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Potential cosmetic application of essential oil extracted from Litsea cubeba fruits from China
Abstract
Litsea cubeba essential oil (LCEO) is widely used as a flavor enhancer in cosmetics and as a folk skin-care agent in southern China. The objective of this paper is to investigate whether LCEO has biological activities that might be useful in modern skin-protection formulations. The present study results revealed that citral (57.4%) was a major component, while LCEO exhibited a potent inhibitory effect on tyrosinase (IC50 values 100 μg/mL), good antioxidative activities (IC50: 17.75 mg/mL for ABTS+., 10.2 mg/mL for O2−), and apparent protective effect against UV–TiO2–NO2−-induced protein oxidation at 0.01 mg/mL and tyrosine nitration at 0.1 mg/mL. Additionally, the biological activities of LCEO were compared with that of its main constituents. The results demonstrated that any individual major component was not the unique contributor to the high activity of LCEO. Based on these results, we suggested that LCEO could serve as a new natural skin-whitening agent.
... As two species, C. kanehirae and P. americana, from the core Lauraceae (including the Laureae-Cinnamomeae group and Persea group) 18 have already been sequenced 12,14 , we here present a chromosome-level assembly of the genome of May Chang tree (Litsea cubeba Lour.), which is from the sister clade to C. kanehirae in the core Lauraceae. It is an important species for producing essential oils (roughly 95% terpenoid) that are widely used in perfumes, cosmetics, and medicine all over the world [19][20][21] . Further, to revisit the phylogenetic position of Magnoliids relative to eudicots and monocots [11][12][13] and to study the evolutionary relationships within the Lauraceae, we sequence the genomes of 47 species of 20 genera in Lauraceae at a low coverage. ...
... Mono-TPS involved in volatiles production in Lauraceae. The essential oils produced by Lauraceae are widely used commercially, and contain a variety of components (Supplementary Table 29), such as geranial, neral, limonene, and linalool 7,12,19,20 . ...
... Transient overexpression and enzyme activity assay both demonstrated that LcuTPS22 catalyzed the accumulation of α-pinene, β-pinene, eucalyptol, camphene, eucalyptol, and camphor, which are the main volatile components of the leaves of Lauraceae species (Fig. 5). In addition, LcuTPS18, 19,20,25,26, and 42 were all highly expressed in the L. cubeba fruits ( Fig. 4 and Supplementary Fig. 17). Transient overexpression and enzyme activity assay also indicated that LcuTPS42 catalyzed the biosynthesis of linalool, phellandrene, and geraniol, which are the main components of the specific scents in Lauraceae (Fig. 5 and Supplementary Fig. 18). ...
The laurel family within the Magnoliids has attracted attentions owing to its scents, variable inflorescences, and controversial phylogenetic position. Here, we present a chromosome-level assembly of the Litsea cubeba genome, together with low-coverage genomic and transcriptomic data for many other Lauraceae. Phylogenomic analyses show phylogenetic discordance at the position of Magnoliids, suggesting incomplete lineage sorting during the divergence of monocots, eudicots, and Magnoliids. An ancient whole-genome duplication (WGD) event occurred just before the divergence of Laurales and Magnoliales; subsequently, independent WGDs occurred almost simultaneously in the three Lauralean lineages. The phylogenetic relationships within Lauraceae correspond to the divergence of inflorescences, as evidenced by the phylogeny of FUWA, a conserved gene involved in determining panicle architecture in Lauraceae. Monoterpene synthases responsible for production of specific volatile compounds in Lauraceae are functionally verified. Our work sheds light on the evolution of the Lauraceae, the genetic basis for floral evolution and specific scents.
... Citral is obtained from the essential oils (EOs) of several botanical species, including Cymbopogon schoenanthus (L.) Spreng., Litsea cubeba (Lour.) Pers., Melissa officinalis L., and Verbena officinalis L. To the best of the authors' knowledge, only L. cubeba EO has been investigated for its tyrosinase inhibitory activity [16]. Therefore, this study aims to evaluate the tyrosinase inhibitory activities of C. schoenanthus, L. cubeba, M. officinalis, and V. officinalis EOs, using an in vitro colorimetric assay, to assess whether the different chemical compositions influence the overall EO inhibitory activities via any possible synergistic, additive and/or competitive interactions between their components. ...
... As previously described, the EOs of C. schoenanthus, M. officinalis, L. cubeba, and V. officinalis present high levels of citral, which is characterized by non-competitive inhibitory activity against a fungal source of tyrosinase [8,16,21]. This study aimed at examining the in vitro tyrosinase inhibitory activities of these EOs to explore whether their inhibitory activity can be ascribed to their citral content only, or whether there are other bioactive compounds that influence the inhibitory effects of the EOs. ...
... Citral is obtained from the essential oils (EOs) of several botanical species, including Cymbopogon schoenanthus (L.) Spreng., Litsea cubeba (Lour.) Pers., Melissa officinalis L., and Verbena officinalis L. To the best of the authors' knowledge, only L. cubeba EO has been investigated for its tyrosinase inhibitory activity [16]. Therefore, this study aims to evaluate the tyrosinase inhibitory activities of C. schoenanthus, L. cubeba, M. officinalis, and V. officinalis EOs, using an in vitro colorimetric assay, to assess whether the different chemical compositions influence the overall EO inhibitory activities via any possible synergistic, additive and/or competitive interactions between their components. ...
... As previously described, the EOs of C. schoenanthus, M. officinalis, L. cubeba, and V. officinalis present high levels of citral, which is characterized by non-competitive inhibitory activity against a fungal source of tyrosinase [8,16,21]. This study aimed at examining the in vitro tyrosinase inhibitory activities of these EOs to explore whether their inhibitory activity can be ascribed to their citral content only, or whether there are other bioactive compounds that influence the inhibitory effects of the EOs. ...
Excessive melanin production causes serious dermatological conditions as well as minor aesthetic problems (i.e., freckles and solar lentigo). The downregulation of tyrosinase is a widespread approach for the treatment of such disorders, and plant extracts have often proven to be valuable sources of tyrosinase inhibitors. Citral (a mixture of neral and geranial) is an important fragrance ingredient that has shown anti-tyrosinase potential. It is highly concentrated in the essential oils (EOs) of Cymbopogon schoenanthus (L.) Spreng., Litsea cubeba (Lour.) Pers., Melissa officinalis L., and Verbena officinalis L. However, only L. cubeba EO has been investigated for use as a potential skin-whitening agent. This work evaluates the in vitro tyrosinase inhibitory activity of these EOs and studies, using bio-assay oriented fractionation, whether their differing chemical compositions influence the overall EO inhibitory activities via possible synergistic, additive, and/or competitive interactions between EOs components. The inhibitory activity of C. schoenanthus EO and that of M. officinalis EOs, with negligible (+)-citronellal amounts, were in-line with their citral content. On the other hand, L. cubeba and V. officinalis EOs inhibited tyrosinase to considerably greater extents as they contained β-myrcene, which contributed to the overall EO activities. Similar observations were made for M. officinalis EO, which bears high (+)-citronellal content which increased citral activity.
... The results indicated that L. cubeba oil is a potent N. cincticeps control agent (Chakira et al., 2017). Huang et al. (2013) reported the potential cosmeceutical properties of L. cubeba essential oil. The major component of the essential oil was citral. ...
... The individual compounds showed inferior activities in all the tests, which indicated that the bioactivity of L. cubeba essential oil was a synergistic effect of several bioactive constituents. The results claimed that L. cubeba oil could be a promising natural skin-whitening agent (Huang et al., 2013). ...
Litsea cubeba (Lour.) Pers. is a valuable essential oil-producing plant species. It is a shrub and is mostly found in India, China, Japan, Taiwan, and, Northern Thailand. L. cubeba essential oil, which is rich in citral, has been used as a traditional medicine to
treat several diseases. The fresh fruits of L. cubeba are used for the extraction of essential oil, and the oil is intense yellowish in color, fresh and has a sweet aromatic flavor. The composition of essential oil varies based on the extraction method, cultivar, plant parts, time of sampling and processing. The current manuscript summarizes the composition as well as pharmacological and economic importance of L. cubeba essential oil. The literature review revealed that the essential oil of L. cubeba exhibited antioxidant,
antimicrobial, and antiproliferative activities; also, it can be used as pesticide, repellent and fragrance agent in cosmetics. However, further studies are required to bridge the scientific gap of transferring the scientific findings into commercially valuable products.
Also, studies on the potential of L. cubeba essential oil in other possible fields like aromatherapy and cognition are desirable.
... These volatile compounds are also commercialized in pharmaceutical industry due to their potential multiple bioactivities, including anti-carcinogenic, digestive, analgesic, antioxidative, antiviral and antimicrobial properties (Koroch, Juliani, and Zygadlo 2007). In addition, these compounds are engaged in cosmetic industry because of their flavoring, antiaging and whitening functions (Huang et al. 2013). ...
... The extensive use of the fruit peel aroma compounds is also attributed to two distinctive properties: antiaging and whitening effects (Manosroi and Manosroi 2003). Antiaging effects are based on antioxidative activity by free radical scavenging, while whitening effects are due to the inhibition of tyrosinase that facilitate melanogenesis in the skin (Huang et al. 2013). Eureka lemon peel essential oil was reported as skin-whitening agent in soap, cosmetology and perfumery due to its radical scavenging components (c-terpinene, terpinolene and geraniol) and tyrosinase inhibitory components (myrcene and citral) (Matsuura, Ukeda, and Sawamura 2006). ...
Fruit peel is an agricultural by-product and potential source to extract natural aroma compounds with low cost. In the past few decades, the extraction of plant aroma volatiles experienced a transition from traditional to modern technologies. This review summarizes the main aroma compounds in different fruit peels, evaluates modern extraction techniques applicable for these aroma compounds in terms of mechanism, procedure, merits and demerits, and practice. Additionally, the applications of fruit peel aroma extract in food, pharmaceutical and cosmetic industries are also discussed. This review provides comprehensive information for extraction and application of aroma compounds from fruit peels, which could facilitate the valorization of the agricultural by-products and reduce environmental impacts.
... The essential oil and bioactive compound of L. cuceba was shown potential as antioxidant. The methanol extract, CHCl 3 fraction, and buthanolic fraction Ied to 89-90% inhibition of lipid peroxidation in TBA method (Thiobarbituric acid test) [54], [55]. The bark extract of L. glutinosa had a antioxidant activity, which showed higher metal chelating activity with IC 50 values 15.25 mg/mL [56]. ...
... LCEO exerted a potent inhibitory effect on tyrosinase (IC 50 value of 100 g/mL), good antioxidative activities (IC 50 : 17.75 mg/mL for ABTS(+.), 10.2 mg/mL for O 2 -), and an apparent protective effect on UV-TiO 2 -NO 2 induced protein oxidation at 0.01mg/mL and tyrosine nitration at 0.1 mg/mL [55]. Citral, the dominant constituent of the L. cubeba oil, possessed antiarrhythmic function in vivo. ...
ABSTRACT
The Litsea genus is one of the most diverse genera of evergreen trees belong to Lauraceae. Litsea species is an indigenous widely grown species on secondary forest and wetland in Indonesia. These genus can also be found in peat swamp forest, particularly in Kalimantan and Sumatra. The genus have been used globally in traditional medicine for treatment of variouse diseases including influenza, stomach aches, diarrhea, diabetes, vomiting, bone pain, inflammation, and other ailment. In Indonesia, utilization of Litsea have not being widely known yet. This paper aims to provide information about ethnobotany, pharmacology properties, and evaluate potential utilization related active compound of Litsea. Information on the Litsea species was collected via electronic search (using Pubmed, SciFinder, Google Scholar, and Web of Science) and a library for articles published in peer-reviewed journals. The result showed that 6 plants of genus Litsea from Indonesia were found to be potential medicinal plant. The crude extracts and the isolated metabolites of these species have exhibited in vitro and in vivo pharmacology effect, including antimicrobial activity, antioxidant activity, antiinflammatory activity, antiasthmatic activity, anticholelithogenic activity, as well as function on central nervous system.
Keywords: Litsea, medicinal plant, ethnobotany, pharmacology
... Sikkim-Darjeeling Himalayan tribe use Litsea as an antidiabetic plant (Chhetri, Parajuli & Subba, 2005). L. cubeba oil is employed as raw material in the production of citral, vitamin A, E and K, ionine and methylionine, perfumes, cosmetic application and also has anti-microbial and insecticidal properties (Jiang et al., 2009;Huang et al., 2013;Wang et al., 2016;Bajracharya & Pratigya, 2019;Wei et al., 2019). Ho et al. (2010) reported that the Litsea oil have cytotoxic activity against liver, stomach and mouth cancer. ...
