Displaying publications 101 - 118 of 118 in total

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  1. Maizura M, Fazilah A, Norziah MH, Karim AA
    J Food Sci, 2007 Aug;72(6):C324-30.
    PMID: 17995673
    Edible films were prepared from a mixture of partially hydrolyzed sago starch and alginate (SA). Lemongrass oil (0.1% to 0.4%, v/w) and glycerol (0% and 20%, w/w) were incorporated in the films to act as natural antimicrobial agent and plasticizer, respectively. The films were characterized for antimicrobial activity, water vapor permeability (WVP), tensile strength (TS), percent elongation at break (%E), and water solubility (WS). Fourier transform infrared (FTIR) spectroscopy was conducted to determine functional group interactions between the matrix and lemongrass oil. The zone of inhibition was increased significantly (P < 0.05) by addition of lemongrass oil at all levels in the presence and the absence of glycerol. This indicates that the film containing lemongrass oil was effective against Escherichia coli O157:H7 at all levels. In the absence of glycerol, the tensile strength of film decreased as the oil content increased, but there was no significant (P > 0.05) difference in percent elongation. The percent elongation at break and WVP values for film with 20% glycerol was found to be increased significantly (P < 0.05) with an increase in lemongrass oil content. Addition of lemongrass oil did not have any interaction with the functional groups of films as measured by FTIR.
    Matched MeSH terms: Terpenes/pharmacology*
  2. Hassan M, Maarof ND, Ali ZM, Noor NM, Othman R, Mori N
    Biosci Biotechnol Biochem, 2012;76(8):1463-70.
    PMID: 22878188
    NADP(+)-dependent geraniol dehydrogenase (EC 1.1.1.183) is an enzyme that catalyzes the oxidation of geraniol to geranial. Stable, highly active cell-free extract was obtained from Polygonum minus leaves using polyvinylpolypyrrolidone, Amberlite XAD-4, glycerol, 2-mercaptoethanol, thiourea, and phenylmethylsulfonylfluoride in tricine-NaOH buffer (pH 7.5). The enzyme preparation was separated into two activity peaks, geraniol-DH I and II, by DEAE-Toyopearl 650M column chromatography at pH 7.5. Both isoenzymes were purified to homogeneity in three chromatographic steps. The geraniol-DH isoenzymes were similar in molecular mass, optimal temperature, and pH, but the isoelectric point, substrate specificity, and kinetic parameters were different. The K(m) values for geraniol of geraniol-DH I and II appeared to be 0.4 mM and 0.185 mM respectively. P. minus geraniol-DHs are unusual among geraniol-DHs in view of their thermal stability and optimal temperatures, and also their high specificity for allylic alcohols and NADP(+).
    Matched MeSH terms: Terpenes/chemistry*; Monoterpenes/chemistry*
  3. Suleiman JB, Mohamed M, Abu Bakar AB, Nna VU, Zakaria Z, Othman ZA, et al.
    Molecules, 2021 Aug 15;26(16).
    PMID: 34443531 DOI: 10.3390/molecules26164943
    The aim of the study was to determine the chemical profile, antioxidant properties and antimicrobial activities of Heterotrigona itama bee bread from Malaysia. The pH, presence of phytochemicals, antioxidant properties, total phenolic content (TPC) and total flavonoid content (TFC), as well as antimicrobial activities, were assessed. Results revealed a decrease in the pH of bee bread water extract (BBW) relative to bee bread ethanolic extract (BBE) and bee bread hot water extract (BBH). Further, alkaloids, flavonoids, phenols, tannins, saponins, terpenoids, resins, glycosides and xanthoproteins were detected in BBW, BBH and BBE. Also, significant decreases in TPC, TFC, DPPH activity and FRAP were detected in BBW relative to BBH and BBE. We detected phenolic acids such as gallic acid, caffeic acid, trans-ferulic acid, trans 3-hydroxycinnamic acid and 2-hydroxycinnamic acid, and flavonoids such as quercetin, kaempferol, apigenin and mangiferin in BBE using high-performance liquid chromatography analysis. The strongest antimicrobial activity was observed in Klebsilla pneumonia (MIC50 1.914 µg/mL), followed by E. coli (MIC50 1.923 µg/mL), Shigella (MIC50 1.813 µg/mL) and Salmonella typhi (MIC50 1.617 µg/mL). Bee bread samples possess antioxidant and antimicrobial properties. Bee bread contains phenolic acids and flavonoids, and could be beneficial in the management and treatment of metabolic diseases.
