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Bioactive terpenoids 1 and 2 along with a known compound, β-sitosterol, have been isolated from the DCM extract of the fruits of Lagerstroemia speciosa. Structures of 1 and 2 have been established by spectroscopic analysis. In vitro antibacterial and antifungal activity of 1 and 2 have been reported. Compound 1 showed poor activity, but compound 2 exhibited significant antibacterial and antifungal activities. Molecular docking study of 2 also showed a good docking score within the binding pocket of the selected proteins. [ABSTRACT FROM AUTHOR]

Strigolactones (SLs) are plant hormones that regulate shoot branching and diverse developmental processes. They are biosynthesized from carotenoid molecules via a key biosynthetic precursor called carlactone (CL) and its carboxylated analog, carlactonoic acid (CLA). We have previously identified the methyl esterified derivative of CLA, methyl carlactonoate (MeCLA), as an endogenous SL-like molecule in Arabidopsis. Neither CL nor CLA could interact with the receptor protein, Arabidopsis DWARF14 (AtD14), in vitro, while MeCLA could, suggesting that the methylation step of CLA is critical to convert a biologically inactive precursor to a bioactive compound in the shoot branching inhibition pathway. Here, we show that a member of the SABATH protein family (At4g36470) efficiently catalyzes methyl esterification of CLA using S-adenosyl-L-methionine (SAM) as a methyl donor. We named this enzyme CLAMT for CLA methyltransferase. The Arabidopsis loss-of-function clamt mutant accumulated CLA and had substantially reduced MeCLA content compared with wild type (WT), showing that CLAMT is the main enzyme that catalyzes CLA methylation in Arabidopsis. The clamt mutant displayed an increased branching phenotype, yet the branch number was less than that of severe SL biosynthetic mutants. Exogenously applied MeCLA, but not CLA, restored the branching phenotype of the clamt mutant. In addition, grafting experiments using the clamt and other SL biosynthetic mutants suggest that CL and CLA are transmissible from root to shoot. Taken together, our results demonstrate a significant role of CLAMT in the shoot branching inhibition pathway in Arabidopsis. [ABSTRACT FROM AUTHOR]

Elicitor treatments play an important role in inducing some protective signal transmitter enzymes in cells and regulating phenylalanine ammonia-lyase (PAL) activity. The aim of this study was to determine the effects of elicitors [silver nitrate (AgNO3), salicylic acid (SA) and yeast extract (YE)], which were added individually or in combination to Ocimum basilicum L. cell suspension cultures, on the production and antioxidant activity of secondary metabolites (SMs). Calluses were obtained from the leaves of O. basilicum kept on Murashige and Skoog (MS) medium containing 0.5 mg/1 kinetin (KIN) + 2.5 mg/1 naphthalene-acetic acid (NAA) and cell suspension cultures were initiated. Then elicitors were applied to the cell suspension cultures individually or in combination, and cells were harvested at the end of the second, fourth, and eighth days. Compared with the control culture, the maximum rosmarinic and chicoric acid production was obtained at the end of the 4th day from SA (24 μM) + YE (80 mg/1) treatment as 20.19 mg/gDW (118%) and 7.55 mg/g DW (123%), respectively. The maximum biosynthesis of isoquercetin and rutin compared with the control culture was 3.88 mg/g DW [YE (80 mg/1)] with a 1.6-fold increase and 6.35 mg/g DW [YE (80 m g∕l) + AgNO3 (6 μM)] with a 1.76-fold increase, respectively. Estragole and linalool's highest values compared with the control culture were 4.50 μg∕g DW [AgNO3 (6μM) + SA (24 μM)] and 3.02 μg∕g DW [SA (24 μM)], respectively. Results clearly show that the elicitor treatment could enhance the biosynthesis of phenolic compounds and terpenoid content in cell suspension cultures of 0. basilicum and may be used for commercial supply in the future for therapeutic applications. [ABSTRACT FROM AUTHOR]

Terpenoids, which constitute one of the most diverse groups of bioactive compounds in plants, contribute to about 60% of the known natural compounds. Tea (Camellia sinensis), which is a highly preferred beverage throughout the world, is also rich in these flavor-imparting bioactive compounds. In this study, a simplified spectrophotometric method has been developed for the quantitative estimation of terpenoids in polyphenol-rich tea plant. Furthermore, terpenoid content in leaves and flowers of tea plant and their respective in vitro cultured cells have also been estimated. Terpenoid content was found to be up to five folds higher in flowers (123.9 mg/g DW) than in leaves (24.2 mg/g DW), and up to 1.7 folds higher in cultured flower cells (184.8 mg/g DW) as compared to in vitro cultured leaf cells (110.1 mg/g DW). Additionally, comparison of terpenoid content in tea leaves across the four different plucking seasons revealed a unique pattern wherein second (42.2 mg/g) and fourth flush (42.6 mg/g) tea were found to have the highest terpenoid content. First of its kind, this study provides an inexpensive method for screening of cultivars with better flavour and defense attributes. Furthermore, it also paves a way for future research in tea flowers which have high terpenoid content and the utilization of these therapeutic bioactive terpenoids in the development of diverse products for human health and wellness. [ABSTRACT FROM AUTHOR]

Background and Aims Climate change is subjecting subarctic ecosystems to elevated temperature, increased nutrient availability and reduced light availability (due to increasing cloud cover). This may affect subarctic vegetation by altering the emissions of biogenic volatile organic compounds (BVOCs) and leaf anatomy. We investigated the effects of increased nutrient availability on BVOC emissions and leaf anatomy of three subarctic dwarf shrub species, Empetrum hermaphroditum , Cassiope tetragona and Betula nana , and if increased nutrient availability modifies the responses to warming and shading. Methods Measurements of BVOCs were performed in situ in long-term field experiments in the Subarctic using a dynamic enclosure system and collection of BVOCs into adsorbent cartridges analysed by gas chromatography–mass spectrometry. Leaf anatomy was studied using light microscopy and scanning electron microscopy. Key Results Increased nutrient availability increased monoterpene emission rates and altered the emission profile of B. nana , and increased sesquiterpene and oxygenated monoterpene emissions of C. tetragona. Increased nutrient availability increased leaf tissue thicknesses of B. nana and C. tetragona , while it caused thinner epidermis and the highest fraction of functional (intact) glandular trichomes for E. hermaphroditum. Increased nutrient availability and warming synergistically increased mesophyll intercellular space of B. nana and glandular trichome density of C. tetragona , while treatments combining increased nutrient availability and shading had an opposite effect in C. tetragona. Conclusions Increased nutrient availability may enhance the protection capacity against biotic and abiotic stresses (especially heat and drought) in subarctic shrubs under future warming conditions as opposed to increased cloudiness, which could lead to decreased resistance. The study emphasizes the importance of changes in nutrient availability in the Subarctic, which can interact with climate warming and increased cloudiness effects. [ABSTRACT FROM AUTHOR]