Litsea cubeba (Lour.) Pers. is an evergreen, tree of laurel family native to Southeast Asia. In India, the species is found in Eastern Himalayas from Sikkim to Mishmi Hills. The fruit of the plant is a massive source of essential oil (EO) resembling citronella oil. The study explores the variation of EO content of L. cubeba fruit/seeds from 16 different populations from North East India. Sixteen numbers of populations were selected with 10 accessions for the study. Fruits were crushed to hydro distillation by using Clevenger apparatus for 5-6 h and the essential oil was extracted with dichloromethane and finally oil yield was estimated. The highest oil yield (6.15±0.05%) was extracted from Mebo area followed by Pashighat (5.47±0.1%) and Kasom Khullen (5.32±0.07%). Otherwise, Jowai (1.53±0.21%), Latyrke (1.53±0.09%) and Sohomi village (1.50±0.16%) exhibited the lowest EO yield. Variation in climato-ecological characteristics of different geographical locations influenced in oil content studied among the population. The present investigation is intended for selection of superior population with high EO yield. The study identified as superior in EO yield of Mebo and Pashighat population and could be potential for large scale cultivation and industrial utilization.
... L. cubeba fruit has the potential as a pain reliever, improve blood circulation, and relieve gastric distention, asthma, dementia, diarrhea, and injuries. The L. cubeba essential oil is widely used in cosmetics and perfume (Huang et al. 2013). ...
Aini IN, Wisanti. 2023. Characterization of morphological, micromorphological, anatomical structures and matK gene-based identification of aromatic litsea (Litsea cubeba). Biodiversitas 24: 4557-4567. Aromatic litsea or krangean (Litsea cubeba (Lour.) Persoon) has potential as a drug. L. cubeba's status based on the IUCN red list is the least concern. This research aimed to (i) characterize morphology, micromorphology, and anatomy; (ii) indetify L. cubeba species based on DNA barcodes. The research samples were collected in the Mt. Anjasmoro, East Java, Indonesia at three different altitudes. Data in the form of various characters were analyzed using the one-way ANOVA method to determine the significance of the difference. The statistical test analysis of the quantitative character of L. cubeba showed a significant difference between heights (? = 0.05). The results showed that the characterization of L. cubeba includes (i) morphology: structure of lenticels, color, and substance that coats the lower surface of leaves, type of flower, fruit taste, and aroma; (ii) micromorphology: glands lining the abaxial surface of the lamina, trichomes on both surfaces of the lamina, structure of abaxial epidermal cells, the shape of pollen, shape and distribution of exin (iii) anatomy: cuticle thickness, epidermal cell shape, and presence of secretory cells in the lamina. The molecular identification in the form of L. cubeba barcode DNA based on the matK gene marker matched the Litsea cubeba sequence in NCBI (AB259073.1).
... Many species of the family are of great economic importance. For example, the avocado (Persea americana) is a widely cultivated tropical fruit (Chen et al., 2008); the bark of the shoots of Cinnamomum aromaticum produces cinnamon (Fujita, 1967), while Litsea cubeba is an important species for essential oils widely used in perfumes, cosmetics and medicines (Huang et al., 2013;Su and Ho, 2016). However, deforestation activities have resulted in massive habitat loss and fragmentation (Wei and Jiang, 2012). ...
The family Lauraceae is characterized by numerous species and is an important element in tropical and subtropical forests in China. Altogether 99 species of the family have been considered as threatened, caused mainly by over exploitation and habitat loss, and 13 were listed in the National Key Protected Wild Plants (NKPWP, vers. 2021). However, the distribution characteristics and conservation status of these threatened species in China have not been established. Here we assemble a new distribution database of Lauraceae species in China, then analyze the geographic pattern of Lauraceae richness and the underlying environmental determinants, and further investigate the conservation status of these species. In total, our database contains 36,479 distribution records of 510 native species (including infraspecific taxa), including 2233 records of the 99 threatened species and 1066 records of the 13 NKPWP species. The results indicate that overall species richness of Lauraceae decreases with latitude, and is positively correlated with aridity index (AI), precipitation of warmest quarter (PWQ) and precipitation of coldest quarter (PCQ) while richness of threatened species is mainly influenced by isothermality (ISN) and temperature seasonality (TSN), slightly increases along ISN but decreases with TSN. Eighty-eight of the 99 endangered species (88.9% of the total) are protected in nature reserves. Eleven of the 13 NKPWP species (84.6% of the total) are distributed in different nature reserves, but two species (Cinnamomum chago and Sinopora hongkongensis) are not included in any nature reserves. The richness of NKPWP is positively correlated with the AI, but slowly decreasing with the increasing of precipitation seasonality (PSN) and PWQ. We found that 413 species (85.9% of the total) are distributed in nature reserves and the protection effectiveness of the family is high, but nine threatened species and two NKPWP species have not been conserved in any nature reserves. We propose taking in situ conservation actions urgently, especially for those species with extremely small populations including Machilus longipes, Cinnamomum chago and Sinopora hon-gkongensis. We reveal the distribution characteristics and identify conservation gaps of overall, threatened and NKPWP species of Lauraceae in China, and propose targeted strategies for further conservation, which is important for the conservation of Lauraceae in China.
... Studies on the essential oil of Litsea cubeba, including optimization of the extraction process of Litsea cubeba essential oil (Huang et al., 2021), analysis of essential oil components from different parts of Litsea cubeba (Ho et al., 2021;Wang et al., 2010), and rich biological characteristics of Litsea cubeba essential oil such as antioxidant activity (Jae- Kwan et al., 2005) and antibacterial or antifungal activity Wu et al., 2019). There are also some studies on the application of Litsea cubeba essential oil, including the potential application of Litsea cubeba essential oil in the cosmetic industry (Huang et al., 2013) and the possibility of Litsea cubeba essential oil as an e cient and environmentally friendly antifungal fumigant (Li et al., 2016). In addition, the medical application of Litsea cubeba has been extensively studied in recent years. ...
Litsea cubeba (Lour.) Pers. is an important spice plant in southern China. The whole plant of Litsea cubeba contains essential oils, among which the fruit has the highest essential oil content. And there is a significant market demand and widespread use of essential oil of Litsea cubeba fruit. However, there are few systematic studies on the growth and development of the Litsea cubeba fruit. This study aims to determine the regularity of annual changes in fruit morphology, essential oil content, and components of Litsea cubeba essential oil to determine the optimal harvest period and improve the utilization efficiency of Litsea cubeba resource. The results show that the annual change of fruit morphology of Litsea cubeba was consistent with the double "S" curve, which shows a general trend of rapid growth first, then slow growth, and finally rapid growth again. While the annual change of the essential oil of Litsea cubeba fruits was consistent with a single "S" curve, which shows a general trend of slow growth first, then rapid growth, and finally decreasing rapidly. Correlation analysis showed a significant negative correlation between morphological changes and essential oil accumulation in Litsea cubeba fruit. Combining the growing periods of fruit morphology and essential oil accumulation, the growth and development of Litsea cubeba fruit can be divided into four general periods: the first rapid growth period (rapid growth in fruit diameter and fruit weight with slow accumulation of essential oil), the essential oil accumulation period (rapid accumulation of essential oil with slow growth in fruit diameter and fruit weight), the second rapid growth period (fruit diameter and fruit weight increased rapidly for the second time while the essential oil content started to decrease), and the shriveling period (fruit diameter and weight and essential oil content all decreased rapidly). This study further confirmed that citral was the highest component in the essential oil of Litsea cubeba . When citral extraction is needed, the fruit can be harvested 139–149 days after anthesis.
... Litsea cubeba, widely distributed in tropical or subtropical areas (Kamle et al., 2019), is the most valuable medicinal plant in the Lauraceae family . The main pharmacological activities of L. cubeba essential oil (LEO) include acting as an antiinflammatory mediator (Liao et al., 2015), anti-oxidative properties (Huang et al., 2013), sedative effects (Sattayakhom et al., 2021), and the alleviation of Alzheimer's disease (Lee et al., 2021) and rheumatoid arthritis (Zhao et al., 2020). In addition, the superior anti-microbial activities of LEO suggest that it may have potential as an AGP substitute (Gogoi et al., 2018). ...
This paper was to determine the effects of dietary Litsea cubeba essential oil (LEO) supplementation on growth performance, immune function, antioxidant level, intestinal morphology and microbial composition in weaned piglets. One hundred and ninety-two piglets (Duroc × [Large White × Landrace]) with 6.85 ± 0.22 kg mean body weight weaned at 21 d of age were randomly assigned to 4 treatment groups with 8 replicates and were fed with a basal diet (CON) or CON diet containing 100 (LLEO), 200 (MLEO) and 400 (HLEO) mg/kg LEO. The results revealed that HLEO supplementation (P < 0.05) increased the average daily gain on d 28 compared with CON. MLEO and HLEO supplementation decreased (P < 0.05) feed conversion ratio. LEO-containing diets had a lower (P < 0.05) diarrhea rate. Supplementation with HLEO increased (P < 0.05) total antioxidant capacity (T-AOC) both in the serum and liver. Meanwhile, the supplementation of MLEO and HLEO resulted in higher (P < 0.05) glutathione peroxidase (GPx) activities both in serum and liver. Supplementation of HLEO increased (P < 0.05) serum immunoglobulin A, immunoglobulin G and interleukin-10, whereas supplementation with MLEO and HLEO decreased (P < 0.05) tumor necrosis factor-α. Villus height in the duodenum or jejunum was increased (P < 0.05) in the HLEO group, and the villus height to crypt depth ratio in the jejunum was also improved (P < 0.05) in the MLEO group. The addition of LEO increased (P < 0.05) the richness and diversity of the microbial community in the cecum, which mainly increased the relative abundance of Oscillospiraceae_UCG-005, Faecalibacterium, Blautia and Coprococcus. Piglets supplemented with HLEO increased (P < 0.05) the concentration of short chain fatty acids (SCFA), including acetic acid in the cecum and propionic acid in the colon. In conclusion, these findings indicated that LEO supplementation improved growth performance and intestinal health in weaned piglets.
... Litsea cubeba (Lour.) Pers. is an important species used for producing essential oils that are widely used for perfumes, cosmetics, and medicines (Huang, Feng, Huang, & Li, 2013;Nguyen, Lebrun, Caruso, Chu-Ky, Sarter, van Nguyen, & Meile, 2018;Su & Ho, 2016). Rosewood oil from Aniba rosodora Ducke and bulian timber or Borneo ironwood from Eusideroxylon zwageri Teijsm. ...
Dehaasia pugerensis Koord. & Valeton is a threatened Indonesian Lauraceae species. It is an endemic tree known only from Jember Regency in East Java. To enhance the conservation of D. pugerensis, we conducted a population survey in several locations in Jember where the species were previously collected. The objectives were to: i) assess the current population status of D. pugerensis, ii) collect plant materials (seed, seedling, or cutting) to serve as ex situ collections, and iii) update the conservation status of the species according to IUCN Red List Category and Criteria. We only found D. pugerensis in 6 out of 16 locations in Wuluhan and Ambulu District during the survey. We successfully located 560 individuals of the species, of which 194 individuals (34.6%) were in the mature stage. Based on the diameter and height classes, the population of D. pugerensis formed a reverse J-shaped size distribution. We successfully collected 23 seeds and 15 seedlings of the species for ex situ collections. Our findings showed that the current status of D. pugerensis is Critically Endangered (CR) based on criteria B1ab(i,ii,iii,iv,v)and C2a(ii). Under these categories, the species faces an extremely high risk of extinction in the wild. Therefore, prompt comprehensive conservation actions are needed to ensure the survival of the species.
... Persoon is an aromatic plant widely scattered in Australia, America, Japan, China, and Southeastern Asia [4]. L. cubeba is a potent fumigant plant [5] and also used in cosmetics and foods as essence [6,7]. e chemical composition of the essential oil of different parts of L. cubeba has been reported [7,8]. ...
