Anti-elastase Activity Research Articles

Ocimum sanctum Linn. as a natural source of skin anti-ageing compounds

Ocimum sanctum Linn., widely used in food preparation, has been reported for several biological beneficial activities and thus potential for treatment of various health conditions. However, the biological activities related to skin anti-ageing, including anti-collagenase, anti-elastase, and anti-hyaluronidase activities, have not been reported so far. Therefore, this study aimed to investigate the skin anti-ageing activity of O. sanctum extracts. The aerial part of O. sanctum was extracted by fractionated extraction using n-hexane, ethyl acetate, and ethanol, respectively. Rosmarinic acid and total phenolic content was investigated. Antioxidant activity was determined by in vitro methods. Anti-inflammatory activity was investigated according to the inhibition of nuclear factor kappa B (NF-κB) expression and interleukin-6 (IL-6) secretion. The anti-ageing activity was investigated by in vitro inhibition of collagenase, elastase, and hyaluronidase activities. The ethanolic extract of O. sanctum, which had the highest yield (6.5%), contained the highest rosmarinic acid (19.3% w/w) and the highest total phenolic content (50.2 ± 0.6 mg gallic acid/g sample). Additionally, it possessed the most potent antioxidant activity with the Trolox equivalent antioxidant capacity of 270.1 ± 15.1 μM/mg, equivalent concentration of 459.3 ± 91.4 μM/mg, and inhibition against 2, 2-diphenyl-1-picrylhydrazyl radical of 34.0 ± 0.7%. The ethanolic extract also showed the highest anti-inflammatory activity with the inhibition against IL-6 secretion and NF-κB expression of 54.7 ± 3.1% and 79.3 ± 9.6%, respectively. Moreover, it also exerted the highest inhibition against matrix metallopeptidase-1 and hyaluronidase with the inhibition of 77.7 ± 9.0% and 98.1 ± 0.1%, respectively. Rosmarinic acid was found as the major compound responsible for those anti-ageing activities. Therefore, the ethanolic extract of O. sanctum is an attractive natural source of anti-skin ageing ingredient for further applications in cosmetic and/or cosmeceutical industry.

Antioxidant, anti-urease and anti-elastase activities of Usnea longissima Ach.

Lichens are complex associations composed of mycobiont and one or more algae or cyanobacteria which are living in symbiosis. Lichens are thought to possess therapeutic effects on many illnesses in worldwide. This study was performed to investigate antioxidant, anti-elastase and anti-urease activities of Usnea longissima Ach lichen. U. longissima was extracted with ethanol and ethyl acetate solvents. The antioxidant activities of the extracts of U. longissima were determined with methods such as 1,1-diphenyl-2- picrylhydrazyl (DPPH) radical scavenging activity, 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid (ABTS) radical scavenging activity, copper reducing antioxidant capacity (CUPRAC), total antioxidant capacity, determination of total phenolic content and total flavonoid contents. The binding action of the DPPH and ABTS radicals, CUPRAC activity increases with concentration of the extracts. Ethanol extracts exhibited higher anti-urease and anti-elastase activity. Highest inhibition was found as 49.86% for elastase and 18.38% for urease. Results of the present study suggest that U. longissima extracts can be an alternative to synthetic antioxidant, anti-elastase and anti-urease agents.

Antioxidant and anti-inflammatory properties of Prosopis cineraria based phenolic rich ointment in wound healing

