RESUMO
BACKGROUND: To study the efficacy of 100% Leptospermum medical grade Manuka honey ointment in persistent corneal epithelial defects (CEDs). METHODS: Case series. RESULTS: Case 1 was a 25-year-old female patient who presented to the cornea clinic with a persistent CED (3.5 mm), following acanthamoeba keratitis, that had failed to respond to heavy, frequent lubrication drops and ointment. Two weeks later, after starting Leptospermum honey ointment (4 times per day), the CED healed totally. Case 2 was a 48-year diabatic, single-eyed female patient who presented with a persistent CED (1.5 × 1.5 mm) that had failed to respond to heavy, frequent lubrication drops and ointment. The CED healed three weeks after starting Leptospermum honey ointment (4 times per day). CONCLUSIONS: Leptospermum honey ointment can be a potential treatment for persistent epithelial defect.
Assuntos
Oftalmopatias , Mel , Humanos , Feminino , Adulto , Leptospermum , Pomadas , CórneaRESUMO
The very similar appearance of pollen of the New Zealand Myrtaceous taxa Leptospermum scoparium s.l. (manuka) and Kunzea spp. (kanuka) has led palynologists to combine them in paleoecological and melissopalynological studies. This is unfortunate, as differentiation of these taxa would improve understanding of past ecological change and has potential to add value to the New Zealand honey industry, where manuka honey attracts a premium price. Here, we examine in detail the pollen morphology of the 10 Kunzea species and a number of Leptospermum scoparium morphotypes collected from around New Zealand, using light microscopy, SEM, and Classifynder (an automated palynology system). Our results suggest that at a generic level the New Zealand Leptospermum and Kunzea pollen can be readily differentiated, but the differences between pollen from the morphotypes of Leptospermum or between the species of Kunzea are less discernible. While size is a determinant factor-equatorial diameter of Leptospermum scoparium pollen is 19.08 ± 1.28 µm, compared to 16.30 ± 0.95 µm for Kunzea spp.-other criteria such as surface texture and shape characteristics are also diagnostic. A support vector machine set up to differentiate Leptospermum from Kunzea pollen using images captured by the Classifynder system had a prediction accuracy of ~95%. This study is a step towards future melissopalynological differentiation of manuka honey using automated pollen image capture and classification approaches.
Assuntos
Mel , Kunzea , Myrtaceae , Mel/análise , Leptospermum , Nova Zelândia , PólenRESUMO
Honey production and export are significant contributors to the Aotearoa New Zealand economy, generating over 400 million dollars in revenue. Its main export is manuka (Leptospermum scoparium) honey, which has a high commercial value due to its medicinal properties that are linked to its unique chemical composition. The compound methylglyoxal (MGO) has been identified as the main floral marker and is used as a quality indicator, often labelled as unique manuka factor (UMF). However, the high demand for manuka honey creates pressure on beekeepers and may have negative ecological consequences by favouring extensive manuka monocultures to the detriment of other native species. There are other honeys native to New Zealand, such as kamahi (Weinmannia racemosa), kanuka (Kunzea ericoides), rata (Metrosideros robusta) and rewarewa (Knightia excelsa), that also have medicinal properties; however, they are less well known in the local and global market. Indigenous Maori communities envision the production and commercialization (locally and internationally) of these honeys as an opportunity to generate income and secure a sustainable future in alignment with their worldview (Te Ao Maori) and values (tikanga Maori). Diversifying the market could lead to a more sustainable income for beekeepers and reduce pressure on Maori and the conservation land, while supporting indigenous communities to realize their vision and aspirations. This manuscript provides an extensive review of the scientific literature, technical literature and traditional knowledge databases describing the plants of interest and their traditional medicinal uses (rongoa) and the chemical properties of each honey, potential floral markers and their biological activity. For each honey type, we also identify knowledge gaps and potential research avenues. This information will assist Maori beekeepers, researchers, consumers and other stakeholders in making informed decisions regarding future research and the production, marketing and consumption of these native monofloral honeys.
