Displaying publications 1 - 20 of 149 in total

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  1. Fulltext Zingiber zerumbet (L.) Smith: A Review of Its Ethnomedicinal, Chemical, and Pharmacological Uses
    Yob NJ, Jofrry SM, Affandi MM, Teh LK, Salleh MZ, Zakaria ZA
    Evid Based Complement Alternat Med, 2011;2011:543216.
    PMID: 21584247 DOI: 10.1155/2011/543216
    Zingiber zerumbet Sm., locally known to the Malay as "Lempoyang," is a perennial herb found in many tropical countries, including Malaysia. The rhizomes of Z. zerumbet, particularly, have been regularly used as food flavouring and appetizer in various Malays' cuisines while the rhizomes extracts have been used in Malay traditional medicine to treat various types of ailments (e.g., inflammatory- and pain-mediated diseases, worm infestation and diarrhea). Research carried out using different in vitro and in vivo assays of biological evaluation support most of these claims. The active pharmacological component of Z. zerumbet rhizomes most widely studied is zerumbone. This paper presents the botany, traditional uses, chemistry, and pharmacology of this medicinal plant.
    Matched MeSH terms: Sesquiterpenes
  2. Fulltext Functional characterization of sesquiterpene synthase from Polygonum minus
    Ee SF, Mohamed-Hussein ZA, Othman R, Shaharuddin NA, Ismail I, Zainal Z
    ScientificWorldJournal, 2014;2014:840592.
    PMID: 24678279 DOI: 10.1155/2014/840592
    Polygonum minus is an aromatic plant, which contains high abundance of terpenoids, especially the sesquiterpenes C15H24. Sesquiterpenes were believed to contribute to the many useful biological properties in plants. This study aimed to functionally characterize a full length sesquiterpene synthase gene from P. minus. P. minus sesquiterpene synthase (PmSTS) has a complete open reading frame (ORF) of 1689 base pairs encoding a 562 amino acid protein. Similar to other sesquiterpene synthases, PmSTS has two large domains: the N-terminal domain and the C-terminal metal-binding domain. It also consists of three conserved motifs: the DDXXD, NSE/DTE, and RXR. A three-dimensional protein model for PmSTS built clearly distinguished the two main domains, where conserved motifs were highlighted. We also constructed a phylogenetic tree, which showed that PmSTS belongs to the angiosperm sesquiterpene synthase subfamily Tps-a. To examine the function of PmSTS, we expressed this gene in Arabidopsis thaliana. Two transgenic lines, designated as OE3 and OE7, were further characterized, both molecularly and functionally. The transgenic plants demonstrated smaller basal rosette leaves, shorter and fewer flowering stems, and fewer seeds compared to wild type plants. Gas chromatography-mass spectrometry analysis of the transgenic plants showed that PmSTS was responsible for the production of β -sesquiphellandrene.
    Matched MeSH terms: Sesquiterpenes/metabolism*
  3. Biotransformation of sesquiterpenoids: a recent insight
    Aminudin NI, Ridzuan M, Susanti D, Zainal Abidin ZA
    J Asian Nat Prod Res, 2022 Feb;24(2):103-145.
    PMID: 33783284 DOI: 10.1080/10286020.2021.1906657
    Sesquiterpenoids have been identified as natural compounds showing remarkable biological activities found in medicinal plants. There is great interest in developing methods to obtain sesquiterpenoids derivatives and biotransformation is one of the alternative methods for structural modification of complex sesquiterpenes structures. Biotransformation is a great drug design tool offering high selectivity and green method. The present review describes a comprehensive summary of biotransformation products of sesquiterpenoids and its structural modification utilizing a variety of biocatalysts including microorganisms, plant tissue culture and enzymes. This review covers recent literatures from 2007 until 2020 and highlights the experimental conditions for each biotransformation process.
    Matched MeSH terms: Sesquiterpenes*
  4. Improved oral bioavailability of artemisinin through inclusion complexation with beta- and gamma-cyclodextrins
    Wong JW, Yuen KH
    Int J Pharm, 2001 Oct 04;227(1-2):177-85.