Aromatherapy is one of the complementary therapies to improve health. The aromatic essential oils have been used in the treatment procedure through inhalation of essential oil vapor, massage, and herbal bathing. Litsea species are generally used in traditional medicine, and Litsea cubeba (Lour.) Persoon is a potent fumigant plant, used in cosmetics and foods as essence. The chemical composition of the essential oil of different parts of L. cubeba has been found to be varied. L. cubeba essential oil (LEO) is known for the treatment of cognition-associated discomforts. The current study assessed the impact of inhalation of LEO on mood states and salivary cortisol levels of healthy people. Fifteen healthy volunteers were involved in the study. The Profile of Mood States (POMS) Questionnaire and ELISA methods were employed to determine the mood states and salivary cortisol level, respectively. (-)-β-pinene, β-citral, cis- and trans-citral, citronellal, limonene, linalool, and 6-methyl-5-hepten-2-one were detected in LEO by GC-MS analysis. The heart rate and blood pressure were not affected significantly during LEO exposure. The inhalation of LEO significantly improved the total mood disturbance and reduced the confusion among the healthy human subjects. LEO inhalation reduced the salivary cortisol level at a notable level. The results of the current study warrant further studies on the beneficial effect of LEO aromatherapy in healthy and diseased subjects to uncover the therapeutic nature of the L. cubeba plant.
... Its fruit is edible and the dried fruits are used in traditional Chinese medicine (Yang et al. 2014). The essential oil of L. cubeba also showed the antibacterial, antioxidant, and antiparasitic activity, it also showed genetic toxicity, cytotoxicity and was a potential cancer prevention agent (Wang et al. 2012;Huang et al. 2013). However, there have been no genomic studies on L. cubeba. ...
The first complete chloroplast genome (cpDNA) sequence of Litsea cubeba was determined from Illumina HiSeq pair-end sequencing data in this study. The cpDNA is 152,725 bp in length, contains a large single-copy region (LSC) of 93,673 bp, and a small single-copy region (SSC) of 18,924 bp, which were separated by a pair of inverted repeats (IR) regions of 20,064 bp, each. The genome contains 126 genes, including 82 protein-coding genes, 8 ribosomal RNA genes, and 36 transfer RNA genes. The further phylogenomic analysis showed that L. cubeba and Litsea garrettii clustered in a clade in Lauraceae family.
... In the literature, monoterpenes were already shown to be the major compounds of EOs extracted from L. cubeba, although the identified components were different. Indeed, EOs extracted from fruits of L. cubeba collected in China and Taiwan contained mostly citral (neral and geranial) from 57% to 81% [20][21][22][23][24][25]. The EO extracted from another sample collected in China contained limonene oxide (60%) and limonene (12%) [26]. ...
Human African trypanosomiasis (HAT), known as sleeping sickness and caused by Trypanosoma brucei, is threatening low-income populations in sub-Saharan African countries with 61 million people at risk of infection. In order to discover new natural products against HAT, thirty-seven Vietnamese essential oils (EOs) were screened for their activity in vitro on Trypanosoma brucei brucei (Tbb) and cytotoxicity on mammalian cells (WI38, J774). Based on the selectivity indices (SIs), the more active and selective EOs were analyzed by gas chromatography. The anti-trypanosomal activity and cytotoxicity of some major compounds (isolated or commercial) were also determined. Our results showed for the first time the selective anti-trypanosomal effect of four EOs, extracted from three Zingiberaceae species (Curcuma longa, Curcuma zedoaria, and Zingiber officinale) and one Lauraceae species (Litsea cubeba) with IC 50 values of 3.17 ± 0.72, 2.51 ± 1.08, 3.10 ± 0.08, and 2.67 ± 1.12 nL/mL respectively and SI > 10. Identified compounds accounted for more than 85% for each of them. Among the five major components of Curcuma longa EO, curlone is the most promising anti-trypanosomal candidate with an IC 50 of 1.38 ± 0.45 µg/mL and SIs of 31.7 and 18.2 compared to WI38 and J774 respectively.
... The chemical composition of the EO of L. cubeba has been seen to vary from country to country [14,50]. Despite this, the different EOs possess similar properties and exert antimicrobial, antibacterial, antioxidant, and antiparasitic activity [14,[53][54][55]. In addition to this, Litsea EO has a peculiar property of insecticidal activity and acts as a repellent against several insects, e.g., cabbage looper (Trichoplusia ni), Japanese termite (Reticulitermes speratus), mosquito (Aedes aegypti), maize weevil (Sitophilus zeamais), and red flour beetle (Tribolium castaneum), and also possesses nematicidal activity against the pine wood nematode (Bursaphelenchus xylophilus) [23,24,56,57]. ...
The genus Litsea is predominant in tropical and subtropical regions of India, China, Taiwan, and Japan. The plant possesses medicinal properties and has been traditionally used for curing various gastro-intestinal ailments (e.g., diarrhea, stomachache, indigestion, and gastroenteritis) along with diabetes, edema, cold, arthritis, asthma, and traumatic injury. Besides its medicinal properties, Litsea is known for its essential oil, which has protective action against several bacteria, possesses antioxidant and antiparasitic properties, exerts acute and genetic toxicity as well as cytotoxicity, and can even prevent several cancers. Here we summarize the ethnopharmacological properties, essentials oil, medicinal uses, and health benefits of an indigenous plant of northeast India, emphasizing the profound research to uplift the core and immense potential present in the conventional medicine of the country. This review is intended to provide insights into the gaps in our knowledge that need immediate focus on in-situ conservation strategies of Litsea due to its non-domesticated and dioecious nature, which may be the most viable approach and intense research for the long-term benefits of society and local peoples.
... China has always been the world largest exporter of Litsea cubeba (LC) essential oils in last decades. Such essential oils with an intense lemony scent could be widely applied as raw materials in various areas such as flavor and fragrance, food additives, cosmetic, cigarette, insecticide and bacteriostat (Liu and Yang, 2012;Zhang et al., 2012;Huang et al., 2013;Yang et al., 2014). Nevertheless, a large number of kernel residues will be simultaneously produced during the extraction of LC essential oils with an average yield of around 4% only. ...
Litsea cubeba (LC) is an indigenous industrial crop in China with fruits possessing interesting essential oil content of 3-5%, which production leads to a large number of kernels as wastes. In this study, the performance of four alternative solvents on the extraction of LC kernel oils was firstly evaluated in comparison with n-hexane as the reference solvent. Regardless of the solvent used, all extracted oils were quantitatively and qualitatively analyzed, where green solvents (dimethyl carbonate-DMC and cyclopentyl methyl ether-CPME) were preferred to alcoholic solvents (ethanol and isopropanol) considering their higher extraction yields and similar acylglycerol and fatty acid compositions to oils extracted by n-hexane. Interestingly, micronutrients in oils extracted by green solvents were quantified much higher than that extracted by n-hexane. Apart from common physicochemical properties measured, Hansen solubility parameter and antioxidant activity in vitro were also studied to make a more comprehensive profile for solvent effects and oil functionality. The results indicated that CPME could be the optimal alternative solvent to n-hexane with comparable extractability and selectivity in the green extraction of LC kernel oils as a new promising natural plant oil resource.
... Plants produce a wide variety of volatile compounds, including terpenes, alcohols, aldehydes, esters, ethers, ketones, phenols, and oxides, that play important roles in defense, pollinator attraction, signal transduction, and so on. These volatile compounds are also important resources for the pharmaceutical, food, beverages, perfume, and cosmetics industries, and are thus economically significant [1][2][3]. The mixture of plant volatile compounds, which is also known as essential oil, can be extracted using hydrodistillation, steam distillation, supercritical fluid extraction, Soxhlet s extraction, and ultrasound-assisted extraction [4,5]. ...
Herba Siegesbeckiae (HS), derived from the aerial parts of three plants, Siegesbeckia orientalis (SO), S. glabrescens (SG), and S. pubescens (SP), has been used for the treatment of inflammatory diseases in China for centuries. In the present study, hydrodistillation was applied to extract essential oils from dried SO, SG, and SP aerial parts, and chemical composition analysis by gas chromatography–mass spectrometry (GC-MS) led to the identification of a total of 148 compounds (56 in SO, 62 in SG, and 59 in SP). The main components in the essential oils of SO, SG, and SP differed significantly. In vitro anti-inflammatory activity assays showed that SP essential oils (IC50, 0.97 μg/mL) significantly reduced the ability of lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages to release NO, and the SO essential oil (IC50, 14.99 μg/mL) was better than the others at inhibiting the LPS-induced release of cytokine IL-6. Furthermore, the essential oils exhibited antitumor activities (IC50, 37.72–123.16 μg/mL) against Hep3B (liver) and Hela (cervical) cells. Linear regression analysis showed that, caryophyllene oxide peak area percentages showed remarkably high negative correlation coefficients with IC50 values of Hep3B and Hela cytotoxicity, which suggested the contribution of this compound on the cancer cell cytotoxicity of three essential oils. Finally, the ITS1-5.8S-ITS2 region was amplified and sequenced in order to generate genomic reference sequences for each plant. These can be used to identify the origins of the plants, and will assist other research studies related to these three plants.
... Pharmacological studies indicated that the essential oil of L. cubeba possessed antispasmodic, bronchodilator, antimicrobial, antioxidant, antiparasitic, acute and genetic toxicity, cytotoxic and anticancer activities [9,[21][22][23][24]. The oil was also a potential insecticide and able to repel cabbage looper, Trichoplusia ni, Japanese termite, Reticulitermes speratus, mosquito, Aedes aegypti, maize weevil, Sitophilus zeamais, redflour beetle, Tribolium castaneum, nematode, Bursaphelenchus xylophilus, cigarette beetles, Lasioderma serricorne, and booklouse, Liposcelis bostrychophila [1,2,[25][26][27]. ...
The essential oils from different parts of Litsea cubeba, collected from the highlands of Sarawak, were isolated and their chemical compositions analyzed. This study demonstrated significant variations in the chemical compositions and the chemical profiles of the volatiles and could provide valuable supplementary information on the geographical variations of the species. The fruit essential oil was dominated by citronellal, d-limonene and citronellol, while the leaf oil was high in eucalyptol and a-terpineol. High concentrations of citronellal and citronellol in both the root and bark oils were identified. In the stem, the oil was dominated by eucalyptol, d-limonene and α-terpineol. The activity of the oils against brine shrimp larvae, bacteria, yeast and fungi was determined. The oils were toxic against brine shrimp larvae with LC50 values ranging from 25.1 - 30.9 μL/mL. The oils also demonstrated a wide spectrum of inhibition against microorganisms with inhibition zones between 19.5 - 46.7 mm against Gram-positive bacteria and 10.5 - 90.0 mm against yeast and fungi. However, the oils were not active against Gram-negative bacteria.
... The compo-sitional pattern of neral/sabinene/limonene may represent another chemical form of the oil of L. cubeba. However, the major composition data was in agreement with the results from other studies that citral was the major component 37,38 , whilst the proportion vary widely, which demonstrates the variability of the natural oil. Table 3 represents the summary of major chemical constituents of essential oils from various parts of L. cubeba analysed from different countries 25 . ...
In this paper, the compositional pattern of essential oils from five plants in the genus Litsea (Lauraceae family) cultivated in Vietnam, were being reported. The air-dried plant materials were hydrodistilled and the oils were analysed by Gas chromatography-flame ionization detector (GC-FID) and Gas chromatography coupled with Mass spectrometry (GC-MS). The leaf oil of Litsea helferi Hook.f., was rich in limonene (17.5 %), β-caryophyllene (14.2 %), bicyclogermacrene (13.1 %), bicycloelemene (12.4 %) and α-phellandrene (8.0 %). The main constituents of Litsea ferruginea Liou., leaf oil were dominated by monoterpenes comprising of sabinene (34.5 %), α-pinene (10.1 %), γ-terpinene (7.8 %), limonene (6.9 %) and terpinen-4-ol (6.6 %). The quantitative significant constituents of the leaf oil of Litsea verticillata Hance were also monoterpene compounds represented by linalool (23.4 %), α-pinene (26.1%) and β-pinene (11.7 %). In addition, the monoterpene hydrocarbons (E)-β-ocimene (57.4 %), along with α-pinene (7.8 %) and β-pinene (7.3 %) were the main constituents in the leaf oil of Litsea glutinosa (Lour.) C. B. Rob. The main compounds in the leaf, stem, fruits and roots oils of Litsea cubeba (Lours.) Pers., were (Z)-citral (32.9-66.1 %), sabinene (1.4-14.2 %), limonene (7.0-13.6 %) and linalool (1.9-9.5 %). The chemical compositions of L. helferi, L. ferruginea and L. verticillata are being reported for the first time.
... Some variations in essential oil content and chemical composition of the essential oil were found Yu et al., 2010). Many data indicated that the essential oil possessed antimicrobial, antibacterial, antioxidant, antiparasitic activity, acute and genetic toxicity, cytotoxicity as well as being a potential cancer prevention agent (Wang et al., 1985;Gogoi et al., 1997;Luo et al., 2005;Ho et al., 2010;Wang and Liu, 2010;Wang et al., 2012;Huang et al., 2013). The essential oil of L. cubeba has been demonstrated to possess insecticidal activity as well as repellency against several insects, e.g. the cabbage looper Trichoplusia ni, Japanese termite Reticulitermes speratus Kolbe, mosquito Aedes aegypti, maize weevil Sitophilus zeamais, red flour beetle Tribolium castaneum and nematicidal activity against pine wood nematode Bursaphelenchus xylophilus (Park et al., 2007;Noosidum et al., 2008;Jiang et al., 2009;Ko et al., 2009;Seo et al., 2009). ...
