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Background: The Juan-Bi decoction (JBD) is a classic traditional Chinese medicines (TCMs) prescription for the treatment of rheumatoid arthritis (RA). However, the active compounds of the JBD in RA treatment remain unclear. Aim: The aim of this study is to screen effective compounds in the JBD for RA treatment using systems pharmacology and experimental approaches. Method: Botanical drugs and compounds in the JBD were acquired from multiple public TCM databases. All compounds were initially screened using absorption, distribution, metabolism, excretion, and toxicity (ADMET) and physicochemical properties, and then a target prediction was performed. RA pathological genes were acquired from the DisGeNet database. Potential active compounds were screened by constructing a compound-target-pathogenic gene (C-T-P) network and calculating the cumulative interaction intensity of the compounds on pathogenic genes. The effectiveness of the compounds was verified using lipopolysaccharide (LPS)-induced RAW.264.7 cells and collageninduced arthritis (CIA) mouse models. Results: We screened 15 potentially active compounds in the JBD for RA treatment. These compounds primarily act on multiple metabolic pathways, immune pathways, and signaling transduction pathways. Furthermore, in vivo and in vitro experiments showed that bornyl acetate (BAC) alleviated joint damage, and inflammatory cells infiltrated and facilitated a smooth cartilage surface via the suppression of the steroid hormone biosynthesis. Conclusion: We screened potential compounds in the JBD for the treatment of RA using systems pharmacology approaches. In particular, BAC had an anti-rheumatic effect, and future studies are required to elucidate the underlying mechanisms. [ABSTRACT FROM AUTHOR]

Monoterpene hydrocarbons are the unwanted, off-smelling fractions in most of the essential oils. Due to the absence of functional groups in monoterpene hydrocarbons, it is difficult to solubilize in common solvents such as water, ethanol, etc. Hence, this fraction is removed from the essential oil in deterpenation process before their application in formulations. Pinene (α-,β-), the monoterpene hydrocarbons are found in most of the essential oils. In the present work, pinene isomers are esterified to valuable compounds such as terpinyl acetate, bornyl acetate and fenchyl acetate. They are widely used as fragrance ingredients in various food and cosmetic products with improved organoleptic profiles. Hence, a solvent-free process has been developed for the selective conversion of pinene to terpinyl acetate and bornyl acetate using 1%Pd-β-Zeolite (ZE) at room temperature (30 °C). The different percentage of Pd loading over β-ZE was studied on the transformation of α-pinene. It was attained 98% of conversion with the selectivity to 54.2% of terpinyl acetate, and 34.8% of bornyl acetate at 30 °C in 2 h using 1%Pd-β-ZE. Similarly, the synthesized catalyst (1%Pd-β-ZE) has been shown excellent activity for α-pinene esterification under the 50 psi N2 at 50 °C to produce 83% selectivity towards bornyl acetate. The esterification of monoterpene hydrocarbons-rich essential oils (salaiguggul, guggul, black pepper, rosemary, and nutmeg) were carried out at 30 °C with 1%Pd-β-ZE for selective transformation to bornyl acetate, terpinyl acetate, and fenchyl acetate. Since the reactions are carried out without any additional use of organic solvents, hence, makes the overall process quite attractive. This study will help to develop an eco-friendly strategy for the valorization of bicyclic monoterpene hydrocarbons-rich essential oils. [ABSTRACT FROM AUTHOR]

