Collagenase Inhibitory Activity Research Articles

Investigation of Antioxidant and Enzyme Inhibitory Activities of Echinophora chrysantha: Microwave-Assisted Hydrodistillation and SPME Analysis of its Essential Oils.

Echinophora genus is represented by six species in Türkiye, including three endemics. The objective of this study was to ascertain the antioxidant, tyrosinase, and collagenase inhibitory activities and to analyse the volatile oil and extracts derived from E. chrysantha using GC/MS/SPME. The antioxidant and enzyme inhibition activities were evaluated using spectrophotometric methods. The findings indicated that the methanol extract of E. chrysantha exhibited the highest antioxidant activity. Furthermore, both the methanol extract and volatile oil of the plant demonstrated potent inhibitory effects on tyrosinase and collagenase. A total of 84 volatile compounds were identified from the hydrodistilled oil obtained using a microwave oven, and 23 compounds were detected by the solid-phase microextraction (SPME) method. The most frequently occurring volatile components were α-Phellandrene, o-Cymene, p-Cymene, E-β-Farnesene, Carotol, trans-Caryophyllene, and β-Phellandrene. The results of this study indicate that E. chrysantha has the potential to be developed for the treatment of hyperpigmentation issues and anti-aging applications. Furthermore, it may also have applications in pharmacology, cosmetics and the food industry.

Evaluation of Biotechnological Active Peptides Secreted by Saccharomyces cerevisiae with Potential Skin Benefits.

Biotechnological active peptides are gaining interest in the cosmetics industry due to their antimicrobial, anti-inflammatory, antioxidant, and anti-collagenase (ACE) effects, as well as wound healing properties, making them suitable for cosmetic formulations. The antimicrobial activity of peptides (2-10 kDa) secreted by Saccharomyces cerevisiae Ethanol-Red was evaluated against dermal pathogens using broth microdilution and challenge tests. ACE was assessed using a collagenase activity colorimetric assay, antioxidant activity via spectrophotometric monitoring of nitrotetrazolium blue chloride (NBT) reduction, and anti-inflammatory effects by quantifying TNF-α mRNA in lipopolysaccharides (LPS)-exposed dermal fibroblasts. Wound healing assays involved human fibroblasts, endothelial cells, and dermal keratinocytes. The peptides (2-10 kDa) exhibited antimicrobial activity against 10 dermal pathogens, with the Minimum Inhibitory Concentrations (MICs) ranging from 125 µg/mL for Staphylococcus aureus to 1000 µg/mL for Candida albicans and Streptococcus pyogenes. In the challenge test, peptides at their MICs reduced microbial counts significantly, fulfilling ISO 11930:2019 standards, except against Aspergillus brasiliensis. The peptides combined with MicrocareⓇ SB showed synergy, particularly against C. albicans and A. brasilensis. In vitro, the peptides inhibited collagenase activity by 41.8% and 94.5% at 250 and 1000 µg/mL, respectively, and demonstrated antioxidant capacity. Pre-incubation with peptides decreased TNF-α expression in fibroblasts, indicating anti-inflammatory effects. The peptides do not show to promote or inhibit the angiogenesis of endothelial cells, but are able to attenuate fibrosis, scar formation, and chronic inflammation during the final phases of the wound healing process. The peptides showed antimicrobial, antioxidant, ACE, and anti-inflammatory properties, highlighting their potential as multifunctional bioactive ingredients in skincare, warranting further optimization and exploration in cosmetic applications.

Collagenase and Tyrosinase Inhibitory Compounds from Fish Gut Bacteria Ruegeria atlantica and Pseudoalteromonas neustonica.