During our screening program for agrochemicals from Chinese medicinal herbs and wild plants, the essential oil of Litsea cubeba fruits was found to possess strong contact toxicity against the cigarette beetle Lasioderma serricorne adults and the booklouse Liposcelis bostrychophila, with LD50 values of 27.33 mu g/adult and 71.56 mu g/cm(2), respectively, and also showed strong fumigant toxicity against the two stored product insects with LC50 values of 22.97 and 0.73 mg/L, respectively. The essential oil obtained by hydrodistillation was investigated by GC MS. The main components of the essential oil were identified to be E-citral (geranial) (27.49%), Z-citral (neral) (23.57%) and D-limonene (18.82%) followed by beta-thujene (3.34%), beta-pinene (2.85%), alpha-pinene (2.57%), 6-methyl-5-hepten-2-one (2.40%) and linalool (2.36%). Citral (Z/E-citral), D-limonene, beta-pinene, alpha-pinene and linalool were separated and purified by silica gel column chromatography and preparative thin layer chromatography, and further identified by means of physicochemical and spectrometric analysis. Citral and linalool showed strong contact toxicity against L serricorne and L bostrychophila (LD50 = 11.76, 12.74 mu g/adult and 20.15, 99.97 mu g/cm(2), respectively) and fumigant toxicity against L serricorne and L. bostrychophila (16.54, 18.04 mg/L air and 0.14, 0.71 mg/L air, respectively). Otherwise, citral, D-limonene and linalool were strongly repellent against the cigarette beetle L serricorne as the essential oil whereas beta-pinene and alpha-pinene exhibited weaker repellency against the cigarette beetle compared with the positive control, DEET. Moreover, except alpha-pinene and linalool, the other three compounds as well as the essential oil exhibited comparable repellency against the booklouse relative to DEET. (C) 2014 The Authors.
Tyrosinase is a target enzyme to be inhibited in order to reduce excessive melanin production and prevent typical age-related skin disorders. Essential oils are complex mixtures of volatile compounds, belonging mainly to monoterpenoids and sesquiterpenoids, which have been relatively little studied as tyrosinase inhibitors. Among the monoterpenoids, citral (a mixture of neral and geranial) is a fragrance compound in several essential oils that has shown interesting tyrosinase inhibitory activity. Although citral is listed as an allergen among the 26 fragrances in Annex III of the Cosmetics Directive 2003/15/EC, it can be safely used for the formulation of topical products in amounts that are not expected to cause skin sensitization, as shown by various commercially available products.
The aim of this work was to evaluate two different formulations (oil/water emulsion, oily solution) containing a new combination of essential oils (Litsea cubeba, Pinus mugo, Cymbopogon winterianus) applied to the skin both in nonocclusive and partially occlusive modes. The blend is designed to reduce the concentration of citral to avoid potential skin reactions while taking advantage of the inhibitory activity of citral. Specifically, the amount of citral and other bioactive compounds (myrcene, citronellal) delivered through the skin was studied as a function of formulation and mode of application.
The results show that an oil/water emulsion is preferable because it releases the bioactive compounds rapidly and minimizes their evaporative loss. In addition, semi-occluded conditions are required to prevent evaporation, resulting in higher availability of the bioactive compounds in viable skin.
The essential oil from Litsea cubeba (LCEO) has good antioxidant, antimicrobial, anti-insect properties, which gives it the potential for use as a natural additive to food resources and food products in order to prevent spoilage and extend shelf life. In this study the biological activity related to food preservation was observed. The main volatile organic compounds were geranial (39.4%), neral (29.5%), and limonene (14.3%). Antioxidant activity was 30.9%, which was equal to 167.94 µg of Trolox per mL of sample. Antimicrobial activity showed the strongest inhibition against Serratia marcescens by disk diffusion method and minimum inhibitory concentrations MIC 50 and MIC 90 were the lowest for Micrococcus luteus with values 1.46 and 3.52 µL/mL, respectively. Antimicrobial activity of the LCEO vapor phase showed strong inhibition of microorganisms on apples, pears, potatoes, and kohlrabies. Over 50% of gram-positive and gram-negative bacteria and yeasts were inhibited by a concentration of 500 µL/mL. The inhibition of microorganisms was concentration dependent. Anti-insect activity was also strong, with 100% lethality of Pyrrhocoris apterus at a concentration of 25%. These results suggest that LCEO could be potentially used as a food preservative.
Litsea Lam. is an ecological and economic important genus of the "core Lauraceae" group in the Lauraceae. The few studies to date on the comparative chloroplast genomics and phylo-genomics of Litsea have been conducted as part of other studies on the Lauraceae. Here, we se-quenced the whole chloroplast genome sequence of Litsea auriculata, an endangered tree endemic to eastern China, and compared this with previously published chloroplast genome sequences of 11 other Litsea species. The chloroplast genomes of the 12 Litsea species ranged from 152,132 (L. szemaois) to 154,011 bp (L. garrettii) and exhibited a typical quadripartite structure with conserved genome arrangement and content, with length variations in the inverted repeat regions (IRs). No codon usage preferences were detected within the 30 codons used in the chloroplast genomes, indicating a conserved evolution model for the genus. Ten intergenic spacers (psbE-petL, trnH-psbA, petA-psbJ, ndhF-rpl32, ycf4-cemA, rpl32-trnL, ndhG-ndhI, psbC-trnS, trnE-trnT, and psbM-trnD) and five protein coding genes (ndhD, matK, ccsA, ycf1, and ndhF) were identified as divergence hotspot regions and DNA barcodes of Litsea species. In total, 876 chloroplast microsatellites were located within the 12 chloroplast genomes. Phylogenetic analyses conducted using the 51 additional complete chloroplast genomes of "core Lauraceae" species demonstrated that the 12 Litsea species grouped into four sub-clades within the Laurus-Neolitsea clade, and that Litsea is polyphyletic and closely related to the genera Lindera and Laurus. Our phylogeny strongly supported the monophyly of the following three clades (Laurus-Neolitsea, Cinnamomum-Ocotea, and Machilus-Persea) among the above investigated "core Lauraceae" species. Overall, our study highlighted the taxonomic utility of chloroplast genomes in Litsea, and the genetic markers identified here will facilitate future studies on the evolution, conservation, population genetics, and phylogeography of L. auriculata and other Litsea species.
Lauraceae is a large family of woody plants with high ecological and economic value. The tribal and generic division and phylogenetic relationship of Lauraceae have long been controversial. Based on morphological and molecular evidence, phylogenetic relationships within the Cinnamomeae, Laureae and Perseeae tribes, also called ‘the Core Lauraceae’, have arisen particular attention. In this review, we comprehensively collated the literatures on the phylogeny of Lauraceae published in recent years and summarized progress made in molecular systematic researches employing gene fragments, chloroplast genomes and DNA barcodings analyses. We clarified the phylogenetic relationships and main controversies of ‘the Core Lauraceae’, the systemic position of fuzzy genera (Neocinnamomum, Caryodaphnopsis and Cassytha) and the development of chloroplast genome and DNA barcodes. We further suggested and proposed the whole genome analysis and different inflorescence types would be possible to provide more information for further research on phylogenetic relationships and taxonomy of Lauraceae.
As an important natural product, the sufficient separation of plant essential oil (EO) is helpful to improve its utilization value. In this work, deep eutectic solvent-homogenate based microwave-assisted hydrodistillation (DES-HMAHD) was developed and applied to isolate EO from the fruits of Litsea cubeba (Lour.) Pers. Different types of DES were investigated in terms of the EO kinetics and composition, among which oxalic acid/choline chloride (OA/ChCl) had obvious advantages. Following, molar ratio of OA and ChCl (1:1), water content (50%), liquid-solid ratio (12.5:1 mL/g), homogenate time (2 min), and microwave power (700 W) were found to be the optimum conditions. Gas chromatography-mass spectrometer (GC-MS) analysis showed that the EO isolated from DES-HMAHD contained a large proportion of m-cymene and trans-linalool oxide, which were quite different from the conventionally reported L. cubeba EO. In addition, the proposed DES-HMAHD resulted in higher separation efficiency and economic value, as well as lower environmental impact, as compared with other techniques. Afterwards, the EO isolated by different methods was evaluated from the perspective of biological activity. The EO obtained by DES-HMAHD showed higher antioxidant activity (DPPH and ABTS) but lower antifungal activity, which was related to its chemical composition. In general, DES-HMAHD produced a kind of L. cubeba EO with different components, which provided a scientific foundation for the sufficient isolation of plant EO and its application in the natural products.
There are two chemotypes of Litsea cubeba (Lour.) Pers. (fam. Lauraceae) essential oils (EOs), either dominated by citral and limonene or by citronellal. L. cubeba EOs exhibits broad antimicrobial activity against bacteria and fungi with minimal inhibitory concentrations (MICs) from 0.5 to 2500 µg/mL. This antimicrobial activity is attributed to the monoterpene citral, exhibiting a broad antimicrobial spectrum against bacteria and fungi (MICs 50–1000 µg/mL). Pseudomonas aeruginosa were found most resistant, with MIC values above 1000 µg/mL. Citral's mode of action is not fully investigated. At biocidal concentrations, it affects membrane structure and cell respiration, leading to rapid energy depletion and cell death. Involvement of intracellular reactive oxygen species has not been verified. Limonene exhibits insignificant antimicrobial activity. MICs of d-limonene range from 1 to 20 mg/mL. Citral and L. cubeba EOs were also subjects of food application studies. Promising results have been reported for fresh produce or fruit-juice.
Aqueous two-phase system (ATPS) was used for simultaneous purification of glycyrrhizic acid (GA) and liquiritin (LQ) from crude extract of Chinese licorice root. It was revealed that 87% GA and 94% LQ were retrieved in the ATPS top phase, under the optimum conditions of 25% (w/w) ethanol, 30% (w/w) K2HPO4 and 4% (w/w) loading sample at 10–40°C. Compared with crude extract, the ATPS top-phase extract exhibited the highest antioxidative activity, but no tyrosinase inhibitory effect. Whereas, the ATPS bottom-phase extract was proved to be effective ABTS radical scavenger and tyrosinase inhibitor, suggesting the potency of the alcohol-salt ATPS purification for the different medicinal purposes.
Response surface methodology (RSM) was applied to evaluate the extraction of active compounds from Litsea cubeba fruits. A central composite design (CCD) with five levels and three process parameters (extraction temperature, extraction time and ethanol concentration) was used to investigate the influence of the extraction temperature, extraction time and ethanol concentration on the multiple response variables (TPC, DPPH and ABTS assays). The results of the ANOVA analysis show that the quadratic term of the ethanol concentration was significant for all the response variables. The quadratic model was highly significant (P<0.05) for all the response variables. After optimizing for multi-response, the optimal conditions were determined as an extraction temperature of 42.3 ºC, extraction time of 126.4min and ethanol concentration of 51%. Moreover, the extract of Litsea cubeba fruit attested possessing tyrosinase inhibitory activity, with an IC50 value of 5,720 μg mL⁻¹. The second-order kinetic model represented the kinetic data very well. In addition, the obtained values of the effective diffusivities were in the range of 2.28-5.83×10⁻¹¹m²s⁻¹.
In this study, we investigated the insecticidal activities, including contact toxicity, fumigant toxicity, and repellent activity, of Litsea cubeba fruit extracts against Sitophilus zeamais Motschulsky (Coleoptera: Curculionidae). The extracts, obtained by liquid–liquid extraction in n-hexane, ethyl acetate, chloroform, and water were analyzed by gas chromatography–mass spectrometry. Among the different extract types, chloroform extracts exhibited the strongest repellent, contact, and fumigant activities against S. zeamais. The main components of the chloroform extracts were identified as laurine (21.15%) and 2,6-diisopropyl aniline (16.14%), followed by chlorobutanol (10.54%), 3-O-methyl-N-acetyl-d-glucosamine (10.03%), and 6-methyl-5-hepten-2-one (8.33%). Among the identified components of the chloroform extracts, chlorobutanol showed the strongest fumigant toxicity (LD50 = 21.91 mg/liter), contact toxicity (LD50 = 54.25 µg/adult), and repellent activity against S. zeamais. These results indicate that L. cubeba fruit extracts possess natural insecticide-like activities against S. zeamais.
