Journal of Applied Pharmaceutical Science (JAPS)
Permanent URI for this collection
Editor: Dr. Khalid Akhter Ansari
ISSN: 2231-3354; (Print)
Frequency: 12 issues a year
Language: Englishh
An Official Publication of Open Science Publishers
Open Access Peer-reviewed journal
Web site: https://www.japsonline.com/
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Recent Submissions
Item Role of N-acetyl cysteine on bone marrow-derived hematopoietic stem/progenitor cell cryopreservation: Outcome on the oxidative stress-mediated cryodamage and repopulation Capacity into hematopoietic lineages(Open Science Publishers LLP, 2020-06) Zariyantey, Abdul Hamid; Preshetha, Sellappah; Bharatham, Hemabarathy; Mathialagan, Ramya Dewi; Kannan, Vayithiswary DewiCryopreservation of hematopoietic stem/progenitor cells (HSPCs) is associated with oxidative stress-mediatedcryodamage, hence compromising the therapeutic potency. The roles of N-acetyl cysteine (NAC) on the oxidativestress-mediated cryodamage and repopulation capacity of HSPCs into myeloid, erythroid, and pre-B lymphoidprogenitors were investigated. Mice bone marrow-derived HSPCs were cultured for 24 hours, followed bycryopreservation at 1 × 106/ml cells in cryomedium containing 10% dimethyl sulfoxide with NAC (0.25, 0.5, or 2.0µM) or without for 48 hours, 2 weeks, and 4 weeks at −80°C. Cryopreservation significantly reduced cell viability atpost-thawed (p < 0.05) with long-term cryopreservation conferred a greater cell recovery. NAC improved the bonemarrow-derived HSPC viability (p < 0.05) at 0.5 and 2.0 µM after 48 hours of cryopreservation. Cryopreservationlowered the malondialdehyde level (p < 0.05) although glutathione, superoxide dismutase, and protein carbonyl levelswere not significantly affected. Repopulation capacity of HSPCs into myeloid–erythroid progenitors was greatlyreduced (p < 0.05) after 4 weeks of cryopreservation as compared to precryopreservation group. Meanwhile, NACsupplementation showed no remarkable effect on oxidative stress-mediated cryodamage and repopulation capacity ofHSPCs. Conclusively, the cryoprotective role of NAC on the cryopreservation of HSPCs deserves further investigationItem Antioxidant and hepatoprotective activity of Flemingia tuberosa Dalzell in CCl4-induced hepatotoxicity in rats(Open Science Publishers LLP, 2020-06) Mascarenhas, Reena William; Shailajan, Sunita; Menon, SasikumarFlemingia tuberosa Dalzell is an endemic species of the Western Ghats. It is an ethnomedicinal plant used to curedysentery and vaginal discharge. However, in this study, the hepatoprotective potency of the plant has been evaluatedas it contains flavonoids like kaempferol. The present study was conducted to investigate the hepatoprotective activityof the ethanolic extract of aerial parts of F. tuberosa against Carbon tetrachloride (CCl4)-induced toxicity in rats.The extract was standardized using a validated HPTLC method for kaempferol content. The antioxidant activityof the ethanolic extract of aerial parts of F. tuberosa was assessed by 1,1-diphenyl-2-picrylhydrazyl method. Thehepatoprotective activity was assessed against CCl4-induced liver intoxication, wherein the CCl4-induced albino Wistarrats were treated with three different doses of the standardized extract for 3 days. The results were compared with theestablished positive control, Silymarin. The protective effect on the liver was also monitored histopathologically usinglight and electron microscope and biochemically through observing the levels of biochemical enzymes. The extractshowed potent hepatoprotective activity. This study confirms the protective effect of the ethanolic extract of aerialparts of F. tuberosa against CCl4-induced hepatotoxicityItem Cytotoxicity activity of geldanamycin derivatives against various cancer cell lines(Open Science Publishers LLP, 2020-06) Taechowisan, Thongchai; Tipparat, Samsawat; Winyou, Puckdee; Waya, S. PhutdhawongGeldanamycin (1) was isolated as a major compound from Streptomyces zerumbet W14. It was then used as a precursor tosynthesize two new geldanamycins: 17-(tryptamine)-17-demethoxygeldanamycin (2) and 17-(5′-methoxytryptamine)-17-demethoxygeldanamycin (3). The cytotoxicity activity of these two new compounds was evaluated and comparedwith the cytotoxicity of compound 1. Cytotoxicity activity was evaluated against a normal cell line, and three cancercell lines using an 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) colorimetric assay. Thesolubility of these compounds was