Displaying publications 1 - 20 of 51 in total

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  1. In LL, Arshad NM, Ibrahim H, Azmi MN, Awang K, Nagoor NH
    PMID: 23043547 DOI: 10.1186/1472-6882-12-179
    Oral cancers although preventable, possess a low five-year survival rate which has remained unchanged over the past three decades. In an attempt to find a more safe, affordable and effective treatment option, we describe here the use of 1'S-1'-acetoxychavicol acetate (ACA), a component of Malaysian ginger traditionally used for various medicinal purposes.
    Matched MeSH terms: Zingiberaceae/chemistry*
  2. Tang SW, Sukari MA, Rahmani M, Lajis NH, Ali AM
    Molecules, 2011 Apr 07;16(4):3018-28.
    PMID: 21475124 DOI: 10.3390/molecules16043018
    A new abietene diterpene, kaempfolienol (5S,6S,7S,9S,10S,11R,13S-abiet-8(14)-enepenta-6,7,9,11,13-ol, 1), was isolated from a rhizome extract of Kaempferia angustifolia Rosc. along with the known compounds crotepoxide, boesenboxide, zeylenol, 2'-hydroxy-4,4',6'-trimethoxychalcone, (24S)-24-methyl-5α-lanosta-9(11),25-dien-3β-ol, β-sitosterol and β-sitosterol-3-O-β-D-glucopyranoside. The structures of all compounds were elucidated on the basis of mass spectroscopic and NMR data. Zeylenol (2), the major constituent of the plant, was derivatized into diacetate, triacetate and epoxide derivatives through standard organic reactions. The cytotoxic activity of compounds 1, 2 and the zeylenol derivatives was evaluated against the HL-60, MCF-7, HT-29 and HeLa cell lines.
    Matched MeSH terms: Zingiberaceae/chemistry*
  3. Sulaiman MR, Perimal EK, Akhtar MN, Mohamad AS, Khalid MH, Tasrip NA, et al.
    Fitoterapia, 2010 Oct;81(7):855-8.
    PMID: 20546845 DOI: 10.1016/j.fitote.2010.05.009
    The anti-inflammatory activity of zerumbone (1), a natural cyclic sesquiterpene isolated from Zingiber zerumbet Smith was investigated using carrageenan-induced paw edema and cotton pellet-induced granuloma tissue formation test in mice. It was demonstrated that intraperitoneal administration of 1 at a dose of 5, 10, 50 and 100 mg/kg produced significant dose-dependent inhibition of paw edema induced by carrageenan. It was also demonstrated that 1 at similar doses significantly suppressed granulomatous tissue formation in cotton pellet-induced granuloma test.
    Matched MeSH terms: Zingiberaceae/chemistry*
  4. Zulazmi NA, Gopalsamy B, Farouk AA, Sulaiman MR, Bharatham BH, Perimal EK
    Fitoterapia, 2015 Sep;105:215-21.
    PMID: 26205045 DOI: 10.1016/j.fitote.2015.07.011
    Neuropathic pain is a chronic condition that is difficult to be treated. Current therapies available are either ineffective or non-specific thus requiring newer treatment approaches. In this study, we investigated the antiallodynic and antihyperalgesic effects of zerumbone, a bioactive sesquiterpene from Zingiber zerumbet in chronic constriction injury (CCI)-induced neuropathic pain animal model. Our findings showed that single and repeated dose of intra-peritoneal administration of zerumbone (5, 10, 50, 100 mg/kg) significantly attenuated the CCI-induced neuropathic pain when evaluated using the electronic von Frey anesthesiometer, cold plate, Randall-Selitto analgesiometer and the Hargreaves plantar test. Zerumbone significantly alleviated tactile and cold allodynia as well as mechanical and thermal hyperalgesia. Our findings are in comparison to the positive control drugs thatused gabapentin (20 mg/kgi.p.) and morphine (1 mg/kgi.p.). Together, these results showed that the systemic administration of zerumbone produced marked antiallodynic and antihyperalgesic effects in the CCI-induced neuropathic pain in mice and may serve as a potential lead compound for further analysis.