Oxidative stress and inflammation are the critical factors attributed with delay in wound repairing process. Traditionally Prosopis cineraria (L.) Druce (PC) is used for swift healing of cutaneous wounds. Since there is lack of scientific claim of this medicinal plant on wounds, the main focus of present study was to explore the wound healing effect of PC in rats by using excision and incision wound model as well as biochemical estimation along with inflammatory markers. Considering these facts, ethyl acetate, chloroform and butanol fractions of PC hydroethanolic extract (EFPC, CFPC, BFPC, respectively) investigated for determination of antioxidant activity by in vitro method and then strongest activity possessing fraction was further quantitatively analyzed by HPLC-DAD analysis. in vitro anti-inflammatory and enzyme (collagenase and elastase) inhibitory effect of BFPC were investigated to confirm underlying mechanism of action for wound healing process. BFPC was observed as most active fraction against free radicals among all and presence of protocatechuic acid, chlorogenic acid, ferulic acid and caffeic acid was confirmed by HPLC-DAD analysis. Results showed that BFPC has significant anti-inflammatory as well as anti-collagenase and anti-elastase activities. Application of BFPC ointment for 16 consecutive days on the dorsal wound area of rats confirmed the faster wound repairing process, higher hydroxyproline content, reduction in epithelialization period and inflammatory markers in blood as compared to control group. Histological analysis also endorsed the results by promoting collagen formation, re-epithelialization, angiogenesis and mainly the restoration of cutaneous appendages, i. e., hair follicles. Results of current study implicate that BFPC has potential to act as effective cutaneous wound healing agent.

Phytoconstituents, antioxidant, sun protection and skin anti-wrinkle effects using four solvents fractions of the root bark of the traditional plant Alkanna tinctoria (L.)

IntroductionProtection of skin from wrinkles and pigmentation changes are among the most common challenges for modern science and cosmetics. These are caused by unusual disruption of connective tissue, the formation of free radicals and ultraviolet radiation.The current research is the first study to compare the phytoconstituents, antioxidant, sun protection factor (SPF) and skin wrinkles prevention effects using four different solvents fractions for the traditional plant Alkanna tinctoria (L.) root bark. MethodsQualitative and quantitative phytoconstituents, antioxidant activity, sun protection factor and anti-elastase (skin wrinkles prevention) effects were assessed using standard pharmaceutical and cosmeceuticals assays. ResultsThe results of antioxidant, anti-elastase and sun protection factor activities were the highest for the acetone fraction with IC50 8.51 ± 1.94 μg/ml, 10.02 ± 0.3 μg/ml and SPF value of 6.38, respectively. However, these results may occur due to its high contents of flavonoids and phenols which were 26.55 ± 1.6 mg of QUE/g and 59.48 ± 0.56 mg of GAE/g plant acetone fraction, respectively. ConclusionThe acetone fraction of A. tinctoria root bark could be a promising candidate for cosmetic and pharmaceutical preparations due to the potential antioxidant, anti-elastase enzyme and sun protection activities.

In vivo wound-healing activity of Euphorbia characias subsp. wulfenii: Isolation and quantification of quercetin glycosides as bioactive compounds

Ethnopharmacological relevanceThe latex and the aerial parts of Euphorbia characias L. (Euphorbiaceae) have been used as medicinal plant to treat wounds and warts in traditional medicine. Aim of the studyThe effect of the plant extract was tested in vivo and in vitro with experimental models to find scientific evidence for traditional use in wound healing. Potentially active wound-healer compounds were isolated from the active fraction using fractionation procedures under the guidance of biological assay and the possible role of the compounds in the wound healing process was also determined. Material and methodsN-hexane, ethyl acetate, and methanol extracts were successively prepared from the aerial parts of E. characias subsp. wulfenii. The extracts were tested with linear incision, circular excision wound models and the hydroxyproline assay method to assess the wound-healing activity. The inhibition of the increase in capillary permeability induced by acetic acid, an acute inflammation model, was used to assay the anti-inflammatory activity. Different chromatographic separation techniques on sephadex and silica gel columns, and bioassay guided assay techniques have been used to isolate the active compounds of the plant. Moreover, hyaluronidase, collagenase and elastase enzymes inhibitory effect of active principle were investigated in vitro to find out the mechanism of action. ResultsThe methanol (MeOH-ex) extract of the aerial parts of E. characias subsp. wulfenii showed significant wound healing activity (linear incision wound model: 43.04%; circular excision wound model 65.24%) and anti-inflammatory activity (34.74%). The methanol extract was separated into its fractions by column chromatography for isolation of efficient compounds. Biological activity of the fractions were assessed and further isolation and purification processes have been carried out in the active fraction. Isolation studies were carried out from the MeOH-ex fraction to obtain active constituents and their structures were elucidated to be quercetin-3-O-rhamnoside (quercitrin), quercetin-3-O-galactoside (hyperoside), and quercetin-3-O-arabinoside (guaijaverin). Further in vitro and in vivo assays showed that quercetin derivatives were responsible for the wound-healing activity of the plant, and also found to be significant anti-elastase and anti-collagenase activities. The amounts of three compounds, isolated from active fraction, were determined by using high performance liquid chromatography. Calibration equation was calculated with dilutions, prepared from pure substances, and assay was performed in total extract, prepared from E. characias subsp. wulfenii. It was detected that the plant had 1.22% quercitrin, 0.35% hyperoside, and 0.11% guaijaverin. The validation of the analytical method was performed by linearity, precision, limit of detection, and limit of quantification parameters. ConclusionPresent study supported the traditional use of the aerial parts E. characias subsp. wulfenii as wound healer and quercetin derivatives were isolated as active components from the active fraction by using bioassay-guided fractionation technique.