also determined. The solubility of compounds 2 and 3 in water was 290.69and 348.18 µM, higher than that of compound 1 by about 1.91 and 2.29 times, respectively. Compounds 2 and 3showed moderate cytotoxic activity on Vero and human cervical carcinoma cells with IC50 values of >200.00 µg/ml. The strongest cytotoxicity of compound 3 was observed in human breast carcinoma cells (MCF-7) and humanhepatocellular carcinoma cell line (HepG2) cells with IC50 values of 82.50 and 114.35 µg/ml, respectively, while theIC50 values of compound 2 against MCF-7 and HepG2 cells were 105.62 and 124.57 µg/ml, respectively. The findingsshowed that these new geldanamycin derivatives exhibited selective cytotoxicity toward some cancer cells at a lowerconcentration. Therefore, future studies on these compounds could be useful for the management of some cancersItem Ultrasound-assisted extraction for enhanced retention of physicochemical properties of garlic powder obtained by spray-drying(Open Science Publishers LLP, 2020-05) P., Poojitha; Gimbun, Jolius; Yeop, Afiqah; Athmaselvi, K. A.This work aims to produce garlic powder with the retention of physicochemical properties by using different methods.Garlic is extracted by an ultrasonic-assisted extraction technique to remove the undesired compounds. In this study,garlic powder is incurred through freeze-drying and spray-drying with maltodextrin as a carrier agent. To compare theefficiency of two drying techniques, garlic is dried without maltodextrin. This study is intended to find a techniqueto get garlic powder with the best quality. The physicochemical and microstructural properties of the garlic powderobtained were analyzed and compared. It was found that garlic powder spray-dried with maltodextrin has the highestretention of physicochemical properties compared to those treated with other techniques. Although freeze-driedand spray-dried powder developed without carrier agent could maintain the flavor and color, they failed to hold thestructure and formed into clusters soon after they are exposed to air. Thus, the obtained results showed spray-dryingwith maltodextrin as the best drying technology for the maintenance of its physical and chemical properties.Item Synthesis and biological evaluation of novel substituted pyrrolo[2,3-d]pyrimidines as anticancer agents(Open Science Publishers LLP, 2020-06) Dholakia, Sandip P.; Kanada, Kaushik B.; Parmar, Ghanshyam R.Pyrrolopyrimidines are well known scaffold, which play a critical role as anticancer agents, so it thought of interest tosynthesize a series of novel substituted pyrrolo[2,3-d]pyrimidines having diverse groups at position C4 and N7 of thepyrrolo[2,3-d]pyrimidine core and performed in vitro screening against MDA-MB-468 (breast cancer cell line) cellline. The details of the synthetic methods and characterization data of the synthesized compounds have been presentedin this study. Compounds 8a, 8h, 8j, 9h, 9i, 9j, 9m, 9n, and 9o showed the excellent anticancer activity compared tostandard doxorubicin with an IC50 value of 6.17 µM/ml against MDA-MB-468 (breast cancer cell line), which wasnon-toxic to normal vero cell line.Item Novel aminoalkylated chalcone: Synthesis, biological evaluation, and docking simulation as potent antimalarial agents(Open Science Publishers LLP, 2020-06) Syahri, Jufrizal; Nasution, Hasmalina; Nurohmah, Beta Achromi; Purwono, Bambang; Yuanita, EmmyThree chalcone derivatives with amine groups (4a–c) were synthesized and evaluated for their antimalarial activity.Three aminoalkylated chalcone derivatives (4a–c) have been prepared through Claisen–Schmidt condensation reactionfrom vanillin and chloroacetophenone, followed by the Mannich reaction to add amine group. The structure of thecompounds was confirmed by the spectrophotometric analysis using mass spectrometers (MS) and proton and carbonnuclear magnetic resonance (1H- and 13C-NMR) spectroscopy. Antimalarial activity of 4a–c was evaluated againstPlasmodium falciparum (3D7) strain, and the molecular docking of 4b was performed to understand the interactionagainst Pf DHFR-TS protein (1J3I.pdb). The prepared aminoalkylated chalcone (4a–c) was obtained in a yield of 80%,75%, and 70%. The addition of morpholine (4a), piperidine (4b), and diethylamine (4c) as amine groups significantlycould improve the antimalarial activity with IC50 of 0.62, 0.54, and 1.12 µM, respectively (strong activity), comparedwith the chalcone without amine group (3) with IC50 of 25.84 µM (moderate activity). The molecular