    Matched MeSH terms: Zingiberaceae/chemistry
  5. Kamazeri TS, Samah OA, Taher M, Susanti D, Qaralleh H
    Asian Pac J Trop Med, 2012 Mar;5(3):202-9.
    PMID: 22305785 DOI: 10.1016/S1995-7645(12)60025-X
    OBJECTIVE: To analyze the chemical composition of the essential oils of Curcuma aeruginosa (C. aeruginosa), Curcuma mangga (C. mangga), and Zingiber cassumunar (Z. cassumunar), and study their antimicrobial activity.

    METHODS: Essential oils obtained by steam distillation were analyzed by gas chromatography-mass spectrometry (GC-MS). The antimicrobial activity of the essential oils was evaluated against four bacteria: Bacillus cereus (B. cereus), Staphylococcus aureus (S. aureus), Escherichia coli (E. coli), and Pseudomonas aeruginosa (P. aeruginosa); and two fungi: Candida albicans (C. albicans) and Cyptococcus neoformans (C. neoformans), using disc-diffusion and broth microdilution methods.

    RESULTS: Cycloisolongifolene, 8,9-dehydro formyl (35.29%) and dihydrocostunolide (22.51%) were the major compounds in C. aeruginosa oil; whereas caryophyllene oxide (18.71%) and caryophyllene (12.69%) were the major compounds in C. mangga oil; and 2,6,9,9-tetramethyl-2,6,10-cycloundecatrien-1-one (60.77%) and α-caryophyllene (23.92%) were abundant in Z. cassumunar oil. The essential oils displayed varying degrees of antimicrobial activity against all tested microorganisms. C. mangga oil had the highest and most broad-spectrum activity by inhibiting all microorganisms tested, with C. neoformans being the most sensitive microorganism by having the lowest minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) values of 0.1 μL/mL. C. aeruginosa oil showed mild antimicrobial activity, whereas Z. cassumunar had very low or weak activity against the tested microorganisms.

    CONCLUSIONS: The preliminary results suggest promising antimicrobial properties of C. mangga and C. aeruginosa, which may be useful for food preservation, pharmaceutical treatment and natural therapies.

    Matched MeSH terms: Zingiberaceae/chemistry*
  6. Ping CP, Tengku Mohamad TAS, Akhtar MN, Perimal EK, Akira A, Israf Ali DA, et al.
    Molecules, 2018 Sep 03;23(9).
    PMID: 30177603 DOI: 10.3390/molecules23092237
    Pain is one of the most common cause for hospital visits. It plays an important role in inflammation and serves as a warning sign to avoid further injury. Analgesics are used to manage pain and provide comfort to patients. However, prolonged usage of pain treatments like opioids and NSAIDs are accompanied with undesirable side effects. Therefore, research to identify novel compounds that produce analgesia with lesser side effects are necessary. The present study investigated the antinociceptive potentials of a natural compound, cardamonin, isolated from Boesenbergia rotunda (L) Mansf. using chemical and thermal models of nociception. Our findings showed that intraperitoneal and oral administration of cardamonin (0.3, 1, 3, and 10 mg/kg) produced significant and dose-dependent inhibition of pain in abdominal writhing responses induced by acetic acid. The present study also demonstrated that cardamonin produced significant analgesia in formalin-, capsaicin-, and glutamate-induced paw licking tests. In the thermal-induced nociception model, cardamonin exhibited significant increase in response latency time of animals subjected to hot-plate thermal stimuli. The rota-rod assessment confirmed that the antinociceptive activities elicited by cardamonin was not related to muscle relaxant or sedative effects of the compound. In conclusion, the present findings showed that cardamonin exerted significant peripheral and central antinociception through chemical- and thermal-induced nociception in mice through the involvement of TRPV₁, glutamate, and opioid receptors.