Chemical composition and antifungal activities of Ziziphora tenuir and Z. clinopodioides essential oils against dermatophytes

Summary Introduction: Ziziphora species are traditionally used for treatment of different infectious and non-infectious diseases as antiseptic agents. Objective: The aim of this study was to evaluate the chemical composition of Ziziphora clinopodioides and Z. tenuir essential oils and their antifungal effects againt five strains of dermatophytes. Methods: GC and GC-MS methods were used for essentional oils analize. The anti-elastase activities were determined by porcine pancreatic elastase assays. Results: 48 different compounds were identified in these two essential oils, which thymol, p-cymene, 1,8-cineole and γ-terpinene were their major components. The anti-dermatophyte activities of essential oils against dermatophytes showed that the essential oils (150 ppm) inhibited the mycelium growth, about 5–100%, which Z. clinopodioides essential oil had higher mycelium growth inhibition (28–100%) than that of Z. tenuir oil. The MIC and MFC values of essential oils were 0.01–1 µl/ml. 0.5 µl/ml essential oils inhibited porcine pancreatic elastase, dose-dependently. Conclusions: Due to the anti-dermatophyte and anti-elastase effects of Ziziphora sp., it can be considered as natural antifungal agent for more clinical and pre-clinical trials.

Antiacne-causing Bacteria, Antioxidant, Anti-Tyrosinase, Anti-Elastase and Anti-Collagenase Activities of Blend Essential Oil comprising Rose, Bergamot and Patchouli Oils

Blended essential oil comprising rose, bergamot and patchouli (RBP) oils with the volume ratio of 6:3:1, respectively have been tested for various biological activities. The blended oil showed antimicrobial activity against Propionibacterium acnes and Staphylococcus epidermidis with minimum inhibitory concentration (MIC) of 0.003125 %v/v and 0.125 %v/v, respectively. For antioxidant, blended oil showed the half inhibitory concentration (IC50) at 0.67 %v/v and 0.14 %v/v while tested with 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-azinobis(3-ethylbenzothiazoline-6 sulphonic acid) (ATBS) assays, respectively. Blended oil also has anti-tyrosinase activity with 45±4.6%tyrosinase inhibition at 4 mg/mL concentration using modified dopachrome method. However it has no activity on anti-collagenase and anti-elastase.

Point Mutation of a Non-Elastase-Binding Site in Human α1-Antitrypsin Alters Its Anti-Inflammatory Properties.

