygen species (ROS) to result in oxidative damage and disturbed metabolic activities of P. acnes. In addition to the efficient drug delivery, the ZIF-8 carrier could selectively degrade in response to the acidic microenvironment of acne lesions, and the released Zn2+ also exhibited a potent antimicrobial activity. The fabricated ZIF-8-ICG@MNs presented an outstanding synergistic anti-acne efficiency both in vitro and in vivo. This bioresponsive microneedle patch is expected to be readily adapted as a generalized, modular strategy for noninvasive therapeutics delivery against superficial skin diseases.


Subject(s)
Acne Vulgaris/drug therapy , Anti-Bacterial Agents/therapeutic use , Anti-Inflammatory Agents/therapeutic use , Imidazoles/therapeutic use , Indocyanine Green/therapeutic use , Metal-Organic Frameworks/therapeutic use , Photosensitizing Agents/therapeutic use , Acne Vulgaris/pathology , Animals , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/radiation effects , Anti-Bacterial Agents/toxicity , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/radiation effects , Anti-Inflammatory Agents/toxicity , HEK293 Cells , Humans , Imidazoles/chemistry , Imidazoles/radiation effects , Imidazoles/toxicity , Indocyanine Green/chemistry , Indocyanine Green/radiation effects , Indocyanine Green/toxicity , Infrared Rays , Male , Metal-Organic Frameworks/chemistry , Metal-Organic Frameworks/radiation effects , Metal-Organic Frameworks/toxicity , Mice, Inbred BALB C , Photochemotherapy , Photosensitizing Agents/chemistry , Photosensitizing Agents/radiation effects , Photosensitizing Agents/toxicity , Propionibacterium acnes/drug effects , Rats , Skin/drug effects , Skin/pathology , Swine , Zinc/chemistry , Zinc/radiation effects , Zinc/therapeutic use , Zinc/toxicity
7.
Phytomedicine ; 91: 153710, 2021 Oct.
Article in English | MEDLINE | ID: mdl-34461422

ABSTRACT

BACKGROUND: Cutibacterium acnes is a major colonizer and inhabitant of human skin and contributes to the pathogenesis of acne vulgaris. C. acnes either alone or with Staphylococcus aureus, which also inhabits skin, readily forms biofilms that are often tolerant of conventional antibiotics and the host immune system. It was hypothesized that the amphiphilic nature of some fatty acids (FAs) inhibit C. acnes or mixed biofilm formation. PURPOSE: The antibacterial and antibiofilm activities of 24 saturated and unsaturated FAs were investigated against C. acnes as well as a mixture of the bacteria C. acnes and S. aureus. METHODS: Anti-biofilm assays, antimicrobial assays, confocal laser scanning microscopy, scanning electron microscopy, extracellular polymeric substance production, and microbial adherence to hydrocarbon assay were utilized to elucidate how active FAs influence biofilm development. RESULTS: Seventeen FAs at 20 µg/ml inhibited C. acnes biofilm formation by 60-99%. The minimum inhibitory concentrations (MICs) of 20 FAs were ≥ 500 µg/ml but 4 medium-chain FAs had MICs in a range 15 to 200 µg/ml. Interestingly, myristoleic acid inhibited biofilm formation at 1 µg/ml. Myristoleic acid also inhibited the formation of S. aureus and mixed C. acnes/S. aureus biofilms. FAs reduced C. acnes hydrophobicity and we found this was generally correlated with their antibiofilm forming efficacies. Transcriptional analyses showed that myristoleic acid modulates the expression of several biofilm-related genes such as lipase, hyaluronate lyase, and virulence-related genes. CONCLUSION: This study shows myristoleic acid and other FAs inhibit biofilm formation by C. acnes and mixed biofilm formation by C. acnes and S. aureus. Hence, myristoleic acid might be useful for treating or preventing acne and C. acnes associated diseases.