    Matched MeSH terms: Zingiberaceae/chemistry
  7. Sulaiman MR, Tengku Mohamad TA, Shaik Mossadeq WM, Moin S, Yusof M, Mokhtar AF, et al.
    Planta Med, 2010 Feb;76(2):107-12.
    PMID: 19637111 DOI: 10.1055/s-0029-1185950
    In the present study, the rhizome essential oil from Zingiber zerumbet (Zingiberaceae) was evaluated for antinociceptive activity using chemical and thermal models of nociception, namely, the acetic acid-induced abdominal writhing test, the hot-plate test and the formalin-induced paw licking test. It was demonstrated that intraperitoneal administration of the essential oil of Z. zerumbet (EOZZ) at the doses of 30, 100 and 300 mg/kg produced significant dose-dependent inhibition of acetic acid-induced abdominal writhing, comparable to that of obtained with acetylsalicylic acid (100 mg/kg). At the same doses, the EOZZ produced significant dose-dependent increases in the latency time in the hot-plate test with respect to controls, and in the formalin-induced paw licking test, the EOZZ also significantly reduced the painful stimulus in both neurogenic and inflammatory phase of the test. In addition, the antinociceptive effect of the EOZZ in the formalin-induced paw licking test as well as hot-plate test was reversed by the nonselective opioid receptor antagonist, naloxone suggesting that the opioid system was involved in its analgesic mechanism of action. On the basis of these data, we concluded that the EOZZ possessed both central and peripheral antinociceptive activities which justifying its popular folkloric use to relieve some pain conditions.
    Matched MeSH terms: Zingiberaceae/chemistry*
  8. Sulaiman MR, Zakaria ZA, Daud IA, Ng FN, Ng YC, Hidayat MT
    J Nat Med, 2008 Apr;62(2):221-7.
    PMID: 18404328 DOI: 10.1007/s11418-007-0210-3
    This study was performed to determine the antinociceptive and anti-inflammatory activities of aqueous extract of Kaempferia galanga leaves using various animal models. The extract, in the doses of 30, 100, and 300 mg/kg, was prepared by soaking (1:10; w/v) the air-dried powdered leaves (40 g) in distilled water (dH(2)O) for 72 h and administered subcutaneously in mice/rats 30 min prior to the tests. The extract exhibited significant (P < 0.05) antinociceptive activity when assessed using the abdominal constriction, hot-plate and formalin tests, with activity observed in all tests occurring in a dose-dependent manner. Furthermore, the antinociceptive activity of K. galanga extract was significantly (P < 0.05) reversed when prechallenged with 10 mg/kg naloxone. The extract also produced a significantly (P < 0.05) dose-dependent anti-inflammatory activity when assessed using the carrageenan-induced paw-edema test. In conclusion, this study demonstrated that K. galanga leaves possessed antinociceptive and anti-inflammatory activities and thus supports the Malay's traditional uses of the plant for treatments of mouth ulcer, headache, sore throat, etc.
    Matched MeSH terms: Zingiberaceae/chemistry*
  9. Hashim SE, Sirat HM, Yen KH, Ismail IS, Matsuki SN
    Nat Prod Commun, 2015 Sep;10(9):1561-3.
    PMID: 26594759
    Seven compounds were isolated from the n-hexane and chloroform extracts of the flowers and leaves of four Hornstedtia species and their structures were identified using spectroscopic techniques as 3,7,4'-trimethylkaempferol (1), 3,7-dimethylkaempferol (2), 7,4'-dimethylkaempferol (3), 3,5-dimethylkaempferol (4), 3-methylkaempferol (5), stigmast-4-en-3-one (6), and 6-hydroxy-stigmast-4-en-3-one (7). Compounds 1 to 7 were isolated from these species for the first time. They were assayed for free radical scavenging and α-glucosidase inhibition activities. The DPPH assay showed that 3-methylkaempferol (5) was the most potent antioxidant agent with an IC50 value 78.6 µM, followed by 7,4'-dimethylkaempferol (3) (IC50 = 86.1 µM). For α-glucosidase inhibition activity, 3-methylkaempferol (5) exhibited significant inhibitory activity with an IC50 value 21.0 µM. The present study revealed that Hornstedtia species have potential activities as antioxidant and α-glucosidase inhibitors.