    PMID: 11564552
    The bioavailability of beta- and gamma-cyclodextrin artemisinin complexes was evaluated in comparison with a normal commercially available preparation, Artemisinin 250. Twelve healthy male volunteers participated in the study conducted according to a three-way crossover design. The bioavailability was compared using the parameters, total area under the plasma level-time curve (AUC(0-infinity)), peak plasma concentration (C(max)), and time to reach peak plasma concentration (T(max)). A statistically significant difference was observed between the values of the complexes and Artemisinin 250 for the three parameters. However, no statistically significant difference was observed between the values of the beta- and gamma-cyclodextrin complexes. Moreover, the 90% confidence interval for the ratio of the AUC(0-infinity) values of the beta-cyclodextrin complex over those of Artemisinin 250 was estimated to be between 1.51-2.04, while that of C(max) was between 1.73-2.93. For the gamma-cyclodextrin complex, the respective intervals were 1.30-1.76 and 1.43-2.43. These findings indicated that the beta- and gamma-cyclodextrin complexes had a much higher rate and extent of bioavailability compared to Artemisinin 250. In addition, the absorption of artemisinin was observed to be poor and negligible when the preparations started to arrive in the colon. This could be attributed to poor dissolution of artemisinin in the semi-solid faecal matter in the lower part of the gastrointestinal tract.
    Matched MeSH terms: Sesquiterpenes/pharmacokinetics*
  5. Inclusion complexation of artemisinin with alpha-, beta-, and gamma-cyclodextrins
    Wong JW, Yuen KH
    Drug Dev Ind Pharm, 2003 Oct;29(9):1035-44.
    PMID: 14606667
    The present study was conducted to investigate the inclusion complexation of artemisinin (ART) with natural cyclodextrins (CyD), namely alpha-, beta-, and gamma-CyDs with the aim of improving its solubility and dissolution rate. Complex formation in aqueous solution and solid state was studied by solubility analysis, dissolution, and thermal analysis. Solubility diagrams indicated that the complexation of ART and the three CyDs occurred at a molar ratio of 1:1, and showed a remarkable increase in ART solubility. Moreover, the thermodynamic parameters calculated by using the van't Hoff equation revealed that the complexation process was associated with negative enthalpy of formation and occurred spontaneously. The complexation capability of CyDs with ART increased in the order of alpha- < gamma- < beta-CyDs and could be ascribed to the structural compatibility between the molecular size of ART and the diameter of the CyD cavities. Dissolution profiles of the three complexes demonstrated an increased rate and extent of dissolution compared with those of their respective physical mixtures and a commercial preparation. In solid-state analysis, using differential scanning calorimetry, the gamma-CyD was capable of complexing the highest percentage of ART, followed by beta- and alpha-CyDs. The respective estimated percentage of ART complexed by the CyDs were 85%, 40%, and 12%.
    Matched MeSH terms: Sesquiterpenes/metabolism; Sesquiterpenes/chemistry*
  6. Chemical compositions and antibacterial activity of the leaf and stem oils of Piper porphyrophyllum (Lindl.) N.E. Br
    Salleh WM, Ahmad F, Sirat HM, Yen KH
    EXCLI J, 2012;11:399-406.
    PMID: 27418915
    The essential oils obtained by hydrodistillation from the fresh leaf and stem of Piper porphyrophyllum N.E. Br. were analyzed by GC and GC/MS. Thirty four constituents were identified in the leaf oil, while thirty eight constituents were identified in the stems oil. The most abundant components in the leaf oil included bicyclogermacrene (14.7 %), α-copaene (13.2 %) and β-phellandrene (9.5 %) while sabinene (15.5 %), bicyclogermacrene (12.3 %) and α-copaene (8.1 %) were the main constituents in the stem oil. The evaluation of antibacterial activity by using micro-dilution method revealed that both oils were moderately active against all the Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis) and Gram-negative bacteria (Pseudomonas aeruginosa, Pseudomonas putida and Escherichia coli) with minimum inhibitory concentration (MIC) values in the range 125-1000 µg/ml.
    Matched MeSH terms: Sesquiterpenes
  7. Fulltext Zerumbone-loaded nanostructured lipid carriers: preparation, characterization, and antileukemic effect
    Rahman HS, Rasedee A, How CW, Abdul AB, Zeenathul NA, Othman HH, et al.