Ruegeria atlantica and Pseudoalteromonas neustonica are fish gut bacteria that have been isolated from the guts of Pagrus major and Acanthopagrus schlegelii, respectively. A total of 22 compounds (1-22) were isolated from these two bacteria; 16 compounds (1-16) from R. atalantica and 6 compounds (17-22) from P. neustonica. Their chemical structures were elucidated by spectroscopic and spectrometric data analysis and chemical synthesis. Compounds 11 and 13 showed strong collagenase inhibitory activity, with 31.91% and 36.43% at 20 μM, respectively, comparable to or surpassing that of the positive control epigallocatechin gallate (EGCG, 34.66%). Also, compounds 11 and 14 exhibited a mild tyrosinase inhibitory effect of 6.73% and 13.68%, respectively. All of the tested compounds displayed no significant antibacterial activity against Escherichia coli and Bacillus subtilis up to 100 μM. The collagenase- and tyrosinase-inhibitory compound 11, cyclo(l-Pro-d-Leu), was found to be stable under heat (50 °C) and UV light (254 and 365 nm) for up to 6 days. These results indicate that compound 11 could be developed into a cosmeceutical with antiaging effects.

IN VITRO ANTIOXIDANT AND ANTI-AGING ACTIVITY OF KESUM LEAVES (Polygonum minusHUDS.) ETHANOL EXTRACT

Skin aging is a biological process in humans characterized by the skin becoming rough or scaly, dry, black spots appearing, dull, and even wrinkles. The study was conducted to determine the biological activity of kesum leaves (Polygonum minus Huds.) as an anti-aging active ingredient in vitro. The process of making the extract using the maceration method. Secondary metabolites were identified using a phytochemical screening test. Antioxidant activity was measured using the free radical scavenging test of 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)(ABTS). The inhibitory effect of skin-degrading enzymes was measured by the percentage of inhibition of the collagenase enzymes. Based on phytochemical screening, the ethanolic extract of kesum leaves contains flavonoids, saponins, and tannins. The results of the antioxidant activity of kesum leaves have an IC50value of 41.46 g/mL and are included in the category of strong antioxidants. The results of collagenase enzyme inhibition showed that at concentrations of 50, 100, and 200 g/mL, collagenase activity could inhibit collagenase activity by 83%, 82%, and 82%. Based on the results of the research that has been carried out, it was found that the ethanol extract of the tested kesum leaves has antioxidant activity and has the potential to anti-aging.

Protective Effects of the Postbiotic Levilactobacillus brevis BK3 against H2O2-Induced Oxidative Damage in Skin Cells.

Postbiotics have various functional effects, such as antioxidant, anti-inflammatory, and anti-obesity. Levilactobacillus brevis BK3, the subject of this study, was derived from lactic acid bacteria isolated from Kimchi, a traditional Korean fermented food. The antioxidant activity of BK3 was confirmed through the measurements of 2,2-diphenyl-1-picryl-hydrazyl (DPPH), 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and total antioxidant capacity (TAC). The wrinkle improvement effect was validated by assessing elastase inhibitory activity and collagenase inhibitory activity. The intracellular activity was confirmed using human keratinocytes (HaCaT) and human fibroblasts (HFF-1). BK3 protects skin cells from oxidative stress induced by H2O2 and reduces intracellular reactive oxygen species (ROS) production. In addition, the expressions of the antioxidant genes superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx) were upregulated. Meanwhile, matrix metalloproteinase-1 (MMP-1) and collagen type I alpha 1 (COL1A1), involved in collagen degradation and synthesis, were significantly regulated. These results suggest the possibility of utilizing BK3 as a functional ingredient with antioxidant and wrinkle-improving effects.

Potential of Bioactive Protein and Protein Hydrolysate from Apis mellifera Larvae as Cosmeceutical Active Ingredients for Anti-Skin Aging.