    Matched MeSH terms: Zingiberaceae/chemistry*
  10. Mohamad H, Lajis NH, Abas F, Ali AM, Sukari MA, Kikuzaki H, et al.
    J Nat Prod, 2005 Feb;68(2):285-8.
    PMID: 15730265
    Phytochemical studies on the rhizomes of Etlingera elatior have resulted in the isolation of 1,7-bis(4-hydroxyphenyl)-2,4,6-heptatrienone (1), demethoxycurcumin (2), 1,7-bis(4-hydroxyphenyl)-1,4,6-heptatrien-3-one (3), 16-hydroxylabda-8(17),11,13-trien-15,16-olide (4), stigmast-4-en-3-one, stigmast-4-ene-3,6-dione, stigmast-4-en-6beta-ol-3-one, and 5alpha,8alpha-epidioxyergosta-6,22-dien-3beta-ol. Compounds 1 and 4 are new, and their structures were elucidated by analysis of spectroscopic data. Diarylheptanoids 1-3 were found to inhibit lipid peroxidation in a more potent manner than alpha-tocopherol.
    Matched MeSH terms: Zingiberaceae/chemistry*
  11. Sidahmed HM, Hashim NM, Abdulla MA, Ali HM, Mohan S, Abdelwahab SI, et al.
    PLoS One, 2015;10(3):e0121060.
    PMID: 25798602 DOI: 10.1371/journal.pone.0121060
    BACKGROUND: Zingiber zerumbet Smith is a perennial herb, broadly distributed in many tropical areas. In Malaysia, it's locally known among the Malay people as "lempoyang" and its rhizomes, particularly, is widely used in traditional medicine for the treatment of peptic ulcer disease beyond other gastric disorders.

    AIM OF THE STUDY: The aim of the current study is to evaluate the gastroprotective effect of zerumbone, the main bioactive compound of Zingiber zerumbet rhizome, against ethanol-induced gastric ulcer model in rats.

    MATERIALS AND METHODS: Rats were pre-treated with zerumbone and subsequently exposed to acute gastric ulcer induced by absolute ethanol administration. Following treatment, gastric juice acidity, ulcer index, mucus content, histological analysis (HE and PAS), immunohistochemical localization for HSP-70, prostaglandin E2 synthesis (PGE2), non-protein sulfhydryl gastric content (NP-SH), reduced glutathione level (GSH), and malondialdehyde level (MDA) were evaluated in ethanol-induced ulcer in vivo. Ferric reducing antioxidant power assay (FRAP) and anti-H. pylori activity were investigated in vitro.

    RESULTS: The results showed that the intragastric administration of zerumbone protected the gastric mucosa from the aggressive effect of ethanol-induced gastric ulcer, coincided with reduced submucosal edema and leukocyte infiltration. This observed gastroprotective effect of zerumbone was accompanied with a significant (p <0.05) effect of the compound to restore the lowered NP-SH and GSH levels, and to reduce the elevated MDA level into the gastric homogenate. Moreover, the compound induced HSP-70 up-regulation into the gastric tissue. Furthermore, zerumbone significantly (p <0.05) enhanced mucus production, showed intense PAS stain and maintained PG content near to the normal level. The compound exhibited antisecretory activity and an interesting minimum inhibitory concentration (MIC) against H. pylori strain.

    CONCLUSION: The results of the present study revealed that zerumbone promotes ulcer protection, which might be attributed to the maintenance of mucus integrity, antioxidant activity, and HSP-70 induction. Zerumbone also exhibited antibacterial action against H. pylori.

    Matched MeSH terms: Zingiberaceae/chemistry*
  12. Othman R, Ibrahim H, Mohd MA, Mustafa MR, Awang K
    Phytomedicine, 2006 Jan;13(1-2):61-6.
