Azorean Black Tea (Camellia sinensis) Antidermatophytic and Fungicidal Properties.

The treatment of dermatophytoses, the most common human fungal infections, requires new alternatives. The aim of this study was to determine the antidermatophytic activity of the aqueous Azorean Black Tea extract (ABT), together with an approach to the mechanisms of action. The phytochemical analysis of ABT extract was performed by HPLC. The dermatophytes susceptibility was assessed using a broth microdilution assay; potential synergies with terbinafine and griseofulvin were evaluated by the checkerboard assay. The mechanism of action was appraised by the quantification of the fungal cell wall chitin and ß-1,3-glucan, and by membrane ergosterol. The presence of ultrastructural modifications was studied by Transmission Electron Microscopy (TEM). The ABT extract contained organic and phenolic acids, flavonoids, theaflavins and alkaloids. It showed an antidermatophytic effect, with MIC values of 250 µg/mL for Trichophyton mentagrophytes, 125 µg/mL for Trichophyton rubrum and 500 µg/mL for Microsporum canis; at these concentrations, the extract was fungicidal. An additive effect of ABT in association to terbinafine on these three dermatophytes was observed. The ABT extract caused a significant reduction in ß-1,3-glucan content, indicating the synthesis of this cell wall component as a possible target. The present study identifies the antidermatophytic activity of the ABT and highlights its potential to improve the effectiveness of conventional topical treatment currently used for the management of skin or mucosal fungal infections.

Biological activities of organic extracts and specialized metabolites from different parts of Cryptomeria japonica (Cupressaceae) - A critical review.

Forest operations and wood industry generate large amounts of residues that are discarded in the field and cause environmental pollution. However, these biomass residues are still raw materials to obtain value-added products, such as essential oils, organic/aqueous extracts and resins that are among the great natural sources of bioactive metabolites. Thus, in recent years, the scientific community is giving special attention to their valorization. To date, different uses of biomass residues have been proposed, such as a source of renewable energy, fertilizers, animal feed and bioactive molecules. In this context, Cryptomeria japonica biomass residues (e.g., bark and its exudate, heartwood, sapwood, leaves, cones and roots) represent a source of diverse specialized metabolites (e.g., sesqui-, di-, tri- and sesquarterpenes, flavonoids, lignans and norlignans) with potential application in different fields, particularly in the agrochemical, food, cosmeceutical, pharmaceutical, phytomedicine and esthetic, due to their valuable multi-bioactivities determined over the last decades. Thus, this review provides an overview of the reported biological activities of organic extracts/fractions and their specialized metabolites obtained from different parts of C. japonica, in order to encourage the alternative uses of C. japonica wastes/byproducts, and implement a sustainable and circular bioeconomy.

Bromelain, a Group of Pineapple Proteolytic Complex Enzymes (Ananas comosus) and Their Possible Therapeutic and Clinical Effects. A Summary.

Bromelain is a complex combination of multiple endopeptidases of thiol and other compounds derived from the pineapple fruit, stem and/or root. Fruit bromelain and stem bromelain are produced completely distinctly and comprise unique compounds of enzymes, and the descriptor "Bromelain" originally referred in actuality to stem bromelain. Due to the efficacy of oral administration in the body, as a safe phytotherapeutic medication, bromelain was commonly suited for patients due to lack of compromise in its peptidase efficacy and the absence of undesired side effects. Various in vivo and in vitro studies have shown that they are anti-edematous, anti-inflammatory, anti-cancerous, anti-thrombotic, fibrinolytic, and facilitate the death of apoptotic cells. The pharmacological properties of bromelain are, in part, related to its arachidonate cascade modulation, inhibition of platelet aggregation, such as interference with malignant cell growth; anti-inflammatory action; fibrinolytic activity; skin debridement properties, and reduction of the severe effects of SARS-Cov-2. In this paper, we concentrated primarily on the potential of bromelain's important characteristics and meditative and therapeutic effects, along with the possible mechanism of action.

Afrostyrax lepidophyllus Mildbr. and Monodora myristica (Gaertn.) Dunal Extracts Decrease Doxorubicin Cytotoxicity on H9c2 Cardiomyoblasts.