Assuntos
Mel , Kunzea , Humanos , Leptospermum/química , Havaiano Nativo ou Outro Ilhéu do Pacífico , Nova ZelândiaRESUMO
Manuka oil, an essential oil derived from the Leptospermum scoparium, has been traditionally used for wound care and as a topical antibacterial, antifungal, and anti-inflammatory. However, the essential oil is not well retained at mucosal sites, such as the oral cavity, where the benefits of the aforementioned properties could be utilized toward the treatment of persistent biofilms. Within this study, L. scoparium essential oil was incorporated into a semisolid emulsion for improved delivery. The safety profile of L. scoparium essential oil on human gingival fibroblasts was determined via cell viability, cytotoxicity, and caspase activation. The minimal bactericidal concentration of L. scoparium essential oil was determined, and the emulsion's antibiofilm effects visualized using confocal laser scanning microscopy. L. scoparium essential oil demonstrated a lower IC50 (0.02% at 48 h) when compared to the clinical control chlorhexidine (0.002% at 48 h) and displayed lower cumulative cytotoxicity. Higher concentrations of L. scoparium essential oil (≥ 0.1%) at 6 h resulted in higher caspase 3/7 activation, suggesting an apoptotic pathway of cell death. A minimal bactericidal concentration of 0.1% w/w was observed for 6 oral bacteria and 0.01% w/v for Porphyromonas gingivalis. Textural and rheometric analysis indicated increased stability of emulsion with a 1â:â3 ratio of L. scoparium essential oil: Oryza sativa carrier oil. The optimized 5% w/w L. scoparium essential oil emulsion showed increased bactericidal penetrative effects on Streptococci gordonii biofilms compared to oil alone and to chlorhexidine controls. This study has demonstrated the safety, formulation, and antimicrobial activity of L. scoparium essential oil emulsion for potential antibacterial applications at mucosal sites.
Assuntos
Leptospermum , Óleos Voláteis , Antibacterianos/farmacologia , Biofilmes , Emulsões , Óleos Voláteis/farmacologiaRESUMO
Leptospermum petersonii (family Myrtaceae) is often cultivated for ornamental purposes but also serves as a rich source of bioactive essential oils. While several studies focused on the activities of the essential oils, this study analysed the potential of spent L. petersonii leaves as a natural food preservative. METHOD: We investigated the in vitro antioxidant and antimicrobial activities of crude L. petersonii extracts against activities of the purified isolated flavonoid, 6-methyltectochrysin, which was characterized using spectroscopic methods. The antioxidant assays followed ORAC, FRAP and TEAC tests. The antimicrobial activities of the extract and purified flavonoid were analysed against six multi-drug resistant microbial strains in broth dilution assays. RESULT: The results revealed that both the crude extracts and isolated 6-methyltectochrysin exhibited positive radical ion scavenging antioxidant potential, however the crude extract was about 6-fold more potent antioxidant than the purified 6-methyltectochrysin. The crude extract also showed strong antimicrobial activities against Bacillus cereus, and even more potent antimicrobial agent than the reference ampicillin antibiotic against Klebsiella pneumoniae subsp. pneumoniae. A higher resistance was observed for the tested Gram-negative strains than for the Gram-positive ones. 6-methyltectochrysin was generally inactive in the antimicrobial assays. CONCLUSION: The crude methanolic extract showed significant bioactivity which validates the medicinal relevance of the plant. The observed biological activities, especially against a notorious strain of B. cereus, suggest that L. petersonii could be a promising natural source of food preservatives.
Assuntos
Produtos Biológicos/química , Produtos Biológicos/farmacologia , Conservantes de Alimentos/química , Conservantes de Alimentos/farmacologia , Leptospermum/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Estrutura Molecular , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
Methylglyoxal (MGO) is the main antimicrobial determinant associated with using Manuka Honey as a topical dressing. While direct mechanisms of Manuka honey MGO's antimicrobial activity have been demonstrated, such as disruption of bacterial fimbria and flagella, no interaction of Manuka honey-derived MGO with antimicrobial effector cells of the immune system, such as mucosal-associated invariant T cells (MAIT cells), has yet been reported. MAIT cells are an abundant subset of human T cells, critical for regulating a diverse range of immune functions, including antimicrobial defense mechanisms but also mucosal barrier integrity. MAIT cells become activated by recognition of an important microbial metabolite, 5-amino-6-d-ribitylaminouracil (5-A-RU), which is produced by a wide range of microbial pathogens and commensals. Recognition is afforded when 5-A-RU condenses with mammalian-cell derived MGO to form the potent MAIT cell activator, 5-(2-oxopropylideneamino)-6-d-ribitylaminouracil (5-OP-RU). Formation of 5-OP-RU and its subsequent presentation to MAIT cells by major histocompatibility (MHC)-related molecule 1 (MR1) facilitates host-pathogen and host-commensal interactions. While MGO is a metabolite naturally present in mammalian cells, it is unclear whether exogenous dietary MGO sources, such as those obtained from Manuka honey intake, can contribute to 5-OP-RU formation and enhance MAIT cell activation. In this work, we report that endogenous MGO is the rate-limiting substrate for converting microbial 5-A-RU to 5-OP-RU and that Manuka honey-derived MGO significantly enhances MAIT cell activation in vitro. Our findings posit a novel mechanism by which intake of a food item, such as Manuka honey, can potentially support immune homeostasis by enhancing MAIT cell-specific microbial sensing.