Subject(s)
Anti-Bacterial Agents , Biofilms/drug effects , Fatty Acids, Monounsaturated/pharmacology , Propionibacterium acnes/drug effects , Staphylococcus aureus , Anti-Bacterial Agents/pharmacology , Extracellular Polymeric Substance Matrix , Humans , Hydrophobic and Hydrophilic Interactions , Microbial Sensitivity Tests , Staphylococcus aureus/drug effects
8.
Int J Mol Sci ; 22(14)2021 Jul 12.
Article in English | MEDLINE | ID: mdl-34299085

ABSTRACT

The ongoing search for effective treatment of Acne vulgaris is concentrated, i.a., on natural peptides with antimicrobial properties. The aim of this work was the development of new amino acid derivatives with potential activity on dermal infections against selected microorganisms, including the facultative anaerobe C. acne. The peptides P1-P6 were synthesized via Fmoc solid phase peptide synthesis using Rink amide AM resin, analyzed by RP-HPLC-MS, FTIR, DPPH radical scavenging activity, and evaluated against C. acne and S. aureus, both deposited and non-deposited in BC. Peptides P1-P6 presented a lack of cytotoxicity, antimicrobial activity, or antioxidative properties correlated with selected structural properties. P2 and P4-P6 sorption in BC resulted in variable data, i.a., confirming the prospective topical application of these peptides in a BC carrier.


Subject(s)
Acne Vulgaris/drug therapy , Anti-Bacterial Agents/pharmacology , Antioxidants/pharmacology , Cellulose/metabolism , Peptide Fragments/pharmacology , Propionibacterium acnes/drug effects , Staphylococcus aureus/drug effects , Acne Vulgaris/metabolism , Humans , Staphylococcus aureus/metabolism
9.
Sci Rep ; 11(1): 8695, 2021 04 22.
Article in English | MEDLINE | ID: mdl-33888782

ABSTRACT

Human skin is populated by various microorganisms, the so-called microbiota, such as bacteria, viruses, yeasts, fungi, and archaea. The skin microbiota is in constant contact with the surrounding environment which can alter its eubiotic state. Recently it has been also observed that the application of cosmetic products can alter the balance of the skin microbiota. This effect may be attributed to many factors including the residual activity of the preservatives on the skin. In the present work, we studied the effect of eleven preservatives commonly found in cosmetic products on Propionibacterium acnes, Staphylococcus epidermidis, and Staphylococcus aureus in vitro using 3D skin models and culture-dependent methods. Also, the effect on Histone deacetylase 3 (HDAC3) has been investigated. Among tested combinations, three resulted as the best suitable for restoring a pre-existing dysbiosis since they act moderately inhibiting C. acnes and strongly S. aureus without simultaneously inhibiting the growth of S. epidermidis. The other four combinations resulted as the best suitable for use in topical products for skin and scalp in which it is necessary to preserve the eubiosis of the microbiota. Some of the tested were also able to increase HDAC3 expression. Taking together these data highlight the role of preservatives of skin resident microflora dynamics and could provide a reference for correctly choice preservatives and dosage in cosmetic formulations to preserve or restore homeostasis of skin microbiota.


Subject(s)
Cosmetics/chemistry , Microbiota/drug effects , Preservatives, Pharmaceutical/pharmacology , Skin/microbiology , Histone Deacetylases/metabolism , Humans , Propionibacterium acnes/drug effects , Skin/enzymology , Staphylococcus aureus/drug effects , Staphylococcus epidermidis/drug effects
10.
Eur J Dermatol ; 31(1): 32-40, 2021 Feb 01.
Article in English | MEDLINE | ID: mdl-33648912