This study aimed to extract bioactive proteins and protein hydrolysates from Apis mellifera larvae and assess their potential application in cosmetics as well as their irritation properties. The larvae were defatted and extracted using various mediums, including DI water, along with 0.5 M aqueous solutions of sodium hydroxide, ascorbic acid, citric acid, and hydrochloric acid. Subsequently, the crude proteins were hydrolyzed using the Alcalase® enzyme. All extracts underwent testing for antioxidant activities via the 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) and Griess assays. Anti-aging properties were evaluated in terms of anti-collagenase and anti-hyaluronidase effects. Irritation potential was assessed using the hen's egg chorioallantoic membrane (HET-CAM) test. The results revealed that the sodium hydroxide extraction showed promising outcomes in terms of yield, protein content, and effectiveness in inhibiting hyaluronidase, with the highest inhibition at 78.1 ± 1.5%, comparable to that of oleanolic acid. Conversely, crude protein extracted with ascorbic acid and its hydrolysate showed notable antioxidant and collagenase-inhibitory activities. Remarkably, their anti-collagenase effects were comparable to those of ascorbic acid and lysine. Additionally, it demonstrated safety upon testing with the CAM. In conclusion, the findings provided valuable insights into the utilization of A. mellifera larval proteins as active ingredients with a wide range of cosmeceutical applications, particularly due to their antioxidant, anti-aging, and low irritation properties, which hold significant promise for anti-skin wrinkles.

Study on Chemical Composition and Biological Activity of Psidium guajava Leaf Extracts.

Guava (Psidium guajava) is a plant widely distributed in tropical and subtropical regions. Its leaves contain a large amount of physiological molecules such as flavonoid, sesquiterpene, triterpenoid, coumarin, alkaloid, and tannin molecules with antioxidative and anti-inflammatory effects. In this study, the use of concentrated P. guajava leaf extract molecules as a functional natural material was evaluated by confirming the extract's antioxidative, antibacterial, tyrosinase activity inhibition, and collagenase activity inhibition effects and its trans-2-nonenal removal ability. As a result of the analysis of the antioxidant and antibacterial components of concentrated P. guajava leaf extract molecules through GC-MS, a large amount of aromatic hydrocarbon molecules were detected. When different concentrations of ethanol were used for extraction, the leaf extract concentrated with 70% ethanol showed the most effective active molecules. As a result of measuring DPPH radical scavenging activity, a concentration-dependent antioxidant activity was confirmed. The antioxidant activity tended to increase when the ethanol content used for extraction was increased. Molecules such as 2,4-di-tert-butylphenol, caryophyllene oxide, and γ-muurolene in P. guajava leaf extract concentrate appeared to have antibacterial activities against S. aureus bacteria known to cause atopy. As ethanol content increased, the inhibitory effect on tyrosinase activity was increased. In addition, when ethanol content was 50%, the concentrated leaf extract was able to remove trans-2-nonenal by 52.4%. As a result of determining the concentrated leaf extract's collagenase inhibition activity, an inhibition rate close to that of ascorbic acid, a positive control, was confirmed. The concentrated guajava leaf extract molecules were confirmed to have whitening and wrinkle-improving functionality. Thus, the P. guajava leaf extract has high potential as a food and natural cosmetic material.

Volatiles from French and Croatian Sea Fennel Ecotypes: Chemical Profiles and the Antioxidant, Antimicrobial and Antiageing Activity of Essential Oils and Hydrolates.

Sea fennel is a halophytic plant rich in valuable nutritional components and is characterized by pleasant organoleptic properties. While its essential oils (EOs) are well investigated, there are no reports on the volatiles from their corresponding hydrolates, which are the main by-products of EO isolation, as well as on their biological activity. Therefore, the composition and biological activities of EOs and corresponding hydrolates of sea fennel from Atlantic (French, FRA) and Mediterranean (Croatian, CRO) ecotypes were investigated and compared. The EO from the CRO sample was characterized by an abundance of sabinene and limonene, while that from the FRA ecotype was rich in dillapiol and carvacryl methyl ether. The CRO hydrolate was rich in terpinen-4-ol and 10-(acetylmethyl)-3-carene, while dillapiol, thymyl methyl ether and γ-terpinene were the main compounds in the FRA sea fennel hydrolate. The biological activities of the EOs and hydrolates were evaluated for their antioxidant (with DPPH, NO, FRAP and ORAC bioassays), antimicrobial (against some Gram+ and Gram- spoilage bacteria) and antiageing (tyrosinase, elastase and collagenase inhibition) activities. Both EOs showed low reducing powers and antiradical activities while the ability of both hydrolates to quench NO was slightly higher (35-39% if inhibition). The FRA EO showed low activity against Staphylococcus aureus (8 mm), while CRO moderately inhibited the growth of P. aeruginosa (8 mm), but strongly inhibited the other two bacterial strains. While the French EO showed no antityrosinase and anticollagenase activity, the Croatian oil significantly inhibited both enzymes (IC50 of 650 µg/mL and IC50 of 2570 µg/mL, respectively) probably due to the dominance of limonene and sabinene. Neither EO exhibited antielastase properties, while the hydrolates from both ecotypes showed no antiageing activity, regardless of the enzyme tested. The EOs from the aerial parts of sea fennel from FRA and CRO differed greatly in composition, resulting in different activities. The Croatian samples appeared to have better biological properties and are therefore good candidates for applications as preservatives or antiageing agents.