MATERIALS AND METHODS: Bark extracts of these plants (1 and 25 µg/mL) were added 3 hours before coincubating H9c2 cardiomyoblasts with Dox (0.5 and 1 µM) for 24 hours more. We measured cell mass and metabolic viability, mitochondrial transmembrane potential, superoxide anion content, and activity-like of caspase-3 and caspase-9 following treatment with the extracts and/or Dox. Also, selenium and vitamin C contents were measured in the plant extracts. RESULTS: The results confirmed that Dox treatment decreased cell mass, mitochondrial membrane potential and metabolic viability, increased mitochondrial superoxide anion, and stimulated caspase-3 and caspase-9-like activities. Pretreatment of the cells with the plant extracts significantly inhibited Dox cytotoxicity, with more significant results at the higher concentration. Measurements of selenium and vitamin C in the extracts revealed higher concentration of both when compared with other Cameroonian spices. CONCLUSION: Both extracts of A. lepidophyllus and M. myristica were effective against Dox-induced cytotoxicity, most likely due to their content in antioxidants.

Seasonal Variability of the Biochemical Composition and Antioxidant Properties of Fucus spiralis at Two Azorean Islands.

This study evaluates, for the first time, the seasonal (winter and summer) and geographical (São Miguel⁻SMG and Santa Maria⁻SMA Islands) variability of Fucus spiralis (Fs) biochemical composition (dry weight basis) and antioxidant properties. Protein and carbohydrates presented higher values in Fs-SMGwinter, lipids, total dietary fiber, and energy value in Fs-SMAsummer, and ash and soluble dietary fiber/insoluble dietary fiber ratio in Fs-SMAwinter. The fatty acid (FA) profiles showed a lower SFA in Fs-SMGsummer, whereas MUFA and PUFA presented higher values in Fs-SMGsummer and Fs-SMGwinter, respectively. Excellent dietary ratios of n6/n3 PUFA and hypocholesterolemic/hypercholesterolemic FA were found, with lower values in Fs-SMAwinter and higher in Fs-SMGsummer, respectively. The highest total phenolics was found in Fs-SMAsummer acetone:water extract and total flavonoids showed the higher value in Fs-SMGwinter methanol extract. The best free radical-scavenging activity was observed in the Fs-SMAwinter methanol (EC50 = 0.045 mg/mL) and acetone:water (EC50 = 0.059 mg/mL) extracts. The ferric-reducing antioxidant power showed the best results in Fs-SMAwinter methanol extract (EC50 = 0.016 mg/mL) and Fs-SMAsummer acetone:water extract (EC50 = 0.017 mg/mL). The best ferrous ion-chelating activity was found in Fs-SMGwinter acetone:water extract. Overall, results revealed that F. spiralis nutritional and functional bioactivity values have geographical and seasonal variations and that its regular consumption may add benefits to human health.

Angiotensin I-Converting Enzyme (ACE) Inhibitory Activity, Antioxidant Properties, Phenolic Content and Amino Acid Profiles of Fucus spiralis L. Protein Hydrolysate Fractions.

Food protein-derived hydrolysates with multi-bioactivities such as antihypertensive and antioxidant properties have recently received special attention since both activities can play significant roles in preventing cardiovascular diseases. This study reports, for the first time, the angiotensin I-converting enzyme (ACE)-inhibition and antioxidant properties of ultrafiltrate fractions (UF) with different molecular weight ranges (<1, 1-3 and ≥3 kDa) obtained from Fucus spiralis protein hydrolysate (FSPH) digested with cellulase-bromelain. The amino acids profile, recovery yield, protein, peptide and total phenolic contents of these FSPH-UF, and the in vitro digestibility of F. spiralis crude protein were also investigated. FSPH-UF ≥3 kDa presented remarkably higher ACE-inhibition, yield, peptide and polyphenolic (phlorotannins) contents. Antioxidant analysis showed that FSPH-UF <1 kDa and ≥3 kDa exhibited significantly higher scavenging of 2,2-diphenyl-1-picrylhydrazyl radical and ferrous ion-chelating (FIC) activity. FSPH-UF ≥3 kDa had also notably higher ferric reducing antioxidant power (FRAP). Strong correlations were observed between ACE-inhibition and antioxidant activities (FIC and FRAP). The results suggest that ACE-inhibition and antioxidant properties of FSPH-UF may be due to the bioactive peptides and polyphenols released during the enzymatic hydrolysis. In conclusion, this study shows the potential use of defined size FSPH-UF for the prevention/treatment of hypertension and/or oxidative stress-related diseases.

Nutritional and Functional Bioactivity Value of Selected Azorean Macroalgae: Ulva compressa, Ulva rigida, Gelidium microdon, and Pterocladiella capillacea.