ABSTRACT

BACKGROUND: Acne vulgaris is a common pilosebaceous disease associated with Propionibacterium acnes (P. acnes). Resolution of comedones may occur in association with shrunken sebaceous glands (SGs) containing de-differentiated cells, however the role of P. acnes is unclear. OBJECTIVES: To investigate the effects of P. acnes on aryl hydrocarbon receptor (AhR) activation, lipogenesis and differentiation in cultured immortalized human SZ95 sebocytes. MATERIALS & METHODS: Cultured sebocytes were incubated with formalin-killed (f-) P. acnes (f-P. acnes) at different ratios of multiplicity of infection. The mRNA levels of the AhR downstream cytochrome P450 (CYP) genes were measured by quantitative RT-PCR, nuclear translocation of AhR by western blot and immunofluorescence, lipogenesis and keratinization by gene set enrichment analysis (GSEA), lipid related analysis by Oil red O staining and Nile red staining, and sebaceous differentiation-related gene expression by western blot. RESULTS: f-P. acnes upregulated CYPs mRNA levels and induced translocation of AhR protein from the cytoplasm into the nucleus. GSEA revealed downregulation of lipogenesis and upregulation of keratinization. f-P. acnes inhibited linoleic acid-induced neutral lipid synthesis and expression of sebocyte markers, keratin 7 and mucin1/EMA, but increased expression of keratinocyte markers, keratin 10 and involucrin, which were abolished by AhR gene silencing. Inhibition of lipogenesis-related genes, such as sterol response element-binding protein, was also observed. CONCLUSION: f-P. acnes inhibits lipogenesis and induces terminal differentiation of sebocytes, into keratinocyte-like cells, via activation of the AhR pathway in vitro, suggesting that follicular P. acnes is not only acnegenic but also promotes acne remission through feedback regulation of sebum production.


Subject(s)
Cell Differentiation/physiology , Formaldehyde/pharmacology , Propionibacterium acnes/drug effects , Propionibacterium acnes/physiology , Receptors, Aryl Hydrocarbon/physiology , Sebaceous Glands/cytology , Cells, Cultured , Humans
11.
Am J Clin Dermatol ; 22(2): 193-204, 2021 Mar.
Article in English | MEDLINE | ID: mdl-32918267

ABSTRACT

Oral antibiotics are integral for treating inflammatory acne based on what is understood about the pathogenesis as well as the role of Cutibacterium acnes. However, rising concerns of antibiotic resistance and the perception of "antibiotic phobia" create potential limitations on their integration in an acne treatment regimen. When prescribing oral antibiotics, dermatologists need to consider dosage, duration, and frequency, and to avoid their use as monotherapy. These considerations are important, along with the use of newer strategies and compounds, to reduce adverse-event profiles, antibiotic resistance, and to optimize outcomes. Aside from concomitant medications, allergies, and disease severity, costs and patient demographics can influence variability in prescribing plans. There are multiple published guidelines and consensus statements for the USA and Europe to promote safe antibiotic use by dermatologists. However, there is a lack of head-to-head studies and evidence for comparative superiority of any individual antibiotic, as well as any evidence to support the use of agents other than tetracyclines. Although oral antibiotics are one of the main options for moderate to severe acne, non-antibiotic therapy such as isotretinoin and hormonal therapies should be considered. As newer therapies and more outcomes data emerge, so will improved management of antibiotic therapy to foster patient safety.


Subject(s)
Acne Vulgaris/drug therapy , Anti-Bacterial Agents/therapeutic use , Propionibacterium acnes/drug effects , Acne Vulgaris/microbiology , Administration, Oral , Anti-Bacterial Agents/pharmacology , Contraceptives, Oral/therapeutic use , Dermatology/methods , Dermatology/standards , Drug Prescriptions/standards , Drug Resistance, Bacterial , Drug Therapy, Combination/methods , Humans , Isotretinoin/therapeutic use , Microbial Sensitivity Tests/standards , Practice Guidelines as Topic , Propionibacterium acnes/isolation & purification , Spironolactone/therapeutic use , Treatment Outcome
12.
Z Naturforsch C J Biosci ; 76(1-2): 55-65, 2021 Jan 27.
Article in English | MEDLINE | ID: mdl-32897872