Ethnopharmacological relevance:
The genus Litsea is one of the most diverse genera of evergreen trees or shrubs belong to Lauraceae, and comprises roughly 400 species of tree that are distributed abundantly throughout tropical and subtropical Asia, North and South America. Litsea species have been used globally in traditional medicine for the treatment of various diseases including influenza, stomach aches, diarrhea, diabetes, vomiting, bone pain, inflammation, illness related to the central nervous system and other ailments. The purpose of this review is to provide updated, comprehensive and categorized information on the ethnobotany, phytochemistry and pharmacological research of Litsea species in order to explore their therapeutic potential and evaluate future research opportunities.
Materials and methods:
All the available information on Litsea species was actualised by systematically searching the scientific literatures including Chinese, Korean, Japanese, Indian, and South American herbal classics, library catalogs and scientific databases (PubMed, SciFinder, Web of Science, Google Scholar, VIP and Wanfang). The Plant List, International Plant Name index and Scientific Database of China Plant Species were used to validate scientific names.
Results:
407 secondary metabolites have been reported from Litsea species. Litsea Species are sources of secondary metabolites with interesting chemical structures (alkaloids, lactones, sesquiterpenes, flavonoids, lignans, and essential oils) and significant bioactivities. Crude extracts, fractions and phytochemical constituents isolated from Litsea show a wide spectrum of in vitro and in vivo pharmacological activities including anticancer, anti-inflammatory, antimicrobial, antioxidant, antidiabetic, anti-HIV, insecticidal, etc.
Conclusions:
From data collected in this review, the genus Litsea comprises a wide range of therapeutically promising and valuable plants, and has attracted much attention owing to its multiple functions. Many traditional uses of Litsea species have now been validated by modern pharmacology research. Deep and systematic phytochemical investigation of the genus Litsea and the pharmacological properties, especially its mechanism of action and toxicology, to illustrate its ethnomedicinal use, explore the therapeutic potential and support further health-care product development will undoubtedly be the focus of further research. Therefore, detailed and extensive studies and clinical evaluation of Litsea species should be carried out in future for the safety approval of therapeutic applications.
Fig fruits (Ficus carica L.) are excellent source of phenolic compounds. However, the presence of free sugars affects the quality of phenolic compounds. In this study, aqueous two-phase system was selected for purification of the phenolic compounds. The optimization of system parameters rendered conditions (ethanol 18% (w/w), K2HPO4 25% (w/w), temperature 10-30ºC and sample loading 3% (w/w)), under which more than 75% of phenolic compounds and 95% sugars were respectively recovered in the top and bottom phase. Moreover, some specific phenolic compounds content was enhanced and relatively high antioxidant activity was found after the purification process.
A simple micellar electrokinetic chromatography (MEKC) method was developed for determination of citronellal, citral (Z; E), α -pinene, limonene, linalool and eugenol in plant essential oils (EOs). A buffer consisting of 20 mM Na2B4O7, 50 mM SDS, 20% (v:v) methanol adjusted to pH 9.5 was found to provide a very efficient and stable electrophoretic system for the analysis. The validation of the method included linearity, LODs, LOQs, precision (intra - and inter - day variation of migration time and peak area) and recovery. Seven terpenoids were in good linearity (R > 0.9960) within the test ranges, LODs (S/N = 3) and LOQs (S/N = 10) were 0.2 - 1.8 µg/mL and 0.8 - 5.9 µg/mL, respectively. The precision and accuracy were satisfactory, with the overall intra - and inter - day variation (for migration time and peak area, RSD%) being less than 7.0%, and recoveries of this method were greater than 91% at spiked levels. The proposed method was successfully applied to the determination of seven terpenoids in clove oil, litsea cubeba oil and citronella oil, respectively.
The inclusion interactions of β-cyclodextrin (β-CD), heptakis (2,6-di-methyl)-β-CD (DM-β-CD), mono[2-O-(2-hydroxyethyl)]-β-CD (HE-β-CD), and mono[2-O-(2-hydroxy-propyl)]-β-CD (HP-β-CD) with Litsea cubeba essential oil (LCEO) were investigated by ultraviolet spectrophotometry, and the various factors affecting the inclusion
process were examined in detail. At the same time, the formation constants at different temperatures and the thermodynamic
parameters (ΔH, ΔS and ΔG) were calculated. The results suggest that the stoichiometry of the LCEO–CDs inclusion complexes was 1:1 (molar ratio), the
formation constants of CDs with LCEO decreased with the increasing of temperature, and the order that the capability associated
with LCEO was HP-β-CD > HE-β-CD > DM-β-CD > β-CD. The thermodynamic measurements showed that the inclusive process was an
exothermic and enthalpy-driven process accompanied with a negative entropic contribution, and Van der Waals force plays an
important role in the process. In addition, the molecular microcapsule of LCEO in β-CD was prepared by suspension method.
The content of LCEO in the microcapsules was 0.12g/g and their stabilities were obviously improved because of Van der Waals
forces and the steric hindrance. Furthermore, the formation of the inclusion complex was characterized by FTIR.
The anti-inflammatory effects and antioxidant activities of individual isoflavones are well established although little is known about the photoprotective effect of their combination. The aim of this study was to investigate the photoprotective effects of different concentrations of genistein and daidzein individually or combined. We measured the expression levels of the cyclo-oxygenase-2 (COX-2) and growth arrest and DNA-damage inducible (Gadd45) genes, which are involved in inflammation and DNA repair, respectively, in BJ-5ta human skin fibroblasts irradiated with 60 mJ/cm(2) UVB. We also determined the cellular response to UVB-induced DNA damage by Comet assay. We report that genistein and daidzein when administered combined, and at a specific concentration and ratio, exerted a synergistic photoprotective effect that was greater than the effect obtained with each isoflavone alone. The results reported herein suggest that low concentrations of genistein and daidzein combined may be good candidate ingredients for protective agents against UV-induced photodamage.
Cosmetic formulations may contain nano-emulsions and microscopic vesicles consisting of traditional cosmetic materials, although it is uncertain whether they should be qualified as actual nanomaterials. Vesicle materials do not penetrate into living human skin. Vesicle formulations may enhance or reduce skin absorption of ingredients, albeit at a limited scale. Sunscreens contain TiO2 or ZnO nanoparticles (NP), which are efficient UV filters. A number of studies suggest that insoluble NP do not penetrate into or through human skin. The results of in vivo toxicity tests showed that TiO2 and ZnO NP are non-toxic. In vitro and in vivo cytotoxicity, genotoxicity, photogenotoxicity, acute toxicity, sensitisation and ecotoxicology studies on TiO2 NP found no difference in the safety profile of micro- or nano-sized materials, all of which were non-toxic. Although some in vitro investigations on TiO2 particles reported cell uptake, oxidative cell damage or genotoxicity, these results may be secondary to phagocytosis of cells exposed to excessive particle concentrations. Studies on wear debris nano- and microparticles support the traditional view that toxicity of small particles is related to their chemistry, rather than their particle size. There is little evidence supporting a general rule that adverse effects of particles on the skin or other tissues increase with smaller particle size, or produce novel toxicities relative to those of larger particles. Overall, the current evidence suggests that nano-sized cosmetic or sunscreen ingredients pose no potential risk to human health, whereas their use in sunscreens has large benefits, such as the protection of human skin against skin cancer.
In the past several years, there has been a trend in the sunscreen/cosmetics industry to replace micron-sized titanium dioxide (TiO2) particles with nanoscale materials. The increased use of nanoscale TiO2 has resulted in questions about these and other nanoproducts. This study examines the effects of using nanoscale TiO2 on ultraviolet (UV) attenuation in simple to complex sunscreen formulations. UV light attenuation, product stability, and potential damage to the skin barrier were examined with both nanoscale and microscale TiO2 particles. Results indicate that none of the formulations decreased the barrier function of the skin and the best UV attenuation occurs when the TiO2 particles are stabilized with a coating and evenly distributed such as with non-agglomerated coated nanoscale materials. This indicates that nanoscale TiO2 may have better efficacy while lacking toxicity.
Au cours des dernières années, nous avons constaté une tendance dans l’industrie solaire/cosmétique pour le remplacement des particules micron-taille de dioxyde de titane (TiO2) avec des matériaux de nano-échelle. L’utilisation accrue des particules de TiO2 l’échelle du nanométre a engendré des questions sur tous les produits contenant des matériaux nano-échelle. Cette étude examine les effets de l’utilisation de particule de TiO2 a l’échelle du nanomètre sur l’atténuation des rayons UV dans les formulations de crème solaire simple et complexe. Nous avons étudié l’atténuation de la luminosité ultraviolet (UV), la stabilité du produit et les effets sur la fonction barrière de la peau, avec les particules de TiO2 nano-échelle et micro-échelle. Les résultats indiquent que les particules a l’échelle du nanométre, enduits et non-aggloméré, fournissent une excellente atténuation UV, sans diminuer la fonction barrière de la peau. Ceci suggére que les particules de TiO2 a l’échelle du nanométre ont une meilleure efficacité, sans poser des inquiétudes en ce qui concerne leur securité.
A new C₉ monoterpenoid acid (litseacubebic acid, 1) and a known monoterpene lactone (6R)-3,7-dimethyl-7-hydroxy-2-octen-6-olide (2), along with three known compounds--vanillic acid (3), trans-3,4,5-trimethoxylcinnamyl alcohol (4), and oxonantenine (5)--were isolated with bioassay-guided purification from the fruit extract of Litsea cubeba collected in Tibet. The structure of 1 was elucidated by MS, ¹H-NMR, ¹³C-NMR, COSY, HSQC, HMBC, NOE spectral data as 2,6-dimethyl-6-hydroxy-2E,4E-hepta-2,4-diene acid. Additionally 33 compounds were identified from the essential oil of L. cubeba. The preliminary bioassay results showed that 1 and 2 have good fungicidal activities against Sclerotinia sclerotiorum, Thanatephorus cucumeris, Pseudocer-cospora musae and Colletotrichum gloeosporioides at the concentration of 588 and 272 μM, and the essential oil has good fungicidal activities against T. cucumeris and S. sclerotiorum, with IC₅₀ values of 115.58 and 151.25 μg/mL, repectively.
The leaf and fruit essential oils of Litsea cubeba, extracted by hydrodistillation, were assessed for anticancer activities. A total of 53 and 50 compounds were identified, respectively from the leaf and fruit oils, and their yields were 13.9 +/- 0.09% and 4.0 +/- 0.03%, v/w, of the oven-dried materials, respectively. The main compound in the leaf oil was 1,8-cineol, and in the fruit oil, citral. The fruit oil, but not that of the leaf, exhibited cytotoxic activity against human lung, liver and oral cancer cells.
Litsea cubeba oil is an aromatic essential oil extracted from the fresh fruits of Litsea cubeba (Lour.) Pers. It is used as a flavor enhancer in foods, cosmetics, and cigarettes; as a raw material in the manufacture of citral, vitamins A, E, and K, ionone, methyl ionone, and perfumes; and as an antimicrobial and insecticide. Based on the widespread use of L. cubeba oil, its insolubility in water, resulting in its partition in soil sediment, and its volatility when exposed to the atmosphere, risk of injury due to consumption and occupational exposure may be significant. In the present study, we studied the toxicity of L. cubeba oil with a battery of acute and genetic toxicity tests in Institute of Cancer Research mice and Sprague-Dawley rats. The oral, dermal, and inhalation 50% lethal dose and concentration (LD50 and LC50) of L. cubeba oil were determined. Results indicated that the oral LD50, the dermal LD50, and the inhalation LC50 are approximately 4,000 mg/kg of body weight, in excess of 5,000 mg/kg, and approximatively 12,500 ppm, respectively. We therefore conclude that L. cubeba oil is slightly toxic. In addition, the genetic toxicity of L. cubeba oil was assessed with Salmonella Typhimurium, by determination of the induction of micronuclei in bone marrow cells, and also by testing for chromosome aberration in spermatocyte cells of Institute of Cancer Research mice. The results of genetic toxicity testing of L. cubeba oil in vitro and in vivo were negative.
The chemical composition of Litsea cubeba essential oils obtained from leaves harvested in six provinces of Vietnam were investigated using a combination of capillary GC, GC/MS and C-NMR spectroscopy. Three compositions were found, dominated by 1,8-cineole (0.2–51.7%), linalool (0.4–91.1%) and sabinene (0–48.1%).