Cannabis spp. are some of the most controversial medicinal plants in the world. They contain great amounts of biologically active secondary metabolites, including the typical phenolic compounds called cannabinoids. Because of their low toxicity and complex biological activities, cannabinoids can be useful in the therapy of various diseases, but adverse psychological effects (of Δ9-THC in particular) raise concerns. This review summarizes the current knowledge of selected active C. indica compounds and their therapeutic potential. We summarize the main compounds contained in cannabis, the mechanisms of their effects, and their potential therapeutic applications. Further, we mention some of the clinical tests used to evaluate the efficacy of cannabinoids in therapy. [ABSTRACT FROM AUTHOR]

Rosa rugosa is not only cultivated as a landscaping plant, but also used in cosmetics, the medical and food industries. However, little information is currently available on the gene regulatory networks involved in its scent and color biosynthesis and metabolism. In this study, R. rugosa Thunb. f. rosea Rehd with red petals (RR) and its white petal variant (WR), were used to study the molecular mechanisms in flower color and scent. Sixty-five differential flavonoid metabolites and 15 volatiles were found to have significant differences between RR and WR. Correspondingly, the key regulators (MYB-bHLH-WD40) of anthocyanin synthesis pathway and their structural genes involved in flavonoid biosynthesis, benzenoid/phenylpropanoid biosynthesis, terpenoid biosynthesis pathways were also found to be differentially expressed by comparative transcriptome. Further, qPCR permitted the identification of some transcripts encoding proteins that were putatively associated with scent and color biosynthesis in roses. Particularly, the results showed that the ACT gene (encoding CoA geraniol/citronellol acetyltransferase, GeneID: 112190420), which expressed lower in WR, was involved in three pathways: flavonoid biosynthesis, phenylpropanoid biosynthesis and terpenoid biosynthesis, however, GT5 (anthocyanin glycosylation gene, GeneID:112186660), expressed higher in WR, was involved in both flavonoid and phenylpropanoid biosynthesis pathways. These results suggested that ACT and GT5 might play important roles in regulating the relationship of color pigmentation and volatile emission.

The Mango parasite is a parasitic plant that is very detrimental to mango plant owners but has the potential as a producer of secondary metabolites which are expected to inhibit the growth of the fungus Candida albicans. This study aimed to obtain antifungal activity fractions, to obtain pure compound eluates which were active as antifungals, to determine the class of compounds active as antifungals, and to determine the Minimum Inhibitory Concentration (MIC) against the fungus C. albicans. Based on the research that has been done, the fractions that are active as antifungals are the n-hexane and ethyl acetate fractions. The results of purification of the n-hexane and ethyl acetate fractions using gravity column chromatography showed the presence of two pure n-hexane compounds that were active in inhibiting C. albicans, namely N-1 and N4 eluates with inhibition zone diameters of 12 mm and 10 mm, respectively. Purification of the ethyl acetate fraction produced two active compounds, namely eluate E-1 and eluate E-5 which were able to inhibit C. albicans by 10 mm and 12 mm, respectively. The MIC values ​​for N-1, N-4, and E-1 eluates were able to inhibit at a concentration of 500 ppm and were classified as quite strong. The E-5 eluate capable of inhibiting at a concentration of 1000 ppm is classified as weak. Tests for the class of compounds using Thin Layer Chromatography (TLC) and the R¦ value of the biautography results showed the color spots on the N-1 eluate (R¦: 0.9) were blue in the terpenoid group, on the N-4 eluate (R¦: 0.6) Alkaloid group is orange in color, the E-1 eluate (R¦: 0.8) is yellow in the Phenolic group, the E-5 eluate (R¦: 0.9) is purple in the terpenoid group.

Degraded limonoids are a subclass of limonoid natural products that derive from ring-intact or ring-rearranged limonoids. Establishment of robust synthetic routes to access them could provide valuable materials to identify the simplest active pharmacophore responsible for the observed biological activities of the parent molecules. This communication delineates the development of a divergent strategy to furnish melazolide B and several other related congeners from a common keto-lactone intermediate, which was rapidly assembled from α-ionone. A chemoselective carbonyl α,β-dehydrogenation and a Wharton reduction were key strategic steps in this synthetic pathway.

With the increasing advancement of supramolecular chemistry, the focus is gradually shifting from the preparation of traditional polymeric materials to the development of multifunctional supramolecular materials. Among the building blocks of supramolecular materials, natural small molecules with intrinsic assembly properties are preferred over synthetic molecules due to their lower toxicity, better biocompatibility, biodegradability, and bioactivity. Terpenoids, as a kind of natural product with a wide range of supply sources, numerous modification sites, and abundant functions, have become a promising platform for the construction of supramolecular materials. Currently, many supramolecular materials based on different terpenoids have been successfully developed, which play an important role in tissue engineering, biomedicine, food science, and flexible electronics. This review comprehensively integrates and summarises current research findings on typical terpenoid-based supramolecular materials, including low-molecular-weight gels, nanocarriers for drug delivery, chiral self-assembled materials, and emulsion gels, focusing on their preparation methods, assembly processes, structural characteristics, and applications. The aim of this review is to draw attention to the potential of natural terpenoids, promote their exploitation and utilisation, and offer more alternatives for the creation of supramolecular materials. [ABSTRACT FROM AUTHOR]

Public use of Salvia species and their importance in the scientific world is continually increasing. It is known that this use and the importance of Salvia species are mostly due to the terpenoid compounds that they contain. In this context, the terpenoid–steroid–flavonoid contents of extracts of six endemic Salvia (S. kurdica, S. pseudeuphratica, S. rosifolia, S. siirtica, S. cerino‐pruinosa var. cerino‐pruinosa and S. cerino‐pruinosa var. elazigensis) species prepared with different solvents were determined by gas chromatography–mass spectrometry. Within the framework of the ingredient analysis, content analysis of the ethanol extracts of the root, branch, leaf and flower parts of the species collected in the same period between 2015 and 2017 years was performed. In general, extracts prepared with chloroform and ethanol were found to contain a wide variety of compounds while petroleum ether extracts were found to contain much less varied compounds. In addition, in general, root extracts are richer in terpenoid compounds than aerial part extracts. Some species can be used as source species in terms of ferruginol, cryptanol, 6,7‐dehydroroyleanone, lup‐(20)29‐ene‐2α‐hydroxy‐3β‐acetate, salvigenin and β‐sitosterol contents (52,114.28, 75,979.08, 101,247.41, 40,071.29, 33,952.13 and 34,010.90 μg analyte/g extract, respectively). [ABSTRACT FROM AUTHOR]