ABSTRACT

Various Achillea species are rich in bioactive compounds and are important medicinal plants in phytotherapy. In the present study, Achillea millefolium L., Achillea moschata Wulfen, and Achillea atrata L. were compared with respect to their phenolic profile and antibacterial activity against gram-positive bacteria strains (Staphylococcus, Propionibacterium). Particular focus was given to A. atrata, which has hardly been studied so far. Based on the metabolite profile, A. atrata exhibited more similarities to A. moschata than to A. millefolium. The former two only differed in the occurrence of four compounds. The flavonols syringetin-3-O-glucoside and mearnsetin-hexoside, not reported for an Achillea species before, have been detected in A. atrata and A. moschata. All Achillea species reduced growth of the tested bacteria. A. atrata demonstrated highest activity against Propionibacterium acnes and Staphylococcus epidermidis, both being involved in the pathogenesis of acne vulgaris. Furthermore, A. atrata has a pronounced anti-methicillin-resistant Staphylococcus aureus potential. Bioassay-guided fractionation revealed that only the most polar fraction of A. moschata displayed antimicrobial activity, which was attributed to phenolics such as apigenin, centaureidin, and nevadensin, being present in high amounts in A. atrata. Thus, this alpine species shows promising antimicrobial activity and might be a potential source for developing novel dermal/topical drugs.


Subject(s)
Achillea/chemistry , Anti-Bacterial Agents/chemistry , Phytochemicals/chemistry , Anti-Bacterial Agents/pharmacology , Apigenin/analysis , Flavones/analysis , Flavonoids/analysis , Phytochemicals/pharmacology , Propionibacterium acnes/drug effects , Staphylococcus aureus/drug effects
13.
J Ethnopharmacol ; 268: 113552, 2021 Mar 25.
Article in English | MEDLINE | ID: mdl-33152431

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Sapindus mukorossi Gaertn. (S. mukorossi), known as 'mu huan zi' in Chinese folklore, belongs to the family Sapindaceae and it has been traditionally used for treating coughing and excessive salivation, removing freckle, whitening skin, etc. Evidence-based medicine also verified the antimicrobial, anti-tyrosinase and anti-acne activity of S. mukorossi extract, suggesting that it has the potential to be a pharmaceutical and cosmetic additive. AIM OF THE STUDY: The present study was intended to evaluate the freckle-removing and skin-whitening activities of S. mukorossi extracts, and further analyzing the potential anti-acne mechanism. METHODS: Saponin fractions were purified by using the semi-preparative high-performance liquid chromatography, and their antibacterial activity was detected against Propionibacterium acnes (P. acnes), which was the leading cause of inflamed lesions in acne vulgaris. The anti-lipase and anti-tyrosinase activities were assayed using a commercial kit, while the potential anti-acne mechanism was predicted on the basis of the network pharmacology. Active components of saponin fraction were identified by HPLC-MS analysis. Furthermore, the different toxicity level of compounds was predicted according to the quantitative structure-activity relationship, and the first application of crude extract and saponin fraction to facial masks was analyzed based on the comprehensive evaluation method. RESULTS: The saponin fraction (F4) purified from the fermentation liquid-based water extract (SWF) showed the best antibacterial activity against P. acnes ATCC 6919 with the MIC of 0.06 mg/mL, which was 33-fold of its parent SWF (with the MIC of 2.0 mg/mL). Compared with SWF, the application of F4 caused greater inhibition rates on lipase and tyrosinase. Chemical constituents of F4 were evaluated, from which four oleanane-type triterpenoid saponins were detected to contribute to the above biological activities of F4. The mechanism of the four compounds on anti-acne was predicted, and seven targets such as PTGS2 and F2RL1 were obtained to be important for the treatment of acne. The four compounds were also predicted to have different levels of toxicity to various species, and they were not harmful to rats. Besides, F4 and SWF were applied to facial masks and there was no significant influence on the physicochemical properties including pH, stability, and sensory characteristics. CONCLUSION: This work demonstrated that oleanane-type triterpenoid saponins were speculated to contribute to the skin-whitening, freckle-removing, and anti-acne activities of F4. These findings will facilitate the development of the S. mukorossi extract and the allied products as the new and natural anti-acne agent and cosmetic additives.