    Matched MeSH terms: Terpenes/chemistry
  4. Koga Y, Yoshida I, Kimura A, Yoshino M, Yamashita F, Sinniah D
    Pediatr Res, 1987 Aug;22(2):184-7.
    PMID: 3658544
    Margosa oil (MO), a fatty acid-rich extract of the seeds of the neem tree and a reported cause of Reye's syndrome, has been used in the induction of an experimental model of Reye's syndrome in rats. It has been reported that MO causes a decrease in in vivo mitochondrial enzyme activity similar to that seen in Reye's syndrome. We have attempted to uncover some of the biochemical mechanisms of MO's toxicity by examining its effect in vitro on isolated rat liver mitochondria. Male rat liver mitochondria were isolated by centrifugation; oxygen uptake, reduced forms of cytochrome b, c + c1, a + a3, and flavoprotein, intramitochondrial concentrations of acetyl coA, acid-soluble coA, acid-insoluble coA, and ATP content were measured after incubation with and without MO. Our results reveal that MO is a mitochondrial uncoupler. State 4 respiration was increased while the respiratory control ratio was decreased. The intramitochondrial content of ATP was also decreased. There were substantial changes in the reduction of the respiratory chain components after incubation of mitochondria with MO. This decelerative effect on mitochondrial electron transport was alleviated by the addition of coenzyme Q and/or carnitine. These effects of MO on mitochondrial respiration may be due to changes in fatty acid metabolism caused by MO as MO caused a shift in the proportion of acid-soluble or acid-insoluble coA esters. Supplementary therapy with L-carnitine and coenzyme Q may be useful in the management of MO-induced Reye's syndrome.
    Matched MeSH terms: Terpenes/toxicity*
  5. Kambara H, Yamada T, Tsujioka M, Matsunaga S, Tanaka R, Ali HI, et al.
    Chem Biodivers, 2006 Dec;3(12):1301-6.
    PMID: 17193244
    As a part of our chemical studies on Malaysian medicinal plants, five Malaysian plant species were evaluated by cytotoxicity assays using P388 murine leukemia cells. Since Acalypha siamensis exhibited the strongest growth inhibition, its constituents were studied as the object of search for bioactive materials. A novel tetraterpene, acalyphaser A (1), was isolated in the course of the purification. Its structure was elucidated on the basis of 1D- and 2D-NMR techniques, and mass spectrometry.
    Matched MeSH terms: Terpenes/chemistry*
  6. Chow KS, Mat-Isa MN, Bahari A, Ghazali AK, Alias H, Mohd-Zainuddin Z, et al.
    J Exp Bot, 2012 Mar;63(5):1863-71.
    PMID: 22162870 DOI: 10.1093/jxb/err363
    The cytosolic mevalonate (MVA) pathway in Hevea brasiliensis latex is the conventionally accepted pathway which provides isopentenyl diphosphate (IPP) for cis-polyisoprene (rubber) biosynthesis. However, the plastidic 2-C-methyl-D-erythritol 4-phosphate (MEP) pathway may be an alternative source of IPP since its more recent discovery in plants. Quantitative RT-PCR (qRT-PCR) expression profiles of genes from both pathways in latex showed that subcellular compartmentalization of IPP for cis-polyisoprene synthesis is related to the degree of plastidic carotenoid synthesis. From this, the occurrence of two schemes of IPP partitioning and utilization within one species is proposed whereby the supply of IPP for cis-polyisoprene from the MEP pathway is related to carotenoid production in latex. Subsequently, a set of latex unique gene transcripts was sequenced and assembled and they were then mapped to IPP-requiring pathways. Up to eight such pathways, including cis-polyisoprene biosynthesis, were identified. Our findings on pre- and post-IPP metabolic routes form an important aspect of a pathway knowledge-driven approach to enhancing cis-polyisoprene biosynthesis in transgenic rubber trees.
