Inclusion of biopiperine in the kappa-carrageenan complex might improve its bioaccessibility and in vivo anti-inflammatory activity in edema-induced Wistar rats

Piper nigrum has been used in Indonesian traditional medicine to alleviate pain. Piperine, a nitrogenous substanceisolated from the plant, has been reported for its anti-inflammatory activity. However, this compound is slightlysoluble in water, which impacts its bioaccessibility. A recent study reported that a co-ground mixture of piperine andβ-cyclodextrin revealed a significant increase of dissolved piperine at 15 minutes of dissolution test compared to thatof pure piperine. This work was aimed to study the bioaccessibility of the carrageenan-complexed piperine in Wistarrats and assayed its anti-inflammatory activity on the edema-induced paw of the rats. Both isolated (from P. nigrum)and synthetic (TCI, Tokyo Chemical Industry) piperines were used as the standards for the bioaccessibility assay,whereas acetosal was the standard drug for the anti-inflammatory activity study. The carrageenan-complexed piperinerevealed a better bioaccessibility (Cmax = 0.34 µg/ml; Tmax at 30 minutes) than that of the isolated piperine (Cmax = 0.12µg/ml, Tmax at 60 minutes), whereas the synthetic piperine showed the best absorption (Cmax = 0.48 µg/ml, Tmax at 30minutes). The anti-inflammatory activity of carrageenan-complexed piperine at a dose of 393 mg/kg body weight(BW) (contains 100 mg of piperine) equals to the acetosal dose of 45 mg/kg BW. Thus, the inclusion of biopiperinein the carrageenan complex might improve its bioaccessibility and in vivo anti-inflammatory activity in Wistar rats.

Quality of life of patients receiving a single or combination of calcium channel blocker-angiotensin receptor blocker: A cross-sectional study in West Java, Indonesia

The prevalence of hypertension, based on the Indonesian Basic Health Research 2018, was 34.1%. Hypertensivepatients usually show a low quality of life (QoL) due to their lifelong drug dependence. This cross-sectional study wasconducted to determine the QoL of adult hypertensive patients treated with a single calcium channel blocker (CCB)and combination of CCB and angiotensin receptor blocker (ARB) at a primary referral hospital in West Java duringDecember 2018–February 2019. The QoL of the patients was determined using the Indonesian validated Euroqol 5dimensions 5 level and Euroqol visual analog scale questionnaires. 83 adult hypertensive outpatients were recruitedand agreed to participate in this study. Of the 83 hypertensive patients, 44.6% were being treated with a single CCBand 55.4% were being given the combination of CCB and ARB. The characteristics of the patients were as follows:the age was 51 ± 1.04 years, 71.3% were female, 84.3% were married, 66.2% never undertook physical activity, dailydrugs consumed 4 ± 0.19 items, and the duration of hypertensive therapy was 20 ± 3.3 months. Most of the patientsindicated problems in the area of pain and anxiety. The hypertensive patients treated with a combination of nifedipineand candesartan indicated the best QoL, whereas the lowest QoL was found in patients treated with a combination ofnifedipine and valsartan.

Insights of phytoconstituents and pharmacology activities of Salacca plants

In the last 20 years, plant-based therapy had become the world's attention. Our country Indonesia is popular in itsmegabiodiversity, among which is Salacca zalacca Gaert. (Voss.), or salak. The fruit of this plant is generally utilizedas pickles, chips, etc. However, its benefits for health remain unexplored. Library searches using PubMed, GoogleScholar, Science Direct, and Google resulted that S. zalacca, which contains flavonoids, alkaloids, terpenoids, andsitosterols exerts various pharmacology activities, e.g., antioxidant, cholesterol reducer, antidiabetic, skin whitening,antihyperuricemia, antibacterial, immune system enhancer, cancer cell growth inhibitor, and adsorbent.

Determination of ligand position in aspartic proteases by correlating tanimoto coefficient and binding affinity with root mean square deviation.

The objective of this study was to develop and validate of Structure-Based Virtual Screening (SBVS) protocol which was used to select the best pose of inhibitor-aspartic protease complex interaction in the active sites of HIV-1 protease, plasmepsin I, II, and IV. Retrospective validation was performed on enhanced dataset of ligands and decoys (DUD-E) for HIV-1 protease. The crystal structures 1XL2, 3QS1, 1SME, and 1LS5 were obtained from Protein Data Bank. The protocol was then challenged to re-dock the ligands to its origin places in the active sites by correlating Tanimoto coefficient (Tc) and binding affinity (Ei) with Root Mean Square Deviation (RMSD). Enrichment factor at 1% false positives (EF1%) values for Tc and Ei were 18.26 and 9.03, respectively, while the Area Under Curve (AUC) values for Tc and Ei were 76.84 and 60.95. The SBVS protocol was valid and showed better virtual screening qualities in ligand identification for HIV-1 protease compared to the original protocol accompanying the release of DUD-E and showed its ability to reproduce the co-crystal pose in the HIV-1 protease, plasmepsin I, II, and IV to its origin places in the active sites.

Virtual screening of co-formers for ketoprofen co-crystallization and the molecular properties of the co-crystal.

Ketoprofen or [2-(3-benzoylphenyl)propionic acid] is a nonsteroidal antiinflammatory and analgesic agent. The positive qualities of ketoprofen are based on optimal physicochemical and structural characteristics, its ability to penetrate into and accumulate in the inflammation centers and compatibility with other classes of drugs. This compound is practically insoluble in water, therefore as most of NSAID drugs, it is categorized as Biopharmaceutics Classification System (BCS) class II. A widely used to enhance the solubility of poorly water soluble drugs is co-crystallization. A co-crystal is a multi-component crystal which involves non-covalent interactions between API and its co-formers. In this work, we developed virtual screening of co-formers for ketoprofen by employing molecular docking method. AutoDock was used for docking. Parameters observed were type and energy (Ei) of interaction. The work was continued by co-crystallization process and solubility assay of the mixtures according to Higuchi and Connor method using UV spectrophotometer. Based on molecular docking, the best co-former is saccharin (Ei = -3.14 kcal/mol). The docking result fits the solubility assay of the ketoprofen-saccharin co-crystal (300.62 μg/mL in water or 256.54% increasing of solubility compared to ketoprofen). Ketoprofen co-crystal shows better curve (90.15 % in 60 minutes) than ketoprofen (78.87 % in 60 minutes). Co-crystallization of ketoprofen with saccharin increases the dissolution profile of ketoprofen.