    PMID: 16360934
    Bioassay-guided fractionation was performed on a crude dichloromethane extract of Kaempferia galanga L. using chromatography techniques. Screening of the extract for biological activity started with the brine shrimp lethality bioassay, followed by the study of its antihypertensive activity on anaesthetized rats, which involved monitoring of the extract's effect on mean arterial blood pressure. The components of the fractions obtained from the separation procedures were analyzed using gas chromatography (GC). The yield of the CH(2)Cl(2) extract was 0.29% of the crude plant extract. Analysis of the data for brine shrimp lethality test using the Finney computer program showed that this extract exhibited potent bioactivity with an ED(50) value of 7.92+/-0.13 microgml(-1). Intravenous administration of the extract induced a dose-related reduction of basal mean arterial pressure (MAP) (130+/-5 mmHg) in the anaesthetized rat, with maximal effects seen after 5-10 min of injection. The gas chromatogram showed that the common compound in the active fractions obtained from the bioassay-guided fractionation of the CH(2)Cl(2) extract was ethyl cinnamate. This vasorelaxant active compound, ethyl cinnamate, was isolated as a colorless oil. Ethyl p-methoxycinnamic acid was also isolated as white needles but did not exhibit any relaxant effect on the precontracted thoracic rat aorta.
    Matched MeSH terms: Zingiberaceae/chemistry*
  13. Rahman HS, Rasedee A, Yeap SK, Othman HH, Chartrand MS, Namvar F, et al.
    Biomed Res Int, 2014;2014:920742.
    PMID: 25025076 DOI: 10.1155/2014/920742
    Zerumbone (ZER) is a naturally occurring dietary compound, present in many natural foods consumed today. The compound derived from several plant species of the Zingiberaceae family that has been found to possess multiple biomedical properties, such as antiproliferative, antioxidant, anti-inflammatory, and anticancer activities. However, evidence of efficacy is sparse, pointing to the need for a more systematic review for assessing scientific evidence to support therapeutic claims made for ZER and to identify future research needs. This review provides an updated overview of in vitro and in vivo investigations of ZER, its cancer chemopreventive properties, and mechanisms of action. Therapeutic effects of ZER were found to be scientifically plausible and could be explained partially by in vivo and in vitro pharmacological activities. Much of the research outlined in this paper will serve as a foundation to explain ZER anticancer bioactivity, which will open the door for the development of strategies in the treatment of malignancies using ZER.
    Matched MeSH terms: Zingiberaceae/chemistry
  14. Voon FL, Sulaiman MR, Akhtar MN, Idris MF, Akira A, Perimal EK, et al.
    Eur J Pharmacol, 2017 Jan 05;794:127-134.
    PMID: 27845065 DOI: 10.1016/j.ejphar.2016.11.009
    Boesenbergia rotunda (L.) Mansf. had been traditionally used as herbs to treat pain and rheumatism. Cardamonin (2',4'-dihydroxy-6'-methoxychalcone) is a compound isolated from Boesenbergia rotunda (L.) Mansf.. Previous study had shown the potential of cardamonin in inhibiting the release of pro-inflammatory cytokines such as tumour necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and interleukin-6 (IL-6) in vitro. Thus, the possible therapeutic effect of cardamonin in the rheumatoid arthritis (RA) joints is postulated. This study was performed to investigate the anti-arthritic properties of cardamonin in rat model of induced RA, particularly on the inflammatory and pain response of RA. Rheumatoid arthritis paw inflammation was induced by intraplantar (i.pl.) injection of complete Freund's adjuvant (CFA) in Sprague Dawley rats. Using four doses of cardamonin (0.625, 1.25, 2.5, and 5.0mg/kg), anti-arthritic activity was evaluated through the paw edema, mechanical allodynia and thermal hyperalgesia responses. Enzyme-linked immunosorbent assay (ELISA) was carried out to evaluate the plasma level of TNF-α, IL-1β, and IL-6. Histological slides were prepared from the harvested rat paws to observe the arthritic changes in the joints. Behavioral, biochemical, and histological studies showed that cardamonin demonstrated significant inhibition on RA-induced inflammatory and pain responses as well as progression of joint destruction in rats. ELISA results showed that there was significant inhibition in TNF-α, IL-1β, and IL-6 levels in plasma of the cardamonin-treated RA rats. Overall, cardamonin possesses potential anti-arthritic properties in CFA-induced RA rat model.