Copyright of Boletín Latinoamericano y del Caribe de Plantas Medicinales y Aromáticas is the property of Universidad de Santiago de Chile and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Background: β-amyloid (Aβ) deposition and tau protein abnormality are the major pathogenesis of Alzheimer's disease (AD). Autophagy is contributed to eliminating the misfolded proteins or organelles and alleviated cellular injury. Our pre-experimental findings showed that bornyl acetate (BA), the main component of the volatile oil of Amomum villosum, has a neuroprotective effect in okadaic acid (OA)–induced PC12 cells. However, the protective mechanism of autophagy that BA relieves OA-induced cellular injury is still unclear. Objectives: The purpose of our experiment was to elucidate the mechanism of treatment of AD. Materials and Methods: To explore how BA has therapeutic effects on AD, a model of OA-induced PC12 cells was established. The OA modelling induction and BA treatment in cells were evaluated by LDH and CCK-8 methods; ELISA assay was used to detect the tau hyperphosphorylation (p-tau), Aβ42 and β-secretase levels; The expression of p-Akt and p-mTOR were detected by western blot analysis; and immunohistochemical, immunofluorescence methods and western blot analysis were used to detect Beclin-1 expression. Autophagosomes in each group were observed by transmission electron microscopy (TEM). 175 nM OA for 48 hr was applied to OA modelling induction. Results: Compared to the control group, the OA-induced AD model cells displayed higher levels of p-tau, Aβ42 and β-secretase (P < 0.01), suggesting that the AD model was successfully established. Compared to the OA model group alone, p-tau, Aβ42 and β-secretase levels and autophagy promoter Beclin-1 expression decreased significantly in the BA group (P < 0.05), whereas p-Akt and p-mTOR increased (P < 0.01). Conclusion: BA exhibited a neuroprotection effect against OA-induced cellular injury in the AD model by suppressing the Beclin-1-dependent autophagy pathway, indicating that BA might be an appealing potential strategy to treat AD. [ABSTRACT FROM AUTHOR]

Chamaecyparis obtusa, Chamaecyparis pisifera, and Thuja occidentalis produce essential oils of good wood and industrial benefits, including food additives, perfumes, odorants and disinfectants. To identify a single antifungal monoterpene with antifungal activity against Botrytis cinerea, we identified a single antifungal compound by chemically profiling essential oils from three coniferous species. The antifungal activity of coniferous essential oil was slightly different depending on the species but showed high antifungal activity, and T. occidentalis essential oil had the highest antifungal activity among the three essential oils. The chemical composition of essential oils from three coniferous leaves was profiled using GC-MS. The chemical profiles of C. obtusa and C. pisifera were very similar, but T. occidentalis was relatively different from the two species. The chemical composition of the three conifer oils contained 20 each. As a result of profiling three essential oil components with high antifungal activity, the compounds present in all three species were bornyl acetate and terpinyl acetate. These compounds of C. obtusa essential oil were 26.49%, C. pisifera essential oil 25.04% and T. occidentalis essential oil 12.60%. These two compounds were estimated to be antifungal agents. The antifungal activity of the six monoterpenes was different, and the single monoterpene with the highest antifungal activity was bornyl acetate followed by terpinyl acetate. Therefore, it was possible to search for antifungal activity monoterpene components by chemical profiling. Terpinyl acetate and bornyl acetate can be used for environmental-friendly insecticidal active materials.

Bornyl acetate (BA) is known as a natural aromatic monoterpene ester with a wide range of pharmacological and biological activities. Borneol acetyltransferase (BAT), catalyzing borneol and acetyl-CoA to synthesize BA, is alcohol acetyltransferase, which belongs to the BAHD super acyltransferase family, however, BAT, responsible for the biosynthesis of BA, has not yet been characterized. The seeds of Wurfbainia villosa (homotypic synonym: Amomum villosum) are rich in BA. Here we identified 64 members of the BAHD gene family from the genome of W. villosa using both PF02458 (transferase) and PF07247 (AATase) as Hidden Markov Model (HMM) to screen the BAHD genes. A total of sixty-four WvBAHDs are distributed on 14 chromosomes and nine unanchored contigs, clustering into six clades; three WvBAHDs with PF07247 have formed a separated and novel clade: clade VI. Twelve candidate genes belonging to clade I-a, I-b, and VI were selected to clone and characterize in vitro , among which eight genes have been identified to encode BATs acetylating at least one type of borneol to synthesize BA. All eight WvBATs can utilize (−)-borneol as substrates, but only five WvBATs can catalyze (+)-borneol, which is the endogenous borneol substrate in the seeds of W. villosa ; WvBAT3 and WvBAT4 present the better catalytic efficiency on (+)-borneol than the others. The temporal and spatial expression patterns of WvBATs indicate that WvBAT3 and WvBAT4 are seed-specific expression genes, and their expression levels are correlated with the accumulation of BA, suggesting WvBAT3 and WvBAT4 might be the two key BATs for BA synthesis in the seeds of W. villosa. This is the first report on BAT responsible for the last biosynthetic step of BA, which will contribute to further studies on BA biosynthesis and metabolism engineering of BA in other plants or heterologous hosts. [ABSTRACT FROM AUTHOR]