docking ofcompound 4b exhibited strong hydrogen bond interaction with ILE112, ILE64, SER111, SER108, ASP54, TYR170,and PRO113 residues with CDOCKER interaction energy of −48.84 kcal/mol. Thus, aminoalkylated chalcone couldbe proposed for further studies and developed into antimalarial drug candidatesItem In silico and in vitro cytotoxicity profile of hydroalcoholic extract/ fraction(s) of Pachygone ovata(Open Science Publishers LLP, 2020-05) Rodrigues, Jeswiny; Hullatti, Kiran Kumar; Khanal, PukarMedicinal plants have been used in the past for the treatment of diseases and continue to be an important reservoirfor the development of new drugs. With the increasing burden of cancer globally, there is a need to find neweranticancer agents. The process of identification and evaluation of cytotoxic molecules from plants can be achievedconveniently by using simple yet reliable screening models and combining with in silico techniques. Pachygone ovata,least explored plant from Menispermaceae family, is known to be rich in alkaloids. This study aimed to identify thecytotoxic constituents from Pachygone ovata through bioactivity-guided fractionation using Brine shrimp lethalitybioassay as a screening model. The active fraction in this assay was evaluated for its in vitro cytotoxic activity onhuman tumor cell lines. Some reported alkaloids were studied for their binding affinities with topoisomerase II bymolecular docking. The study revealed the cytotoxic constituents from P. ovata. The study also revealed alkaloids withhigher binding affinity with topoisomerase II, and the scope for further use leads to the development of new drugs.Item Marine sponge compounds with antiplasmodial properties: Focus on in vitro study against Plasmodium falciparum(Open Science Publishers LLP, 2020-05) Hikmawan, Baso Didik; Subagus, Wahyuono; Erna, Prawita SetyowatiMalaria continues to be a major cause of morbidity and mortality in many tropical countries. The lack of progressin drug discovery and the spread of drug resistance become the reason behind this. Porifera (sponges) is a potentialsource of novel bioactive compounds to provide future drugs against malaria. In this review, we summarized 243isolated molecules belonging to 35 different genera that active against Plasmodium falciparum from published paperuntil March 2019. The molecules were classified into potent, good, moderate, low, and inactive based on their IC50, andamong observed bioactive metabolites, there were 57 marine sponge molecules reported to act as potent antiplasmodiumagainst various strains of P. falciparum including drug resistance and nondrug resistance. Table 2 represents the listof isolated compounds with “potent” antimalarial activity. The class of the listed compounds includes manzaminealkaloid, guanidine alkaloids, bispyrroloiminoquinone alkaloids, pyrroloiminoquinone alkaloids, ingamine alkaloids,bromotyrosine alkaloids, sesquiterpenoids, diterpene formamides, aminoimidazole, β-galactosylceramides, β-lactam,meroterpene, trisoxazole macrolides, peroxides, thiazine alkaloids, and sterols. With this up-to-date review, we attemptto present new perspectives for the rational discovery of novel sponge metabolites that can be used as lead compoundsin antimalarial drug development.Item Effectiveness of educational interventions on knowledge and counseling regarding common cold management: The case of community pharmacists in Hue, Vietnam(Open Science Publishers LLP, 2020-05) Thi, Quynh Le; Thi, Minh Nguyet Le; Thi, Hong Phuong Vo; Viet, Thanh Truong; Thi, Hong Diep Phan; Quang, Trung Tran; Chuyen, Le; Ba, Hoang Anh Mai; Tran, Thao Nguyen Nguyen; The, Thanh Nguyen; Erwin, Martinez Faller; Thi, Ha VoObjective: The aim of the study was to assess the effectiveness of educational interventions on the knowledge andcounseling practice of community pharmacists in Hue, Vietnam with respect to common cold management.Method: Thirty-eight pharmacists were invited to participate in educational initiatives, including in-class training andreference to a printed pocket handbook. The knowledge was measured before and after the interventions via a paperbased test, and actual practice was evaluated via a pseudo customer experiment a week later.Results: The interventions significantly improved pharmacists’ knowledge (p = 0.001). In the pre-test, only 37.4%of the participants provided correct answers, but this increased to 83.9% in the post-test. In the pseudo customerexperiment, pharmacists asked about patient identification, age, and