Subject(s)
Acne Vulgaris/drug therapy , Cosmetics/administration & dosage , Plant Extracts/administration & dosage , Propionibacterium acnes/drug effects , Sapindus , Saponins/administration & dosage , Acne Vulgaris/diagnosis , Acne Vulgaris/microbiology , Adult , Cosmetics/isolation & purification , Cosmetics/toxicity , Drug Evaluation, Preclinical/methods , Female , Forecasting , Humans , Male , Microbial Sensitivity Tests/methods , Plant Extracts/isolation & purification , Plant Extracts/toxicity , Propionibacterium acnes/physiology , Saponins/isolation & purification , Saponins/toxicity , Young Adult
14.
Biomedica ; 40(4): 693-701, 2020 12 02.
Article in English, Spanish | MEDLINE | ID: mdl-33275348

ABSTRACT

Introduction: Tea tree oil is an essential oil recognized for its antimicrobial properties. Objective: To evaluate the composition, features, and antimicrobial effect at 2% v/v, and its minimal inhibitory concentration (MIC) against Cutibacterium acnes (Propionibacterium acnes). Materials and methods: Three different batches of tea tree oil were evaluated. We characterized its chemotype by gas chromatography and its 2% v/v antimicrobial activity against C. acnes by agar diffusion assay (guide M11-A8 CLSI). Results: The three batches of oil had the chemotypes required by the ISO 4730 standard, which indicates that it is a high-quality product. Additionally, they had 30% to 40% of terpinen-4-ol, a compound that favors its antimicrobial activity. Antimicrobial activity against C. acnes for all batches had a concentration-dependent effect with microbial growth inhibitory activity in all assays at 2% v/v. The MIC obtained against C. acnes for all batches was 0.25% v/v. The antimicrobial activity of tea tree oil against this microorganism has been previously reported with a MIC between 0.05% and 1.25% v/v, a range that covers the one obtained in this study. Conclusion: These results show the high quality of the oil and its capacity as an antibacterial agent against C. acnes. New studies should be conducted to confirm its activity and that of its components in isolates of the microorganism from patients with acne vulgaris.


Introducción. El aceite del árbol de té es un aceite esencial reconocido por sus propiedades antimicrobianas. Objetivos. Evaluar la composición, características y efecto antimicrobiano del aceite al 2 % del árbol de té y su concentración inhibitoria mínima (CIM) contra Cutibacterium acnes (Propionibacterium acnes). Materiales y métodos. Se evaluó el quimiotipo en tres lotes diferentes de este aceite mediante cromatografía de gases, así como su actividad antimicrobiana en concentración al 2 % v/v y la CIM contra C. acnes mediante ensayo de difusión en agar (guía M11-A8 CLSI). Resultados. Los lotes evaluados presentaron los quimiotipos ajustados a la norma ISO 4730, lo que indicó la alta calidad del producto. Los lotes contenían de 30 a 40 % de terpinen-4-ol, compuesto que favorece la actividad antimicrobiana, la cual presentó en todos los lotes un efecto dependiente de la concentración contra C. acnes, con una inhibición del crecimiento microbiano en concentración al 2 % v/v en todas las pruebas. La concentración inhibitoria mínima fue de 0,25 % v/v. La actividad antimicrobiana del aceite del árbol de té contra este microorganismo ya ha sido reportada con una concentración inhibitoria mínima entre 0,05 y 1,25 % v/v, rango que cobija la obtenida en este estudio. Conclusiones. Los resultados evidenciaron la gran calidad de este producto y su capacidad como agente antibacteriano contra C. acnes. Se deben hacer estudios con otros aislamientos del microorganismo provenientes de pacientes con acné vulgar para confirmar su actividad general y la de cada uno de sus componentes.


Subject(s)
Anti-Infective Agents, Local/chemistry , Anti-Infective Agents, Local/pharmacology , Propionibacterium acnes/drug effects , Tea Tree Oil/pharmacology , Anti-Infective Agents, Local/standards , Color , Flame Ionization , Microbial Sensitivity Tests , Propionibacterium acnes/growth & development , Refractometry , Tea Tree Oil/administration & dosage , Tea Tree Oil/chemistry , Tea Tree Oil/standards , Terpenes/analysis
15.
BMC Dermatol ; 20(1): 17, 2020 11 17.
Article in English | MEDLINE | ID: mdl-33203374