Members of the Abies genus (Pinaceae) have been used in traditional medicines in their natural ranges, and essential oils derived from Abies species have found use in aromatic therapy. In this work, the foliar (leaves and twigs) essential oil of Abies concolor have been obtained from mature trees growing in southwestern Idaho and analyzed using gas chromatographic techniques. The essential oils were rich in α-pinene (15.2-20.5%), camphene (7.5-10.2%), β-pinene (24.2-25.6%), δ-3-carene (5.5-6.5%), limonene (5.4-6.9%), and bornyl acetate (14.6-22.1%). The dominant enantiomers for the major terpenoids were (+)-α-pinene, (–)-camphene, (–)-β-pinene, (+)-δ-3-carene, (–)-limonene, and (–)-bornyl acetate. The essential oil compositions are qualitatively similar to other Abies species, but the enantiomeric distributions for α-pinene, β-pinene, and camphene did reveal notable variation between Abies essential oils. [ABSTRACT FROM AUTHOR]

Bornyl acetate (BA) is known as a natural aromatic monoterpene ester with a wide range of pharmacological and biological activities. Borneol acetyltransferase (BAT), catalyzing borneol and acetyl-CoA to synthesize BA, is alcohol acetyltransferase, which belongs to the BAHD super acyltransferase family, however, BAT, responsible for the biosynthesis of BA, has not yet been characterized. The seeds of Wurfbainia villosa (homotypic synonym: Amomum villosum) are rich in BA. Here we identified 64 members of the BAHD gene family from the genome of W. villosa using both PF02458 (transferase) and PF07247 (AATase) as Hidden Markov Model (HMM) to screen the BAHD genes. A total of sixty-four WvBAHDs are distributed on 14 chromosomes and nine unanchored contigs, clustering into six clades; three WvBAHDs with PF07247 have formed a separated and novel clade: clade VI. Twelve candidate genes belonging to clade I-a, I-b, and VI were selected to clone and characterize in vitro, among which eight genes have been identified to encode BATs acetylating at least one type of borneol to synthesize BA. All eight WvBATs can utilize (−)-borneol as substrates, but only five WvBATs can catalyze (+)-borneol, which is the endogenous borneol substrate in the seeds of W. villosa; WvBAT3 and WvBAT4 present the better catalytic efficiency on (+)-borneol than the others. The temporal and spatial expression patterns of WvBATs indicate that WvBAT3 and WvBAT4 are seed-specific expression genes, and their expression levels are correlated with the accumulation of BA, suggesting WvBAT3 and WvBAT4 might be the two key BATs for BA synthesis in the seeds of W. villosa. This is the first report on BAT responsible for the last biosynthetic step of BA, which will contribute to further studies on BA biosynthesis and metabolism engineering of BA in other plants or heterologous hosts.

The fruits of Amomum villosum and Amomum longiligulare are both used medicinally as Fructus Amomi the famous traditional Chinese medicine, however, the medicinal quality of A. villosum is better than that of A. longiligulare. Volatile terpenoids in the seeds, especially bornyl acetate and borneol, are the medicinal components of Fructus Amomi. The volatile terpenoids and transcriptome of developing seeds of A. villosum and A. longiligulare were compared in this study. The result revealed that the bornyl acetate and borneol contents were higher in A. villosum than in A. longiligulare. Additionally, six terpenoid synthase genes (AlTPS1–AlTPS6) were screened from the transcriptome of A. longiligulare, and AlTPS2 and AlTPS3 were found to share 98 and 83% identity with AvTPS2 and AvBPPS (bornyl diphosphate synthase) from A. villosum, respectively. BPPS is the key enzyme for the biosynthesis of borneol and bornyl acetate. Biochemical assays improved that AlTPS2 had an identical function to AvTPS2 as linalool synthase; however, AlTPS3 produced camphene as the major product and bornyl diphosphate (BPP) as the secondary product, whereas AvBPPS produced BPP as its major product. There was only one different amino acid between AlTPS3 (A496) and AvBPPS (G495) in their conserved motifs, and the site-directed mutation of A496G in DTE motif of AlTPS3 changed the major product from camphene to BPP. Molecular docking suggests that A496G mutation narrows the camphene-binding pocket and decreases the BPP-binding energy, thus increases the product BPP selectivity of enzyme. In addition, the expression level of AvBPPS was significantly higher than that of AlTPS3 in seeds, which was consistent with the related-metabolites contents. This study provides insight into the TPS-related molecular bases for the biosynthesis and accumulation differences of the bioactive terpenoids between A. villosum and A. longiligulare. BPPS, the key gene involved in the biosynthesis of the active compound, was identified as a target gene that could be applied for the quality-related identification and breeding of Fructus Amomi.