Assuntos
Mel , Fatores Imunológicos/farmacologia , Leptospermum , Ativação Linfocitária/efeitos dos fármacos , Células T Invariantes Associadas à Mucosa/metabolismo , Aldeído Pirúvico/farmacologia , Antibacterianos/farmacologia , Apiterapia , Humanos , Aldeído Pirúvico/metabolismo , Ribitol/análogos & derivados , Ribitol/metabolismo , Uracila/análogos & derivados , Uracila/metabolismoRESUMO
The chemical investigation on Eutypella scoparia SCBG-8, an endophytic fungus isolated from the leaves of Leptospermum brachyandrum, has resulted in the isolation of six new phenolic compounds eutyscoparols A-F (1-6) and one new natural product eutyscoparol G (7). The structures and absolute configurations of compounds 1-7 were determined by extensive chemical and spectroscopic analyses such as single crystal X-ray diffractions. Moreover, all compounds were evaluated for their antibacterial and cytotoxic activities in vitro.
Assuntos
Ascomicetos/química , Leptospermum/microbiologia , Policetídeos/isolamento & purificação , Linhagem Celular Tumoral , China , Cristalografia por Raios X , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Folhas de Planta/microbiologia , Policetídeos/químicaRESUMO
AIM: To evaluate the effects of a proprietary formulated eye drop with Leptospermum spp honey versus a conventional lubricant eye drop on tear film properties in subjects with symptoms related to dry eye disease after 28 days of treatment. METHODS: Forty-six subjects with symptoms related to dry eye (Ocular Surface Disease Index (OSDI) score >12) were enrolled and randomly assigned to receive either the test formulated eye drop (Optimel by Melcare Biomedical Pty Ltd) or control eye drops (Alcon, USA) in this double-masked study. Inferior lipid layer thickness (LLT), tear film evaporation rate (TER), fluorescein tear film break-up time (TBUT), corneal staining and subjective symptoms (OSDI and visual analogue scales (VAS)) were measured before and after 28 days of instilling the eye drops. RESULTS: Forty-two subjects completed the study (21 subjects in each group). After 28 days of treatment, TER showed a significantly greater reduction with the formulated eye drop compared with the control (p=0.01). TBUT showed a slight but not statistically significant increase with the formulated eye drop compared with the control (p=0.06), and a significantly greater reduction (improvement) in OSDI scores was observed with the formulated eye drop compared with the control (p=0.01). No significant differences were found between the two groups for inferior LLT, corneal staining and any of the VAS scores. CONCLUSIONS: The formulated eye drops were effective in reducing tear film evaporation rate and were more effective for improving symptoms of dry eye compared with the control eye drops after 28 days of treatment. TRIAL REGISTRATION NUMBER: NCT03622619.