A novel method for the quantification of minor 3-nitrotyrosine in the NaNO2-H2O2-hemin-tyrosine system was established by micellar electrokinetic chromatography with on-column high-salt stacking. The optimum CE separation conditions were as follows: 36 mM Na2B4O7 as the running buffer contained 30 mM SDS at pH 9.3; injection time 30 s at pressure of 3.44 kPa; separation voltage 20 kV, a temperature of 25°C; and a sample matrix containing 100 mM of NaCl. Under CE conditions, the linear relationship range from 0.78 to 50 μM (r = 0.9953), and the limit of detection (LOD) was 0.1 μM (S/N = 3). The RSDs of migration time for inter- and intra-day were 1.6% and 2.8%, respectively. The recoveries were 95.2%–103.1% and the RSDs for inter- and intra-day were less than 3% at various spiked levels. This study provides a useful method for the direct analysis of minor 3-NT in biological samples. This method is simple, rapid, and sensitive.
Cuminaldehyde (p-isopropylbenzaldehyde) was identified as a potent mushroom tyrosinase inhibitor from cumin, a common food spice. This benzaldehyde derivative was found to inhibit the oxidation of l-3,4-dihydroxyphenylalanine (l-DOPA) by mushroom tyrosinase with an ID50 of 7.7 μg/mL (0.05 mM). Its oxidized analogue, cumic acid (p-isopropylbenzoic acid), was also characterized to inhibit this oxidation with an ID50 of 43 μg/mL (0.26 mM). These two inhibitors affect mushroom tyrosinase activity in different ways. Keywords: Cumin; cuminaldehyde; cumic acid; tyrosinase inhibitory activity; noncompetitive inhibition; Schiff base formation
Hydro-distillated volatile oils of Ephedra sinica Stapf. from six populations of Inner Mongolia in Northeastern China were analyzed by using GC/MS. Ninety-nine compounds were identified in the oils and a relatively high variation in their contents was found. The main constituents of the essential oils were α-terpineol (19.28–52.23%), p-vinylanisole (0.59–11.64%), 3-methyl-2-buten-1-ol (0–5.44%), tetramethylpyrazine (0.63–8.99%), terpine-4-ol (1.17–4.37%), α-linalool (1.62–5.15%), phytol (1.24–15.73%), γ-eudesmol (0–7.77%), and eudesm-7(11)-en-4-ol (0.41–6.13). Six populations were divided into two chemotypes based on cluster analysis and principal component analysis (PCA); one rich in α-terpineol and p-vinylanisole, and the other rich in phytol, γ-eudesmol, and eudesm-7(11)-en-4-ol.
The main polyphenols were isolated from the leaves of six selected persimmon cultivars. Seven compounds were obtained by reverse-phase HPLC, and their structures were elucidated by multiple NMR measurements. These compounds are hyperoside, isoquercitrin, trifolin, astragalin, chrysontemin, quercetin-3-O-(2''-O-galloyl-β-D-glucopyranoside) (QOG), and kaempferol-3-O-(2''-O-galloyl-β-D-glucopyranoside) (KOG). Their inhibitory activity was tested against tyrosinase for the oxidation of L-DOPA, and only chrysontemin showed inhibitory activity. To investigate the differences of their inhibitory effects, the tyrosinase inhibitory activities of their aglycons, cyanidin, quercetin, and kaempferol, were also tested. As a result, it was confirmed that the most influential moiety for tyrosinase inhibition was the 3',4'-dihydroxy groups of the catechol moiety. Moreover, the tyrosinase inhibitory activity of chrysontemin, which was identified in persimmon leaves for the first time, is supported by a simulated model of chrysontemin docking into mushroom tyrosinase.
Four new megastigmane glycosides, named gusanlungionosides A-D (1-4), together with 10 known compounds (5-14), were isolated from the stems of Arcangelisia gusanlung. The structures and absolute configurations of 1-4 were elucidated by comprehensive analysis of their NMR and CD data. Compounds 1-4 exhibited strong inhibitory effects not only on the mushroom tyrosinase activity in vitro but also on melanogenesis in cells. (Chemical Equation Presented). © 2011 The American Chemical Society and American Society of Pharmacognosy.
Sunscreens are believed to be a valuable tool in providing photoprotection against the detrimental effects of UV radiation, a known carcinogen. However, a number of controversies have developed regarding their safety and efficacy. This review summarizes the relevant studies surrounding these controversies.
Evidence of the prevention of skin cancer, an oft-cited reason for sunscreen use, was examined as it pertains to squamous cell carcinoma, basal cell carcinoma and melanoma. We also reviewed studies examining the effects of sunscreen on the synthesis of vitamin D, an essential nutrient whose role in health and disease continues to grow. Lastly, we analyzed studies surrounding the safety and toxicity of oxybenzone, retinyl palmitate and nanoparticles of zinc oxide (ZnO) and titanium dioxide (TiO2 ).
The overwhelming majority of available data is drawn from studies conducted using antiquated sunscreen formulations. Nonetheless, our research revealed that topical use of sunscreen protects against squamous cell carcinoma, does not cause vitamin D deficiency/insufficiency in practice and has not been demonstrated to adversely affect the health of humans.
Given the established benefits of UV protection, the use of sunscreens remains an important part of an overall photoprotective strategy. Future sunscreens with improved formulation should ideally offer superior protection. With increased usage of sunscreen by the public, continuous and vigilant monitoring of the overall safety of future products is also needed.
Iron overload is one of the most common iron-related toxicities, and liver is the major organ that is injured. Although oxidative stress is well accepted in the pathological mechanism of iron overload, nitrative modification in liver and the role of iron are relatively unknown. In this work, the nitrative and oxidative stress in liver was investigated in an iron-overload rat model. It was found that after 15 weeks of iron dextran administration, consistent with the increase of iron content in rat liver, both protein tyrosine nitration and protein oxidation were clearly elevated. By means of immunoprecipitation analysis, it was found that enolase nitration and oxidation status were significantly increased in iron-overload liver, whereas both α-enolase expression and activity were clearly decreased. The effects of different forms of iron on NaNO(2)-H(2)O(2)- and peroxynitrite (ONOO(-))-dependent enolase nitration and oxidation were further investigated in vitro to elucidate the possible role of iron in enolase dysfunction in vivo. Compared with EDTA-Fe(III), ferric citrate, and ferritin, heme (hemin and hemoglobin) showed higher efficiency in catalyzing protein nitration in both models. Besides the major contribution of free iron (Fe(2+) and Fe(3+)) to catalyze protein oxidation, Fe(2+) also directly acted as a competitive inhibitor and produced a significant decrease in enzyme activity. These results suggest that the existence of various forms of iron is an important contributing factor to the elevated nitrative/oxidative modifications and diminished activity of α-enolase in the development and progress of iron-overload-associated syndromes.
In our screening program for new agrochemicals from local wild plants, Artemisia lavandulaefolia and A. sieversiana were found to possess insecticidal activity against the maize weevil Sitophilus zeamais. The essential oils of the aerial parts of the two plants were obtained by hydrodistillation and analyzed by GC and GC/MS. The main components of A. lavandulaefolia oil were caryophyllene (15.5%), beta-thujone (13.8%), eucalyptol (13.1%), and beta-farnesene (12.3%), and the principal compounds identified in A. sieversiana oil were eucalyptol (9.2%), geranyl butyrate (9.2%), borneol (7.9%), and camphor (7.9%). The essential oils of A. lavandulaefolia and A. sieversiana possessed fumigant toxicity against S. zeamais adults with LC(50) values of 11.2 and 15.0 mg/l air, respectively. Both essential oils also showed contact toxicity against S. zeamais adults with LD(50) values of 55.2 and 112.7 microg/adult, respectively.
In this study, we analyzed the antioxidant and antimelanogenic properties of a variety of solvent extracts of pre-bloom and full-bloom chestnut flowers. Among the solvent extracts, a pre-bloom methanol extract (preM) and an ethanol extract (preE) showed the highest amounts of phenolics (467.92+/-0.45 and 456.24+/-5.88 mg of gallic acid equivalent/g of extract) and flavonoids (60.96+/-1.86 and 41.59+/-8.57 mg of quercetin equivalent/g of extract). These extracts exhibited the highest DPPH radical and reducing activities, as well as the greatest mushroom tyrosinase inhibition activity. In addition, preE effectively protected the skin against ultraviolet (UV) rays. Further, extracts were tested for cytotoxicity on human melanoma cells (SK-MEL-2), and we observed that all the extracts were non-cytotoxic for the cells. Their effects on tyrosinase and melanin inhibitory action were further assessed, and we found that all the extracts reduced the tyrosinase activity and melanin formation of SK-MEL-2 cells as effectively as arbutin. Moreover, the protein level expression of tyrosinase decreased dramatically. However, the protein levels of the other melanogenic enzymes, tyrosinase-related protein 1 (TRP1) and dopachrome tautomerase (DCT), were not altered significantly. Therefore, the antimelanogenic effects of chestnut flower extracts were attributable to their inhibitory effects on tyrosinase via their anti-oxidative action, making them a strong candidate for use in food, cosmetics, and pharmaceutical applications.
The aim of this study, linked-up with a previous study on bergamot oils, was the evaluation of phototoxic potential of essential oils (orange, lemon and Litsea cubeba), used as cosmetic ingredients. The applied tiered testing strategy included chemical analysis of the substances (by means of capillary gas chromatography/mass spectrometry), in vitro 3T3 NRU phototoxicity test and EpiDerm™ skin phototoxicity test. In order to clarify the situation in man, the highest non-phototoxic/non-cytotoxic concentrations and concentrations 10 x lower (safety factor 10) were tested xin vivo by means of human skin photopatch test in a limited group of human volunteers. The study revealed, that phototoxicity of the essential oils was dependent on the content of photoactive components and the solvent used. The highest non-phototoxic concentrations obtained by the skin model assay proved to be a useful starting point for subsequent confirmatory human photopatch test aimed to identify safe concentration for human use. However, the highest non-phototoxic concentration obtained in the skin model assay cannot be applied directly for human practice (3 of 8 tested oils evoked a phototoxic reaction). A safety factor of 10 should be applied for extrapolation of experimental data from the skin model assay to man.
In this study, potential inhibitory effect of 21 species of marine algae on melanogenesis was assessed via tyrosinase inhibitory effect. The Ishige okamurae extract tested herein evidenced profound tyrosinase inhibitory effect, compared to that exhibited by other marine algae extracts. Thus, I. okamurae was selected for use in further experiments, and was partitioned with different organic solvents. Profound tyrosinase inhibitory effect was detected in the ethyl acetate fraction, and the active compound was identified as the carmalol derivative, diphlorethohydroxycarmalol (DPHC), which evidenced higher levels of activity than that of commercial whitening agent. Intracellular reactive oxygen species (ROS) induced by ultraviolet (UV)-B radiation was reduced by the addition of DPHC and cell viability was dose-dependently increased. Moreover, DPHC demonstrated strong protective properties against UV-B radiation via damaged DNA tail length and morphological changes in fibroblast. Hence, these results indicate that DPHC isolated from I. okamurae has potential whitening effects and prominent protective effects on UV-B radiation-induced cell damages which might be used in pharmaceutical and cosmeceutical industries.
The composition of the essential oils obtained by hydrodistillation of different parts of Litsea cubeba, including roots, stems, leaves, alabastra (flower buds), flowers, and fruits, were investigated by GC (RI) and GC/MS. The antimicrobial activity of the oils was assessed with disc diffusion and microbroth dilution assays. The results showed large variations in the composition among the different oils. The major components in the oils from roots and fruits, from stems, leaves, and alabastra, and from flowers were citral B (neral), beta-phellandrene, and beta-terpinene, respectively. The inhibition zone (DD) and MIC values for the bacterial strains tested, which were all sensitive to the essential oil of L. cubeba, were in the range of 10.1-35.0 mm and 100-1000 microg/ml, respectively. Hence, the oils of the various parts showed moderate activity against the tested bacteria. This investigation showed that the antibacterial activity of L. cubeba was attributed to the essential oils, thus they can be a potential medicinal resource.