The fruits of Amomum villosum and Amomum longiligulare are both used medicinally as Fructus Amomi the famous traditional Chinese medicine, however, the medicinal quality of A. villosum is better than that of A. longiligulare. Volatile terpenoids in the seeds, especially bornyl acetate and borneol, are the medicinal components of Fructus Amomi. The volatile terpenoids and transcriptome of developing seeds of A. villosum and A. longiligulare were compared in this study. The result revealed that the bornyl acetate and borneol contents were higher in A. villosum than in A. longiligulare. Additionally, six terpenoid synthase genes (AlTPS1–AlTPS6) were screened from the transcriptome of A. longiligulare , and AlTPS2 and AlTPS3 were found to share 98 and 83% identity with AvTPS2 and AvBPPS (bornyl diphosphate synthase) from A. villosum , respectively. BPPS is the key enzyme for the biosynthesis of borneol and bornyl acetate. Biochemical assays improved that AlTPS2 had an identical function to AvTPS2 as linalool synthase; however, AlTPS3 produced camphene as the major product and bornyl diphosphate (BPP) as the secondary product, whereas AvBPPS produced BPP as its major product. There was only one different amino acid between AlTPS3 (A496) and AvBPPS (G495) in their conserved motifs, and the site-directed mutation of A496G in DTE motif of AlTPS3 changed the major product from camphene to BPP. Molecular docking suggests that A496G mutation narrows the camphene-binding pocket and decreases the BPP-binding energy, thus increases the product BPP selectivity of enzyme. In addition, the expression level of AvBPPS was significantly higher than that of AlTPS3 in seeds, which was consistent with the related-metabolites contents. This study provides insight into the TPS-related molecular bases for the biosynthesis and accumulation differences of the bioactive terpenoids between A. villosum and A. longiligulare. BPPS , the key gene involved in the biosynthesis of the active compound, was identified as a target gene that could be applied for the quality-related identification and breeding of Fructus Amomi. [ABSTRACT FROM AUTHOR]

Differences in female/male plant metabolism for dioecious species are poorly understood but relevant if the economic exploitation of such resources is the objective. In this work, the composition of Baccharis tridentata Vahl essential oil from the flowering aerial parts of male and female plants was analysed separately by GC-MS (gas chromatography-mass spectrometry; area percentage and internal standard), and CPGC-MS (chiral phase gas chromatography analysis using modified β-cyclodextrin), reporting the enantiomeric distribution of monoterpene hydrocarbons as a genuineness criterion. The results confirmed high qualitative similarities between the essential oils from both genders, but quantitative differences in the main components α-pinene, β-pinene, limonene and bornyl acetate. Regarding the CPGC-MS analysis of monoterpene hydrocarbons, both sexes presented both enantiomers in the same ratios, which is in contrast to the values reported in the literature for related plants. However, natural bornyl acetate (isolated from B. tridentata essential oil) demonstrated a 100% enantiomeric excess of the levogyre enantiomer, a fact that has chemotaxonomic relevance. [ABSTRACT FROM AUTHOR]