ABSTRACT

BACKGROUND: Antibiotics have been used for decades against Cutibacterium acnes (previously known as Propionibacterium acnes; C. acnes). Alarmingly, antibiotic resistance to this bacterium has become a worldwide problem in recent years. No studies are available on the antibiotic susceptibility patterns of C. acnes among Jordanian acne patients and how that is influenced by antibiotic use. This study aims to assess antibiotic resistance patterns of C. acnes clinical isolates and neighboring Gram-positive normal flora of the skin obtained from acne patients attending dermatology clinics in Amman -Jordan appraising the role of antibiotic consumption. METHODS: This is a cross-sectional study of acne patients presenting to selected dermatology outpatient clinics over a 6-month study period. Swabs obtained from inflamed lesions were cultured aerobically and anaerobically. Isolates were identified and screened for antibiotic susceptibility. In addition, all patients were asked to fill in a questionnaire that included questions about the history of antibiotic treatment. RESULTS: C. acnes was isolated from lesions of 100 patients out of 115 participants included in this study. 73% of the isolates were resistant to erythromycin and 59% to clindamycin 37% to doxycycline, 36% to tetracycline, 31% to trimethoprim / sulfamethoxazole, 15% to levofloxacin, and 3% to minocycline. Multi drug resistance (MDR) in C. acnes isolates as well as Staphylococcus aureus (S. aureus) and Staphylococcus epidermidis (S. epidermidis) with a similar pattern of resistance were detected from the same patient in most cases. A pattern of higher resistance towards variable antibiotic was observed in patients previously treated with antibiotics for acne management. CONCLUSIONS: The findings of this study demonstrate the distribution of antibiotic resistance of C. acnes towards used antibiotics and emphasizes the influence of antibiotic consumption on development of antibiotic resistance. The similar pattern of resistance between skin bacteria tested in this study highlights the genetic transfer of resistance between skin commensals including S. aureus and S. epidermidis hence promoting its circulation in the community.


Subject(s)
Acne Vulgaris/drug therapy , Anti-Bacterial Agents/pharmacology , Drug Resistance, Multiple, Bacterial , Propionibacterium acnes/drug effects , Skin/microbiology , Acne Vulgaris/epidemiology , Acne Vulgaris/microbiology , Adolescent , Anti-Bacterial Agents/therapeutic use , Cross-Sectional Studies , Female , Humans , Jordan/epidemiology , Male , Microbial Sensitivity Tests , Prevalence , Propionibacterium acnes/isolation & purification , Staphylococcus aureus/drug effects , Staphylococcus aureus/isolation & purification , Staphylococcus epidermidis/drug effects , Staphylococcus epidermidis/isolation & purification , Young Adult
16.
Am J Clin Dermatol ; 21(6): 813-819, 2020 Dec.
Article in English | MEDLINE | ID: mdl-32889707

ABSTRACT

Antibiotic resistance in acne was first observed in the 1970s, and since the 1980s has become a major concern in dermatologic daily practice. The mechanisms for this type of resistance include biofilm formation that promotes virulence and the transmission of resistant bacterial strains. Genetic mutations with modification of ribosomal RNA, alteration in efflux pumps, and enzymatic inactivation are able to create resistance to tetracyclines and macrolides. The state of art in acne treatment is no longer to use antimicrobials as monotherapy. There should be a time limit for its use plus the employment of non-antibiotic maintenance. Earlier initiation of oral isotretinoin therapy should be considered in patients with insufficient response to antimicrobials, severe acne, or a history of repeated antimicrobial use. A better understanding of acne pathogenesis, the subtypes of Propionibacterium (also known as Cutibacterium) acnes, homeostasis of the skin microbiota, and the mechanisms of antibiotic resistance would be useful in the selection of narrow-spectrum or species-specific antimicrobials, as well as the non-antimicrobial, anti-inflammatory treatment of acne. A number of novel treatments awaiting clinical proof may include the use of bacteriophages, natural or synthetic antimicrobial peptides, probiotics, and biofilm-targeting agents, as well as the reassessment of phototherapy.