Human α1-antitrypsin (hAAT) is a 394-amino acid long anti-inflammatory, neutrophil elastase inhibitor, which binds elastase via a sequence-specific molecular protrusion (reactive center loop, RCL; positions 357-366). hAAT formulations that lack protease inhibition were shown to maintain their anti-inflammatory activities, suggesting that some attributes of the molecule may reside in extra-RCL segments. Here, we compare the protease-inhibitory and anti-inflammatory profiles of an extra-RCL mutation (cys232pro) and two intra-RCL mutations (pro357cys, pro357ala), to naïve [wild-type (WT)] recombinant hAAT, in vitro, and in vivo. His-tag recombinant point-mutated hAAT constructs were expressed in HEK-293F cells. Purified proteins were evaluated for elastase inhibition, and their anti-inflammatory activities were assessed using several cell-types: RAW264.7 cells, mouse bone marrow-derived macrophages, and primary peritoneal macrophages. The pharmacokinetics of the recombinant variants and their effect on LPS-induced peritonitis were determined in vivo. Compared to WT and to RCL-mutated hAAT variants, cys232pro exhibited superior anti-inflammatory activities, as well as a longer circulating half-life, despite all three mutated forms of hAAT lacking anti-elastase activity. TNFα expression and its proteolytic membranal shedding were differently affected by the variants; specifically, cys232pro and pro357cys altered supernatant and serum TNFα dynamics without suppressing transcription or shedding. Our data suggest that the anti-inflammatory profile of hAAT extends beyond direct RCL regions. Such regions might be relevant for the elaboration of hAAT formulations, as well as hAAT-based drugs, with enhanced anti-inflammatory attributes.

Alpha-1 Antitrypsin Inhibits ATP-Mediated Release of Interleukin-1β via CD36 and Nicotinic Acetylcholine Receptors.

While interleukin (IL)-1β is a potent pro-inflammatory cytokine involved in host defense, high levels can cause life-threatening sterile inflammation including systemic inflammatory response syndrome. Hence, the control of IL-1β secretion is of outstanding biomedical importance. In response to a first inflammatory stimulus such as lipopolysaccharide, pro-IL-1β is synthesized as a cytoplasmic inactive pro-form. Extracellular ATP originating from injured cells is a prototypical second signal for inflammasome-dependent maturation and release of IL-1β. The human anti-protease alpha-1 antitrypsin (AAT) and IL-1β regulate each other via mechanisms that are only partially understood. Here, we demonstrate that physiological concentrations of AAT efficiently inhibit ATP-induced release of IL-1β from primary human blood mononuclear cells, monocytic U937 cells, and rat lung tissue, whereas ATP-independent IL-1β release is not impaired. Both, native and oxidized AAT are active, suggesting that the inhibition of IL-1β release is independent of the anti-elastase activity of AAT. Signaling of AAT in monocytic cells involves the lipid scavenger receptor CD36, calcium-independent phospholipase A2β, and the release of a small soluble mediator. This mediator leads to the activation of nicotinic acetylcholine receptors, which efficiently inhibit ATP-induced P2X7 receptor activation and inflammasome assembly. We suggest that AAT controls ATP-induced IL-1β release from human mononuclear blood cells by a novel triple-membrane-passing signaling pathway. This pathway may have clinical implications for the prevention of sterile pulmonary and systemic inflammation.

Inhibition of UVB-induced pro-inflammatory cytokines and MMP expression by Zanthoxylum rhetsa bark extract and its active constituent hesperidin.

The antiphoto aging property of Zanthoxylum rhetsa obtained from Pangkor Island, Malaysia, was evaluated. Solvent fractions of different polarity obtained from the methanolic extract of the bark material were initially tested for anticollagenase and antielastase activities. The ethyl acetate fraction showed bioactivity against the protease enzymes. Hence, it was subjected to further purification via column chromatography, to yield a major constituent, hesperidin. Subsequently, the ethyl acetate fraction and hesperidin were tested for their effects against UVB-induced cytotoxicity and expressions of inflammatory cytokines (IL-6, IL-1β, and TNF-α), NF-κB, and MMPs (MMP1, 3, and 9) in human dermal fibroblasts (HDF). Both fraction and pure compound prevented UVB-induced cytotoxicity in HDF cells, in a dose dependent manner. Moreover, the ethyl acetate fraction inhibited the increase of pro-inflammatory cytokines induced by UVB to a level similar to the control (without UV treatment). Additionally, the fraction significantly inhibited the expressions of NF-κB, MMP 1, MMP 3, and MMP 9 in HDF cells treated with UVB. Similar effects were observed with hesperidin. The results obtained suggested that the ethyl acetate fraction of Z.rhetsa and its bioactive constituent, hesperidin, have the potential to be used as active ingredients in sunscreen and antiphoto aging formulations.

