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  1. See I, Ee GCL, Jong VYM, Teh SS, Acuña CLC, Mah SH
    Nat Prod Res, 2020 Oct 23.
    PMID: 33094642 DOI: 10.1080/14786419.2020.1836629
    Four xanthones, α-mangostin (1), β-mangostin (2), mangostenol (3), mangaxanthone B (4), three benzophenones, mangaphenone (5), benthamianone (6), congestiflorone (7) and one sterol, stigmasterol (8) were isolated from the stem barks of Garcinia mangostana L. and G. benthamiana (Planch. & Triana) Pipoly. Compounds 1, 2, 4 and 5 exhibited significant cytotoxicity through MTT assay towards MCF-7 and MDA-MB-231 cells with the IC50 values range from 4.4 to 12.0 µM. Remarkably, mangaphenone (5) showed non-cytotoxicity against normal Vero cells, revealing its potential as lead compound for anti-breast cancer drug. Structure-activity relationship postulated that the prenyl and hydroxyl groups present in xanthones are important in promoting anti-proliferative effects. Molecular docking simulation study of 1, 2, 4 and 5 with 2OCF and 4PIV implied that the induction of apoptosis for both cancer cells involve ER and FAS signaling pathways. Future study on the lead optimization of 5 is highly recommended.
  2. Idrus SNW, Salleh WMNHW, Salihu AS, Arzmi MH, Cespedes-Acuña CL
    PMID: 40082080 DOI: 10.1515/znc-2024-0227
    This study aimed to investigate the chemical composition, and anticholinesterase and anti-tyrosinase activities of the essential oil extracted from the leaves of Piper frustratum Boerl., growing in Malaysia. Nineteen chemical components were identified using gas chromatography-flame ionization detection (GC-FID) and gas chromatography-mass spectrometry (GC-MS), accounting for 99.6 % of the essential oil. The identified major components include β-caryophyllene (12.6 %), β-asarone (10.7 %), myristicin (10.4 %), α-copaene (9.6 %), methyl eugenol (7.2 %), and β-cubebene (6.5 %). Anticholinesterase activity was assessed using the Ellman's method, while anti-tyrosinase activity was evaluated against mushroom tyrosinase. The essential oil demonstrated moderate inhibitory activity against acetylcholinesterase (IC50 value of 84.2 μg/mL), butyrylcholinesterase (IC50 value of 98.5 μg/mL), and tyrosinase (IC50 value of 95.4 μg/mL) enzymes. This study is the first to report the chemical composition and bioactivities of the essential oil obtained from P. frustratum, which may have implications on the characterization, pharmaceutical, and therapeutic applications of Piper essential oils.
  3. Kirubakaran R, Stocker SL, Carlos L, Day RO, Carland JE
    Ther Drug Monit, 2021 Dec 01;43(6):736-746.
    PMID: 34126624 DOI: 10.1097/FTD.0000000000000909
    BACKGROUND: Therapeutic drug monitoring is recommended to guide tacrolimus dosing because of its narrow therapeutic window and considerable pharmacokinetic variability. This study assessed tacrolimus dosing and monitoring practices in heart transplant recipients and evaluated the predictive performance of a Bayesian forecasting software using a renal transplant-derived tacrolimus model to predict tacrolimus concentrations.

    METHODS: A retrospective audit of heart transplant recipients (n = 87) treated with tacrolimus was performed. Relevant data were collected from the time of transplant to discharge. The concordance of tacrolimus dosing and monitoring according to hospital guidelines was assessed. The observed and software-predicted tacrolimus concentrations (n = 931) were compared for the first 3 weeks of oral immediate-release tacrolimus (Prograf) therapy, and the predictive performance (bias and imprecision) of the software was evaluated.

    RESULTS: The majority (96%) of initial oral tacrolimus doses were guideline concordant. Most initial intravenous doses (93%) were lower than the guideline recommendations. Overall, 36% of initial tacrolimus doses were administered to transplant recipients with an estimated glomerular filtration rate of <60 mL/min/1.73 m despite recommendations to delay the commencement of therapy. Of the tacrolimus concentrations collected during oral therapy (n = 1498), 25% were trough concentrations obtained at steady-state. The software displayed acceptable predictions of tacrolimus concentration from day 12 (bias: -6%; 95%confidence interval, -11.8 to 2.5; imprecision: 16%; 95% confidence interval, 8.7-24.3) of therapy.

    CONCLUSIONS: Tacrolimus dosing and monitoring were discordant with the guidelines. The Bayesian forecasting software was suitable for guiding tacrolimus dosing after 11 days of therapy in heart transplant recipients. Understanding the factors contributing to the variability in tacrolimus pharmacokinetics immediately after transplant may help improve software predictions.

  4. Suwanwela NC, Chen CLH, Lee CF, Young SH, Tay SS, Umapathi T, et al.
    Cerebrovasc Dis, 2018;46(1-2):82-88.
    PMID: 30184553 DOI: 10.1159/000492625
    BACKGROUND AND PURPOSE: MLC601 has been shown in preclinical studies to enhance neurorestorative mechanisms after stroke. The aim of this post hoc analysis was to assess whether combining MLC601 and rehabilitation has an effect on improving functional outcomes after stroke.

    METHODS: Data from the CHInese Medicine NeuroAiD Efficacy on Stroke (CHIMES) and CHIMES-Extension (CHIMES-E) studies were analyzed. CHIMES-E was a 24-month follow-up study of subjects included in CHIMES, a multi-centre, double-blind placebo-controlled trial which randomized subjects with acute ischemic stroke, to either MLC601 or placebo for 3 months in addition to standard stroke treatment and rehabilitation. Subjects were stratified according to whether they received or did not receive persistent rehabilitation up to month (M)3 (non- randomized allocation) and by treatment group. The modified Rankin Scale (mRS) and Barthel Index were assessed at month (M) 3, M6, M12, M18, and M24.

    RESULTS: Of 880 subjects in CHIMES-E, data on rehabilitation at M3 were available in 807 (91.7%, mean age 61.8 ± 11.3 years, 36% female). After adjusting for prognostic factors of poor outcome (age, sex, pre-stroke mRS, baseline National Institute of Health Stroke Scale, and stroke onset-to-study-treatment time), subjects who received persistent rehabilitation showed consistently higher treatment effect in favor of MLC601 for all time points on mRS 0-1 dichotomy analysis (ORs 1.85 at M3, 2.18 at M6, 2.42 at M12, 1.94 at M18, 1.87 at M24), mRS ordinal analysis (ORs 1.37 at M3, 1.40 at M6, 1.53 at M12, 1.50 at M18, 1.38 at M24), and BI ≥95 dichotomy analysis (ORs 1.39 at M3, 1.95 at M6, 1.56 at M12, 1.56 at M18, 1.46 at M24) compared to those who did not receive persistent rehabilitation.

    CONCLUSIONS: More subjects on MLC601 improved to functional independence compared to placebo among subjects receiving persistent rehabilitation up to M3. The larger treatment effect of MLC601 was sustained over 2 years which supports the hypothesis that MLC601 combined with rehabilitation might have beneficial and sustained effects on neuro-repair processes after stroke. There is a need for more data on the effect of combining rehabilitation programs with stroke recovery treatments.

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