    Int J Nanomedicine, 2013;8:2769-81.
    PMID: 23946649 DOI: 10.2147/IJN.S45313
    Zerumbone, a natural dietary lipophilic compound with low water solubility (1.296 mg/L at 25°C) was used in this investigation. The zerumbone was loaded into nanostructured lipid carriers using a hot, high-pressure homogenization technique. The physicochemical properties of the zerumbone-loaded nanostructured lipid carriers (ZER-NLC) were determined. The ZER-NLC particles had an average size of 52.68 ± 0.1 nm and a polydispersity index of 0.29 ± 0.004 μm. Transmission electron microscopy showed that the particles were spherical in shape. The zeta potential of the ZER-NLC was -25.03 ± 1.24 mV, entrapment efficiency was 99.03%, and drug loading was 7.92%. In vitro drug release of zerumbone from ZER-NLC was 46.7%, and for a pure zerumbone dispersion was 90.5% over 48 hours, following a zero equation. Using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay in human T-cell acute lymphoblastic leukemia (Jurkat) cells, the half maximal inhibitory concentration (IC50) of ZER-NLC was 5.64 ± 0.38 μg/mL, and for free zerumbone was 5.39 ± 0.43 μg/mL after 72 hours of treatment. This study strongly suggests that ZER-NLC have potential as a sustained-release drug carrier system for the treatment of leukemia.
    Matched MeSH terms: Sesquiterpenes/pharmacokinetics; Sesquiterpenes/pharmacology; Sesquiterpenes/chemistry*
  8. Anti-infective activities of 11 plants species used in traditional medicine in Malaysia
    Nor Azman NS, Hossan MS, Nissapatorn V, Uthaipibull C, Prommana P, Jin KT, et al.
    Exp Parasitol, 2018 Nov;194:67-78.
    PMID: 30268422 DOI: 10.1016/j.exppara.2018.09.020
    Treatment of drug resistant protozoa, bacteria, and viruses requires new drugs with alternative chemotypes. Such compounds could be found from Southeast Asian medicinal plants. The present study examines the cytotoxic, antileishmanial, and antiplasmodial effects of 11 ethnopharmacologically important plant species in Malaysia. Chloroform extracts were tested for their toxicity against MRC-5 cells and Leishmania donovani by MTT, and chloroquine-resistant Plasmodium falciparum K1 strain by Histidine-Rich Protein II ELISA assays. None of the extract tested was cytotoxic to MRC-5 cells. Extracts of Uvaria grandiflora, Chilocarpus costatus, Tabernaemontana peduncularis, and Leuconotis eugenifolius had good activities against L. donovani with IC50 
    Matched MeSH terms: Sesquiterpenes/isolation & purification; Sesquiterpenes/pharmacology; Sesquiterpenes/toxicity; Sesquiterpenes/chemistry
  9. Single dose pharmacokinetics of oral artemether in healthy Malaysian volunteers
    Mordi MN, Mansor SM, Navaratnam V, Wernsdorfer WH
    Br J Clin Pharmacol, 1997 Apr;43(4):363-5.
    PMID: 9146847
    AIMS: To determine the pharmacokinetics of artemether (ARM) and its principal active metabolite, dihydroartemisinin (DHA) in healthy volunteers.

    METHODS: Six healthy male Malaysian subjects were given a single oral dose of 200 mg artemether. Blood samples were collected to 72 h. Plasma concentrations of the two compounds were measured simultaneously by reversed-phase h.p.l.c. with electro-chemical detection in the reductive mode.

    RESULTS: Mean (+/- s.d.) maximum concentrations of ARM, 310 +/- 153 micrograms l-1, were reached 1.88 +/- 0.21 h after drug intake. The mean elimination half-life was 2.00 +/- 0.59 h, and the mean AUC 671 +/- 271 micrograms l-1 h. The mean Cmax of DHA, 273 +/- 64 micrograms l-1 was observed at 1.92 +/- 0.13 h. The mean AUC of DHA was 753 +/- 233 micrograms h l-1'. ARM and DHA were stable at < or = -20 degrees C for at least 4 months in plasma samples.