symptoms (93.3%, 80.0%, and 80.0%,respectively) but not about medical and medication histories or allergies (less than 20%). All pharmacists offeredadvice as regards dosage, but only half of them shared information on drug names and indications. A third providedguidance on drug interactions. Practices related to inappropriate drug dispensing included the issuance of incorrectmedications or the sale of prescription-only drugs to customers with no prescriptions.Conclusion: Although educational interventions effectively enhance the knowledge and counseling practice ofpharmacists, a huge gap continues to exist between these variables.Item Dentists knowledge about over the counter-NSAIDs: An emerging need for NSAID-avoidance education(Open Science Publishers LLP, 2020-01) Hoxha, Malvina; Malaj, Visar; Spahiu, Erila; Spahiu, MishelObjectives of the study: Non-steroidal anti-inflammatory drugs (NSAIDs) belong to a group of drugs used in themanagement of pain. The aim of this study is to assess dentists’ knowledge of NSAIDs risks and to determine the mostprescribed NSAIDs by dentists.Materials and Methods: We collected information concerning the dentists’ knowledge of NSAIDs use and adverseeffects. A questionnaire consisting of 22 questions was distributed to 123 Albanian dentists reached in different dentalclinics, out of which only 87 agreed to participate. Only 70.73% of the distributed questionnaires were completed.Results: Respondents demonstrated poor knowledge of NSAIDs. Most of the respondents did not respond correctlyto the questions with 39.08% of incorrect answers regarding the implications of NSAIDs in elderly patients and only3.44% responded correctly to the contraindication of NSAIDs. The most common prescriptions were ketoprofen,ibuprofen, followed by ketorolac, aspirin, and diclofenac.Conclusions: Dentists who participated in the survey have limited knowledge of NSAIDs use, contraindication, andsafety limitation which can affect patients’ safety and well-being. Dentists should pay particular attention to informingpatients on NSAIDs use and should also keep updated on NSAIDs, through continuing education programs.Item Comparative evaluation of the antioxidant capacity of ferulic acid and synthesized propionyl ferulate(Open Science Publishers LLP, 2020-05) Adeyemi, Oluyomi Stephen; Ayonote, Divine Ayebakuro; Oluwakemi, Josephine Awakan; Olubunmi, Atolani; Opeyemi, Adejumo; Adewole, Ibrahim; Damilare, Rotimi; Gaber, El-Saber Batiha; John, Olusegun OjediranFerulic acid (FA) is a polyphenolic compound with demonstrated antioxidant capacity. In this study, propionylferulate (PF) was synthesized and characterized using melting point, ultraviolet spectroscopy, Fourier-transforminfrared spectroscopy, and mass spectrometry. The propionyl ferulate was comparatively evaluated for antioxidantpotential which included the ability to quench reactive species of 2,2-diphenyl-2-picrazyl-hydrazyl (DPPH), hydroxyl,nitric oxide, and superoxide anion. In addition, the total antioxidant capacity and membrane stabilizing properties ofthe ferulate were determined. Comparatively, the spectroscopically characterized PF showed superior scavengingcapacity for the DPPH, hydroxyl, and nitric oxide free radicals when compared to FA. On the contrary, PF showed apoor scavenging capacity for superoxide anion radicals. Furthermore, PF showed little or no potential for membranestability. In conclusion, the data suggest that structurally modifying FA to PF improved the antioxidant capacity forseveral free radicals.Item Assessment of the anti-diabetic effect of Bauhinia variegata gold nano-extract against streptozotocin induced diabetes mellitus in rats(Open Science Publishers LLP, 2020-05) Abdel-Halim, Abeer Hamed; Fyiad, Amal Abdel Azeem; Aboulthana, Wael Mahmoud; El-Sammad, Nermin Mohammed; Youssef, Ahmed Mahmoud; Ali, Mamdouh MoawadDiabetes mellitus (DM) is the most common type of the metabolic endocrine disorders. It is categorized as the thirdcause of death after heart and cancer diseases. Due to the undesirable side effects of the synthetic anti-diabetic drugs,the medicinal plants were selected for DM treatment. The recent studies directed to use nanotechnology in medicine toovercome restrictions of the drugs that were represented by weak bioavailability, insolubility in water, low absorptionby the intestine, and inability to reach to the appropriate site of action. The study aimed to investigate the antioxidant,antidiabetic, and hypolipidemic effect of Bauhinia