Inhibition of Photoaging by Anthocyanin Metabolites Derived from Rose Petal Extract.

Rose petal extract (RPE) shows a significant antioxidant effect through its anthocyanin content. However, the mechanism underlying the anti-aging effects of orally administered RPE remains unclear. This study aims to describe the anti-aging effect and mechanism of action of orally administered RPE in ultraviolet (UV)B-induced skin aging. This study evaluates the protein expression of collagen type I alpha 1 (COL1A1) and matrix metalloproteinase 1 (MMP-1) and the mRNA expression of hyaluronic synthase 2 (HAS2) in human dermal fibroblasts. In addition, the hyaluronidase and collagenase inhibitory activities of RPE are confirmed. To evaluate the anti-aging effects of RPE, SKH-1 hairless mice are administered RPE daily for 12 weeks. Wrinkle formation, transepidermal water loss (TEWL), and skin moisture loss induced by UVB irradiation are suppressed in the dorsal skin of SKH-1 hairless mice orally administered RPE. Oral administration of RPE suppresses UVB irradiation-induced collagen disruption and reduction of hyaluronic acid. To find the bioactive compound in the RPE, serum protocatechuic acid (PCA), an anthocyanin metabolite, is analyzed using liquid chromatography-tandem mass spectrometry (LC-MS/MS). Anthocyanins in RPE are metabolized to PCA in the body and circulated through the bloodstream to exhibit anti-aging effects on the skin.

Lactobacillus brevis 발효가 참꽃마리(Trigonotis radicans var. sericeas) 에탄올 추출물의 항산화, 미백 및 주름 개선 활성에 미치는 영향

This study was designed to compare the effects on antioxidant, whitening, and anti-wrinkle improvement of 60% ethanol extracts from Trigonotis radicans var. sericea (TR) and Lactobacillus brevis-fermented T. radicans var. sericea (FTR). The total phenolics contents of TR was 18.6 mg/g, and FTR was 18.2 mg/g. The HPLC analysis confirmed more phenolic compounds were produced in FTR by bioconversion than in TR. The FTR showed higher 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity than TR. The results of the 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation decolorization assay, FTR and TR showed higher activity than BHT (positive control). The FTR (1.21-1.29 PF) showed higher antioxidant protection factor (PF) activity than the TR (1.15-1.22 PF) and showed higher tyrosinase, collagenase and elastase inhibitory activities. This results showed L. brevis-fermentation of Trigonotis radicans var. sericea changed the composition profile and has effects on antioxidant, whitening and anti-wrinkle improvement.

Skin protective effect of Indian gooseberry and barley sprout complex on skin dryness, wrinkles, and melanogenesis by cell models.