Many studies have reported that oxidative and nitrative stress might be important in the pathogenesis of diabetes. By means of immunoprecipitation analysis, alpha-enolase (EC 4.2.1.11, 2-phospho-d-glycerate hydrolyase) was identified as the important target for oxidative and nitrative modifications in diabetic cardiac proteins. The levels of protein carbonyls and 3-nitrotyrosine residues in alpha-enolase (biomarkers of oxidative and nitrative damage, respectively) from cardiac proteins of diabetic rats were determined and compared with age-matched controls. After 6 weeks of streptozotocin administration, the cardiac proteins from diabetic rats showed: (a) the levels of alpha-enolase expression and nitration were clearly increased, whereas (b) the enolase activity and oxidation status were not significantly changed. By means of immunoprecipitation and liquid chromatography-tandem mass spectrometry analysis, it was found that Tyr 257 and Tyr 131 of alpha-enolase were the most susceptible to nitration in diabetic rat heart. Further studies in vitro revealed a significant contribution of protein tyrosine nitration to the inactivation of enolase. These results suggest that tyrosine nitration of alpha-enolase could contribute to an impaired glycolytic activity in diabetic cardiomyopathy. Meanwhile, the up-regulation of alpha-enolase expression could be a protective mechanism to neutralize oxidative and nitrative stress in diabetes.
This study was designed to examine the composition of extracts and essential oil components from Nelumbo nucifera leaves from the principal habitats in China. The amounts of phenolics, flavonoids, and proanthocyanidins in the lotus leaf extracts varied widely, ranging from 354 to 487 mg/g gallic acid equivalents, from 172 to 236 mg/g rutin equivalents, and from 124 to 179 mg/g catechin equivalents, respectively. All of the extracts had strong antioxidant activity in comparison to the standard compounds butylated hydroxytoluene and vitamin C. Wild lotus samples from Baiyangdian Lake and Weishan Lake exhibited a stronger free radical scavenging effect and greater reducing power than the cultural samples, but no such differences were observed in the inhibition of lipid oxidation. Chemical variation in the essential oils from the various samples was analyzed by GC-MS. The main constituents were l-(+)-ascorbic acid 2,6-dihexadecanoate (0-33.5%), trans-phytol (5.1-24.1%), hexahydrofarnesyl acetone (5.6-15.3%), pentadecyl acrylate (2.2-12.4%), geranyl acetone (1.9-8.0%), and beta-ionone (0-8.0%). The rhizome lotus and seed lotus samples were clustered into separate groups by hierarchical cluster analysis according to the composition of the corresponding essential oils. No significant relationship was found between essential oil composition and geographical distribution of the 11 populations. However, the results indicated that region of origin and growing conditions could significantly affect both the bioactivities of the lotus leaf and the content of bioactive compounds in the leaves. Thus, the existence of chemical polymorphism in the N. nucifera leaf in China was demonstrated.
Synopsis
This study aimed to evaluate the free radical scavenging and inhibition properties of five medicinal plants, including Quercus infectoria Olive., Terminalia chebula Retz. , Lavendula stoechas L., Mentha longifolia L., Rheum palmatum L., toward the activity of mushroom tyrosinase using l ‐tyrosine and l ‐3,4‐dihydroxyphenylalanine ( l ‐DOPA) as the substrate. The methanol extracts of Q. infectoria and T. chebula showed strong radical scavenging effect in 2,2′‐dipheny l ‐1‐picrylhydrazyl (DPPH) assay (IC 50 = 15.3 and 82.2 μg mL ⁻¹ respectively). These plants also showed inhibitory effects against the activity of mushroom tyrosinase in hydroxylation of l ‐tyrosine (85.9% and 82.2% inhibition, respectively). These two plants also inhibited the oxidation of l ‐DOPA similar to kojic acid as positive control (IC 50 = 102.8 and 192.6 μg mL ⁻¹ respectively). In general Q. infectoria and T. chebula significantly inhibited tyrosinase activity and DPPH radical. Both activities were concentration‐dependant but not in linear manner. It is needed to study the cytotoxicity of these plant extracts in pigment cell culture before further evaluation and moving to in vivo conditions.
Contact toxicity of essential oils of Litsea pungens Hemsl. and L. cubeba (Lour.) Pers. (Lauraceae) and of blends of their major constituents was assessed against third-instar Trichoplusia ni larvae via topical application. Both oils showed moderate activity against T. ni larvae with LD(50) values of 87.1 and 112.5 microg/larva, respectively. 1,8-Cineole from the essential oil of L. pungens and gamma-terpinene from the oil of L. cubeba accounted for much of the toxicity of the oils to T. ni larvae. The toxicity of blends of selected constituents indicated a synergistic effect among putatively active and inactive constituents, with the presence of all constituents necessary for full toxicity of the natural oils. The results show that essential oils of L. pungens and L. cubeba and some of their constituents have potential for development as botanical insecticides.
To investigate the physiological functions of polyphenols from acerola (Malpighia emarginata DC.) fruit, the effects on melanogenesis were studied. The crude polyphenol concentrated extract from acerola (C-AP) was used to examine the skin-lightening effect on brownish guinea pigs which had been subjected to controlled UVB irradiation. The results show that C-AP significantly lightened the UVB-irradiated skin pigmentation. Furthermore, treatment with C-AP reduced the content of melanin in B16 melanoma cells, suggesting that the in vivo skin-lightening effect of C-AP was due to the suppression of melanin biosynthesis in melanocytes. In addition, we found that C-AP could effectively inhibit mushroom tyrosinase activity, the main constituents responsible for this effect being thought to be such anthocyanins as cyanidin-3-alpha-O-rhamnoside (C3R) and pelargonidin-3-alpha-O-rhamnoside (P3R). This result indicates that the skin-lightening effect of C-AP can be partly attributed to the suppression of melanogenesis through the inhibition of tyrosinase activity in melanocytes. An oral ingestion of C-AP may therefore be efficacious for reducing UVB-induced hyper-pigmentation by inhibiting the tyrosinase in melanocytes.
A new method for determining the size of titanium dioxide particles is proposed and assayed in a commercial sunscreen product. Today many sun protection cosmetics incorporate physical UV filters as active ingredients, and there are no official methods for determining these compounds in sunscreen cosmetics. Here flow field-flow fractionation (FlFFF) has been tested, first to sort two different types of TiO2 nano- and microstandard materials (AeroxideTiO2 Degussa P-25 and TiO2 rutile 0.1-0.2-microm size) and then to fractionate TiO2 particles, extracted from a commercial sunscreen lotion. All the TiO2 FlFFF separations were detected by UV but during elution fractions were collected and their Ti content measured by inductively coupled plasma-atomic emission spectrometer (ICP-AES); the Ti concentration profiles obtained by ICP-AES were well correlated with the UV signals. The TiO2 particle mass-size distribution were calculated from the UV profiles. This methodology is relatively simple and rapid, and the sample treatment is as a whole easy and low cost.
Nitric oxide (NO) is known to be synthesized by mammalian cells from L-arginine by a group of NO synthase enzymes. We now show that NO is generated from human skin and propose a different mechanism of production. Whereas enzymatic NO synthesis is inhibited by monomethyl L-arginine, this arginine analog, when infused into the brachial artery at concentrations sufficient to inhibit endothelial NO synthase activity, has little effect on hand skin NO production. Hand skin NO production is increased by topical acidification of the skin surface and greatly increased by the addition of nitrite solutions. We propose that NO generation from skin derives from sweat nitrite (the concentration of which was found to average 3.4 microM in six subjects) due to chemical reduction consequent to the acidic nature of sweat. Sweat contains nitrate in appreciable amounts, and skin commensal bacteria can synthesize nitrate reductase enzyme. Patients on long-term tetracycline antibiotics showed significantly reduced skin NO synthesis, although topical antiseptic and antibiotics had little effect on NO generation in the short-term. We propose that NO generation from skin is dependent on bacterial nitrate reduction to nitrite and subsequent reduction by acidification. We speculate that this has a physiologic role in the inhibition of infection by pathogenic fungi and other susceptible microorganisms and may affect cutaneous T-cell function, keratinocyte differentiation, and skin blood flow.
A method for the screening of antioxidant activity is reported as a decolorization assay applicable to both lipophilic and hydrophilic antioxidants, including flavonoids, hydroxycinnamates, carotenoids, and plasma antioxidants. The pre-formed radical monocation of 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS*+) is generated by oxidation of ABTS with potassium persulfate and is reduced in the presence of such hydrogen-donating antioxidants. The influences of both the concentration of antioxidant and duration of reaction on the inhibition of the radical cation absorption are taken into account when determining the antioxidant activity. This assay clearly improves the original TEAC assay (the ferryl myoglobin/ABTS assay) for the determination of antioxidant activity in a number of ways. First, the chemistry involves the direct generation of the ABTS radical monocation with no involvement of an intermediary radical. Second, it is a decolorization assay; thus the radical cation is pre-formed prior to addition of antioxidant test systems, rather than the generation of the radical taking place continually in the presence of the antioxidant. Hence the results obtained with the improved system may not always be directly comparable with those obtained using the original TEAC assay. Third, it is applicable to both aqueous and lipophilic systems.
Thymus pulegioides L. with lemon and carvacrol odor form the major part of plants growing wild in all 10 investigated localities during 1995-1997. The main components of the citral-geraniol chemotype of lemon-scented essential oil are the following (%): geraniol (14.9-30. 8), geranial (trans-citral, 9.7-19.7), beta-caryophylene (6.0-11.4), nerol (4.1-11.8), and neral (cis-citral, 0.1-9.5). The essential oil of carvacrol chemotypes contain more compounds that are characteristic of the thyme genus (%): carvacrol (16.0-22.2), beta-bisabolene (11.1-20.2), beta-caryophyllene (11.1-19.1), gamma-terpinene (5.8-16.2), p-cimene (5.5-10.4), thymol (3.3-9.8), and carvacrol methyl ether (5.6-8.6). The correlation between the odor and composition of the essential oil will help the users of wild thyme to choose the necessary chemotype for their purposes.
During a photo-induced catalytic reaction under near UV irradiation to an aqueous suspension of Ti4O2, about 95% of NO2- was oxidized to NO3-, but NH4+ was not detected. The oxidation was inhibited by the addition of mannitol or under anaerobic conditions. The nitration of HPA was observed in the presence of t-buthanol, suggesting the formation of ONOO. An ESR spectrum gave a triplet signal at g = 2.041,in the presence of NO2-, mannitol, FeSO4, and MGD, indicating the reduction of NO2- to NO.
Phenol photonitration and photonitrosation were studied both in homogeneous and in heterogeneous phase in the presence of TiO2 particles. The effect of pH as well as of the semiconductor particles on the kinetics and products of the reaction was observed. Formation of nitrophenols is enhanced at acidic pH, due to thermal processes initiated by nitrous acid, as well as in the presence of TiO2, due to the photocatalytic oxidation of nitrite.
There is a large body of evidence implicating oxidative damage in the pathogenesis of both normal aging and neurodegenerative diseases. Oxidative damage to proteins has been well established. Although there are a large number of potential oxidative modifications only a few have been systematically studied. The most frequently studied marker of oxidative damage to proteins is protein carbonyl groups. 3-Nitrotyrosine is thought to be a relatively specific marker of oxidative damage mediated by peroxynitrite. Increased concentrations of both protein carbonyls and 3-nitrotyrosine have been documented in both normal aging as well as in Alzheimer's disease (AD), Parkinson's disease (PD), and amyotrophic lateral sclerosis (ALS). These findings help to provide a rationale for trials of antioxidants in neurodegenerative diseases.
The versatile benefit effects of flavonoids lead some nutritionists to believe that they are micronutrients. However, excess intake of flavonoids may cause side effects. In this paper, the effects produced by a higher intake of rutin and baicalin on antioxidant status as well as trace minerals such as iron, copper and zinc in rat tissues were studied. When rats were fed a rutin or baicalin containing diet (1%) for 20 days, the body weight gain was lower than that of the control group. Both rutin and baicalin caused significant a decrease of catalase activity and a moderate increase of total superoxide dismutase activity in the liver. The total antioxidant status of flavonoid fed rats was increased in the liver but decreased in the serum. In comparison to the control group, the lipid peroxidation level in the liver of the rutin fed group was significantly decreased; however, there was no statistical significance in the liver of the baicalin fed group and the brain of both flavonoids groups. The liver homogenates of both flavonoid fed rats significantly inhibited alkyl radical-induced lipid peroxidation. The iron contents in the liver of flavonoid fed rats were significantly decreased; rutin also caused zinc and copper decrease in the liver. These results indicated that high flavonoid intake can improve rat antioxidant systems in the liver; while it can also cause a trace mineral decrease and, in turn, reduce the activities of some metal-containing enzymes and may cause harmful effects on health.