Taraxerol is an oleanane-type pentacyclic triterpenoid compound distributed in many plant species that has good effects on the treatment of inflammation and tumors. However, the taraxerol content in medicinal plants is low, and chemical extraction requires considerable energy and time, so taraxerol production is a problem. It is a promising strategy to produce taraxerol by applying recombinant microorganisms. In this study, a Saccharomyces cerevisiae strain WKde2 was constructed to produce taraxerol with a titer of 1.85 mg·l–1, and the taraxerol titer was further increased to 12.51 mg·l–1 through multiple metabolic engineering strategies. The endoplasmic reticulum (ER) size regulatory factor INO2, which was reported to increase squalene and cytochrome P450-mediated 2,3-oxidosqualene production, was overexpressed in this study, and the resultant strain WTK11 showed a taraxerol titer of 17.35 mg·l–1. Eventually, the highest reported titer of 59.55 mg·l–1 taraxerol was achieved in a 5 l bioreactor. These results will serve as a general strategy for the production of other triterpenoids in yeast. [ABSTRACT FROM AUTHOR]

Although comprehensive exertions have been made in late decades for treating advanced lung cancer with inclusive therapies but efficient anti‐lung cancer therapeutics are statically inadequate in the clinics. Hence, compelling novel anti‐lung cancer drugs are considerably desired. This backdrop enticed us to unveil anticancer efficacy of astrakurkurol, derivative of wild edible mushroom against lung cancer, whose effects have not yet been described. Mechanistic analysis disclosed that sensitizing effect of astrakurkurol is due to cell cycle arrest at G0/G1 phase, increased level of Fas, FADD, decreased ratio of Bax/Bcl‐2, and increased cleaved form of caspase 9, 8, and 3. Apart from the induction of apoptosis, it was demonstrated for the first time that astrakurkurol induced an autophagic response as evidenced by the development of acidic vesicular organelles (AVOs) with up‐regulation of beclin‐1, Atg7, and downregulated p62. Apoptosis and autophagy can be sparked by the same stimuli, which was as evident from the astrakurkurol‐induced inactivation of PI3K/AKT signaling. The thorough scanning of the mechanism of crosstalk between apoptosis and autophagy is requisite for prosperous anticancer remedy. Triterpenoid has evidently intensified cytotoxicity, induced apoptosis and autophagy on A549 cells. Besides astrakurkurol could also curb migration and regress the size of tumor in ex ovo xenograft model. All these findings put forth astrakurkurol as a convincing novel anti‐cancer agent, for scrutinizing the lung cancer therapies and as a robust contender for future in vitro and in vivo analysis. [ABSTRACT FROM AUTHOR]

The genus Fissistigma belongs to Annonaceae family and is mainly distributed in tropical areas of Asia. Many species from this genus have long been used for medicinal purposes in China and Vietnam. To date, there have been a number of studies on both phytochemical and pharmacological aspects of Fissistigma species, which indicated that the genus is a rich source of diverse and novel bioactive compounds, including alkaloids, terpenoids and phenolic derivatives. The review aims to summarise past study results as well as analyse future directions of Fissistigma species research. [ABSTRACT FROM AUTHOR]

This article attempts to report native growth, plant description, phytochemical constituents and bioactivities of Syzygium aqueum, S. aromaticum, S. cumini, S. guineense and S. samarangense. Those are the large public species in the Syzygium genus and some of them have been used as traditional medicines. Different parts (leaves, seeds, fruits, barks, stem barks and flower buds) of each species plant are rich in phytochemical constituents such as flavonoids, terpenoids, tannins, glycosides and phenolics. Antioxidant, antidiabetic, anticancer, toxicity, antimicrobial, anti-inflammatory and anthelmintic activities are reported in various extracts (methanol, ethanol and aqueous) from different parts of Syzygium sp. The bioactivities were studied by using 1,1-diphenyl-2-picrylhydrazyl and ferric reducing antioxidant power assays for antioxidant, 5-(3-carboxymethoxyphenyl)-2-(4,5-dimethyl-thiazoly)-3-(4-sulfophenyl) tetrazolium and 3-(4,5-dimethylthiazol-2-yl)-2-5-diphenyltetrazolium bromide assays for anticancer, α-glucosidase and α-amylase inhibition assays for antidiabetic, agar well diffusion method for antimicrobial and brine shrimp lethality assay for toxicity. Moreover, this review shows that phytochemical constituents of each species significantly presented various bioactivities. Therefore, this review suggests that there is great potential for obtaining the lead drug from these species.

Efficacy of fungi Volatile Organic Compounds. A review Introduction. Excessive use of chemical fungicides continues to drive research towards environmentally friendly and innovative alternatives for crop protection. Literature. Fungi produce various mixtures of compounds in the gas phase, called Volatile Organic Compounds (VOCs). They are able to diffuse into the soil and into the atmosphere and inhibit the activities of fungal pathogens. In this section, we will summarize recent knowledge on the inhibitory potential of Volatile Organic Compounds against pathogenic fungi with a focus on the effect of fungal VOCs. In practice, we will unveil initial research revealing their mode of action and any non-specific phytotoxic effects on the environmental microbiome and on plants. Conclusions. This article discusses new techniques used by researchers that focus on mycofumigation to optimize the formulation of a new generation of biofungicides. Thus, a new horizon is emerging for biological control of crop diseases.

Abstract Background Climate plays an essential role in forest health, and climate change may increase forest productivity losses due to abiotic and biotic stress. Increased temperature leads to the increased formation of ozone (O3). Ozone is formed by the interaction of sunlight, molecular oxygen and by the reactions of chemicals commonly found in industrial and automobile emissions such as nitrogen oxides and volatile organic compounds. Although it is well known that productivity of Northern red oak (Quercus rubra) (NRO), an ecologically and economically important species in the forests of eastern North America, is reduced by exposure to O3, limited information is available on its responses to exogenous stimuli at the level of gene expression. Results RNA sequencing yielded more than 323 million high-quality raw sequence reads. De novo assembly generated 52,662 unigenes, of which more than 42,000 sequences could be annotated through homology-based searches. A total of 4140 differential expressed genes (DEGs) were detected in response to O3 stress, as compared to their respective controls. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses of the O3-response DEGs revealed perturbation of several biological pathways including energy, lipid, amino acid, carbohydrate and terpenoid metabolism as well as plant-pathogen interaction. Conclusion This study provides the first reference transcriptome for NRO and initial insights into the genomic responses of NRO to O3. Gene expression profiling reveals altered primary and secondary metabolism of NRO seedlings, including known defense responses such as terpenoid biosynthesis.