UV radiation is a major factor contributing to DNA damage in skin cells, including stem cells and mesenchymal stem cells, leading to the depletion of these crucial cells. This study examined whether a mixture of Indian gooseberry and barley sprout (IB) could inhibit UVB irradiation and 3-isobutyl-1-methylxanthine (IBMX)-induced photoaging and oxidative stress in the skin using HaCaT, Hs27, and B16F10 cells. The moisturizing-related factors, the collagen synthesis-related c-Jun N-terminal kinase (JNK)/c-Fos/c-Jun/matrix metalloproteinases (MMPs) pathway, and the melanogenesis-related cyclic adenosine monophosphate (cAMP)/protein kinase A (PKA)/cAMP-responsive binding protein (CREB)/melanocyte inducing transcription factor (MITF)/tyrosinase-related protein (TRP)/tyrosinase activation pathways were analyzed in vitro by an enzyme-linked immunosorbent assay, real-time polymerase chain reaction, and Western blot analysis. The IB complex increased the hyaluronic acid and sphingomyelin levels and the collagenase inhibitory activity, enhanced hydration-related factors, including collagen, hyaluronic acid synthase (HAS), elastin, long chain base subunit 1 (LCB1) (serine palmitoyltransferase; SPT), and delta 4-desaturase sphingolipid 1 (DEGS1), modulated the inflammatory cytokines levels, antioxidant enzyme activities and the NF-κB/MMPs/cyclooxygenase-2 (COX-2) pathway in UVB-irradiated HaCaT cells, and inhibited wrinkle formation by down-regulation of the JNK/c-Fos/c-Jun/MMP pathway and up-regulation of the transforming growth factor-β receptor I (TGFβR1)/small mothers against decapentaplegic homolog (Smad3)/procollagen type І pathway in UVB-irradiated Hs27 cells. Moreover, the IB complex prevented melanin production by down-regulating the PKA/CREB/MITF/TRP-1/TRP-2 pathway in IBMX-induced B16F10 cells. These findings suggest that the IB complex has the potential to serve as a safeguard, shielding the skin from UVB radiation-induced photo-damage.

Strain inhibition of bacterial collagenase is consistent with a collagen fibril uncrimping mechanism in rat tail tendons

Mechanical strain inhibits bacterial collagenase from cleaving collagen. Additionally, the toe region of a soft tissue’s force–elongation curve arises from sequentially engaging collagen fibrils as the tissue lengthens. Together, these phenomena suggest that mechanical strain may gradually inhibit collagenase activity through a soft tissue’s toe region. Therefore, this investigation sought to test this hypothesis.92 rat tail tendon fascicles from 3 female sentinel animals underwent preliminary stiffness tests, and their force–elongation curves were fit to a collagen distribution model. This distribution-based model calculated the force magnitude corresponding to p% of collagen fibril engagement. Specimens were separated into one of five levels of p, and that level of force was maintained for two hours while being exposed to 0.054 U/mL of bacterial collagenase from C. histolyticum. The specimens were strained to failure following the creep test, and the relative reduction in stiffness was quantified to estimate the fraction of digested fibrils.Every 10% additional collagen engagement corresponded to a 6.3% (97% highest density interval: 4.3 – 8.4%) retention of stiffness, which indicated collagenase inhibition.The results of this investigation were consistent with a strain-inhibition hypothesis along with the established uncrimping mechanism in the toe region. These results support an interaction between mechanical strain and collagenolysis, which may be valuable for disease prevention or treatment.

Effect of Electron-Beam Irradiation on Functional Compounds and Biological Activities in Peanut Shells.

Peanut shells, rich in antioxidants, remain underutilized due to limited research. The present study investigated the changes in the functional compound content and skin aging-related enzyme inhibitory activities of peanut shells by electron-beam treatment with different sample states and irradiation doses. In addition, phenolic compounds in the peanut shells were identified and quantified using ultra-performance liquid chromatography with ion mobility mass spectrometry-quadrupole time-of-flight and high-performance liquid chromatography with a photodiode array detector, respectively. Total phenolic compound content in solid treatment gradually increased from 110.31 to 189.03 mg gallic acid equivalent/g as the irradiation dose increased. Additionally, electron-beam irradiation significantly increased 5,7-dihydroxychrome, eriodictyol, and luteolin content in the solid treatment compared to the control. However, liquid treatment was less effective in terms of functional compound content compared to the solid treatment. The enhanced functional compound content in the solid treatment clearly augmented the antioxidant activity of the peanut shells irradiated with an electron-beam. Similarly, electron-beam irradiation substantially increased collagenase and elastase inhibitory activities in the solid treatment. Mutagenicity assay confirmed the stability of toxicity associated with the electron-beam irradiation. In conclusion, electron-beam-irradiated peanut shells could serve as an important by-product with potential applications in functional cosmetic materials.