Investigations of anti-aging potential of Hypericum origanifolium Willd. for skincare formulations

Skin aging is caused by increased activation of extracellular matrix disruption enzymes, oxidative stress and DNA damage. Inhibition of these mechanisms by natural plants may be an encouraging approach to prevent skin aging. Hypericum is medically important plant and a source of several promising compounds. Nevertheless, there are no studies about the anti-aging potential of Hypericum origanifolium Willd (Guttiferae). The purpose of this study was to research the anti-collagenase, anti-elastase and anti-hyaluronidase effects, together with the antioxidant and genotoxic/antigenotoxic activities of H. origanifolium. Ethanol extract of H. origanifolium harvested from Turkey was tested for anti-collagenase, anti-elastase and anti-hyaluronidase activities. The extract inhibited collagenase and elastase activity. The highest ECM-degrade enzyme inhibition was demonstrated against collagenase (79.39%). The phenolic constituent and antioxidant activity were tested by Folin-Ciocalteu method (FCM), 2,2-dipenyl-1-picrylhydrazyl (DPPH) radical-scavenging and β-carotene bleaching assay. The total phenol content revealed to be 93.4 ± 1.6 mg GAE/g dry extract. IC50 values observed in DPPH and β-carotene bleaching assays were 270 ± 0.1 and 230 ± 0.2 μg/mL, respectively. Finally, the extract was investigated for its genotoxic/antigenotoxic effects using Ames Salmonella/microsome test system. Results indicated no sign of mutagenicity, and depending upon the concentration, the antigenotoxicity was noted with an inhibition of mutagenicity going from 21.54 to 84.90%. The results suggest that H. origanifolium can be considered as new natural sources to be potentially used as anti-aging ingredients in skin care formulations.

Antioxidants, anticollagenase and antielastase potentials of ethanolic extract of ripe sesoot (Garcinia picrorrhiza Miq.) fruit as antiaging

Introduction: Nitric oxide (NO) is a free radical that belongs to reactive nitrogen species (RNS). The excess amount of NO in body generates physical changing on skin as a consequence of alteration in connective tissue through formation of lipid peroxides, cell content, and enzymes. These free radicals induce damage to extracellular matrix (ECM) and are responsible in reducing skin elasticity. Antioxidants possess significant role in delaying aging process by scavenging free radicals and preventing collagenase and elastase enzymes activities. This study aimed to evaluate antioxidants, anticollagenase and antielastase potentials of ethanolic extract of ripe sesoot (Garcinia picrorrhiza Miq.) fruit (GpKar) as antiaging remedy. Methods: Antioxidant activity was performed by NO scavenging activity assay, while anti-aging activity was performed through inhibitory effects of collagenase and elastase activities. Results: In antioxidant activity, GpKar had lower NO scavenging activity (IC50=1530.34 μg/mL) compared to xanthone (IC50=85.40 μg/mL). In collagenase inhibitory activity, GpKar also had lower inhibition collagenase activity (IC50= 1169.31 μg/mL) compared to xanthone (IC50= 286.32 μg/mL). In elastase inhibitory activity, GpKar had lower inhibition elastase activity (IC50= 152.93 μg/mL) compared to xanthone (IC50= 21.26 μg/mL). Conclusion: In summary, GpKar and its compounds possess antioxidant, anticollagenase, and antielastase activities for antiaging, and might be beneficial in these subjects.