Abstract Background Celastrol is a promising anti-obesity agent that acts as a sensitizer of the protein hormone leptin. Despite its potent activity, a sustainable source of celastrol and celastrol derivatives for further pharmacological studies is lacking. Results To elucidate the celastrol biosynthetic pathway and reconstruct it in Saccharomyces cerevisiae, we mined a root-transcriptome of Tripterygium wilfordii and identified four oxidosqualene cyclases and 49 cytochrome P450s as candidates to be involved in the early steps of celastrol biosynthesis. Using functional screening of the candidate genes in Nicotiana benthamiana, TwOSC4 was characterized as a novel oxidosqualene cyclase that produces friedelin, the presumed triterpenoid backbone of celastrol. In addition, three P450s (CYP712K1, CYP712K2, and CYP712K3) that act downstream of TwOSC4 were found to effectively oxidize friedelin and form the likely celastrol biosynthesis intermediates 29-hydroxy-friedelin and polpunonic acid. To facilitate production of friedelin, the yeast strain AM254 was constructed by deleting UBC7, which afforded a fivefold increase in friedelin titer. This platform was further expanded with CYP712K1 to produce polpunonic acid and a method for the facile extraction of products from the yeast culture medium, resulting in polpunonic acid titers of 1.4 mg/L. Conclusion Our study elucidates the early steps of celastrol biosynthesis and paves the way for future biotechnological production of this pharmacologically promising compound in engineered yeast strains.

Halocynthia roretzi, the edible ascidian, has been demonstrated to be an important source of bioactive natural metabolites. Here, we reported a novel terpenoid compound named Halorotetin A that was isolated from tunic ethanol extract of H. roretzi by silica gel column chromatography, preparative layer chromatography (PLC), and semipreparative-HPLC. 1H and 13C NMRs, 1H-1H COSY, HSQC, HMBC, NOESY, and HRESIMS profiles revealed that Halorotetin A was a novel terpenoid compound with antitumor potentials. We therefore treated the culture cells with Halorotetin A and found that it significantly inhibited the proliferation of a series of tumor cells by exerting cytotoxicity, especially for the liver carcinoma cell line (HepG-2 cells). Further studies revealed that Halorotetin A affected the expression of several genes associated with the development of hepatocellular carcinoma (HCC), including oncogenes (c-myc and c-met) and HCC suppressor genes (TP53 and KEAP1). In addition, we compared the cytotoxicities of Halorotetin A and doxorubicin on HepG-2 cells. To our surprise, the cytotoxicities of Halorotetin A and doxorubicin on HepG-2 cells were similar at the same concentration and Halorotetin A did not significantly reduce the viability of the normal cells. Thus, our study identified a novel compound that significantly inhibited the proliferation of tumor cells, which provided the basis for the discovery of leading compounds for antitumor drugs.

Sulfur cements have drawn significant attention as binders because sulfur is a byproduct of fossil fuel refining. Sulfur cements that can be formed by the vulcanization of elemental sulfur and plant-derived olefins such as terpenoids are particularly promising from a sustainability standpoint. A range of terpenoid–sulfur cements have shown compressional and flexural properties exceeding those of some commercial structural mineral cements. Pozzolans such as fly ash (FA), silica fume (SF), and ground granulated blast furnace slag (GGBFS) and abundant clay resources such as metakaolin (MK) are attractive fines for addition to binders. Herein, we report 10 composites prepared by a combination of sulfur, terpenoids (geraniol or citronellol), and these pozzolans. This study reveals the extent to which the addition of the pozzolan fines to the sulfur–terpenoid cements influences their mechanical properties and chemical resistance. The sulfur–terpenoid composites CitS and GerS were prepared by the reaction of 90 wt% sulfur and 10 wt% citronellol or geraniol oil, respectively. The density of the composites fell within the range of 1800–1900 kg/m3 and after 24 h submersion in water at room temperature, none of the materials absorbed more than 0.7 wt% water. The compressional strength of the as-prepared materials ranged from 9.1–23.2 MPa, and the percentage of compressional strength retained after acid challenge (submersion in 0.1 M H2SO4 for 24 h) ranged from 80–100%. Incorporating pozzolan fines into the already strong CitS (18.8 MPa) had negligible effects on its compressional strength within the statistical error of the measurement. CitS-SF and CitS-MK had slightly higher compressive strengths of 20.4 MPa and 23.2 MPa, respectively. CitS-GGBFS and CitS-FA resulted in slightly lower compressive strengths of 17.0 MPa and 15.8 MPa, respectively. In contrast, the compressional strength of initially softer GerS (11.7 MPa) benefited greatly after incorporating hard mineral fines. All GerS derivatives had higher compressive strengths than GerS, with GerS-MK having the highest compressive strength of 19.8 MPa. The compressional strengths of several of the composites compare favorably to those required by traditional mineral cements for residential building foundations (17 MPa), whereas such mineral products disintegrate upon similar acid challenge.

Introduction: Ibrexafungerp is a new triterpenoid antifungal agent with activity against a variety of fungal species, including Aspergillus spp. and echinocandin-resistant Candida spp., Areas Covered: This evaluation will summarize currently available clinical evidence on the use of ibrexafungerp in the treatment/prevention of vulvovaginal candidiasis (VVC) and detail the mechanism of action, pharmacokinetic/pharmacodynamic parameters, and ongoing/latest research involving ibrexafungerp., Expert Opinion: The evidence involving the utilization of ibrexafungerp for the treatment of VVC shows that it is superior when compared to placebo and has comparable clinical cure rates when compared with fluconazole. Ibrexafungerp demonstrates reliable coverage against several Candida spp. including echinocandin-resistant strains, Candida auris , and Aspergillus spp. For VVC, a dose of 300 mg (two 150 mg tablets) twice daily is recommended and does not require dose adjustments based on renal or hepatic function. The use of ibrexafungerp outside of VVC is currently under study with several ongoing trials showing promising interim data.

Green waste, e.g., grass clippings, is currently insufficiently recycled and has untapped potential as a valuable resource. Our aim was to use juice from grass clippings as a growth medium for microorganisms. Herein, we demonstrate the production of the sesquiterpene α-humulene with the versatile organism Cupriavidus necator pKR-hum on a growth medium from grass clippings. The medium was compared with established media in terms of microbial growth and terpene production. C. necator pKR-hum shows a maximum growth rate of 0.43 h−1 in the grass medium and 0.50 h−1 in a lysogeny broth (LB) medium. With the grass medium, 2 mg/L of α-humulene were produced compared to 10 mg/L with the LB medium. By concentrating the grass medium and using a controlled bioreactor in combination with an optimized in situ product removal, comparable product concentrations could likely be achieved. To the best of our knowledge, this is the first time that juice from grass clippings has been used as a growth medium without any further additives for microbial product synthesis. This use of green waste as a material represents a new bioeconomic utilization option of waste materials and could contribute to improving the economics of grass biorefineries.