Effect of etchant containing an Urushiol monomer from lacquer sap on dentin biostability and bonding performance.

Objectives: This study aimed to evaluate the effectiveness of urushiol as an additive to surface acid etchant on dentin structure, by assessing the biostability of dentin, and determine the bonding strengths of dentin and enamel to the composite in the complicated oral microecology. Methods: Etchants with different concentrations of urushiol (0.5, 1, or 3 wt%) were formulated and tested for their bonding performance. Demineralized dentin beams that were etched with experimental etchants were incubated in simulated body fluid solutions by evaluating the weight decrement after 1month. The effects of urushiol on dentin and matrix metalloproteinases were confirmed by scanning electron microscopy (SEM). Moreover, the antibiotic actions of urushiol on the common cariogenic bacteria Streptococcus mutans, Streptococcus sanguinis, and Streptococcus gordonii as well as the biofilm were evaluated, and its effect on bacterial morphology was observed by scanning electron microscopy. Finally, enamel and dentin specimens were prepared from human molars to determine the depth of demineralization by the etchants and the relationship with the resin bond strengths to enamel and dentin (μTBS) and the morphology of the bonding interface. Results: Urushiol could interact with dentine and inhibit collagenase activity, resulting in biostable dentine. The application of the etchants containing 0.5, 1, or 3 wt% urushiol significantly improved the durability of the dentin bonding interface with its instinctive antibacterial property (p < 0.05). Conclusion: Urushiol not only improves dentin stability by interacting with collagen and inactivating MMP activity but also plays a role in the antibacterial effects in the complicated oral microecology. The effectiveness of urushiol etchant prolongs the longevity of bonded dental restorations without compromising clinical operation time.

Anti-aging and Antimicrobial Effects of the Stems and Roots of Sedum kamtschaticum in Cosmetic Production

Purpose: Sedum kamtschaticum Fisch. (SK), a plant native to Korea, was studied as a natural preservative and antiaging cosmetic ingredient.Methods: The stems and roots of SK were separated; extracted through reflux with 70% ethanol; and fractionated with n-hexane, chloroform, ethyl acetate, n-butyl alcohol, and water. The ethyl acetate fractions were evaluated for their antiaging effects, including antiglycation activity and elastase and collagenase inhibitory activity. Their antimicrobial activity on seven microorganisms was evaluated using the paper disk diffusion method and challenge test. In addition, the stability of lotion formulations and skin penetration were assessed using the Franz diffusion cell method.Results: The ethyl acetate fractions of SK with the best antioxidant effects exhibited better antiglycation and collagenase-inhibitory activity than the positive control as well as excellent antibacterial effects against Escherichia coli and Staphylococcus aureus. Emulsion formulations containing 0.05% and 0.1% SK stem extract exhibited synergistic preservative effects. The SK stem extract displayed the ability to penetrate into an artificial membrane and human cadaver skin.Conclusion: SK extracts can be used as antiaging and antimicrobial cosmetic materials.

Antioxidant, Collagenase Inhibitory, and Antibacterial Effects of Bioactive Peptides Derived from Enzymatic Hydrolysate of Ulva australis.