    Matched MeSH terms: Terpenes/metabolism
  7. Chaudhry GE, Rahman NH, Sevakumaran V, Ahmad A, Mohamad H, Zafar MN, et al.
    J Adv Pharm Technol Res, 2020 10 10;11(4):233-237.
    PMID: 33425710 DOI: 10.4103/japtr.JAPTR_81_20
    Breast cancer is among the frequently occurring cancer worldwide. The foremost underline aim of this study was to determine the growth inhibitory effect along with mechanistic study of a Bruguiera gymnorrhiza extract on MCF-7. The cytotoxicity activity was determined by using the MTS assay. Butanol extract exhibited the maximum cytotoxicity activity against the MCF-7 cells with IC50 of 3.39 μg/mL, followed by diethyl ether and methanol extract (IC50 at 16.22 μg/mL and 37.15 μg/mL, respectively) at 72 h. The DeadEndTM Colorimetric Apoptosis Detection System confirmed the induction of apoptosis (via DNA fragmentation) in MCF-7 cells. Both butanol and diethyl ether extracts of B. gymnorrhiza significantly increase the caspase-3 level. However, the diethyl ether extract induced higher caspase-9 levels compared to caspase-8, suggesting that the intrinsic pathway was the major route in the process of apoptosis. Thin-layer chromatography profiling demonstrated the presence of phenolic, terpene, and alkaloid compounds in crude methanol, diethyl ether, and butanol extracts. The phytochemicals present in the extracts of B. gymnorrhiza might have the potential to be a future therapeutic agent against breast cancer.
    Matched MeSH terms: Terpenes
  8. Yap WF, Tay V, Tan SH, Yow YY, Chew J
    Antibiotics (Basel), 2019 Sep 17;8(3).
    PMID: 31533237 DOI: 10.3390/antibiotics8030152
    Seaweeds are gaining a considerable amount of attention for their antioxidant and antibacterial properties. Caulerpa racemosa and Caulerpa lentillifera, also known as 'sea grapes', are green seaweeds commonly found in different parts of the world, but the antioxidant and antibacterial potentials of Malaysian C. racemosa and C. lentillifera have not been thoroughly explored. In this study, crude extracts of the seaweeds were prepared using chloroform, methanol, and water. Total phenolic content (TPC) and total flavonoid content (TFC) were measured, followed by in vitro antioxidant activity determination using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay. Antibacterial activities of these extracts were tested against Methicillin-resistant Staphylococcus aureus (MRSA) and neuropathogenic Escherichia coli K1. Liquid chromatography-mass spectrometry (LCMS) analysis was then used to determine the possible compounds present in the extract with the most potent antioxidant and antibacterial activity. Results showed that C. racemosa chloroform extract had the highest TPC (13.41 ± 0.86 mg GAE/g), antioxidant effect (EC50 at 0.65 ± 0.03 mg/mL), and the strongest antibacterial effect (97.7 ± 0.30%) against MRSA. LCMS analysis proposed that the chloroform extracts of C. racemosa are mainly polyunsaturated and monounsaturated fatty acids, terpenes, and alkaloids. In conclusion, C. racemosa can be a great source of novel antioxidant and antibacterial agents, but isolation and purification of the bioactive compounds are needed to study their mechanism of action.
    Matched MeSH terms: Terpenes
  9. Agatonovic-Kustrin S, Kustrin E, Morton DW
    Neural Regen Res, 2019 Mar;14(3):441-445.