Yeasts from the Candida parapsilosis complex are clinically relevant due to their high virulence and pathogenicity potential, such as adherence to epithelial cells and emission of filamentous structures, as well as their low susceptibility to antifungals. D-limonene, a natural compound, emerges as a promising alternative with previously described antibacterial, antiparasitic, and antifungal activity; however, its mechanisms of action and antivirulence activity against C. parapsilosis complex species have not been elucidated. Therefore, in the present study, we aimed to evaluate the antifungal and antivirulence action, as well as the mechanism of action of D-limonene against isolates from this complex. D-limonene exhibited relevant antifungal activity against C. parapsilosis complex yeasts, as well as excellent antivirulence activity by inhibiting yeast morphogenesis and adherence to the human epithelium. Furthermore, the apoptotic mechanism induced by this compound, which is not induced by oxidative stress, represents an important target for the development of new antifungal drugs.

Arthropod-borne pathogens and parasites are major threats to human health and global agriculture. They may directly or indirectly manipulate behaviors of arthropod vector for rapid transmission between hosts. The largest genus of plant viruses, Begomovirus, is transmitted exclusively by whitefly (Bemisia tabaci), a complex of at least 34 morphologically indistinguishable species. We have previously shown that plants infected with the tomato yellowleaf curl China virus (TYLCCNV) and its associated betasatellite (TYLCCNB) attract their whitefly vectors by subverting plant MYC2-regulated terpenoid biosynthesis, therefore forming an indirect mutualism between virus and vector via plant. However, the evolutionary mechanism of interactions between begomoviruses and their whitefly vectors is still poorly understood. Here we present evidence to suggest that indirect mutualism may happen over a millennium ago and at present extensively prevails. Detailed bioinformatics and functional analysis identified the serine-33 as an evolutionary conserved phosphorylation site in 105 of 119 Betasatellite species-encoded βC1 proteins, which are responsible for suppressing plant terpenoid-based defense by interfering with MYC2 dimerization and are essential to promote whitefly performance. The substitution of serine-33 of βC1 proteins with either aspartate (phosphorylation mimic mutants) or cysteine, the amino acid in the non-functional sβC1 encoded by Siegesbeckia yellow vein betasatellite SiYVB) impaired the ability of βC1 functions on suppression of MYC2 dimerization, whitefly attraction and fitness. Moreover the gain of function mutation of cysteine-31 to serine in sβC1 protein of SiYVB restored these functions of βC1 protein. Thus, the dynamic phosphorylation of serine-33 in βC1 proteins helps the virus to evade host defense against insect vectors with an evolutionarily conserved manner. Our data provide a mechanistic explanation of how arboviruses evolutionarily modulate host defenses for rapid transmission.

Introduction: Camphora longepaniculata , a crucial commercial crop and a fundamental component of traditional Chinese medicine, is renowned for its abundant production of volatile terpenoids. However, the lack of available genomic information has hindered pertinent research efforts in the past., Methods: To bridge this gap, the present study aimed to use PacBio HiFi, short-read, and highthroughput chromosome conformation capture sequencing to construct a chromosome-level assembly of the C. longepaniculata genome., Results and Discussion: With twelve chromosomes accounting for 99.82% (766.69 Mb) of the final genome assembly, which covered 768.10 Mb, it was very complete. Remarkably, the assembly's contig and scaffold N50 values are exceptional as well-41.12 and 63.78 Mb, respectively-highlighting its excellent quality and intact structure. Furthermore, a total of 39,173 protein-coding genes were predicted, with 38,766 (98.96%) of them being functionally annotated. The completeness of the genome was confirmed by the Benchmarking Universal Single-Copy Ortholog evaluation, which revealed 99.01% of highly conserved plant genes. As the first comprehensive assembly of the C. longepaniculata genome, it provides a crucial starting point for deciphering the complex pathways involved in terpenoid production. Furthermore, this excellent genome serves as a vital resource for upcoming research on the breeding and genetics of C. longepaniculata ., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2024 Yan, Zhu, Cao, Meng, Li, Zhang, Liu, Wang, Feng, Soaud, Elhamid, Heakel, Wei, El-Sappah and Ru.)

Sclareol, a diterpene alcohol, is the most common starting material for the synthesis of ambrox, which serves as a sustainable substitute for ambergris, a valuable fragrance secreted by sperm whales. Sclareol has also been proposed to possess antibacterial, antifungal, and anticancer activities. However, in nature, sclareol is only produced by a few plant species, including Cistus creticus , Cleome spinosa , Nicotiana glutinosa , and Salvia sclarea , which limits its commercial application. In this study, we cloned the two genes responsible for sclareol biosynthesis in S. sclarea , labda-13-en-8-ol diphosphate synthase ( LPPS ) and sclareol synthase ( SS ), and overexpressed them in tobacco ( Nicotiana tabacum L.). The best transgenic tobacco lines accumulated 4.1 μg/cm 2 of sclareol, which is comparable to the sclareol production of N. glutinosa , a natural sclareol producer. Thus, sclareol synthesis in tobacco represents a potential alternative means for the production of this high-value compound.

This document discusses the abundance of camphor, a plant essential oil, in various plants and their different parts. Camphor is a natural product derived from the wood of camphor laurel trees and is also found in other plants such as Salvia officinalis, Rosemary, lavender, Artemisia annua, and Achillea. Camphor has various uses, including as an aromatic material, antioxidant, antidiabetic, antibacterial, and local analgesic. The document provides a table showing the percentage of camphor available in different parts of these plants. The authors suggest that by purifying camphor in plants with the highest amount of this compound, a large amount of camphor can be produced for medicinal purposes. [Extracted from the article]

ROS, RNS, and carcinogenic metabolites generate excessive oxidative stress, which changes the basal cellular status and leads to epigenetic modification, genomic instability, and initiation of cancer. Epigenetic modification may inhibit tumor-suppressor genes and activate oncogenes, enabling cells to have cancer promoting properties. The nuclear factor erythroid 2-related factor 2 (Nrf2) is a transcription factor that in humans is encoded by the NFE2L2 gene, and is activated in response to cellular stress. It can regulate redox homoeostasis by expressing several cytoprotective enzymes, including NADPH quinine oxidoreductase, heme oxygenase-1, UDP-glucuronosyltransferase, glutathione peroxidase, glutathione-S-transferase, etc. There is accumulating evidence supporting the idea that dietary nutraceuticals derived from commonly used fruits, vegetables, and spices have the ability to produce cancer chemopreventive activity by inducing Nrf2-mediated detoxifying enzymes. In this review, we discuss the importance of these nutraceuticals in cancer chemoprevention and summarize the role of dietary terpenoids in this respect. This approach was taken to accumulate the mechanistic function of these terpenoids to develop a comprehensive understanding of their direct and indirect roles in modulating the Keap1-Nrf2-ARE signaling system. [ABSTRACT FROM AUTHOR]