variegata (B. variegata) extract before and after incorporating goldnanoparticles (Au-NPs) against DM induced by streptozotocin (STZ) in rats. The present study conducted on 36 malealbino Western rats divided into six groups {control, B. variegata extract treated group, B. variegata gold nano-extracttreated group, diabetic group [injected by STZ intrapretinoally (i.p.) at a dose of 60 mg/kg], diabetic rats treatedwith B. variegata extract, and B. variegata gold nano-extract groups}. The DM related biochemical functions (liverand kidney functions, glucose, insulin, and lipid profile) were assayed. Moreover, the enzymatic and non-enzymaticantioxidants were assayed in addition to lipid peroxidation products in liver and pancreas. Furthermore, the nativeprotein, lipoprotein patterns, and isoenzymes were electrophoretically studied. It was found that the administrationof both B. variegata extract and nano-extract to diabetic rats ameliorated the deleterious effects that occurred asa result of STZ injection and restored the biochemical functions in addition to levels of hepatic and pancreaticantioxidants to normalcy. These findings were supported by the histopathological examination. It was concluded thatB. variegata nano-extract exhibited more antidiabetic effect through restoring the normal architecture of pancreaticβ-cells in addition to the antioxidant and hypolipidemic effect than extract alone, which indicated that the efficacy ofB. variegata extract was increased after the incorporation of Au-NPs.Item Isolation, characterization, and validation of RP-HPLC method for the quantification of quercetin in Huberantha senjiana leaf extract(Open Science Publishers LLP, 2020-05) Pandiyan, Rajakannu; Ilango, KaliappanHuberantha senjiana (Annonaceae) – an endemic tree of Pakkamalai Reserve Forest Gingee Hills, Tamil Nadu, Indiawas subjected to preliminary phytochemical tests and high-performance liquid chromatography (HPLC) fingerprintchromatogram was established for use in future research. Subsequently, the HPLC-DAD-ESI (+) MS analysis toidentify the common biomarkers revealed the presence of Quercetin, a polyphenolic flavonol in the ethyl acetateextract of the leaves. An isocratic reversed-phase (RP)-HPLC method for the quantification of quercetin was developedwith phenomenex, RP C18 column using mobile phase [(H2O (0.1% formic acid, A); (MeOH: ACN, (40:15v/v), B),40:60 (v/v)] with a flow rate of 0.8 ml/min, detection max at 254 nm with a retention time of 7.58 minutes and wasvalidated according to the International Conference on Harmonization Q2B guidelines. Linearity was achieved withthe concentration range of 5.0–17.5 μg/ml with a R2 value of 0.996. Sensitivity was demonstrated with the limit ofdetection of 2.28 µg/ml and the limit of quantification of 6.92 µg/ml. The robustness was estimated from purposefulchanges in the composition of the mobile phase, wavelength, and flow rate and the limits were Not More Than (NMT)4%. The foliar concentration of quercetin was found to be 0.0055% w/w. The structural confirmation was done by theisolation and characterization by the divergent spectral analysis. This is the first published report on the identification,quantification, and isolation of quercetin in the leaves of H. senjiana speciesItem LC-MS method development for the quantitation of potential genotoxic impurity 2-Methyl-6-nitro aniline in Telmisartan API(Open Science Publishers LLP, 2020-05) Suryakala, Duvvuri; Susarla, Sivakumar; Rao, Bandlamudi MallikarjunaCurrent work discloses the sensitive LC-MS/MS method development for the trace level determination of genotoxicimpurity 2-Methyl-6-nitro aniline in Telmisartan. 2-Methyl-6-nitro aniline was determined by LC-MS/MS methodin selected ion monitoring mode using LiChrospher RP-18 (100 × 4.6 mm) 5.0 µm column. Gradient technique wasapplied for the elution of analytes using acetonitrile (mobile phase A) and 0.01 M ammonium acetate buffer (mobilephase B) in different ratios. The gradient program (T/%B) was set as 0/5, 2.50/15, 5.00/30, 10.00/50, 15.00/95, and20.00/95. Developed method was validated as per International Conference on Harmonization guidelines. The limit ofdetection and limit of quantitation values found for 2-Methyl-6-nitro aniline were 0.05 and 0.1 µg/ml. The developedmethod serves as an upright tool in quality control for quantitation of 2-Methyl-6-nitro aniline impurity at trace levelsin Telmisartan.Item In situ green synthesis of antibacterial copper nanocomposite cotton fabrics using