    PMID: 30539810 DOI: 10.4103/1673-5374.245467
    As total life expectancy increases, the prevalence of age-related diseases such as diabetes and Alzheimer's disease is also increasing. Many hypotheses about Alzheimer's disease have been developed, including cholinergic neuron damage, oxidative stress, and inflammation. Acetylcholine is a major neurotransmitter in the brain and cholinergic deficits leads to cognitive dysfunction and decline. Recent studies have linked diabetes as a risk factor in developing Alzheimer's disease and other types of dementia. The incidence of patients with type II diabetes and increased levels and activity of α-amylase is higher in patients with dementia. It has been shown that aromatherapy with essential oils from the mint family can improve cognitive performance in Alzheimer's disease patients. Selected monoterpenoids from these essential oils are reported to inhibit acetylcholinesterase, both in vitro and in vivo. Terpenoids are small, fat-soluble organic molecules that can transfer across nasal mucosa if inhaled, or penetrate through the skin after topical application, enter into the blood and cross the blood-brain barrier. Recent evidence supports the idea that the common constituents of essential oils also inhibit α-amylase, a starch digestive enzyme that plays an important role in the control of diabetes. The mint family is a fragrant plant family that contains most of the culinary herbs found in the Mediterranean diet. The Mediterranean diet is considered to be one of the healthiest diets in the world, and is found to be beneficial not only for the heart but also for the brain. Herbs used in this diet are rich in antioxidants that can prevent oxidative damage caused by free radicals. However, our study shows that they also contain biologically active compounds with potent α-amylase and acetylcholinesterase inhibitory activities. Consumption of fresh herbs can help boost memory and reduce sugar levels in the body. The use of herbs as a functional food could lead to significant improvements in health. Cognitive stimulation with medical food and medical herbs could delay development of cognitive decline, and improve the quality of life of Alzheimer's disease patients. This effect can be enhanced if combined with aromatherapy, topically or by inhalation, and/or by ingestion. Terpenes and terpenoids, the primary constituents of these essential oils are small, lipid soluble organic molecules that can be absorbed through the skin or across nasal mucosa into the systemic blood circulation. Many terpenes can also cross the blood-brain barrier. Therefore, topical application or inhalation of essential oils will also produce a systemic effect.
    Matched MeSH terms: Terpenes; Monoterpenes
  10. Alam I, Forid MS, Roney M, Aluwi MFFM, Huq AM
    Data Brief, 2021 Apr;35:106839.
    PMID: 33659597 DOI: 10.1016/j.dib.2021.106839
    The current data report describes the predictive identification of phytochemical constituents in the bioactive extract of Ipomoea mauritiana (IM) whole plant. For several formulations this plant was commonly used as 'Vidari' for Ayurvedic medicine. Traditionally, IM tubers are used to alleviate spinal cord pain, improve breast milk, as a tonic, increase sperm count and treating jaundice. The methanol extract can potentially scavenge free radicals and possess antibacterial activity that could be correlated with its chemical composition. So it is crucial to identify the major compounds of IM. An ultra-performance liquid chromatography coupled electrospray ionization quadrupole time-of-flight mass spectrometry (UPLC-ESI-QTOF/MS) method was adopted to detect the flavonoids, saponins, alkaloids, terpenoids in IM methanol extract. Data presented here is related to a published work Antioxidant and antibacterial activity of Ipomoea mauritiana Jacq.: A traditionally used medicinal plant in Bangladesh (Alam et al., 2020). Secondary metabolites were analyzed by the comparison of the mass fragmentation arrangements with Waters UNIFI library that enables for positive identification of the compounds based on the spectral match.