Introduction: The new discovery of the active substance in Sargassum sp marks the new era for drug industry as it is very effective as the new migraine medication compared to analgesics which have already been popular previously in treating migraine. By using the in silico methods, this study intended to identify the preventive effect of the active substance in Sargassum sp within the stage of pain and inflammation development in migraine. In migraine pathophysiology, the clinical findings would build and verify the role of CGRP and TNF-a. Methods: This research applied a one-shot experimental study and by employing the potential test through PubChem (https://pubchem.ncbi.nlm.nih.gov/), the result of this study proved that tannins, terpenoids and fucoidone were contained in the active substance of Sargassum sp leading to the possession of potential as the drug to treat migraine. Results: Terpenoids and tannin binding affinity value is higher than other substances. Terpenoids and fucoidon had similar amino acid residues with controls. Seaweed metabolites have great potential as inhibitors of CGRP and TNF-a because the binding affinity score is close to control. Conclusion: The active substance in Sargassum sp has an inhibitory effect on the occurrence of CGRP and TNF-a in migraine based on in silico studies. [ABSTRACT FROM AUTHOR]

Inonotus obliquus is a rare, edible and medicinal fungus that is widely used as a remedy for various diseases. Its main bioactive substances are polysaccharides and terpenoids. In this study, we characterized and investigated the pan-genome of three strains of I. obliquus. The genome sizes of JL01, HE, and NBRC8681 were 32.04, 29.04, and 31.78 Mb, respectively. There were 6 543 core gene families and 6 197 accessory gene families among the three strains, with 14 polysaccharide-related core gene families and seven accessory gene families. For terpenoids, there were 13 core gene families and 17 accessory gene families. Pan-genome sequencing of I. obliquus has improved our understanding of biological characteristics related to the biosynthesis of polysaccharides and terpenoids at the molecular level, which in turn will enable us to increase the production of polysaccharides and terpenoids by this mushroom. [ABSTRACT FROM AUTHOR]

Nepeta is one of the most important genus from the fam. lamiaceae with more than 280 species. In this study, N. haussknechtii Bornm. was collected at the flowering stage from Ardabil province, Iran and its chloroform extract was prepared. The chloroform crude extract was subjected to the successive column chromatography on the silica gel using n-hexane-ethyl acetate solvent gradient to yield 29 fractions. Further purification of the fraction No.5 resulted in the isolation of one known steroid namely -sitosterol (1). In addition, the known triterpenoid oleanolic acid (2) was identified from the purification of the more polar fraction No.9. The compounds were assigned by the mass spectrometry, IR, 1H NMR, 13C NMR, DEPT, and 1H1H COSY. Finally, the structures of compounds were confirmed by comparison of the spectral data with those described in the literature. [ABSTRACT FROM AUTHOR]

One new iridoid glycoside (1), shanzhiside N-L-phenylalanyl ester along with seven known compounds, mussaenoside (2), shanzhiside methyl ester (3), barlerin (4), mussaendodise G (5), mussaendodise U (6), mussaendodise P (7), and mussaglaoside B (8) have been isolated from Mussaenda pilosissima Valeton. Their chemical structures were elucidated by spectroscopic methods, 1 D-, 2 D-NMR, and mass spectra. Compounds 1-7 showed significant inhibitory activity on LPS-stimulated NO production in BV2 cells with the IC50 values ranging from 43.5 to 65.2 µM. [ABSTRACT FROM AUTHOR]

Soil water deficit seriously affects crop production, and soil arbuscular mycorrhizal fungi (AMF) enhance drought tolerance in crops by unclear mechanisms. Our study aimed to analyze changes in non-targeted metabolomics in roots of trifoliate orange (Poncirus trifoliata) seedlings under well-watered and soil drought after inoculation with Rhizophagus intraradices , with a focus on terpenoid profile. Root mycorrhizal fungal colonization varied from 70% under soil drought to 85% under soil well-watered, and shoot and root biomass was increased by AMF inoculation, independent of soil water regimes. A total of 643 secondary metabolites in roots were examined, and 210 and 105 differential metabolites were regulated by mycorrhizal fungi under normal water and drought stress, along with 88 and 17 metabolites being up-and down-regulated under drought conditions, respectively. KEGG annotation analysis of differential metabolites showed 38 and 36 metabolic pathways by mycorrhizal inoculation under normal water and drought stress conditions, respectively. Among them, 33 metabolic pathways for mycorrhization under drought stress included purine metabolism, pyrimidine metabolism, alanine, aspartate and glutamate metabolism, etc. We also identified 10 terpenoid substances, namely albiflorin, artemisinin (−)-camphor, capsanthin, β-caryophyllene, limonin, phytol, roseoside, sweroside, and α-terpineol. AMF colonization triggered the decline of almost all differential terpenoids, except for β-caryophyllene, which was up-regulated by mycorrhizas under drought, suggesting potential increase in volatile organic compounds to initiate plant defense responses. This study provided an overview of AMF-induced metabolites and metabolic pathways in plants under drought, focusing on the terpenoid profile. [ABSTRACT FROM AUTHOR]

Terpenoids are potentially sustainable replacements for petrochemical olefins. Sulfur is a waste product produced in large quantities from fossil fuel refining. Several composites with attractive properties have recently been made from terpenoids and sulfur. This report details the extent to which the ratio of sulfur to terpenoid and the terpenoid olefin content influences the thermal and mechanical properties of such terpenoid-sulfur composites. The terpenoids selected were diunsaturated geraniol and triunsaturated farnesol that, upon their inverse vulcanization with elemental sulfur, yield composites GerSx and FarSx, respectively (x = wt % sulfur). The wt % sulfur in the monomer feed was varied from 30–95 for this study, providing twelve materials. Mechanical analysis of these materials was undertaken by compressive and tensile strength techniques. Differential scanning calorimetric analysis revealed both polymeric and orthorhombic sulfur present in the materials with glass transition temperatures (Tg) of −37 ◦C to −13 ◦C and melt temperatures (Tm) of 119 to 104 ◦C. The crystallinity of composites decreases as the weight fraction of sulfur decreases and composites having the highest olefin content exhibit no detectable crystalline microstructures. The compressive strength of the materials showed increasing strength for higher olefin-content materials for both GerSx (with compressive strength of up to 32 MPa) and FarSx (with compressive strength of up to 43 MPa). The improved strength with increasing olefin content levels off at around 80–85% of terpenoid, after which point both tensile and compressive strength diminish [ABSTRACT FROM AUTHOR]