The protein extract of Ulva australis hydrolyzed with Alcalase and Flavourzyme was found to have multi-functional properties, including total antioxidant capacity (TAC), collagenase inhibitory, and antibacterial activities. The #5 fraction (SP5) and #7 fraction (SP7) of U. australis hydrolysate from cation-exchange chromatography displayed significantly high TAC, collagenase inhibitory, and antibacterial effects against Propionibacterium acnes, and only the Q3 fraction from anion-exchange chromatography displayed high multi-functional activities. Eight of 42 peptides identified by MALDI-TOF/MS and Q-TOF/MS/MS were selected from the results for screening with molecular docking on target proteins and were then synthesized. Thr-Gly-Thr-Trp (TGTW) displayed ABTS [2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid)] radical scavenging activity. The effect of TAC as Trolox equivalence was dependent on the concentration of TGTW. Asn-Arg-Asp-Tyr (NRDY) and Arg-Asp-Arg-Phe (RDRF) exhibited collagenase inhibitory activity, which increased according to the increase in concentration, and their IC50 values were 0.95 mM and 0.84 mM, respectively. Peptides RDRF and His-Ala-Val-Tyr (HAVY) displayed anti-P. Acnes effects, with IC50 values of 8.57 mM and 13.23 mM, respectively. These results suggest that the U. australis hydrolysate could be a resource for the application of effective nutraceuticals and cosmetics.

Antioxidant, antitumoral, antimetastatic effect and inhibition of collagenase enzyme activity of Eleutherine bulbosa (Dayak onion) extract: In vitro, in vivo and in silico approaches

Ethnopharmacological relevanceEleutherine bulbosa (Mill.) Urb., known in Brazil as “marupazinho”, is a medicinal plant native to the Amazon region. The bulbs of this species are traditionally used in the form of tea or consumed in natura (salads) for the treatment of hypertension, diabetes, gastrointestinal problems, breast cancer, and female fertility. It has been reported that this species possess cytotoxic compounds with anticancer action and limited underlying mechanisms. Aim of the studyThis study aimed to analyze extract of E. bulbosa bulbs and evaluate antioxidant activity, antitumor and antimetastatic effects against murine B16F10-Nex2 melanoma cells, and collagenase inhibitory activity by in vitro, in vivo, and in silico approaches. Materials and methodsDetermination of total polyphenols, flavonoids and anthocyanins content were performed. In addition, high performance liquid chromatography-mass spectrometry (HPLC-MS) was carried out to identify phytoconstituents from extract. Antioxidant evaluation was performed using DPPH radical scavenging, ferric ion reducing antioxidant power (FRAP), Thiobarbituric acid reactive species (TBARS) and nitric oxide (NO) tests. Antitumoral and antimetastatic activities of extract on murine B16F10-Nex2 melanoma cells were determined and inhibitory activity on collagenase was evaluated. Molecular interactions between compounds and DNA or collagenase was evaluated by molecular docking analyses. ResultsPhytochemical evaluation demonstrated the presence of polyphenols, flavonoids and anthocyanins, and HPLC-MS identified the major presence of eleutherin, isoeleutherin and eleutherinol. Antioxidant evaluation showed that the extract present significant activity in all methods evaluated. In silico assay demonstrated interaction between bioactive compounds and DNA or collagenase. In addition, extract exhibited antitumor and antimetastatic actions promoted by melanoma cells and showed collagenase inhibitory activity. ConclusionsThe results showed that E. bulbosa bulb extract contains bioactive compounds as flavonoids, anthocyanins and quinones of which may be responsible for the antioxidant, antitumor, antimetastatic and collagenase enzyme inhibitory activity observed in this study by in vivo, in vitro and in silico bioassays.

Biological Activities of Ceratonia siliqua Pod and Seed Extracts: A Comparative Analysis of Two Cretan Cultivars.