This study presents information on the biochemical composition (dry weight basis), nutritional aspects, and angiotensin I-converting enzyme (ACE) inhibitory properties of selected macroalgae (Ulva compressa, Ulva rigida, Gelidium microdon, and Pterocladiella capillacea) from Azores. Moisture content was very high (83.2% to 90.0% of fresh weight). Total dietary fiber (33.7% to 41.0%) that presented a good balance of both soluble and insoluble fibers (15.5% to 19.2% and 18.2% to 21.8%, respectively) was the most abundant component in these macroalgae. Protein and ash (ranged from 15.7% to 23.4% and 10.7% to 20.7%, respectively) were the 2nd most abundant components in red and green macroalgae, respectively. Moderate soluble carbohydrate contents (14.5% to 19.8%) were found in all species. Lipid contents were low (1.0% to 4.3%), particularly in Ulva species (1.0% to 1.7%), but contained higher unsaturated fatty acids (FAs) (7.5% to 32.9% and 29.6% to 69.2% of total FA for monounsaturated fatty acid and polyunsaturated fatty acid groups, respectively) than saturated fatty acid (23.3% to 46.8% of total FA) contents. All the macroalgal proteins had high digestibility in vitro (82.2% to 89.4%, relatively to sodium caseinate), contained high quantity of essential amino acids (45.3% to 58.1% of total amino acids), but in different proportions, and were rich in aspartic and glutamic acids that together account for 17.2% to 36.2% of the total amino acids. These results suggested that regular consumption of the selected macroalgae may improve human health and revealed that they can be used for producing food supplements for human and animal nutrition and/or pharmaceuticals with potential effect on the regional economy. Furthermore, the ACE-inhibitory IC50 values of 0.095 to 0.695 mg/mL for the <1 kDa protein hydrolysate fraction revealed a potential impact on hypertension disorder.

Health-promoting ingredients from four selected Azorean macroalgae.

This study presents, for the first time, the nutritional and health promoting aspects of four selected Azorean macroalgae (Ulva compressa, Ulva rigida, Gelidium microdon and Pterocladiella capillacea) in terms of total lipids, fatty acids (FA) profile, n6/n3 and hypocholesterolemic (h)/hypercholesterolemic (H) FA ratios, minerals, total essential amino acids (AA), anti-ageing and anti-phenylketonuria AA content, coenzyme Q10, α-tocopherol, total phenolics, antioxidant properties and energy value, on a dry weight basis. The results revealed low lipid content (1.02-4.32%) but significant PUFA content (29.57-69.22% of total FA), suitable FA ratios (0.48-9.49 for n6/n3 and 1.26-4.22 for h/H), balanced macromineral ratios (0.27-1.91 for Na/K and 0.15-1.07 for Ca/Mg), appreciable amount of essential AA (45.27-58.13% of total AA), high amount of anti-ageing AA, low Phe content, coenzyme Q10 (1.25-8.27µg/g), α-tocopherol (2.61-9.14mg/100g), high total phenolic content (27.70-55.07mg of gallic acid equivalents/g extract), significant free radical scavenging activity (29.32-47.73%) and valuable energy content (6.80-9.80kJ/g). A regular consumption of these algae either directly or through food supplements may improve human health or may have a protective effect on some diseases and ageing process. They can also be used for producing pharmaceuticals and cosmeceuticals with potential economic value.

Chemical composition and antibacterial activity of the essential oil of Ruilopezia bracteosa.

The essential oil from the leaves ofRuilopezia bracteosa was obtained by hydrodistillation, and analyzed by GC-MS. Eighteen components, which made up 99.6% of the oil were identified, the most abundant being ß-myrcene (34.2%), α-pinene (24.3%), 7-epi-α-selinene (9.1%), ß-pinene (8.5%) and 6,9-guaiadiene (4.4%). Antibacterial activity was tested against Gram-positive and Gram-negative bacteria using broth microdilution and disk agar diffusion methods. MIC values found presented significant differences between both methods, which may be due to diffusion factors.

Content of hypericins from plants and in vitro shoots of Hypericum undulatum Schousb. ex Willd.

This study reports the first quantification study of pseudohypericin (PsHyp) and hypericin (Hyp) in Hypericum undulatum Schousb. ex Willd in vitro cultures developed by a Portuguese company. Both compounds were quantified by high-performance liquid chromatography and their levels were compared with those in commercial samples of Hypericum perforatum. PsHyp was found to be the major naphthodianthrone of H. undulatum, with an average ratio of 3.73:1 compared to Hyp. Significant statistical differences were found between the content of Hyp and PsHyp in H. undulatum regenerated shoots compared to in vivo samples. The mean concentration of total Hyps varied from 178.41 to 358.93 µg g(-1) dry extract in H. undulatum regenerated shoots, which is on average two to three times less than naphthodianthrone levels found in H. undulatum in vivo and H. perforatum commercial samples. However, none of the analysed samples presented the levels of Hyps required by the European and United States Pharmacopoeias.