Anti-elastase and anti-collagenase potential of Lactobacilli exopolysaccharides on human fibroblast

Polysaccharides could be used as biodegradable and biocompatible polymers for scaffolds and carriers matrix. Numerous algal, fungi and herbal polysaccharides can attenuate degradation of skin matrix by the inhibition of elastase, collagenase and matrix metalloproteinases (MMPs). In this study, we investigate anti-elastase and anti-collagenase potential of Lactobacilli exopolysaccharides (LEPS) on normal human fibroblast. Among 60 Lactobacilli isolated from herbal plants and dairy products, selected LEPS showed high anti-collagenase (up to 100%), anti-elastase (up to 87%) and antioxidant activity (up to 60%). Most of them had no cytotoxicity effect on fibroblast, and some of them promote cell proliferation (up to 10%). In scratch assay, all the investigated EPSs stimulated wound healing process in fibroblast (up to 99%). MMP1, MMP2, MMP3, MMP9 and MMP10 were down-regulated significantly and TIMP1 and TIMP2 were up-regulated slightly in LEPS of B9-1 from L. casei with high anti-collagenase and anti-elastase activity; however, no meaningful alteration was observed in MMPs expression level for LEPS of P35 from L. plantarum with low anti-collagenase and anti-elastase activity. By consideration of high anti-collagenase, anti-elastase, antioxidant activity and wound healing of LEPS, they could be considered as good candidate of skin anti-aging agents for tissue engineering and skin regeneration scaffolds.

Anti-aging potential of extracts from Sclerocarya birrea (A. Rich.) Hochst and its chemical profiling by UPLC-Q-TOF-MS

BackgroundDegradation of components of the extracellular matrix such as elastin and collagen by elastase and collagenase accelerates skin aging. Phytochemicals that inhibit the activity of these enzymes can be developed as anti-aging ingredients. In this study, an investigation of the anti-aging properties of Sclerocarya birrea (A. Rich.) Hochst (Marula) extracts was conducted in vitro with the aim of developing chemically characterized anti-aging ingredients.MethodsMarula stems, leaves and fruits were extracted using methanol:dichloromethane (DCM) (1:1). The stems were later extracted using acetone, ethanol, methanol:DCM (1:1) and sequentially using hexane, DCM, ethyl acetate and methanol. The stem ethanol extract was defatted and concentrated. Elastase and collagenase inhibition activities of these extracts and Marula oil were determined using spectrophotometric methods. The chemical profile of the ethanolic stem extract was developed using Ultra-performance-liquid chromatography quadrupole-time-of-flight mass spectrometry (UPLC-Q-TOF-MS) with MassLynx software. Pure standards were used to confirm the identity of major compounds and were screened for anti-elastase and anti-collagenase activity.ResultsMarula stems extracts were the most active as they exhibited anti-elastase activity comparable to that of elafin (> 88%) and anti-collagenase activity as potent as EDTA (> 76%). The leaf extract had moderate anti-elastase activity (54%) but was inactive agains collagenase. Marula fruits and oil exhibited limited activity in both assays. The ethanolic extract of Marula stems was the most suitable based on its acceptability to the cosmetic industry and its anti-collagenase activity (99%). Defatting and concentration improved its antiaging activity and lowered the colour intensity. Six compounds have been tentatively identified in the chemical profile of the ethanolic extract of Marula stems of which four; quinic acid, catechin, epigallocatechin gallate and epicatechin gallate have been confirmed using pure standards. Epigallocatechin gallate and epicatechin gallate were as potent (p < 0.05) as EDTA at 5 μg/ml in the anti-collagenase assay.ConclusionsThe ethanolic extract of Marula stems can be developed into an anti-aging ingredient as it exhibited very good in vitro anti-aging activity and its chemical profile has been developed. Epicatechin gallate and epigallocatechin gallate contribute to the anti-aging activity of Marula stem ethanol extract.