    CONCLUSIONS: The relatively short half-life of ARM may be one of the factors responsible for the poor radical cure rate of falciparum malaria with regimens employing daily dosing. In view of the rapid loss of DHA in plasma samples held at room temperature (26 degrees C) it is recommended to store them at a temperature of < or = -20 degrees C as early as possible after sample collection.

    Matched MeSH terms: Sesquiterpenes/administration & dosage; Sesquiterpenes/blood*; Sesquiterpenes/pharmacokinetics*
  10. GC-MS fingerprint of Pogostemon cablin in China
    Hu LF, Li SP, Cao H, Liu JJ, Gao JL, Yang FQ, et al.
    J Pharm Biomed Anal, 2006 Sep 18;42(2):200-6.
    PMID: 16242880
    Pogostemon cablin, originating in Malaysia and India, is cultivated in southern China including Guangdong and Hainan Province, which was called GuangHuoXiang to differentiate it from the HuoXiang of the north, the species Agastache rugosa, that it resembles. Essential oil of P. cablin mainly contributes to the pharmacological activities and the therapeutic properties of the essential oils are directly correlated with their qualitative and quantitative composition. For controlling the quality, standard fingerprint of P. cablin collected from different regions was developed by using GC-MS. Nine compounds including beta-patchoulene, caryophyllene, alpha-guaiene, seychellene, beta-guaiene, delta-guaiene, spathulenol, patchouli alcohol and pogostone were identified among 10 main peaks in P. cablin. Hierarchical clustering analysis based on characteristics of 10 investigated peaks in GC profiles showed that 18 samples were divided into three main clusters, patchouliol-type, pogostone-type and an interim-type, which was the one between the two chemotypes. The simulative mean chromatogram for the three types P. cablin was generated using the Computer Aided Similarity Evaluation System. The fingerprint can help to distinguish the substitute or adulterant, and further assess the differences of P. cablin grown in various areas of China.
    Matched MeSH terms: Sesquiterpenes/analysis*
  11. A new sesquiterpenoid from the rhizomes of Homalomena sagittifolia
    Wong KC, Hamid A, Eldeen IM, Asmawi MZ, Baharuddin S, Abdillahi HS, et al.
    Nat Prod Res, 2012;26(9):850-8.
    PMID: 21999629 DOI: 10.1080/14786419.2010.551770
    A new sesquiterpenoid, 1α,4β,7β-eudesmanetriol (1), was isolated together with the known compounds 1β,4β,7β-eudesmanetriol (2) and oplopanone (3) from the rhizomes of Homalomena sagittifolia. The structures of these compounds were determined by extensive spectral analyses. The compounds 1 and 2 inhibited growth of Pseudomonas stutzeri with a MIC value of 117 µM when evaluated for antibacterial activity using the minimum concentration assay. Both these compounds showed remarkable activities against acetylcholinesterase enzyme with IC(50) values ranging between 25 and 26 µM. The isolation of these sesquiterpenoids and their biological activities observed in this study support the reported traditional uses of H. sagittifolia for the treatment of microbial related diseases and central nervous system disorders.
    Matched MeSH terms: Sesquiterpenes/isolation & purification*; Sesquiterpenes/pharmacology
  12. Fulltext A new norsesquiterpenoid from a Bornean soft coral genus Nephthea
    Ishii T, Matsuura H, Zhaoqi Z, Vairappan CS
    Molecules, 2009;14(11):4591-6.
    PMID: 19924087 DOI: 10.3390/molecules14114591
    A new germacrane-type norsesquiterpenoid, 1-acetoxy-germacra-5E,10(14)-diene-4-one (1), as well as three known compounds, were isolated from the organic extracts of a Bornean soft coral Nephthea sp. Their structures were elucidated on the basis of spectroscopic data analysis.
    Matched MeSH terms: Sesquiterpenes/isolation & purification*; Sesquiterpenes/chemistry*
  13. Fulltext Terpenoids from Marine Soft Coral of the Genus Xenia in 1977 to 2019
    Ng SY, Phan CS, Ishii T, Kamada T, Hamada T, Vairappan CS
    Molecules, 2020 Nov 18;25(22).