    Matched MeSH terms: Zingiberaceae/chemistry*
  15. Xue Mei L, Mohammadi Nafchi A, Ghasemipour F, Mat Easa A, Jafarzadeh S, Al-Hassan AA
    Int J Biol Macromol, 2020 Dec 01;164:4603-4612.
    PMID: 32941902 DOI: 10.1016/j.ijbiomac.2020.09.082
    The development of intelligent packaging based on natural and biodegradable resources is getting more attention by researchers in recent years. The aim of this study was to develop and characterize a pH-sensitive films based on sago starch and incorporated with anthocyanin from torch ginger. The pH-sensitive films were fabricated by casting method with incorporation of different torch ginger extract (TGE) concentration. The surface morphology, physicochemical, barrier, and mechanical properties as well as the pH-sensitivity of films were investigated. The film with the highest concentration of TGE showed the lowest tensile strength (4.26 N/m2), toughness (2.54 MJ/m3), Young's modulus (73.96 MPa) and water vapour permeability (2.6 × 10-4 g·m/day·kPa·m2). However, its elongation at break (85.14%), moisture content (0.27%) and water solubility (37.92%) were the highest compared to other films. pH sensitivity analysis showed that the films containing TGE extract, changes in colour by changing the pH. The colour of films changed from pink to slightly green as the pH increased from pH 4 to 9. Thus, the developed pH-sensitive film with torch ginger extract has potential as intelligent packaging for detection of food freshness or spoilage to ensure their quality and safe consumption.
    Matched MeSH terms: Zingiberaceae/chemistry*
  16. Yusoff MM, Ibrahim H, Hamid NA
    Chem Biodivers, 2011 May;8(5):916-23.
    PMID: 21560240 DOI: 10.1002/cbdv.201000270
    Two poorly studied, morphologically allied Alpinia species endemic to Borneo, viz., A. ligulata and A. nieuwenhuizii, were investigated here for their rhizome essential oil. The oil compositions and antimicrobial activities were compared with those of A. galanga, a better known plant. A fair number of compounds were identified in the oils by GC-FID and GC/MS analyses, with large differences in the oil composition between the three species. The rhizome oil of A. galanga was rich in 1,8-cineole (29.8%), while those of A. ligulata and A. nieuwenhuizii were both found to be extremely rich in (E)-methyl cinnamate (36.4 and 67.8%, resp.). The three oils were screened for their antimicrobial activity against three Gram-positive and three Gram-negative bacteria and two fungal species. The efficiency of growth inhibition of Staphylococcus aureus var. aureus was found to decline in the order of A. nieuwenhuizii>A. ligulata ∼ A. galanga, while that of Escherichia coli decreased in the order of A. galanga>A. nieuwenhuzii ∼ A. ligulata. Only the A. galanga oil inhibited the other bacteria and the fungi tested.
    Matched MeSH terms: Zingiberaceae/chemistry*
  17. Abdelwahab SI, Zaman FQ, Mariod AA, Yaacob M, Abdelmageed AH, Khamis S
    J Sci Food Agric, 2010 Dec;90(15):2682-8.
    PMID: 20945508 DOI: 10.1002/jsfa.4140
    Plant essential oils are widely used as fragrances and flavours. Therefore, the essential oils from the leaves of Cinnamomum pubescens Kochummen (CP) and the whole plant of Etlingera elatior (EE) were investigated for their antioxidant, antibacterial and phytochemical properties.