The modern trend of research is highly focused on finding new bioactive molecules from medicinal plants. As a functional bicyclic monoterpene, Bornyl acetate (BA) has displayed antioxidant and anti-inflammatory properties in different types of cells and tissues. The purpose of this research was to evaluate the probable hypotensive effect of BA, an underlying mechanism(s) backboned by in-silico studies. Mean arterial pressure and heart rate were recorded via invasive blood pressure measuring technique in normotensive Sprague-Dawley rats following the administration of BA (1-80mg/kg). Docking studies were carried out with various targets involved in the pathophysiology of hypertension.RO5 and ADMET properties were also evaluated. In the current study dose-dependent reduction in systolic, diastolic and mean arterial pressure was observed. Pretreatment with atropine and captopril significantly (p<0.001) reduced the hypotensive effect produced by BA. On the other hand docking studies showed pronounced interactions with M2 mAch receptor in an agonistic way and ACE protein in an antagonistic way. BA justified all cut-off limits of RO5 and had an acceptable predicted computational toxicity profile. Results postulate that dose-dependent hypotensive effect of BA is mediated through the muscarinic pathway and ACE inhibitory activity corresponding well with findings of in-silico studies. [ABSTRACT FROM AUTHOR]

In plant secondary metabolite biosynthesis, acylation is a diverse physiological process, with BAHD acyltransferases playing an essential role. Borneol acetyltransferase (BAT) is an alcohol acetyltransferase, which catalyzes borneol and acetyl-CoA to synthesize bornyl acetate (BA). However, the enzymes involved in the biosynthesis of BA have so far only been characterized in Wurfbainia villosa , the studies on the WvBATs have only been conducted in vitro , and the catalytic activity was relatively low. In this research, three genes ( WlBAT1 , WlBAT2 , and WlBAT3 ) have been identified to encode BATs that are capable of acetylating borneol to synthesize BA in vitro . We also determined that WlBAT1 has the highest catalytic efficiency for borneol-type substrates, including (+)-borneol, (-)-borneol, and isoborneol. Furthermore, we found that BATs could catalyze a wide range of substrate types in vitro , but in vivo , they exclusively catalyzed borneol-type substrates. Through molecular simulations and site-directed mutagenesis, it was revealed that residues D32, N36, H168, N297, N355, and H384 are crucial for the catalytic activity of WlBAT1, while the R382I-D385R double mutant of WlBAT1 exhibited an increasing acylation efficiency for borneol-type substrates in vitro and in vivo . These findings offer key genetic elements for the metabolic engineering of plants and synthetic biology to produce BA.

Copyright of Boletín Latinoamericano y del Caribe de Plantas Medicinales y Aromáticas is the property of Universidad de Santiago de Chile and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

The chemical composition of flowers and leaves essential oils of Agastache astromontana 'Pink Pop' was determined by GC/MS method. The essential oils were isolated by hydrodistillation in a Clevenger-type apparatus. The following distillation times were applied in this experiment: 2, 3 and 4 hours. Linalool (23.76-24.65 %), bornyl acetate (27.22-28.61 %), camphene (5.75-7.00 %) and cis-linalool oxide (4.70-5.12 %) dominated in the essential oils isolated from the flowers. Similarly, linalool (36.48-38.01 %), bornyl acetate (15.35-17.31 %), sabinene (4.38-4.66 %) and camphene (4.17-4.52 %) were found to be the main components in the essential oils isolated from the leaves of Agastache. On the base of obtained results of the study it was proved that the distillation time did not significantly affect the essential oil content. Similarly, the part of plant had not a significant effect on the content of essential oil. However, there was a significant interaction found between the essential oil constituent and the distillation time. [ABSTRACT FROM AUTHOR]

The objective of this study was to investigate the effects of 11 active compounds of essential oils (ACEO) on rumen fermentation characteristics and methane production. Two trials were conducted. In trial 1, ACEO (eugenol, carvacrol, citral, limonene, 1,4-cineole, p-cymene, linalool, bornyl acetate, α-pinene, and β-pinene) at a dose of 1,000 μL/L were incubated for 24 h in diluted rumen fluid with a 70:30 forage:concentrate substrate (16.2% crude protein; 36.6% neutral detergent fiber). Three fistulated Holstein cows were used as donors of rumen fluid. The reduction in methane production was observed with nine ACEO (up to 86% reduction) compared with the control (p