Achyranthes aspera leaf extract(Open Science Publishers LLP, 2020-05) Seetha, Jaswanth; Mallavarapu, Umamahesh; Mesa, ArundathiNanomaterials are finding the diversity of application at the leading edge in emerging field of nanotechnology. Coppernanoparticles (CuNPs) were in situ generated on the surface of cotton fabrics, using Achyranthes aspera leaf extract byenvironmentally benign green synthesis. The structural and morphological properties of synthesized nanocompositecotton fabrics (NCFs) were characterized by different spectral studies such as Fourier-transformation infrared (FTIR),scanning electron microscopy (SEM) coupled with energy-dispersive X-ray primary and derivative thermogravimetric(TG-DTG), differential scanning calorimetry (DSC), and X-ray diffractometer (XRD). The molecular functionalitiesof hydroxyl groups in polyphenols of A. aspera leaf extract were identified from FTIR absorption spectrum, and theyare responsible for the bioreduction of Cu+2 into Cu0 for the formation of CuNPs. The average size of the formedCuNPs from SEM studies was found to be 95 nm. The formed CuNPs were exhibited Face centered cubic (FCC)crystalline structure, and it was confirmed by XRD studies. TG-DTG analysis publicized the thermal stability ofNCFs. The tensile strength of NCFs was higher than normal cotton fabrics. These NCFs exhibited good antibacterialproperties which considered for making aprons and wound dressing materials in medicine and for packing materialsItem 3D QSAR and docking studies on benzoylsulfonohydrazides as histone acetyltransferase KAT6A inhibitors(Open Science Publishers LLP, 2020-05) MD., Muzaffar-Ur-Rehman; Akbar, Syed; Bahazeq, Asra AliSixty-one analogs of benzoylsulfonohydrazides were subjected to 3D QSAR studies using CoMFA and CoMSIAtechniques followed by docking studies to develop a correlation of the structure with their respective activities. Thegenerated model had shown good predictability and the contour analysis followed by docking study has provided aninsight to develop new inhibitors. The cross-validation values corresponding to CoMFA and COMSIA were observedto be within the acceptable criterion (q2 > 0.5). The docking analysis of the best active compound shown was −41.81kcal/mol. From the obtained analysis results of CoMFA as well as CoMSIA, the data can be useful to develop morepotent histone acetyltransferase inhibitors.Item Effects of low molecular weight galactomannans based standardized fenugreek seed extract in subjects with high fat mass: A randomized, double-blind, placebo-controlled clinical study(Open Science Publishers LLP, 2020-01) Deshpande, Pallavi Onkar; Bele, Vivek; Joshi, Kedar; Thakurdesai, Prasad ArvindThe present investigation evaluated the effects of low molecular weight galactomannans-based standardized fenugreekseeds extract (LMWGAL-TF) on human subjects with high-fat mass for 8-weeks using a prospective, randomized,double-blind, placebo-controlled design. Twenty-four subjects with percent body fat were randomized to ingest acapsule of LMWGAL-TF (500 mg, once a day) or the matching placebo at a 1:1 ratio for 8 weeks. The outcomemeasurements were recorded at baseline, week-4, and week-8 (end of the treatment). The efficacy outcome includedfat mass (absolute, non-fat mass and %) by skinfold thickness method (along with triceps, suprailiac, and abdominal)and bioelectrical impedance analysis method, body weight, body mass index, and abdominal girth. The standardsafety parameters were measured, such as adverse events, vital signs, hematology, and biochemistry. Eight weeksof LMWGAL-TF supplementation showed significant reduction in suprailiac skinfold thickness (v/s baseline) andabdominal skinfold thickness (v/s baseline and v/s placebo), and percent fat mass, (v/s baseline). The LMWGAL-TFsupplementation was found to be safe and well-tolerated. In conclusion, LMWGAL-TF supplementation showedsafety and efficacy in reducing skinfold thickness (abdominal and suprailiac) and percent body fat in subjects with ahigh fat massItem Metabolomic study and in silico approach of DLBS1442 as progesterone receptor agonist(Open Science Publishers LLP, 2020-05) Rahardjo, Natalia Windari; Emanuel, Dani Ramdani; Raymond, Rubianto Tjandrawinata; YantiEndometriosis prevalence has been known to be quite high among women of reproductive age and with pelvic painand/or infertility. The reason is that the estrogen level in the eutopic endometrium of women with endometriosis ishigher than in normal endometrium which may