Subject(s)
Acne Vulgaris/therapy , Anti-Bacterial Agents/pharmacology , Bacteriophages , Phototherapy , Propionibacterium acnes/drug effects , Acne Vulgaris/diagnosis , Acne Vulgaris/microbiology , Acne Vulgaris/pathology , Administration, Cutaneous , Administration, Oral , Anti-Bacterial Agents/therapeutic use , Anti-Inflammatory Agents/administration & dosage , Biofilms/drug effects , Biofilms/growth & development , Combined Modality Therapy/methods , Drug Resistance, Microbial , Drug Therapy, Combination/methods , Humans , Isotretinoin/administration & dosage , Microbial Sensitivity Tests , Propionibacterium acnes/isolation & purification , Severity of Illness Index , Skin/microbiology , Skin/pathology , Treatment Outcome
17.
Recent Pat Antiinfect Drug Discov ; 15(2): 119-136, 2020.
Article in English | MEDLINE | ID: mdl-32990540

ABSTRACT

BACKGROUND: Acne is an infection of the skin that occurs in both men and women during their lifespan. There are various natural or synthetic products available in the market to prevent and cure this disease. INTRODUCTION: The majority of the world population depends on the herbs or natural resources for the relief of acne disease. These are used to lessen the cost of treatment and the side effects of synthetic analogs. METHODS: We have explored the various authentic web resources to compile information regarding different patented and marketed herbal formulations for acne treatment. RESULTS: It has been found that most of the herbal formulation for acne include the plant actives/extracts having the potential activity against the Propionibacterium acne. The occurrence of this skin disease is also associated with the presence of free radicals in the body, which also causes the inflammation and redness of the skin. Further, the study of various patents also revealed that herbs with anti-oxidant properties have been used in most of the herbal anti-acne formulations. Moreover, the various patents also give the idea that herbal formulations also prevent the appearance of pimples on the skin. CONCLUSION: It has been concluded that the herbal anti-acne formulation is not only used to treat acne but also prevents this disease safely and economically.


Subject(s)
Acne Vulgaris/drug therapy , Patents as Topic , Phytotherapy/methods , Plant Extracts/therapeutic use , Acne Vulgaris/economics , Acne Vulgaris/microbiology , Acne Vulgaris/prevention & control , Administration, Cutaneous , Anti-Bacterial Agents/economics , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/therapeutic use , Antioxidants/economics , Antioxidants/pharmacology , Antioxidants/therapeutic use , Drug Costs , Humans , Phytotherapy/economics , Plant Extracts/economics , Plant Extracts/pharmacology , Propionibacterium acnes/drug effects , Skin/drug effects , Skin/microbiology , Treatment Outcome
18.
Chem Biodivers ; 17(10): e2000489, 2020 Oct.
Article in English | MEDLINE | ID: mdl-32761773

ABSTRACT

Rhotomentodiones C-E, three new polymethylated phloroglucinol meroterpenoids with diverse configurations, were isolated from the twigs and leaves of Rhodomyrtus tomentosa. Their structures and absolute configurations were established mainly by means of comprehensive spectroscopic data and electron circular dichroism (ECD) calculation. Among them, Rhotomentodione D (2) exhibited both antibacterial activity with an MIC value of 12.5 µg/mL against Propionibacterium acnes and AChE inhibitory activity with an IC50 value of 22.9 µm.


Subject(s)
Anti-Bacterial Agents/pharmacology , Cholinesterase Inhibitors/pharmacology , Myrtaceae/chemistry , Phloroglucinol/pharmacology , Plant Extracts/pharmacology , Terpenes/pharmacology , Acetylcholinesterase/metabolism , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/isolation & purification , Cholinesterase Inhibitors/chemistry , Cholinesterase Inhibitors/isolation & purification , Microbial Sensitivity Tests , Phloroglucinol/chemistry , Phloroglucinol/isolation & purification , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plant Leaves/chemistry , Plant Stems/chemistry , Propionibacterium acnes/drug effects , Staphylococcus epidermidis/drug effects , Terpenes/chemistry , Terpenes/isolation & purification
19.
Pharm Dev Technol ; 25(10): 1216-1225, 2020 Dec.
Article in English | MEDLINE | ID: mdl-32744472