Inhibitory Effect of Excoecaria Agallocha L. Extracts on Elastase and Collagenase and Identification of Metabolites Using HPLC-UV-MS Techniques

The present study is aimed at evaluating the anti-elastase and anti-collagenase activity and determining the active constituents of Excoecaria agallocha L. plant extracts. Ethanol extracts of E. agallocha exhibit highest extraction yield (23%) and greater total content of phenolic compounds and flavonoids as compared to other extracts. At a concentration of 80 μg/mL, the ethanol extract produced more significant (p < 0.01) inhibition of elastase (82.7%) and collagenase (76.12%) activity and acted as a non-competitive inhibitor. Fourteen flavonoids were identified in the active ethanol extract. Further studies will provide direct way to the development of elastase and collagenase inhibitors from E. agallocha.

Poly herbal formulation with anti-elastase and anti-oxidant properties for skin anti-aging

BackgroundSkin forms an important part of human innate immune system. Wrinkles, thinning and roughening of skin are some of the symptoms that affect the skin as it ages. Reactive oxygen species induced oxidative stress plays a major role in skin aging by modulating the elastase enzyme level in the skin. Extrinsic factors that affect skin aging such as UV radiation can also cause malignant melanoma. Here we selected four medicinal plant materials, namely, leaves of Nyctanthes arbor-tristis, unripe and ripe Aegle marmelos fruit pulp and the terminal meristem of Musa paradisiaca flower and investigated their anti-aging properties and cytotoxicity in vitro individually as well as in a poly herbal formulation containing the four plant extracts in different ratios.MethodsThe phytochemical contents of the plant extracts were investigated for radical scavenging activity and total reducing power. Based upon its anti-oxidant properties, a poly herbal formulation containing leaves of Nyctanthes arbor-tristis, unripe and ripe fruit pulp of Aegle marmelos, and the terminal meristem of Musa paradisiaca flower in the ratio 6:2:1:1 (Poly Herbal Formulation 1) and 1:1:1:1 (Poly Herbal Formulation 2), respectively were formulated.ResultIt has been observed that the Poly Herbal Formulation 1 was more potent than Poly Herbal Formulation 2 due to better anti-oxidant and anti-elastase activities in NIH3T3 fibroblast cells. In addition Poly Herbal formulation 1 also had better anti-cancer activity in human malignant melanoma cells.ConclusionBased on these results these beneficial plant extracts were identified for its potential application as an anti-aging agent in skin creams as well as an anti-proliferation compound against cancer cells.

In-vitro evaluation of antioxidant, anti-elastase, anti-collagenase, anti-hyaluronidase activities of safranal and determination of its sun protection factor in skin photoaging

Safranal, a monoterpene aldehyde, is present as one of the main volatile constituents of Crocus sativus Linn. (saffron flowers). This volatile constituent not only contributes to the aroma of saffron but has been reported to possess antidiabetic, antiulcer, antiasthamatic, anticonvulsant, antidepressant, cardioprotective, anticancer and UV protective properties. Most of these therapeutic actions are contributed by its potential to quench reactive oxygen species (ROS). Antioxidant properties of phytoconstituents are now being explored for developing photoprotective skin formulations. These bioactives have the potential to protect the epidermal and dermal layers of the skin which mainly comprises of elastin and collagen. When UV rays penetrate the dermal layers, there is an increased production of elastase, collagenase and hyaluronidase leading to degradation of collagen, elastin and hyaluronic acid respectively. These dermal components are responsible to provide strength, elasticity and moisture to the skin. Due to frequent exposure to sunlight, these conditions tend to augment leading to wrinkle formation and sagging of skin.Although antioxidant properties of safranal have been established on various cell lines but till date no studies have been reported regarding the dermal enzyme inhibition activities. In the current research work, a comprehensive in vitro evaluation of antioxidant, anti-elastase, anti-collagenase, anti-hyaluronidase activities of safranal along with determination of sun protection factor (SPF) was carried out. The in vitro antioxidant activity was carried out by diphenylpicrylhydrazyl (DPPH) method and its IC50 value was found to be 22.7 μg/ml. The enzyme inhibition IC50 values of safranal for anti elastase activity were found to be 43.6 μg/ml, 70 μg/ml for antihyaluronidase activity and 9.4 μg/ml for anticollagenase activity. Photoprotective activity of safranal was determined by UV absorbance method and SPF calculated by Mansur equation which was found to be 6.6.The significant inhibitory activity of safranal on matrix metalloproteinases (MMPs) responsible for aging and a higher SPF established that this bioorganic molecule is a strong photoprotective agent. Its established free radical scavenging capability along with above characteristics make it a valuable component to be incorporated into herbal antiaging formulations.