Assuntos
Apiterapia , Síndromes do Olho Seco/tratamento farmacológico , Mel , Leptospermum/química , Lubrificantes Oftálmicos/administração & dosagem , Lágrimas/fisiologia , Adolescente , Adulto , Método Duplo-Cego , Composição de Medicamentos , Síndromes do Olho Seco/fisiopatologia , Feminino , Fluoresceína/administração & dosagem , Corantes Fluorescentes/administração & dosagem , Humanos , Masculino , Preparações Farmacêuticas , Estudos Prospectivos , Coloração e Rotulagem , Inquéritos e Questionários , Lágrimas/química , Acuidade Visual/fisiologia , Adulto JovemRESUMO
BACKGROUND: Manuka honey (MH) has significant antibiofilm activity in vitro and in vivo against Staphylococcus aureus, methicillin-resistant S aureus (MRSA), and Pseudomonas aeruginosa. This is the first randomized, single-blinded, placebo-controlled phase 1 clinical trial investigating the safety and preliminary efficacy of MH with augmented methylglyoxal (MGO) rinses in recalcitrant chronic rhinosinusitis (CRS). METHODS: Patients were included after previously undergoing endoscopic sinus surgery and presenting with signs and symptoms of sinus infection with positive bacterial cultures on sinus swabs. Patients were randomized to receive 14 days of twice-daily 16.5% MH + 1.3 mg/mL MGO sinonasal rinses and concurrent 10 days of placebo tablets (MH), or 14 days of twice-daily saline sinonasal rinses and concurrent 10 days of culture-directed antibiotic therapy (CON). Safety observations included the University of Pennsylvania Smell Identification Test (UPSIT) and adverse-event (AE) reporting. Efficacy was assessed comparing microbiology results, Lund-Kennedy scores (LKSs), and symptom scores using the visual analog scale (VAS) and 22-item Sino-Nasal Outcome Test (SNOT-22). RESULTS: Twenty-five patients completed the study. MH demonstrated a good safety profile with no major AEs and no changes in UPSIT. Six of 10 (60%) MH patients had a reduction in bacterial culture rate with 1 of 10 of those having negative cultures, compared with 12 of 15 (80%) in the control group with 7 of 15 having negative cultures upon completion of the study. CONCLUSION: This study concludes that twice-daily 16.5% MH augmented with 1.3 mg/mL MGO sinonasal rinses alone for 14 days is safe but not superior to culture-directed oral antibiotics and twice-daily saline rinses.
Assuntos
Antibacterianos/uso terapêutico , Apiterapia , Mel , Rinite/terapia , Sinusite/terapia , Adulto , Idoso , Idoso de 80 Anos ou mais , Bactérias/isolamento & purificação , Doença Crônica , Feminino , Humanos , Leptospermum , Masculino , Pessoa de Meia-Idade , Lavagem Nasal , Seios Paranasais/microbiologia , Rinite/microbiologia , Método Simples-Cego , Sinusite/microbiologiaRESUMO
Biowastes are unwanted materials of biological origin. They include biosolids, dairy shed effluent, and sawdust. When applied to soil, biowastes can provide plant nutrients, but also introduce heavy metals, pathogens, or xenobiotics. Biowastes could improve degraded or low-fertility soils and generate revenue through the production of non-food products such as essential oils. We grew New Zealand native plants, manuka (Leptospermum scoparium J.R. Forst & G. Forst) and kanuka (Kunzea robusta de Lange & Toelken) in series of greenhouse experiments in low-to-medium-fertility soils (Bideford clay loam, Lismore stony silt loam, and Pawson silt loam) amended with either biosolids (up to 13500â¯kgâ¯N ha-1 equiv.), biosolids + sawdust (1:0.5-1250 kg N ha-1 equiv.) and dairy shed effluent (200â¯kgâ¯N ha-1 equiv.). Two types of biosolids from Kaikoura (KB) and Christchurch City Council (CB) were used in the experiments. CB (1500â¯kgâ¯N ha-1 equiv.) and dairy shed effluent (200â¯kgâ¯N ha-1 equiv.) increased the biomass of L. scoparium by up to 120% and 31%, and K. robusta by up to 170% and 34%, respectively. Adding sawdust to KB increased the biomass of L. scoparium and K. robusta although it offset the L. scoparium growth increase in the KB-only treatment. The growth response of K. robusta to biowastes was greater than L. scoparium with oil production in K. robusta increasing by up to 211% when 1500â¯kgâ¯N ha-1 equiv. of CB was applied to Lismore stony silt loam. Generally, the treatments had a negligible effect on oil concentration in all the soil types, except for the KB + sawdust treatment, which increased the oil concentration by 82%. Most of the EOs' major components were unaffected by biowaste addition in the soils, although some components increased in the Bideford clay loam following KB and KB + sawdust application. Biosolids increased foliar concentrations of Zn, Cu, and Cd, but these were below risk-threshold concentrations. Applying CB (up to 1500 kg N ha-1 equiv.) to low-fertility soils is recommended to establish ecosystems dominated by L. scoparium and K. robusta that annually would produce ca. 100â¯kgâ¯ha-1 of EOs worth US$ 26k and 24k, respectively. Adding sawdust to CB could have environmental benefits through reduction of N leaching. Field trials are warranted to elucidate critical ecological variables and production economics in biowaste management.