    PMID: 33217924 DOI: 10.3390/molecules25225386
    Members of the marine soft coral genus Xenia are rich in a diversity of diterpenes. A total of 199 terpenes consisting of 14 sesquiterpenes, 180 diterpenes, and 5 steroids have been reported to date. Xenicane diterpenes were reported to be the most common chemical skeleton biosynthesized by members of this genus. Most of the literature reported the chemical diversity of Xenia collected from the coral reefs in the South China Sea and the coastal waters of Taiwan. Although there was a brief review on the terpenoids of Xenia in 2015, the present review is a comprehensive overview of the structural diversity of secondary metabolites isolated from soft coral genus Xenia and their potent biological activity as reported between 1977 to 2019.
    Matched MeSH terms: Sesquiterpenes
  14. Non-halogenated new sesquiterpenes from Bornean Laurencia snackeyi
    Kamada T, Vairappan CS
    Nat Prod Res, 2017 Feb;31(3):333-340.
    PMID: 27707003
    Two new non-halogenated sesquiterpenes, snakeol (1) and snakediol (2) were isolated together with 9 known sesquiterpenes such as (R,Z)-33-dimethyl-5-methylene-4-(3-methylpenta-24-dien-1-yl)cyclohex-1-ene (3), palisol (4), pacifigorgiol (5), palisadin D (6), palisadin A (7), palisadin B (8), 5-acetoxypalisadin B (9), debromolaurinterol (10) and α-bromocuparane (11) from the red algae Laurencia snackeyi. The structures of two new metabolites were determined from their spectroscopic data (IR, 1D and 2D NMR and MS). Compounds 1, 2, 10 and 11 showed strong antibacterial activity against selected human clinical bacterial pathogens.
    Matched MeSH terms: Sesquiterpenes/isolation & purification; Sesquiterpenes/chemistry*
  15. New anti-bacterial halogenated tricyclic sesquiterpenes from Bornean Laurencia majuscula (Harvey) Lucas
    Kamada T, Phan CS, Vairappan CS
    Nat Prod Res, 2019 Feb;33(4):464-471.
    PMID: 29092618 DOI: 10.1080/14786419.2017.1396593
    Three new halogenated tricyclic sesquiterpenes, omphalaurediol (1), rhodolaurenones B (2) and C (3) were isolated together with nine known haloganated sesquiterpenes such as rhodolaurenone A (4), rhodolaureol (5), isorhodolaureol (6), (-)-laurencenone D (7), elatol (8), (+)-deschloroelatol (9), cartilagineol (10), (+)-laurencenone B (11) and 2-chloro-3-hydroxy-α-chamigren-9-one (12) from a population of Bornean red algae Laurencia majuscula. The structures of three new metabolites were determined based on their spectroscopic data (IR, 1D and 2D NMR, and MS). These compounds showed antibacterial activity against three human pathogenic bacteria (Escherichia coli, Salmonella typhi and Vibrio cholera).
    Matched MeSH terms: Sesquiterpenes/isolation & purification; Sesquiterpenes/pharmacology*; Sesquiterpenes/chemistry*
  16. Nangallenes A and B, halogenated nonterpenoid C15-acetogenins from the Bornean red alga Laurencia nangii
    Kamada T, Phan CS, Vairappan CS
    J Asian Nat Prod Res, 2019 Mar;21(3):241-247.
    PMID: 29281900 DOI: 10.1080/10286020.2017.1417265
    Two new halogenated nonterpenoids C15-acetogenins, nangallenes A-B (1-2), together with two known halogenated compounds itomanallene A (3) and 2,10-dibromo-3-chloro-α-chamigrene (4), were isolated and identified from the organic extract of the marine red alga Laurencia nangii Masuda collected from the coastal waters in Semporna, Borneo. Their structures were established by means of spectroscopic analysis including IR, high-resolution electrospray ionization mass spectrometry (HRESI-MS), and 1D and 2D NMR techniques. All these metabolites were submitted for the antifungal assay against four species of selected marine fungi. Compounds 1-4 showed potent activity against Haliphthoros sabahensis and Lagenidium thermophilum.