    Matched MeSH terms: Zingiberaceae/chemistry*
  18. Jani NA, Sirat MH, Ali NM, Aziz A
    Nat Prod Commun, 2013 Apr;8(4):513-4.
    PMID: 23738467
    The chemical compositions of the essential oil of the rhizome, leaf and stem of Hornstedtia leonurus Retz., collected from Negeri Sembilan, Malaysia,are reported for the first time. The essential oils were extracted using hydrodistillation and analyzed by gas chromatography (GC-FID) and gas chromatography/mass spectrometry (GC/MS). Seventeen (96.4%), thirteen (89.2%) and nine components (98.8%) were successfully identified from the rhizome, stem and leaf oils, respectively. Phenylpropanoids were found to be the major fraction, with methyleugenol being the most abundant compound in all oils with percentage compositions of 76.4% (rhizome), 80.3% (stem) and 74.5% (leaf).
    Matched MeSH terms: Zingiberaceae/chemistry*
  19. Lai SL, Wong PF, Lim TK, Lin Q, Mustafa MR
    Proteomics, 2015 May;15(9):1608-21.
    PMID: 25594392 DOI: 10.1002/pmic.201400039
    Melanoma is a lethal form of skin cancer with rising global incidence. However, limited treatment options are available for advanced melanoma and this is further compounded by the development of resistance toward existing drugs. Panduratin A (PA), a cyclohexanyl chalcone found in Boesenbergia rotunda, was investigated for its cytotoxic potentials against human malignant melanoma A375 cells. Our initial findings revealed that mitochondrion is the primary acting site of PA on A375 cancer cells and the cytotoxic mechanisms of PA were further investigated using a temporal quantitative proteomics approach by iTRAQ 2D-LC-MS/MS. Comprehensive proteomics analysis identified 296 proteins that were significantly deregulated in PA-treated A375 cells and revealed the involvement of mitochondrial oxidative phosphorylation, secretory and ER stress pathway, and apoptosis. We further confirmed that the PA-induced apoptosis was mediated by prolonged ER stress at least in part via the PERK/eIF2α/ATF4/CHOP pathway. Pretreatment with cycloheximide, an ER stress inhibitor rescued PA-induced cell death, which was accompanied by the suppression of ER-stress-related HSPA5 and CHOP proteins. The present study provides comprehensive mechanistic insights into the cytotoxic mechanisms of PA.
    Matched MeSH terms: Zingiberaceae/chemistry
  20. Frimayanti N, Chee CF, Zain SM, Rahman NA
    Int J Mol Sci, 2011;12(2):1089-100.
    PMID: 21541045 DOI: 10.3390/ijms12021089
    Dengue is a serious disease which has become a global health burden in the last decade. Currently, there are no approved vaccines or antiviral therapies to combat the disease. The increasing spread and severity of the dengue virus infection emphasizes the importance of drug discovery strategies that could efficiently and cost-effectively identify antiviral drug leads for development into potent drugs. To this effect, several computational approaches were applied in this work. Initially molecular docking studies of reference ligands to the DEN2 NS2B/NS3 serine protease were carried out. These reference ligands consist of reported competitive inhibitors extracted from Boesenbergia rotunda (i.e., 4-hydroxypanduratin A and panduratin A) and three other synthesized panduratin A derivative compounds (i.e., 246DA, 2446DA and 20H46DA). The design of new lead inhibitors was carried out in two stages. In the first stage, the enzyme complexed to the reference ligands was minimized and their complexation energies (i.e., sum of interaction energy and binding energy) were computed. New compounds as potential dengue inhibitors were then designed by putting various substituents successively on the benzyl ring A of the reference molecule. These substituted benzyl compounds were then computed for their enzyme-ligand complexation energies. New enzyme-ligand complexes, exhibiting the lowest complexation energies and closest to the computed energy for the reference compounds, were then chosen for the next stage manipulation and design, which involved substituting positions 4 and 5 of the benzyl ring A (positions 3 and 4 for 2446DA) with various substituents.
    Matched MeSH terms: Zingiberaceae/chemistry
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