Assuntos
Fertilizantes , Kunzea/metabolismo , Leptospermum/metabolismo , Óleos Voláteis/metabolismo , Óleos de Plantas/metabolismo , Indústria de Laticínios , Kunzea/crescimento & desenvolvimento , Leptospermum/crescimento & desenvolvimento , Nova Zelândia , Folhas de Planta/química , Solo/química , Poluentes do Solo/análise , Resíduos SólidosRESUMO
INTRODUCTION: Modern wound management continues to present new challenges. Many patients elect to forego operative debridement secondary to high risk, fear, cost concerns, and personal ideologies on healing. Although operative debridement has long been a tenet of proper wound care, alternative innovative approaches to wound management must be considered. OBJECTIVE: This case series describes the successful outcomes of 12 patients with dissimilar wounds who were managed with medical-grade honey (active Leptospermum honey [ALH]) as an alternative to surgery. MATERIALS AND METHODS: A case series was identified from clinical experience, chart review, and photographic documentation of all patients evaluated by the acute wound care service. To be included, patients had to decline the recommendation of operative debridement or skin grafting, utilize ALH as an alternative to surgery, and have regular follow-up visits. RESULTS: Twelve patients with complex wounds were identified and included in this case series. Five patients were considered high risk for surgery due to comorbidities. Seven patients were at low risk for surgery but desired to avoid operative procedures. The use of ALH facilitated autolytic debridement and healing without surgery or hospital readmission. CONCLUSIONS: The properties of ALH include autolytic debridement, bacterial growth inhibition, anti-inflammatory mediation, and cytokine release, making it a viable option for wound management for patients with contraindications to surgery. However, surgical debridement should remain a tenet of wound care in appropriate patients.
Assuntos
Desbridamento/métodos , Mel , Leptospermum , Preparações de Plantas/farmacologia , Preparações de Plantas/uso terapêutico , Cicatrização/efeitos dos fármacos , Ferimentos e Lesões/terapia , Adulto , Idoso , Idoso de 80 Anos ou mais , Feminino , Humanos , Masculino , Seleção de Pacientes , Fitoterapia , Estudos Retrospectivos , Resultado do Tratamento , Cicatrização/fisiologia , Ferimentos e Lesões/patologia , Ferimentos e Lesões/cirurgiaRESUMO
BACKGROUND: From the past five decades, metronidazole and tinidazole have been used for treating nonresistant and resistant giardiasis and trichomoniasis. However, due to the occurrence of drug resistance to standard therapy idealizes us to explore some additional therapies which is cost-effective, easy accessibility, and natural which has least side effects. Manuka honey obtained from Leptospermum scoparium is well known for its antibacterial and wound healing properties and is thought to be a better option as an additional therapy. OBJECTIVE: The present study was conducted to find out the effect of manuka honey on anaerobic protozoans that includes Giardia and Trichomonas under in vitro conditions in comparison to metronidazole and tinidazole. MATERIALS AND METHODS: Axenic culture of Giardia lamblia strain Portland 1 and Trichomonas vaginalis strain 413 was used for drug sensitivity assay to tinidazole, metronidazole, and manuka honey with the highest concentration of 17.1 µg/ml, 24.7 µg/ml, and 50%v/v by using (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, a tetrazole). For this, head-to-head comparison has been done and IC 50 of the standard drug as well as manuka honey was calculated. RESULTS: The result showed that percentage inhibition on the growth of both the parasites is dependent on concentration as well as exposure time of the drug. The calculated IC 50 was found to be 5.6%v/v and 1.5%v/v for manuka honey with respect to G. lamblia and T. vaginalis. CONCLUSION: The present study suggests that manuka honey can be used as an additional therapy for the patient with giardiasis or trichomoniasis. However, in vivo study in the near future will elucidate more about the effectiveness of honey in treating parasitic infections.