HPLC-UV-ESI-MS analysis of phenolic compounds and antioxidant properties of Hypericum undulatum shoot cultures and wild-growing plants.

LC-UV and LC-MS analysis were used to study the phenolic composition of water extracts of Hypericum undulatum (HU) shoot cultures and wild-growing (WG) plants. Total phenolic content (TPC), determined using the Folin-Ciocalteu assay, and the antioxidant activity measured by two complementary methods were also performed for each sample. Mass spectrometry revealed several phenolics acids with quinic acid moieties, flavonols, mostly quercetin, luteolin and apigenin glycosides, flavan-3-ols (catechin and epicatechin) and the xanthonoid mangiferin. Differences in phenolic composition profile and TPC were found between the samples. The major phenolic in HU culture-growing (CG) samples is chlorogenic acid, followed by epicatechin, quercitrin and isoquercitrin. The WG plants presents hyperoside as the main phenolic, followed by isoquercitrin, chlorogenic acid and quercetin. The TPC and antioxidant activity were higher in samples from WG plants.

Chemical composition and antibacterial activity of the essential oil of Espeletia nana.

The essential oil of the leaves of Espeletia nana Cuatrec., obtained by hydrodistillation, was analyzed by GC-MS, which allowed the identification of 24 components, which made up 99.9% of the oil. The most abundant compounds were a-pinene (38.1%), beta-pinene (17.2%), myrcene (15.0%), spathulenol (4.2%), bicyclogermacrene (4.0%), a-zingiberene (4.0%), and gamma-himachalene (3.7%). Antibacterial activity was tested against Gram-positive and Gram-negative bacteria using the agar disk diffusion method. Activity was observed only against Gram-positive bacteria. MIC values were determined for Staphylococcus aureus ATCC 25923 (200 microg/mL) and Enterococcusfaecalis ATCC 29212 (600 microg/mL).

Molluscicidal activity of crude water and hexane extracts of Hypericum species to snails (Radix peregra).

In spite of intense research on both chemical constituency and biological activity of Hypericum species, potential applications of their active components for pest control have been less well investigated. In the present study, Hypericum androsaemum (tutsan), Hypericum foliosum (malfurada), and Hypericum undulatum (wavy St. John's wort) aqueous and hexane extracts were studied for their molluscicidal and ovicidal activities against Radix peregra. The molluscicidal activity of the aqueous extracts was low, except for H. androsaemum infusion (median lethal concentration [LC50](adults) = 317.1 ppm; LC50(juveniles) = 415 ppm), and less important compared with the toxicity of all three hexane extracts tested: H. androsaemum (LC50(adults) = 30.47 ppm; LC50(juveniles) = 73.25 ppm), H. undulatum (LC50(adults) = 30.55 ppm; LC50(juveniles) = 60.54 ppm), and H. foliosum (LC50(adults) = 48.61 ppm; LC50(juveniles) = 38.81 ppm). An ovicidal effect was observed only with H. androsaemum infusion (1.85% of hatching at 500 ppm) and H. foliosum hexane extract (0.0% of hatching at 100 ppm). A preliminary phytochemical investigation of the lipophylic extracts from these Hypericum sp. revealed a different chemical profile and confirmed the presence of ursolic acid only in H. undulatum as the main compound. The present study indicates that products from hexane extracts of the Hypericum sp. analyzed may be used as potential molluscicides to control snails responsible for transmitting fasciolosis.

Comparison of the endemic Azorean Hypericum foliosum with other Hypericum species: antioxidant activity and phenolic profile.

Water extracts of Hypericum foliosum (HF) from five Azorean Islands were analysed for their antioxidant activity and total phenolic contents. The results were compared with those from medicinal Hypericum species (H. perforatum, H. androsaemum and H. undulatum) and also with Azorean green tea. HF exhibited strong scavenging activity (87-91%) and moderate inhibition of linoleic acid oxidation (56-72%), and presented no significant difference to the other studied plants; in contrast, the synthetic antioxidant butylated hydroxyltoluene showed antioxidant activity values of 22% and 88%, respectively. The average value of phenolics in HF was higher than that in the other Hypericum species and lower than that in tea. Additionally, the phenolic profiles of the Hypericum species were compared by reverse phase-high performance liquid chromatography/ultraviolet (RP-HPLC/UV). The method presented permits the simultaneous determination of phenolic acids, flavonoids, hypericin and hyperforin within 55 min. The most similar profile was observed between HF and H. androsaemum. This study indicates that HF is a source of bioactive compounds with potential health benefits.