    Matched MeSH terms: Sesquiterpenes/isolation & purification; Sesquiterpenes/chemistry
  17. Capgermacrenes D-G, new sesquiterpenoids from a Bornean soft coral, Capnella imbricata
    Phan CS, Vairappan CS
    Nat Prod Res, 2017 Apr;31(7):742-748.
    PMID: 27750446 DOI: 10.1080/14786419.2016.1241997
    Four new bicyclogermacrenes, capgermacrenes D (1) E (2) F (3) and G (4) were isolated from a population of Bornean soft coral Capnella imbricata. The structures of these metabolites were elucidated based on their nuclear magnetic resonance and high-resolution electrospray ionisation mass spectrometry spectral data. These compounds showed bacteriastatic and bacteriacidal activities against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus.
    Matched MeSH terms: Sesquiterpenes/isolation & purification*; Sesquiterpenes/pharmacology*; Sesquiterpenes/chemistry
  18. Fulltext Antisecretory, gastroprotective, antioxidant and anti-Helicobcter pylori activity of zerumbone from Zingiber zerumbet (L.) Smith
    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: Sesquiterpenes/administration & dosage*; Sesquiterpenes/pharmacology
  19. Fulltext Saccharomyces cerevisiae: a potential stereospecific reduction tool for biotransformation of mono- and sesquiterpenoids
    Khor GK, Uzir MH
    Yeast, 2011 Feb;28(2):93-107.
    PMID: 20939023 DOI: 10.1002/yea.1827
    Terpenes and terpenoids are among the key impact substances in the food and fragrance industries. Equipped with pharmacological properties and applications as ideal precursors for the biotechnological production of natural aroma chemicals, interests in these compounds have been escalating. Hence, the syntheses of new derivatives that can show improved properties are often called for. Stereoselective biotransformation offers several benefits to increase the rate of production, in terms of both the percentage yield and its enantiomeric excesses. Baker's yeast (Saccharomyces cerevisiae) is broadly used as a whole cell stereospecific reduction biocatalyst, due to its capability in reducing carbonyls and carbon-carbon double bonds, which also extends its functionality as a versatile biocatalyst in terpenoid biotransformation. This review provides some insights on the development and prospects in the reductive biotransformation of monoterpenoids and sesquiterpenoids using S. cerevisiae, with an overview of strategies to overcome the common challenges in large-scale implementation.
    Matched MeSH terms: Sesquiterpenes/metabolism*
  20. Therapeutic equivalence of a low dose artemisinin formulation in falciparum malaria patients
    Wong JW, Yuen KH, Nagappan S, Shahul WS, Ho SS, Gan EK, et al.
    J Pharm Pharmacol, 2003 Feb;55(2):193-8.
    PMID: 12631411
    We have evaluated the therapeutic equivalence of a beta-cyclodextrin-artemisinin complex at an artemisinin dose of 150 mg, with a commercial reference preparation, Artemisinin 250 at a recommended dose of 250 mg. One hundred uncomplicated falciparum malarial patients were randomly assigned to orally receive either beta-cyclodextrin-artemisinin complex (containing 150 mg artemisinin) twice daily for five days or the active comparator (containing 250 mg artemisinin) twice daily for five days. The patients were hospitalized for seven days and were required to attend follow up assessments on days 14, 21, 28 and 35. All patients in both treatment groups were cured of the infection and achieved therapeutic success. At day seven of treatment, all patient blood was clear of the parasites and the sublingual temperature of all patients was less than 37.5 degrees C. Moreover, the parasite clearance time in both treatment groups was similar, being approximately three days after initiation of treatment. Comparable plasma artemisinin concentrations were observed between patients in both treatment groups at 1.5 and 3.0 h, although slightly higher levels were obtained with patients in the beta-cyclodextrin-artemisinin complex-treated group. The beta-cyclodextrin-artemisinin complex at a dose of 150 mg artemisinin was therapeutically equivalent to 250 mg Artemisinin 250. Additionally, patients receiving beta-cyclodextrin-artemisinin complex showed less variability in their plasma artemisinin concentrations at 1.5 h post-dosing, which suggested a more consistent rate of drug absorption.
    Matched MeSH terms: Sesquiterpenes/blood; Sesquiterpenes/pharmacokinetics; Sesquiterpenes/therapeutic use*
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