Cosmetic and Skincare Benefits of Cultivated Mycelia from the Chinese Caterpillar Mushroom, Ophiocordyceps sinensis (Ascomycetes).

Mushrooms are potential sources of novel natural cosmeceutical ingredients. This study was conducted to evaluate the cosmetic (skincare) benefits of the valuable medicinal species Ophiocordyceps sinensis (=Cordyceps sinensis). The mycelial extracts of 2 O. sinensis strains, Cs-HK1 and Cs-4, prepared sequentially with ethyl acetate, ethanol, and hot water were tested with in vitro assays for tyrosinase-, collagenase-, and elastase-inhibitory activity. The ethyl acetate extracts of both fungal strains showed potent antityrosinase and antielastase activity, with low half-maximal inhibitory concentrations (0.14-0.47 mg/mL) comparable to those of the respective reference compounds (arbutin and epigallocatechin gallate). All mycelial extracts exhibited moderate or significant anticollagenase activity; most extracts showed a significant photoprotective effect with a sun protection factor up to 25. The results from this study show the potential use of O. sinensis as a source of cosmetic ingredients for skincare applications.

Synthesis and Biological Evaluation of S-Substituted Perhalo-2-nitrobuta-1,3-dienes as Novel Xanthine Oxidase, Tyrosinase, Elastase, and Neuraminidase Inhibitors

S-substituted perhalo-2-nitrobuta-1,3-dienes 3a, b were synthesized by the reaction of polyhalo-2-nitrobuta-1,3-dienes 1a, b with allyl mercaptan. 1-(2,3-Dibromopropanethio)-4-bromo-1,3,4-trichloro-2-nitrobuta-1,3-diene 4 was obtained from the addition of bromine to S-substituted polyhalo-2-nitrobuta-1,3-diene 3b in carbon tetrachloride. Sulfoxides 5a, b, and 6 were obtained from the reaction of thiosubstituted polyhalonitrobutadienes 3a, b, and 4 with m-CPBA in CHCl3. The structures of the new compounds were determined by spectroscopic data (FTIR, 1H NMR, 13C NMR, MS). These compounds exhibited antixanthine oxidase, antityrosinase, antielastase, and antineuraminidase activities.

Impact of HIV infection on α1-antitrypsin in the lung.

Emphysema is one of the most common lung diseases in HIV+ individuals. The pathogenesis of HIV-associated emphysema remains unclear; however, radiographic distribution and earlier age of presentation of emphysema in the lungs of HIV+ patients are similar to deficiency of α1-antitrypsin (A1AT), a key elastase inhibitor in the lung. Reduced levels of circulating A1AT in HIV+ patients suggest a potential mechanism for emphysema development. In the present study we asked if A1AT levels and activity in the bronchoalveolar lavage fluid (BALF) differ in HIV+ and HIV- patients with and without emphysema. A1AT levels were measured by ELISA in plasma and BALF from a cohort of 21 HIV+ and 29 HIV- patients with or without emphysematous changes on chest CT scan. To analyze A1AT function, we measured elastase activity in the BALF and assessed oxidation and polymerization of A1AT by Western blotting. Total A1AT was increased in the BALF, but not in the plasma, of HIV+ compared with HIV- patients, regardless of the presence or absence of emphysema. However, antielastase activity was decreased in BALF from HIV+ patients, suggesting impaired A1AT function. Higher levels of the oxidized form of A1AT were detected in BALF from HIV+ than HIV- patients, which may account for the decreased antielastase activity. These findings suggest that, in the lungs of HIV+ patients, posttranslational modifications of A1AT produce a "functional deficiency" of this critical elastase inhibitor, which may contribute to emphysema development.