    Matched MeSH terms: Terpenes
  11. Maizura, M., Fazilah, A., Norziah, M.H., Karim, A.A.
    MyJurnal
    Antibacterial effect of modified sago starch-alginate edible film incorporating lemongrass oil at various concentrations was studied. Edible films were prepared from a mixture of modified sago starch and alginate. Lemongrass oil (0.1 - 0.4%, v/w) and glycerol (0 and 20%, w/w) were incorporated in the films to act as natural antimicrobial agent and plasticizer, respectively. The films were characterized for antibacterial activity against food pathogenic bacteria such as Escherichia coli O157:H7, Salmonella Enteritidis and Staphylococcus aureus. The edible film exhibited antibacterial activity against Escherichia coli O157:H7 and Salmonella Enteritidis by using agar diffusion assay method. For films tested against Escherichia coli O157:H7, the zone of inhibition increased significantly (p < 0.05) with addition of lemongrass oil at all levels both in the presence and absence of glycerol. The films also significantly (p < 0.05) inhibited the growth of Salmonella enteritidis only with 0.4% lemongrass oil (in the presence and absence of glycerol). However, the films containing lemongrass oil did not show any inhibition effect on Staphylococcus aureus.
    Matched MeSH terms: Terpenes
  12. Tang YQ, Lee SH, Sekaran SD
    JUMMEC, 2014;17(2):1-8.
    MyJurnal
    The plants of the genus Phyllanthus (Euphorbiaceae) are distributed in most tropical and subtropical regions of world. This plant has been long used as a traditional medicine to treat problems such as stomach, intestinal infections, kidney and urinary bladder disturbances, diabetes, and hepatitis B. There has been considerable interest in these plants in recent years. This review discusses the antiviral and anticancer aspects of Phyllanthus species. Scientific studies have demonstrated that extracts and purified isolated compounds (flavonoids, lignans, phenols, and terpenes) obtained from these plants possess antiviral effects against herpes simplex (HSV) and dengue virus infections (DENV). These observations are associated with the disruption of essential proteins needed during viral cycle, thus halting the viral replication. In addition, the Phyllanthus species have also been shown to exert inhibitory effects against selected cancers types. In these studies anti-proliferative, anti-metastatic, anti-angiogenic effects and induced apoptosis of human cancers cell lines were observed. These may be explained by the disruption of multiple survival pathways and differential protein expression. CONLCUSION:As a conclusion, tThe Phyllanthus plant possesses multiple medicinal properties, including antiviral and anticancer activities which may potentially be used as a medicinal source for many disease locally.
    Matched MeSH terms: Terpenes
  13. Khoo HE, Azlan A, Abd Kadir NAA
    Front Chem, 2019;7:5.
    PMID: 30766864 DOI: 10.3389/fchem.2019.00005
    This study aims to identify potential phenolic compounds, terpenoids, and other phytochemicals, as well as fatty acid profile and peptides in Canarium odontophyllum (CO) oil and oleoresin, extracted using supercritical carbon dioxide. LC-ESI-MS was applied in separation and tentative identification of phytochemicals in CO oil and oleoresin. Based on the results, 11 common fatty acids and their isomers, monoglycerides, diglycerides, as well as other types of lipid, were tentatively identified in the CO oil and oleoresin. The identified fatty acids consisted of saturated fatty acids (C8-C16), monounsaturated fatty acids (C16:1 and C18:1), polyunsaturated fatty acids (C18:2, C18:3, C18:4, and C20:3), and other unclassified fatty acids. The tentatively identified phenolic compounds were phenolic acids, flavonoids, lignans, and a phenolic monoester. Triterpenes, sesquiterpenes, and apocarotenoids were the terpenoids found in CO oil and oleoresin. Besides these typical bioactives, some volatiles, aromatic compounds, peptides, and other known and unknown phytochemicals were also tentatively identified in the oil and oleoresin of CO. Some of these compounds are new compounds identified in CO oil and oleoresin, which are not found in many other fruit oils. Although CO oil and oleoresin contain a small number of phytochemicals, their contribution as antioxidants may prevent several diseases. In this study, we hypothesized that CO oleoresin contains certain types of fatty acids that render its semi-solid together with other chemical components which are not found in CO oil. This is the first study that tentatively identified fatty acids, peptides, and potential phytochemicals in CO oil and oleoresin using LC-ESI-MS.
    Matched MeSH terms: Sesquiterpenes; Terpenes; Triterpenes
  14. Noordin MAM, Noor MM, Aizat WM
    Mini Rev Med Chem, 2020;20(13):1287-1299.