Seven oxygenated sesquiterpenes 1 to 7 each with a drimane framework were isolated from an organic extract of the nudibranch Ardeadoris rubroannulata collected from Eastern Australia. The structure of pu’ulenal 2 was revised by 1D NOESY, providing a 9Z configuration, while isopu’ulenal 3 has the 9E configuration previously ascribed to pu’ulenal. [ABSTRACT FROM AUTHOR]

Introduction: Marsdenia macrantha is a crucial source of traditional medicine in Northern Namibia. Its roots are used to treat various health conditions ranging from mouth infections to urinary retention. Despite its medicinal application, there is no known knowledge of its therapeutic properties. Thus, we investigated the phytochemical content and antibacterial activity of M. macrantha. Methods: M. macrantha root extracts were obtained using three different solvents (distilled water, methanol and acetone) - in the soxhlet and maceration extraction methods. Total phytochemical (terpenoid, alkaloid and/or flavonoid) content was determined by spectrophotometry. Antibacterial activity against common foodborne pathogens (Staphylococcus aureus, Escherichia coli and Salmonella typhi) was determined by both well and disc diffusion method. Results: we detected the presence of all the tested phytochemicals. Methanol gave the highest percentage yield of extraction (mean: 13.95 ± standard deviation: 0.41%) followed by water (10.92 ± 0.11%) and acetone (6.85 ± 0.23%), F-ratio=326.71 and p<0.0003. The total content determined showed that M. macrantha root extract contained more flavonoids than alkaloids (mg of standard per grams of the dry material). Antibacterial analyses showed inhibitory activity against all the selected pathogens, with the highest inhibition zone against S. typhi (19.7 ± 0.3 mm) - for the acetone-prepared root extract. There were variations in minimum inhibitory concentrations of the extracts prepared by the different solvents. Conclusion: this is the first study demonstrating the presence of phytochemicals and antibacterial properties of M. macrantha roots. Further studies are needed to isolate and characterize the phytochemicals for antibacterial application. [ABSTRACT FROM AUTHOR]

Soil water deficit seriously affects crop production, and soil arbuscular mycorrhizal fungi (AMF) enhance drought tolerance in crops by unclear mechanisms. Our study aimed to analyze changes in non-targeted metabolomics in roots of trifoliate orange (Poncirus trifoliata) seedlings under well-watered and soil drought after inoculation with Rhizophagus intraradices, with a focus on terpenoid profile. Root mycorrhizal fungal colonization varied from 70% under soil drought to 85% under soil well-watered, and shoot and root biomass was increased by AMF inoculation, independent of soil water regimes. A total of 643 secondary metabolites in roots were examined, and 210 and 105 differential metabolites were regulated by mycorrhizal fungi under normal water and drought stress, along with 88 and 17 metabolites being up-and down-regulated under drought conditions, respectively. KEGG annotation analysis of differential metabolites showed 38 and 36 metabolic pathways by mycorrhizal inoculation under normal water and drought stress conditions, respectively. Among them, 33 metabolic pathways for mycorrhization under drought stress included purine metabolism, pyrimidine metabolism, alanine, aspartate and glutamate metabolism, etc. We also identified 10 terpenoid substances, namely albiflorin, artemisinin (−)-camphor, capsanthin, β-caryophyllene, limonin, phytol, roseoside, sweroside, and α-terpineol. AMF colonization triggered the decline of almost all differential terpenoids, except for β-caryophyllene, which was up-regulated by mycorrhizas under drought, suggesting potential increase in volatile organic compounds to initiate plant defense responses. This study provided an overview of AMF-induced metabolites and metabolic pathways in plants under drought, focusing on the terpenoid profile.

The attraction to the Euphorbia genus, with its remarkable diversity in species, is due to its variety of chemical compositions. Euphorbia turcomanica is one of the species of the spurge family growing wildly in Iran. This research aims to investigate the presence of secondary metabolites, specially terpenoid compounds, in terms of structural determination. Samples of E. tucomanica were finely powdered and macerated with acetone/dichloromethane 2:1. Repeated column chromatography using silica gel, MPLC, and HPLC methods followed by the analysis of data obtained from spectroscopic means was carried out to purify and identify the terpenoid constituents. The chemical structures of nine known terpenoids were determined for the first time from E. turcomanica during this study. Loliolide (1), a monoterpene, and eight steroids and triterpenes, including simiarenol (2), isomultiflorenol (3), cycloart-25-ene-3β,24-diol (4), β-sitosterol (5), cycloart-23-ene-3β,25-diol (6), 3α, 11α-dihydroxyurs-12-ene (7), 3β, 24β, 25-trihydroxycycloartane (8), and 7α-hydroxystigmasterol (9) were isolated and identified. E. tucomanica, with a rich terpenoid profile, can be one of the valuable and economic sources providing compounds for drug development.

Terpenoids are widely distributed in nature, especially in the plant kingdom, and exhibit diverse pharmacological activities. In recent years, screening has revealed a wide variety of new terpenoids that are active against different psychiatric disorders. This review synthesized the current published preclinical studies of terpenoid use in psychiatric disorders. This review was extensively investigated to provide empirical evidence regarding the neuropharmacological effects of the vast group of terpenoids in translational models of psychiatric disorders, their relevant mechanisms of action, and treatment regimens with evidence of the safety and psychotropic efficacy. Therefore, we utilized nine (9) electronic databases and performed manual searches of each. The relevant data were retrieved from the articles published until present. We used the search terms “terpenoids” or “terpenes” and “psychiatric disorders” (“psychiatric disorders” OR “psychiatric diseases” OR “neuropsychiatric disorders” OR “psychosis” OR “psychiatric symptoms”). The efficacy of terpenoids or biosynthetic compounds in the terpenoid group was demonstrated in preclinical animal studies. Ginsenosides, bacosides, oleanolic acid, asiatic acid, boswellic acid, mono- and diterpenes, and different forms of saponins and triterpenoids were found to be important bioactive compounds in several preclinical studies of psychosis. Taken together, the findings of the present review indicate that natural terpenoids and their derivatives could achieve remarkable success as an alternative therapeutic option for alleviating the core or associated behavioral features of psychiatric disorders.