possibly be caused by the lack of interaction between progesteroneand progesterone receptor (PR). Dexa Laboratories of Biomolecular Sciences (DLBS) has developed DLBS1442,a bioactive fraction from Phaleria macrocarpa (Scheff) Boerl fruit, which has been found to be potential to treatsymptoms of primary dysmenorrhea and alleviate endometriosis. Therefore, the identification of DLBS1442 activecompounds which act as a PR agonist was necessary. Identification was performed using metabolomics study whichresulted in 14 compounds. Crystal structure of the PR with asoprisnil as the reference was obtained from PDB (4A2J).Virtual screening validation process was performed using Protein-Ligand ANT System (PLANTS) and Pythonbased Protein-Ligand Interaction Fingerprinting (PyPLIF). According to the virtual screening protocol validation,the highest Enrichment Factor (EF) 1% value was obtained with hydrogen interaction with GLN725 and ARG766residue. Virtual screening of the DLBS1442 metabolomics study showed that only glyceryl pentacosanoate exhibited alower Chem Piecewise Linear Potential (ChemPLP) than the cutoff. This compound might have a role as a PR agonistwhich supported the previous findings of DLBS1442 to alleviate endometriosis. However, this finding requires furtherin vitro and/or in vivo study to ensure the agonist activity of glyceryl pentacosanoate as a DLBS1442 active compound.Item The nutraceutical effect of Scenedesmus dimorphus for obesity and nonalcoholic fatty liver disease–linked metabolic syndrome(Open Science Publishers LLP, 2020-05) Armaini, Armaini; Dharma, Abdi; Salim, MarniatiObesity is a major cause of nonalcoholic fatty liver disease (NAFLD), which is identified as a characteristic relatedto metabolic syndrome. This study focuses on the benefits of Scenadesmus dimorphus as a nutraceutical to overcomeNAFLD-linked metabolic syndrome caused by obesity. The research used 30 mice (Mus musculus) divided into sixgroups: normal control, obesity control (OC), and drug control (Orlistat) and S. dimorphus administrated orally for21 days in obese mice with NAFLD-linked metabolic syndrome with doses of 5 mg/20 g body weight (BW), 10mg/20 g BW, and 15 mg/20 g BW. The administration of a high-fat diet can cause obese mice to suffer from NAFLD,resulting in an increase in liver enzymes and changes in lipid metabolism. Administration of S. dimorphus at 15mg/20 g BW decreases the activity of liver enzymes and improves liver function. The statistics test showed significantdifferences (p < 0.05 analysis of variance) to decrease the liver enzyme activity of alanine aminotransferase, aspartateaminotransferase, and alkaline phosphatase compared to OCs. Administration of S. dimorphus resulting in metabolismchanges showed a significant (at p < 0.05) decrease in total cholesterol, triglycerides, and low-density lipoproteincholesterol and increased high-density lipoprotein cholesterol. Microalgae S. dimorphus is beneficial as a nutraceuticalto manage obesity and reverse NAFLD-linked metabolic syndrome in obese mice.Item Application of total error concept in the analytical method validation for the assay of essential amino acids by precolumn derivatization(Open Science Publishers LLP, 2020-05) Aasodi, Ramachandra Reddy; Murugan, V; Premakumari, KBA pre-Ultraperformance Liquid Chromatography (UPLC) column derivatization procedure was developed for thesimultaneous quantification of essential amino acids (EAAs) in the solid oral dosage pharmaceutical formulation.This analytical procedure has been validated with the help of the concept of total error. The total error approach (thecombination of systematic and random error) is a decision-making tool for ensuring the performance of the method.Fluorenylmethyloxycarbonyl chloride was used as a derivatization reagent. The amino acid derivatives were separatedon a C18 column (internal diameter 2.1 × 100 mm, 1.6 µm) by gradient elution with 0.1% trifluoroacetic acid andacetonitrile:water (90:10, v/v), respectively, as mobile phase A and B. About 10 EAAs could be detected at 265 nm in35 minutes with a flow rate of 0.25 ml/min. The linearity range of each amino acid was between 0.1 and 1.0 mg/ml.The accuracy and risk profiles were considered acceptable across the range. The precolumn derivatization procedureand the concept of the validation of total error could be used as an appropriate strategy to demonstrate the suitabilityof the analytical procedure for the separation and evaluation of EAA in solid oral dosage formulations.