    PMID: 32348218 DOI: 10.2174/1389557520666200429101942
    It is expected that in 2050, there will be more than 20% of senior citizens aged over 60 years worldwide. Such alarming statistics require immediate attention to improve the health of the aging population. Since aging is closely related to the loss of antioxidant defense mechanisms, this situation eventually leads to numerous health problems, including fertility reduction. Furthermore, plant extracts have been used in traditional medicine as potent antioxidant sources. Although many experiments had reported the impact of various bioactive compounds on aging or fertility, there is a lack of review papers that combine both subjects. In this review, we have collected and discussed various bioactive compounds from 26 different plant species known to affect both longevity and fertility. These compounds, including phenolics and terpenes, are mostly involved in the antioxidant defense mechanisms of diverse organisms such as rats, mites, fruit flies, roundworms, and even roosters. A human clinical trial should be considered in the future to measure the effects of these bioactive compounds on human health and longevity. Ultimately, these plant-derived compounds could be developed into health supplements or potential medical drugs to ensure a healthy aging population.
    Matched MeSH terms: Terpenes
  15. Norazsida, R., Pakeer, O., Taher, M.
    MyJurnal
    This study was conducted to evaluate the phytochemical contents and antimalarial properties of the oils extracted from the leaves of Malaysian Plectranthus amboinicus in mice infected with Plasmodium berghei. The essential oils were extracted and prepared by using steam distillation technique and subjected to phytochemical screening by using GC-MS. Antimalarial activity of different extract doses of the essential oil was tested in vivo in ICR mice infected with Plasmodium berghei (PZZ1/100) during early, established and residual infections. In all, 5 compounds made up 88.34% of total oil and the major chemical compounds were carvacrol (85.14%), thymoquinone (1.65%), terpinen-4-ol (0.70%), octenol (0.62%) and thymol (0.23%). Antimalarial assay showed this essential oil as a potential prophylactic agent with the percentage chemosuppression of 45.23%, 18.28%, 45.38% and 58.26% while treated with 50, 200, 400 and 1000 µL/kg respectively of essential oil and curative agent with percentage of chemo suppression of 54.10%, 47.35%, 56.75% and 65.38% while treated with the above dose of essential oil. Statistically no reduction of parasitemia was calculated for suppressive test. The extract has prophylactic and curative effects on P.berghei in mice
    Matched MeSH terms: Terpenes; Monoterpenes
  16. Sinniah D, Sinniah R, Baskaran G, Pathmanathan R, Yamashita F, Yoshino M
    Acta Paediatr Jpn, 1990 Aug;32(4):462-8.
    PMID: 2288230
    Glucose and steroids have been used in the treatment of children with Reye's syndrome, while carnitine and coenzyme Q10 have been the subject of some recent studies which suggest that these agents may have a role in the treatment of Reye's syndrome and Reye-like syndrome due to margosa oil poisoning. Because of the paucity of causes of Reye's syndrome seen at any one centre, the clinical variability of the disease, and limited knowledge of definite aetiologic factors, controlled clinical trials are not easy to carry out or to interpret in human cases. These caveats were overcome by evaluation of these four treatment modalities in an established margosa-oil-induced animal model of Reye's syndrome. Effectiveness of the treatment modalities was determined from clinical response and histopathologic parameters (grading of light microscopic fatty changes and ultrastructural changes in the hepatocytes). Results show that carnitine per se produces a small improvement in survival, but statistically, more significant benefit is seen with glucose administration. Carnitine plus 10% dextrose appears to produce better results. Evaluation of coenzyme Q10 and carnitine on histopathologic parameters in the liver after a sublethal dose of margosa oil showed no obvious ameliorating effect on liver pathology. Steroids (dexamethasone/methylprednisolone) had no beneficial effects in reducing mortality, affecting glycogen storage or lipid accumulation. Changes in the mitochondria, ribosomes and endoplasmic reticulum were unaltered from the groups treated with margosa oil alone. While glucose and carnitine supplements appear to be beneficial, the other modes of therapy do not seem to hold much promise in the treatment of Reye-like syndrome in the margosa-oil-induced animal model.