Terpenoids make up the biggest and most diversified class of chemical substances discovered in plants, encompassing over 40,000 individual compounds. In conifers, the production of terpenoids, either as oleoresin or emitted as volatile compounds, play an important role in the physical and chemical defence responses against pathogens and herbivores. In the present work, we examined, for the first time to the best of our knowledge, the terpenic defensive relations of Calabrian pine (Pinus nigra subsp. laricio (Poiret) Maire), facing the attack of the pine processionary moth (Thaumetopoea pityocampa (Denis and Schiffermüller, 1775)), brought about in the open on adult plant individuals growing at two distinct forest sites. Among the volatile terpenoids emitted from pine needles, bornyl acetate [(4,7,7-trimethyl-3-bicyclo[2.2.1]heptanyl) acetate] was the most frequently and selectively associated with the infestation, increasing during the period of most intense trophic activity of the caterpillars (defoliation), and decreasing thereafter. Although further work is needed to clarify whether the observed response reflects defence reactions and/or they are involved in communication among the infested plants and their biotic environment, the present results boost the currently growing interest in the isolation and characterization of plant secondary metabolites that can be used to control pests, pathogens, and weeds.

Amomum villosum, also known as Fructus Amomi, has been used to treat digestive diseases such as abdominal pain, vomiting, and dysentery. Volatile terpenoids are the active metabolites in the essential oil of Fructus Amomi. Nevertheless, downstream genes responsible for activating metabolites biosynthesis in A. villosum still remain unclear. Here, we report the use of an integrative volatile terpenoid profiling and transcriptomics analysis for mining the corresponding genes involved in volatile terpenoid biosynthesis. Ten terpene synthase (TPS) genes were discovered, and two of them were cloned and functionally characterized. AvTPS1 (AvPS: pinene synthase) catalyzed GPP to form α-pinene and β-pinene; AvTPS3 (AvBPPS: bornyl diphosphate synthase) produced bornyl diphosphate as major product and the other three monoterpenoids as minor products. Metabolite accumulation and gene expression pattern combined with AvPS biochemical characterization suggested that AvPS might play a role in biotic defense. On the other hand, the most active ingredient, bornyl acetate, was highly accumulated in seeds and was consistent with the high expression of AvBPPS, which further indicated that AvBPPS is responsible for the biosynthesis of bornyl acetate, the final metabolite of bornyl diphosphate in A. villosum. This study can be used to improve the quality of A. villosum through metabolic engineering, and for the sustainable production of bornyl acetate in heterologous hosts.

The main components of Amomum villosum are volatile components such as bornyl acetate, camphor and borneol.Besides, there arenonvolatile components including polysaccharides, flavonoid glycosides, organic acids and inorganic components. Most of its pharmacological studies are concentrated on the part of volatile oil. Currently, the pharmacological effects of A. villosum are mainly found in the field ofgastrointestinal protection, anti-inflammatory, analgesic, antidiarrheal, hypoglycemic and so on. The species and contents of Amomum constituents are influenced by the base, origin, location and many other factors. The authors found that the highest content of volatile components in the A. villosum isbornyl acetate, while the one in Amomum longiligulare and Amomum villosumLour.var. xanthioides is camphor. In addition, the content of volatile oil in the main A. villosum produced by Yangchun in Guangdong is higher than that in other places, and it is proved that the main volatile components of the A. villosum produced by Xishuangbanna are the highest, indicating that thequality of A. villosum produced by Xishuangbanna is better. [ABSTRACT FROM AUTHOR]

Leukocyte recruitment to the surface of the endothelium plays a pivotal role in the development of cardiovascular diseases. Bornyl acetate is the main volatile constituent present in numerous conifer oils, which has displayed its anti-oxidant and anti-inflammatory properties in different types of tissues and cells. However, little information regarding the effects of bornyl acetate on vascular endothelial inflammation has been reported before. In the current study, we aimed to investigate the pharmacological roles of bornyl acetate against ox-LDL-induced leukocyte adhesion to the endothelium. Our findings indicate that bornyl acetate ameliorated ox-LDL-induced reduction in cell viability of HUVECs. Additionally, bornyl acetate inhibited the attachment of THP-1 monocytes to HUVECs induced by treatment with ox-LDL through ameliorating the expression of ICAM-1, VCAM-1, and E-selectin. Mechanistically, we found that bornyl acetate could suppress activation of the IκBα/NF-κB signaling pathway. Lastly, our results indicate that bornyl acetate mitigated expression of the pro-inflammatory cytokines TNF-α and IL-1β. Our results suggest the therapeutic potential of bornyl acetate in patients with atherosclerosis. [ABSTRACT FROM AUTHOR]