Many of the local UV-induced responses including erythema and edema formation, inflammation, premature aging, and immune suppression can be influenced by nitric oxide synthase (NOS)-produced NO which is known to play a pivotal role in cutaneous physiology. Besides NOS-mediated NO production, UV radiation might trigger an enzyme-independent NO formation in human skin by a mechanism comprising the decomposition of photo-reactive nitrogen oxides. Therefore, we have examined the chemical-storage forms of potential NO-generating agents, the mechanisms and kinetics of their decomposition, and their biological relevance. In normal human skin specimens we find nitrite and S-nitrosothiols (RSNO) at concentrations 25- or 360-fold higher than those found in plasma of healthy volunteers. UVA irradiation of human skin leads to high-output formation of bioactive NO due to photo-decomposition of RSNO and nitrite which represents the primary basis for NO formation during UVA exposure. Interestingly, reduced thiols strongly augment photo-decomposition of nitrite and are essential for maximal NO release. The enzyme-independent NO formation found in human skin opens a completely new field in cutaneous physiology and will extend our understanding of mechanisms contributing to skin aging, inflammation, and cancerogenesis.
Sunscreens protect skin against sunburn. However, studies have demonstrated that UV-irradiated sunscreen components such as titanium dioxide (TiO2) promote the photogeneration of reactive oxygen species (ROS). Because encapsulation of TiO2 within zeolites alters its photocatalytic activity, supramolecular composites based on NaY zeolite hosts containing TiO2 guests were prepared, and the effects on ROS formation in cells under UVA-irradiation evaluated. DCFH-DA (2',7'-dichlorofluorescein diacetate) was used as a profluorescent probe to monitor intracellular ROS. The detection of intracellular 2',7'-dichlorofluorescein (DCF) fluorescence by confocal microscopy revealed that DCFH-DA was taken up, hydrolyzed and oxidized by yeast cells and cultured human skin fibroblasts within 20 and 6 min, respectively. Higher DCF fluorescence was observed in fibroblasts following UVA irradiation in the absence but not in the presence of the radical nitroxide, TEMPOL (4-hydroxy-2,2,6,6-tetramethylpiperydine-1-oxyl), which exhibits superoxide dismutase-mimetic and catalase-mimetic activity. UVA-induced fluorescence increased by approximately 50% in the presence of 32-nm anatase TiO2 particles and decreased by essentially an equal amount in the presence of TiO2 encapsulated within NaY zeolites (TiO2@NaY). Addition of the uncomplexed NaY host also decreased (by approximately 30%) the amount of UVA-induced fluorescence but, unexpectedly, the combination of the free guest and host (TiO2+NaY) caused a doubling of the fluorescence. Protection of cells against TiO2-induced intracellular ROS by encapsulation suggests that supramolecular species may be beneficial in photoprotection of the skin. In contrast, the potentiation of TiO2-induced ROS by uncomplexed NaY points to a critical role for formulation when free TiO2 is used as a sun screen ingredient.
The antioxidant activity of Litsea cubeba was studied in terms of three different assay systems: DPPH assay, peroxidase/guaiacol assay, and TBA test. The L. cubeba methanol extract and its fractions showed remarkable antioxidant activity in comparison with alpha-tocopherol and ascorbic acid.
Ultrafine particles of titanium dioxide (TiO2) are very attractive as a UV protection ingredient in cosmetic products. The UV-scattering behavior of TiO2 suspensions in a silicone oil are studied in relation to rheological properties. To control the dispersion stability of suspensions, two types of polyether-modified silicones are used as dispersants. When the suspensions are prepared with branch-type dispersants in which the polyether groups are incorporated as side chains along the backbone, the flow is shear-thinning even at low shear rates. The appearance of plateaus in the frequency-dependence curves of storage modulus implies the solidlike responses. On the other hand, the suspensions prepared with linear conformation dispersants, in which the silicone group and polyether group are alternately repeated in one long chain, are Newtonian at low shear rates. The suspensions are regarded as liquids, because the storage modulus decreases rapidly in the low-frequency region. The suspension rheology is strongly associated with flocculated structures that are primarily controlled by the interparticle attractions. The differences in rheological behavior can be explained by the differences in the adsorbed conformation of dispersant silicones. From optical measurements, it is confirmed that UV scattering increases with decreasing flocculation degree. Therefore, good agreement is established between rheological properties and UV protection ability.
Essential oils are commonly used fragrance ingredients. The oils themselves are complex mixtures, which may contain naturally occurring contact sensitizers. The local lymph node assay was used to evaluate the dermal sensitization potential of basil, citronella, clove leaf, geranium, litsea cubeba, lemongrass, and palmarosa oils. Three of the major components--citral, eugenol, and geraniol--were included to investigate any difference in sensitization potential arising from their exposure in a mixture. Each fragrance material was tested at five concentration ranging from 2.5% to 50% w/v in 1:3 ethanol:diethyl phthalate. The stimulation index (SI) values were calculated for each dose level, an SI > or = 3 was considered a positive response. The estimated concentration (EC3) required to elicit a positive was calculated and taken as a measure of relative potency. The EC3 values and potency classification for basil, clove leaf, litsea cubeba, lemongrass and palmarosa oils were calculated to be <2.5% (> or = moderate), 7.1% (weak), 8.4% (weak), 6.5% (weak) and 9.6% (weak), respectively. Citronella and geranium oils were negative. The individual components citral, eugenol and geraniol resulted in EC3 values of 6.3%, 5.4% and 11.4%, respectively. In general, the potency of each essential oil did not differ significantly from that observed for its main individual component.
Because tyrosinase catalyzes melanin synthesis, tyrosinase inhibitors are important in cosmetic skin-whitening. Oxidative stress contributes to skin aging and can adversely affect skin health, which means antioxidants active in skin cells may support skin health. We examined 25 traditional Chinese herbal medicines that might be useful for skin-whitening and skin health. Extracts (100microg/mL) were tested for cytotoxicity on human epidermal melanocytes (HEMn); 12 exhibited low cytotoxicity. Their effects on tyrosinase and melanin inhibitory activities and free radical scavenging activities were further assessed. Phenolic contents were evaluated using Folin-Ciocalteu reagent. Four herbs, Pharbitis nil, Sophora japonica, Spatholobus suberectus, and Morus alba, exhibited potent inhibitory effects on tyrosinase (IC(50) values 24.9, 95.6, 83.9, and 78.3microg/mL, respectively). Melanin inhibition was not dose-dependent. Sophora japonica (IC(50): 14.46microg/mL, 1,1-diphenyl-2-picrylhydrazyl (DPPH); 1.95microg/mL, hydroxyl radical) and Spatholobus suberectus (IC(50): 10.51microg/mL, DPPH; 4.36microg/mL, hydroxyl radical) showed good antioxidative activities and high phenolic contents (255 and 189mg of gallic acid/g extract, respectively). Among active anti-tyrosinase extracts, Sophora japonica and Spatholobus suberectus were especially potent in HEMn cells in terms of free radical scavenging effects and high phenolic contents, making them the strongest candidates for cosmetic application found in the current study.
Nitrite (NO(2)(-)) occurs ubiquitously in biological fluids such as blood and sweat. Ultraviolet A-induced nitric oxide formation via decomposition of cutaneous nitrite, accompanied by the production of reactive oxygen (ROS) or nitrogen species (RNS), represents an important source for NO in human skin physiology. Examining the impact of nitrite and the antioxidants glutathione (GSH), Trolox (TRL), and ascorbic acid (ASC) on UVA-induced toxicity of human skin fibroblasts (FB) we found that NO(2)(-) concentration-dependently enhances the susceptibility of FB to the toxic effects of UVA by a mechanism comprising enhanced induction of lipid peroxidation. While ASC completely protects FB cultures from UVA/NO(2)(-)-induced cell damage, GSH or TRL excessively enhances UVA/NO(2)(-)-induced cell death by a mechanism comprising nitrite concentration-dependent TRL radical formation or GSH-derived oxidative stress. Simultaneously, in the presence of GSH or TRL the mode of UVA/NO(2)(-)-induced cell death changes from apoptosis to necrosis. In summary, during photodecomposition of nitrite, ROS or RNS formation may act as strong toxic insults. Although inhibition of oxidative stress by NO and other antioxidants represents a successful strategy for protection from UVA/NO(2)(-)-induced injuries, GSH and TRL may nitrite-dependently aggravate the injurious impact by TRL or GSH radical formation, respectively.
Titanium dioxide (TiO2) nanoparticles are ubiquitously used materials in everyday life (e.g. paints,household products and plastic goods). However, despite the wide array of common applications, their pathogenetic role was also suggested under certain conditions (e.g. pulmonary neoplasias and lung fibrosis). From a dermatological point of view, it is also of great importance that TiO2 also serves as a physical photoprotective agent in sunscreens and is widely used in various cosmetic products. However, the effect of TiO2 on human cutaneous functions is still unknown. Therefore, in the current study, we investigated the in vivo penetration of TiO2 via human skin transplanted to immunodeficient mice and,furthermore, we measured the in vitro effects of nanoparticles on various functional properties of numerous epidermal and dermal cells in culture. Hereby, using various nuclear microscopy methods, we provide the first evidence that TiO2nanoparticles in vivo do not penetrate through the intact epidermal barrier. However, we also report that TiO2, when exposed directly to cell cultures in vitro, exerts significant and cell-type dependent effects on such cellular functions as viability, proliferation, apoptosis and differentiation. Therefore, our novel findings will hopefully inspire one to systemically explore in future, clinically oriented trials whether there is indeed a risk from micronized TiO2-containing products on skin with an impaired stratum corneum barrier function.
Protein tyrosine nitration is a prevalent post-translational modification which occurs as a result of oxidative and nitrative stress, it may be directly involved in the onset and/or progression of diseases. Considering the existence of nano titanium dioxide (TiO(2)) in environment and sunscreen products along with the high content of nitrite in sweat, the UV-exposed skin may be a significant target for the photosensitized damage. In this paper, tyrosine nitration of bovine serum albumin (BSA) was initiated in the UV-irradiated reaction mixture containing 0.2-3.0mg/ml of three commercially nano TiO(2) products and 0.25-1.0mM NO2-. It was found that anatase TiO(2) and Degussa P25 TiO(2) showed prominent photocatalytic activity on promoting the formation of protein tyrosine nitration, and the optimum condition for the reaction was around physiological pH. Meanwhile, the photocatalytic effect of rutile on protein tyrosine nitration was subtle. The potential physiological significance of nano TiO(2)-photocatalytic protein nitration was also demonstrated in mouse skin homogenate. Although the relationship between photocatalytic protein tyrosine nitration and chronic cutaneous diseases needs further study, the toxicity of nano TiO(2) to the skin disease should be paid more attention in the production and utilization process.
To investigate the stem bark of Sideroxylon inerme L. and its compounds for tyrosinase-inhibition activity and to evaluate the mechanism involved of the most potent compounds in tyrosinase inhibition.
Three different extracts (acetone, methanol and dichloromethane) of Sideroxylon inerme L. were evaluated for their inhibitory effect in vitro on the monophenolase and diphenolase activated forms of tyrosinase, using a colorimetric procedure. This test was used for bioactivity-guided isolation of two active compounds using column chromatography and TLC. Active extracts were also investigated for their inhibitory effect on melanogenesis in cultured B16 melanoma cells. Antioxidant activities of the methanolic extract of Sideroxylon inerme and purified compounds were investigated using the 1,2-diphenyl-2-picrylhydrazyl (DPPH) antioxidant assay. The inhibition of tyrosinase activity relative to the inhibition of its activity at the transcriptional level was also studied by determination of the degree of expression of mRNAs for this gene by using extract of Sideroxylon inerme-treated cells (B16F10) and semi-quantitative RT-PCR.
Methanolic and acetonic extracts of the stem bark of Sideroxylon inerme showed significant inhibition of monophenolase activity (IC50 values of 63 microg/ml and 82 microg/ml, respectively). The methanolic extract also exhibited 37% reduction of melanin content at 6.2 microg/ml in melanocytes without being significantly toxic to the cells. Examination for inhibition of monophenoloxidase in situ on TLC, followed by column chromatographic purification of the stem bark extract of Sideroxylon inerme, resulted in the isolation of two active compounds, epigallocatechin gallate and procyanidin B1, with IC50 values against monophenolase of 30 microg/ml and > 200 microg/ml, respectively. Epigallocatechin gallate exhibited a greater anti-tyrosinase activity than arbutin. Sideroxylon inerme bark extracts, epigallocatechin gallate and procyanidin B1 exhibited antioxidant DPPH radical scavenging activities with EC50 values of 1.54 microg/ml, 1.33 microg/ml and 1.68 microg/ml, respectively and were not particularly cytotoxic. During mechanism studies it was evident that at the transcription level, Sideroxylon inerme (25 microg/ml) was acting as a potent tyrosinase inhibitor compared to controls (untreated cells and kojic acid).
The bark extract of Sideroxylon inerme and the two isolated compounds warrant further investigation in clinical studies to be considered as skin-depigmenting agents.