Eukaryotic green microalgae show considerable promise for the sustainable light-driven biosynthesis of high-value fine chemicals, especially terpenoids because of their fast and inexpensive phototrophic growth. Here, the novel isopentenol utilization pathway (IUP) was introduced into Chlamydomonas reinhardtii to enhance the hemiterpene (isopentenyl pyrophosphate, IPP) titers. Then, diphosphate isomerase (IDI) and limonene synthase (MsLS) were further inserted for limonene production. Transgenic algae showed 8.6-fold increase in IPP compared with the wild type, and 23-fold increase in limonene production compared with a single MsLS expressing strain. Following the culture optimization, the highest limonene production reached 117 µg/L, when the strain was cultured in a opt2 medium supplemented with 10 mM isoprenol under a light: dark regimen. This demonstrates that transgenic algae expressing the IUP represent an ideal chassis for the high-value terpenoid production. The IUP will facilitate further the metabolic and enzyme engineering to enhance the terpenoid titers by significantly reducing the number of enzyme steps required for an optimal biosynthesis.

In addition to phytocannabinoids, cannabis contains terpenoids that are claimed to have a myriad of effects on the body. We tested a panel of five common cannabis terpenoids, myrcene, linalool, limonene, α-pinene and nerolidol, in two neuronal models, autaptic hippocampal neurons and dorsal root ganglion (DRG) neurons. Autaptic neurons express a form of cannabinoid CB1 receptor-dependent retrograde plasticity while DRGs express a variety of transient receptor potential (TRP) channels. Most terpenoids had little or no effect on neuronal cannabinoid signaling. The exception was nerolidol, which inhibited endocannabinoid signaling. Notably, this is not via inhibition of CB1 receptors but by inhibiting some aspect of 2-arachidonoylglycerol (2-AG) production/delivery; the mechanism does not involve reducing the activity of the 2-AG-synthesizing diacylglycerol lipases (DAGLs). Nerolidol was also the only terpenoid that activated a sustained calcium response in a small (7%) subpopulation of DRGs. In summary, we found that only one of five terpenoids tested had notable effects on cannabinoid signaling in two neuronal models. Our results suggest that a few terpenoids may indeed interact with some components of the cannabinoid signaling system and may therefore offer interesting insights upon further study.

The viscosity of natural deep eutectic solvent (NADES) plays an important role in determining how they are used industrially. However, most of NADES systems exhibit a relatively high viscosity. Terpene-based mixtures have attracted widespread interest as relatively low-viscosity solvents. The goal of this work was to shed light on the nature of their unique properties by exploring the relationship between viscosity and non-covalent interactions. The microstructure and characteristics of different NADES were investigated through multiple methods and theories. Among these systems, ketone-based and alkenyl alcohol-based terpenoids act as hydrogen bond acceptors, and phenol-based terpenoids are prone to be hydrogen bond donors. The viscosity of studied NADES was low and was synthetically influenced by the number and lifetime of hydrogen bond. To some extent, their viscosity was consistent with the hydrogen-bond lifetime. Additionally, a positive correlation was found between their viscosity and non-bonded interactions energy. The relatively high viscosity mainly was driven by the enhancement of van der Waals force. Through visualization of non-covalent interactions, the results indicated that the appropriate strength and high fluctuations of interactions in the systems were necessary for forming low-viscosity NADES. Furthermore, the vertices on the electrostatic potential of terpenoids are pivotal factors influencing the property of final complex via quantitative analysis of molecular surface. It can be utilized to preliminarily assess the viscosity of NADES without the study of the entire system. The discovery of intrinsic rules paves the way for rational and effective design of novel low-viscosity NADES in the future.

Zinc tetra-ascorbo-camphorate (or drug “C14”) is a synthetic monoterpenoid derivative that has potent anti-HIV-1 activity in vitro. In this study, we evaluated the in vitro antiviral properties of C14 against human papillomavirus (HPV). Inhibition assay of HPV-16-pseudovirus (PsVs) adsorption on COS-7 cells by C14 was used. C14 inhibited HPV-16-PsVs adsorption with IC50 ranging between 2.9 and 8.3 μM and therapeutic indexes between >410 to >3,300. Pretreatment of COS-7 cells with C14 before addition of HPV-16-PsV was associated with more potent anti-HPV activity than simultaneous deposition on COS-7 of HPV-16-PsV and C14, suggesting that C14 is more effective in preventing HPV attachment to target cells than post-HPV adsorption viral events. Overall, these in vitro studies suggest that the monoterpenoid zinc tetra-ascorbo-camphorate molecule may be suitable for further clinical evaluations as potential microbicide or therapeutic drug.

2-Oxoglutarate (2OG)-dependent dioxygenases (2-ODDs) are omnipresent iron-containing non-heme enzymes that catalyze various oxidation-reduction reactions in plant growth and development, nucleic acid modification and secondary metabolism. We systematically summarized recent research on the oxidative modifications of plant 2-ODDs and related enzymes, their vital importance in the biosynthesis of plant special metabolites, and their catalytic specificity/flexibility, and discussed the potential of 2-ODD as a new approach for the identification of pivotal genes and the elucidation of biosynthetic pathway. [ABSTRACT FROM AUTHOR]

The essential oil (EO) from different genotypes of Lippia gracilis Schauer (Verbenaceae) present two distinctive chemotypes containing either thymol or its isomer carvacrol as major compounds, both of which have proven bioactivity against several agricultural pests. Recently, we have shown that L. gracilis accession LGRA 106 and its major compound thymol are toxic and repellent against the coconut mite, Aceria guerreronis Keifer (Acari: Eriophyidae), a key pest of coconut plantations in Asia, Africa and America. Since intraspecific variation affects the chemical composition of EO and hence, its bioactivity, here we assessed the acaricidal and repellent effects of L. gracilis accession LGRA109 to A. guerreronis. Leaves of this accession contain carvacrol (49.35%) as major compound. The LC50 of the EO and of carvacrol estimated for A. guerreronis were 28.01 and 6.84 mg/mL, respectively. Carvacrol, at its LC50, as well as the EO and carvacrol at their LC99, repelled the mite. Our results indicated that carvacrol and the EO of L. gracilis accession LGRA109 were bioactive against A. guerreronis; however, the EO was less effective than its major compound. [ABSTRACT FROM AUTHOR]

The synthesis of (−)‐4‐epi‐Englerin A, the epimer of natural product (−)‐Englerin A, a sesquiterpenoid with exceptional anti‐proliferative activity in renal cancer cells is achieved from (R)‐(+)‐limonene. Key features of the synthesis are Sharpless asymmetric dihydroxylation, aldol reaction, and transannular epoxide opening reactions to install the required functionalities of oxabridged tricyclic core. [ABSTRACT FROM AUTHOR]