ABSTRACT

The objective of this study was to develop resveratrol nanocrystals to solve low water solubility issues of resveratrol and adsorb them to the polycaprolactone nanofibers. Nanocrystals were prepared by microfluidization. Particle size, polydispersity index and zeta potential values were evaluated as dependent variables. Polycaprolactone (PCL) nanofibers were prepared via electrospinning method and the flow rate, electrical voltage and tip-to-collector distance were set to 3 mL/h, 13 kV and 15 cm, respectively. Optimum resveratrol nanocrystals were lyophilized and re-suspended in water and physically adsorbed to PCL nanofibers with two different concentrations (0.2 and 1 mg/cm2). Bioadhesion, wettability, solubility, drug loading and antimicrobial activity against Propionibacterium acnes studies were carried out. Final nanocrystals showed 800 nm of particle size, 0.4 of polydispersity index, and -8 mV of zeta potential. Nanocrystals successfully adsorbed to PCL nanofibers proven on SEM images with adsorption efficiencies >70%. Adsorption of resveratrol nanocrystals decreased the contact angle of PCL from 128° to 50°. The solubility of resveratrol nanocrystals enhanced ∼5-fold in comparison with coarse powder. Effective antimicrobial activity against P. acnes was observed. It is concluded that nanocrystal loading on nanofibers brings advantage into preparing easy to use dermal patches for acne treatment or skin disorders.


Subject(s)
Anti-Bacterial Agents/administration & dosage , Nanofibers , Propionibacterium acnes/drug effects , Resveratrol/administration & dosage , Adsorption , Animals , Anti-Bacterial Agents/pharmacology , Chemistry, Pharmaceutical/methods , Freeze Drying , Nanoparticles , Particle Size , Polyesters/chemistry , Rats , Resveratrol/pharmacology , Solubility , Wettability
20.
Int J Mol Sci ; 21(14)2020 Jul 19.
Article in English | MEDLINE | ID: mdl-32707723

ABSTRACT

The probiotic activity of skin Staphylococcus epidermidis (S. epidermidis) bacteria can elicit diverse biological functions via the fermentation of various carbon sources. Here, we found that polyethylene glycol (PEG)-8 Laurate, a carbon-rich molecule, can selectively induce the fermentation of S. epidermidis, not Cutibacterium acnes (C. acnes), a bacterium associated with acne vulgaris. The PEG-8 Laurate fermentation of S. epidermidis remarkably diminished the growth of C. acnes and the C. acnes-induced production of pro-inflammatory macrophage-inflammatory protein 2 (MIP-2) cytokines in mice. Fermentation media enhanced the anti-C. acnes activity of a low dose (0.1%) clindamycin, a prescription antibiotic commonly used to treat acne vulgaris, in terms of the suppression of C. acnes colonization and MIP-2 production. Furthermore, PEG-8 Laurate fermentation of S. epidermidis boosted the activity of 0.1% clindamycin to reduce the sizes of C. acnes colonies. Our results demonstrated, for the first time, that the PEG-8 Laurate fermentation of S. epidermidis displayed the adjuvant effect on promoting the efficacy of low-dose clindamycin against C. acnes. Targeting C. acnes by lowering the required doses of antibiotics may avoid the risk of creating drug-resistant C. acnes and maintain the bacterial homeostasis in the skin microbiome, leading to a novel modality for the antibiotic treatment of acne vulgaris.


Subject(s)
Clindamycin/administration & dosage , Laurates/metabolism , Polyethylene Glycols/metabolism , Propionibacteriaceae/drug effects , Staphylococcus epidermidis/metabolism , Acne Vulgaris/drug therapy , Acne Vulgaris/microbiology , Animals , Anti-Bacterial Agents/administration & dosage , Fermentation , Gram-Positive Bacterial Infections/drug therapy , Gram-Positive Bacterial Infections/microbiology , Humans , In Vitro Techniques , Mice , Mice, Inbred ICR , Probiotics/metabolism , Propionibacteriaceae/growth & development , Propionibacterium acnes/drug effects , Propionibacterium acnes/growth & development , Skin/drug effects , Skin/metabolism , Skin/microbiology
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