Amomum villosum, also known as Fructus Amomi, has been used to treat digestive diseases such as abdominal pain, vomiting, and dysentery. Volatile terpenoids are the active metabolites in the essential oil of Fructus Amomi. Nevertheless, downstream genes responsible for activating metabolites biosynthesis in A. villosum still remain unclear. Here, we report the use of an integrative volatile terpenoid profiling and transcriptomics analysis for mining the corresponding genes involved in volatile terpenoid biosynthesis. Ten terpene synthase (TPS) genes were discovered, and two of them were cloned and functionally characterized. AvTPS1 (AvPS: pinene synthase) catalyzed GPP to form α-pinene and β-pinene; AvTPS3 (AvBPPS: bornyl diphosphate synthase) produced bornyl diphosphate as major product and the other three monoterpenoids as minor products. Metabolite accumulation and gene expression pattern combined with AvPS biochemical characterization suggested that AvPS might play a role in biotic defense. On the other hand, the most active ingredient, bornyl acetate, was highly accumulated in seeds and was consistent with the high expression of AvBPPS, which further indicated that AvBPPS is responsible for the biosynthesis of bornyl acetate, the final metabolite of bornyl diphosphate in A. villosum. This study can be used to improve the quality of A. villosum through metabolic engineering, and for the sustainable production of bornyl acetate in heterologous hosts. [ABSTRACT FROM AUTHOR]

Amomi Fructus has been used to treat digestive diseases in the context of traditional Chinese medicine, so we evaluated the effects of a volatile oil from Amomum villosum (VOA) on intestinal mucositis induced by 5-fluorouracil (5-FU). We measured the effect of VOA and its main active constituent, bornyl acetate (BA), on body weight, food intake, diarrhea, inflammatory cytokines, the mucosal barrier, and gut microbiota. VOA and BA significantly increased the rats’ body weight, relieved diarrhea, and reversed histopathological changes in the gut and inflammation. VOA significantly inhibited apoptosis and alleviated the endoenteritis by downregulating p38 MAPK and caspase-3 expression. VOA and BA strengthened the intestinal mucosal barrier by increasing zonula occludin-1 and occludin expression. VOA and BA reduced the amount of pathogenic bacteria and increased the abundance of probiotics. Thus, VOA prevented the development and progression of intestinal mucositis after chemotherapy.

an (Zingiberaceae) growing in Vietnam was performed by means of gas chromatography-flame ionization detector (GC-FID) and gas chromatography-mass spectrometry (GC-MS) techniques. The yields of essential oils were 0.22%, 0.16% and 0.30% (v/w) respectively for leaf, stem and root, calculated on a dry weight basis. The main constituents of the leaf oil were δ-elemene (17.0%), β-pinene (12.8%) and β-elemene (8.8%). The stem oil comprised mainly of δ-elemene (20.1%), germacrene D (8.6%) and bicyclogermacrene (8.1%). The root oil had an abundance of β-pinene (21.0%), δ-elemene (12.8%) and bornyl acetate (11.8%). This is the first report on the volatile constituents ofZ. nitens. [ABSTRACT FROM PUBLISHER]

Objective: To investigate the antitumor effects of bornyl acetate (BA) isolated from Sharen ( Fructus Amomi ) in colorectal cancer (CRC) and the underlying mechanisms., Methods: SW480 and HT29 cells were treated with increasing doses of BA in order to determine its antitumor effects in vitro . Cell viability, colony formation, cell cycle, and apoptosis as well as migration and invasion were assessed using various assays. In addition, the in vivo antitumor effects of BA were assessed using a xenograft mouse model. We then assessed the mechanism of action of BA by conducting pathway activator-mediated rescue experiments and assessed the protein levels by Western blot analysis., Results: BA showed anti-CRC tumor activities in vitro by suppressing cell proliferation and colony formation, inducing apoptosis, blocking cell cycle, and inhibiting migration and invasion. These effects were mediated via suppression of the phosphatidylinositol-3-kinase/protein kinase B (PI3K/AKT) pathway. In the tumor xenograft experiment, BA was found to repress tumor growth in vivo with low toxicity., Conclusions: The results demonstrated that BA exerts antitumor effects by suppressing the PI3K/AKT pathway, with low toxicity. Thus, BA might be a potential novel therapeutic agent for CRC.