Assuntos
Antiprotozoários/farmacologia , Giardia lamblia/efeitos dos fármacos , Mel , Trichomonas vaginalis/efeitos dos fármacos , Antiprotozoários/administração & dosagem , Giardíase/tratamento farmacológico , Giardíase/parasitologia , Concentração Inibidora 50 , Leptospermum/química , Metronidazol/farmacologia , Fatores de Tempo , Tinidazol/farmacologia , Tricomoníase/tratamento farmacológico , Tricomoníase/parasitologiaRESUMO
A pair of epimer brachyanins A (1) and B (2), along with a new phloroglucinol brachyanin C (3), were isolated from the leaves of Leptospermum brachyandrum. Brachyanins A (1) and B (2) were the first example of novel meroterpenoid with a unique skeleton that combined a synacrpic acid and a pinene units via a benzyl moiety. Their structures were elucidated through the application of extensive spectroscopic measurements and single-crystal X-ray diffraction analysis and with the absolute configurations of 1 and 2 were confirmed by the quantum chemical CD calculation. The hetero Diels-Alder as the key biotransformation was proposed to account for the biosynthesis of brachyanins A and B sheding light by the potential procursor brachyanin C.
Assuntos
Leptospermum/química , Floroglucinol/isolamento & purificação , Terpenos/isolamento & purificação , China , Testes de Sensibilidade Microbiana , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Folhas de Planta/químicaRESUMO
ETHNOPHARMACOLOGICAL IMPORTANCE: Leptospermum flavescens has been used traditionally in Malaysia to treat various ailments such as constipation, hypertension, diabetes and cancer. AIM OF STUDY: To investigate the potential protective effects of L. flavescens in pancreatic ß cells through inhibition of apoptosis and autophagy cell death mechanisms in in vitro and in vivo models. MATERIALS AND METHODS: L. flavescens leaves were extracted using solvent in increasing polarities: hexane, ethyl acetate, methanol and water. All extracts were tested for INS-1 ß cells viability stimulated by streptozotocin (STZ). The extract which promotes the highest cell protective activity was further evaluated for insulin secretion, apoptosis and autophagy signaling pathways. Then, the acute toxicity of extract was carried out in SD rats according to OECD 423 guideline. The active extract was tested in diabetic rats where the pancreatic ß islets were evaluated for insulin, apoptosis and autophagy protein. RESULTS: The methanolic extract of L. flavescens (MELF) was found to increase INS-1 ß cells viability and insulin secretion against STZ. In addition, MELF has been shown to inhibit INS-1 ß cells apoptosis and autophagy activity. Notably, there was no toxicity observed in SD rats when administered with MELF. Furthermore, MELF exhibited anti-hyperglycemic activity in diabetic rats where apoptosis and autophagy protein expression was found to be suppressed in pancreatic ß islets. CONCLUSION: MELF was found to protect pancreatic ß cells function from STZ-induced apoptosis and autophagy in in vitro and in vivo.
Assuntos
Hipoglicemiantes/farmacologia , Células Secretoras de Insulina/efeitos dos fármacos , Leptospermum , Extratos Vegetais/farmacologia , Animais , Apoptose/efeitos dos fármacos , Autofagia/efeitos dos fármacos , Células Cultivadas , Diabetes Mellitus Experimental/tratamento farmacológico , Feminino , Hipoglicemiantes/uso terapêutico , Células Secretoras de Insulina/fisiologia , Masculino , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Metanol/química , Extratos Vegetais/uso terapêutico , Folhas de Planta , Ratos Sprague-Dawley , Solventes/química , Estreptozocina/farmacologia , Testes de Toxicidade AgudaRESUMO
The development of chemo-sensitizers is urgently needed to overcome 5-fluorouracil (5-FU) therapeutic resistance and adverse toxicity in colorectal cancer. This work aims to evaluate the synergic effects of 5-FU and Manuka honey (MH), a rich source of bioactive compounds, in enhancing the anticancer effects of this drug on human colon cancer HCT-116 and LoVo cells. Compared to 5-FU alone, MH synergistically enhanced the chemotherapeutic effects of 5-FU, by reducing cell proliferation through the suppression of EGFR, HER2, p-Akt and p-mTOR expression, and promoting apoptosis by the modulation pro-apoptotic (p53, Bax, Cyto c, FasL caspase-3, -8, -9 and cleave-PARP) and anti-apoptotic (Bcl-2) markers. The activations of p-p38MAPK and p-Erk1/2 pathways and ROS production were also involved in this process. Downregulation of transcription factor (NF-κB and Nrf2) and antioxidant enzyme activity (SOD, catalase, glutathione peroxidase and glutathione reductase) and expression (SOD, catalase and HO-1) were more evident after the combined treatment, leading to more cell death by oxidative stress. Moreover, additive effects were also observed by increasing lipid and protein oxidation and arresting cell cycle. All the parameters of mitochondrial respiration and glycolysis function decreased and both cells entered the quiescent stage after the combined treatments. MH also influenced the anti-metastasis effects of 5-FU by decreasing migration ability, suppressing the expression of MMP-2, MMP-9 and increasing N-cadherin and E-cadherin. In conclusion, MH could be a useful preventive or adjuvant agent in the treatment of colorectal cancer with 5-FU.