    Matched MeSH terms: Terpenes
  17. Liew SY, Looi CY, Paydar M, Cheah FK, Leong KH, Wong WF, et al.
    PLoS One, 2014;9(2):e87286.
    PMID: 24551054 DOI: 10.1371/journal.pone.0087286
    In this study, a new apoptotic monoterpenoid indole alkaloid, subditine (1), and four known compounds were isolated from the bark of Nauclea subdita. Complete (1)H- and (13)C- NMR data of the new compound were reported. The structures of isolated compounds were elucidated with various spectroscopic methods such as 1D- and 2D- NMR, IR, UV and LCMS. All five compounds were screened for cytotoxic activities on LNCaP and PC-3 human prostate cancer cell-lines. Among the five compounds, the new alkaloid, subditine (1), demonstrated the most potent cell growth inhibition activity and selective against LNCaP with an IC50 of 12.24±0.19 µM and PC-3 with an IC50 of 13.97±0.32 µM, compared to RWPE human normal epithelial cell line (IC50 = 30.48±0.08 µM). Subditine (1) treatment induced apoptosis in LNCaP and PC-3 as evidenced by increased cell permeability, disruption of cytoskeletal structures and increased nuclear fragmentation. In addition, subditine (1) enhanced intracellular reactive oxygen species (ROS) production, as reflected by increased expression of glutathione reductase (GR) to scavenge damaging free radicals in both prostate cancer cell-lines. Excessive ROS could lead to disruption of mitochondrial membrane potential (MMP), release of cytochrome c and subsequent caspase 9, 3/7 activation. Further Western blot analyses showed subditine (1) induced down-regulation of Bcl-2 and Bcl-xl expression, whereas p53 was up-regulated in LNCaP (p53-wild-type), but not in PC-3 (p53-null). Overall, our data demonstrated that the new compound subditine (1) exerts anti-proliferative effect on LNCaP and PC-3 human prostate cancer cells through induction of apoptosis.
    Matched MeSH terms: Terpenes/pharmacology*; Terpenes/chemistry
  18. Coste C, Gérard N, Dinh CP, Bruguière A, Rouger C, Leong ST, et al.
    Biomolecules, 2020 09 02;10(9).
    PMID: 32887413 DOI: 10.3390/biom10091266
    Modulation of major histocompatibility complex (MHC) expression using drugs has been proposed to control immunity. Phytochemical investigations on Garcinia species have allowed the isolation of bioactive compounds such as polycyclic polyprenylated acylphloroglucinols (PPAPs). PPAPs such as guttiferone J (1), display anti-inflammatory and immunoregulatory activities while garcinol (4) is a histone acetyltransferases (HAT) p300 inhibitor. This study reports on the isolation, identification and biological characterization of two other PPAPs, i.e., xanthochymol (2) and guttiferone F (3) from Garcinia bancana, sharing structural analogy with guttiferone J (1) and garcinol (4). We show that PPAPs 1-4 efficiently downregulated the expression of several MHC molecules (HLA-class I, -class II, MICA/B and HLA-E) at the surface of human primary endothelial cells upon inflammation. Mechanistically, PPAPs 1-4 reduce MHC proteins by decreasing the expression and phosphorylation of the transcription factor STAT1 involved in MHC upregulation mediated by IFN-γ. Loss of STAT1 activity results from inhibition of HAT CBP/p300 activity reflected by a hypoacetylation state. The binding interactions to p300 were confirmed through molecular docking. Loss of STAT1 impairs the expression of CIITA and GATA2 but also TAP1 and Tapasin required for peptide loading and transport of MHC. Overall, we identified new PPAPs issued from Garcinia bancana with potential immunoregulatory properties.
    Matched MeSH terms: Terpenes/pharmacology; Terpenes/chemistry
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