Ceratonia siliqua L., commonly known as the carob tree, appears in most Mediterranean countries, often cultivated for the collection of its fruits to be used as food for humans and animals. This study was aimed at the phytochemical characterization of two common Cretan C. siliqua cultivars and the biological evaluation of deseeded pod and seed extracts regarding their putative use in cosmetics. Gas and liquid chromatographic techniques were used to assess their essential oil, fatty acid, and carbohydrate profiles. Cell-free assays, including free-radical scavenging; the inhibition of tyrosinase and collagenase; the blocking of advanced glycation end product (AGE) formation; along with assays in human skin fibroblast cultures, i.e., reactive oxygen species suppression, glutathione stimulation, and protection from oxidative stress and from ultraviolet (UVB) radiation, were also used. Extracts from both cultivars were found to possess antioxidant capacity, tyrosinase- and collagenase-inhibitory activities, an ability to block glucose-induced AGEs, and in certain cases, UVB absorbance and photoprotective activities. Seed extracts were in general more active, while the use of 30% aqueous methanol seemed to be more efficient than n-hexane for extraction. Serial partition of the most active extracts resulted in fractions with enriched biological activities. These properties make Cretan carob extracts and their fractions suitable candidates for use in cosmetics.

Bioprospecting of microalgae for a potential use as enzyme inhibitors, anti-ageing and prebiotic agents

Microalgae are an important source of biologically active metabolites and hold prominence towards pharmaceutical and nutraceutical applications. The current research focused on the discovery of new bioresources with interesting neuroprotective, anti-ageing, prebiotic and anti-diabetic potential. Ethanol extracts from Chlamydomonas sp.EL5, Chloroidium saccharophilum.Mon1, and Nostoc. sp were bioprospected for high value biomolecules. Chlamydomonas sp.EL5 had the highest carotenoids content (1.2 mg/gDE) whereas Nostoc sp. had higher total phenolic content (52.5 mgGAE/gDE). All species had potent (>50% inhibition), and moderate (30–50% inhibition) cholinesterase inhibitory activity. The highest anti-diabetic performance (64%) was detected in Nostoc sp.‘s extract at 5 mg/ml. The extracts had a prominent capacity to chelate Fe2+ ions even at low concentration (1 mg/ml). The potential value in preventing skin aging could be confirmed through potential of Chlamydomonas sp.EL5 on free radical scavenging ability and collagenase inhibitory activity. The increase in the Lactobacillus plantarum growth performance indicated that these microalgae are serious candidates to be considered as prebiotics. GC–MS analysis indicated that linoleic acid (C18:2 ω6) and linolenic acid (C18:3 ω3) are the ones with the highest content among the unsaturated fatty acids. These results strongly suggest that the studied microalgae could be considered sources of high-value co-products that could be used to upgrade the pharmaceutical, cosmeceutical and/or food products value.

Beneficial Bio-Extract of Camellia sinensis var. assamica Fermented with a Combination of Probiotics as a Potential Ingredient for Skin Care

Biotechnology, cosmetics, and aesthetic remedies are now inextricably intertwined due to the production of alternative, more effective, and safer active ingredients. Additionally, there has been an increase in demand for natural cosmetic ingredients across the globe. Camellia sinensis var. assamica (Miang tea) is a good alternative because of several biological activities, and is commercially cultivated as a resource in northern Thailand. The process of fermentation mediated by probiotics can enhance the bioavailability of compounds, transform bioactive compounds, and decrease chemical solvent use for sustainability. This study aims to apply the functional evaluation of Miang tea bio-extracts to promote skin health. On the basis of their bioactive enzymes, β-glucosidase, and antioxidant properties, the strains Lacticaseibacillus rhamnosus (previously Lactobacillus rhamnosus), Lactiplantibacillus plantarum (previously Lactobacillus plantarum), and Saccharomyces cerevisiae were used as mixed probiotic starter cultures. The activities of white, green, and black Miang tea bio-extracts, including ferric reducing antioxidant power, lipid peroxidation, nitric oxide inhibition, tyrosinase inhibition, collagenase inhibition (MMP-1 and MMP-2), and antimicrobial activity, were all considerable after 7 days of fermentation time. Additionally, phenolic antioxidant compounds (gallic acid, epigallocatechin gallate, caffeic acid, caffeine, and p-coumaric acid) were identified. The current study’s findings can determine the most effective fermentation time and dose of bio-extract, as well as suggest improvements in bioactive compounds for use in skin care formulations. These results will be used for testing on human participants in further work.