Assuntos
Neoplasias do Colo/tratamento farmacológico , Sinergismo Farmacológico , Mel , Estresse Oxidativo/efeitos dos fármacos , Apoptose/efeitos dos fármacos , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Neoplasias do Colo/genética , Neoplasias do Colo/patologia , Fluoruracila/farmacologia , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Células HCT116 , Humanos , Leptospermum/química , Metástase Neoplásica , Proteínas de Neoplasias/genéticaRESUMO
The biochemical properties of buckwheat honey, including contents of sugars, proteins, total phenols, methylglyoxal (MGO), minerals and phenolic compounds, were determined in comparison with those of manuka honey. Buckwheat honey has higher contents of sugars, proteins and total phenols but a lower content of MGO than manuka honey. Buckwheat honey contains abundant minerals involved in a number of vital functions of the human body as does manuka honey, and has even higher contents of Fe, Mn and Zn. In buckwheat honey, p-hydroxybenzoic acid, chlorogenic acid and p-coumaric acid are the dominant phenolic compounds. Moreover, the antibacterial and cellular antioxidant activities of buckwheat honey were compared with those of manuka honey. Buckwheat honey exhibits antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa, comparable with manuka honey, and the cellular antioxidant activity of buckwheat honey is higher than that of manuka honey. Our results suggest that buckwheat honey has great nutritional and commercial potentials.
Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Fagopyrum , Mel/análise , Leptospermum , Humanos , Pseudomonas aeruginosa/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacosRESUMO
BACKGROUND: The increase in resistance of head lice to neurotoxic pediculicides and public concern over their safety has led to an increase in alternative treatments, many of which are poorly researched or even untested. METHODS: A multicentre, randomised, assessor-blind, parallel-group trial (Trial 1) was conducted to compare the safety and efficacy of a head lice treatment containing Australian eucalyptus oil and Leptospermum petersonii (EO/LP solution; applied thrice with 7-day intervals between applications) with a neurotoxic treatment containing pyrethrins and piperonyl butoxide (P/PB mousse; applied twice with a 7-day interval) in children. A single-blind, open trial (Trial 2) was conducted to assess the efficacy of EO/LP solution following a single application. In addition, skin irritancy and sensitisation tests using EO/LP solution were performed in adults and children. In vitro tests were performed to further assess the ovicidal and pediculicidal efficacy of EO/LP solution. RESULTS: EO/LP solution was found to be more than twice as effective in curing head lice infestation as P/PB mousse in per-protocol participants (Trial 1; 83% vs 36%, P < 0.0001), and was also found to be 100% pediculicidal following a single application (Trial 2). Adverse events were limited to transient itching, burning or stinging. Further skin testing with the EO/LP solution reported no irritation or sensitisation in adults, or irritation in children. In vitro exposure of lice and eggs to the EO/LP solution resulted in 100% mortality. CONCLUSION: The efficacy, safety and relative ease of use of the EO/LP solution make it a viable alternative in treating head lice.
Assuntos
Eucalyptus , Leptospermum , Infestações por Piolhos/tratamento farmacológico , Óleos Voláteis/uso terapêutico , Pediculus , Óleos de Plantas/uso terapêutico , Dermatoses do Couro Cabeludo/diagnóstico por imagem , Adulto , Idoso , Animais , Pré-Escolar , Feminino , Humanos , Lactente , Inseticidas/uso terapêutico , Masculino , Pessoa de Meia-Idade , Óleos Voláteis/efeitos adversos , Óvulo/efeitos dos fármacos , Pediculus/efeitos dos fármacos , Sinergistas de Praguicidas/uso terapêutico , Butóxido de Piperonila/uso terapêutico , Óleos de Plantas/efeitos adversos , Piretrinas/uso terapêutico , Dermatoses do Couro Cabeludo/parasitologia , Método Simples-CegoRESUMO
Fourteen wild strains of Staphylococcus aureus positive for gene sea were tested for enterotoxins production and the minimum inhibitory concentration of Leptospermum scoparium, Origanum majorana, Origanum vulgare, Satureja montana and Thymus vulgaris essential oils (EOs) were determined. After this trial, bacteria stressed with sub-inhibitory concentration of each EO were tested for enterotoxins production by an immunoenzymatic assay and resistance to the same EO. Oregano oil exhibited the highest antibacterial activity followed by manuka and thyme oils. After the exposure to a sub-inhibitory concentration of EOs, strains displayed an increased sensitivity in more than 95% of the cases. After treatment with oregano and marjoram EOs, few strains showed a modified enterotoxins production, while 43% of the strains were no longer able to produce enterotoxins after treatment with manuka EO. The results obtained in this study highlight that exposure to sub-inhibitory concentration of EO modifies strains enterotoxins production and EOs susceptibility profile.
Assuntos
Antibacterianos/farmacologia , Enterotoxinas/metabolismo , Óleos Voláteis/farmacologia , Óleos de Plantas/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Antibacterianos/administração & dosagem , Avaliação Pré-Clínica de Medicamentos , Leptospermum/química , Testes de Sensibilidade Microbiana , Óleos Voláteis/administração & dosagem , Origanum/química , Staphylococcus aureus/metabolismo , Thymus (Planta)/químicaRESUMO
Essential oils are potential alternatives to synthetic insecticides because they have low mammalian toxicity, degrade rapidly in the environment, and possess complex mixtures of bioactive constituents with multi-modal activity against the target insect populations. Twenty-one essential oils were initially screened for their toxicity against Aedes aegypti (L.) larvae and three out of the seven most toxic essential oils (Manuka, oregano, and clove bud essential oils) were examined for their chemical composition and combined toxicity against Ae. aegypti larvae. Manuka essential oil interacted synergistically with oregano essential oil and antagonistically with clove bud essential oil. GC-MS analysis revealed the presence of 21 components in Manuka essential oil and three components each in oregano and clove bud essential oils. Eugenol (84.9%) and eugenol acetate (9.6%) were the principal constituents in clove bud essential oil while carvacrol (75.8%) and m-isopropyltoluene (15.5%) were the major constituents in oregano essential oil. The major constituents in Manuka essential oil were calamenene (20%) and 3-dodecyl-furandione (11.4%). Manuka essential oil interacted synergistically with eugenol acetate and antagonistically with eugenol, suggesting that eugenol was a major contributor to the antagonistic interaction between Manuka and clove bud essential oils. In addition, Manuka interacted synergistically with carvacrol suggesting its contribution to the synergistic interaction between Manuka and oregano essential oils. These findings provide novel insights that can be used to develop new and safer alternatives to synthetic insecticides.
Assuntos
Aedes , Inseticidas/análise , Óleos Voláteis/química , Animais , Óleo de Cravo/química , Sinergismo Farmacológico , Larva , Leptospermum/química , Origanum/química , Testes de ToxicidadeRESUMO
AIM: Contact lens induced dry eye affects approximately 50% of contact lens wearers. The aim was to assess the effects of Manuka (Leptospermum sp.) honey eye drops (Optimel, Melcare, Australia) on dry eye in contact lens wearers. The safety of the honey eye drops in contact lens wear and contact lens wearers' compliance were also evaluated. DESIGN: Prospective, randomised, cross over study, examiner masked, pilot treatment trial. METHODS: Twenty-four participants aged 20 to 55 years with contact lens related dry eye were recruited and randomised to two treatment groups; 20 completed the study. One group used Optimel eye drops twice a day for two weeks followed by conventional lubricant (Systane Ultra, Alcon) therapy for two weeks; the other group completed the treatments in the reverse order. Before and after each treatment dry eye symptomology, ocular surface inflammation, and tear quantity and quality were assessed. Participants completed a daily log detailing their usage of treatments and any issues. RESULTS: Dry eye symptoms improved significantly after Optimel treatment. Patients with more severe symptoms at baseline showed a greater improvement in symptoms. No significant differences were observed in the objective signs of dry eye; presumably because of the short treatment duration. Seventy-five% of contact lens wearers reported good adherence to Optimel treatment and 95% reported no issues using this product. CONCLUSIONS: Optimel Eye Drops reduce the symptoms of dry eye in contact lens wearers and are safe to use. A longer treatment period to assess the effect on clinical signs of dry eye is required.