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The closure of educational institutions to reduce the impact of the spread of COVID-19 has brought about a change in the education administration. Shifting the face-to-face learning process to an online learning system is one method to overcome this impact. The present study aims to assess the relationship between the online learning process and the achievement of graduate competence. The study was conducted by sharing the Constructive Online Learning Environment Survey (COLLES) questionnaire, which involved 626 responses from 49 schools of pharmacy in Indonesia to the graduates and re-taker of the Pharmacy Profession Program. This questionnaire has 24 items with six domains: relevance, reflection, interactivity, tutor support, peer support, and interpretation. The data were descriptively analyzed, and to find the correlation, the Student-T test was applied. This study showed that the highest score of the Constructive Online Learning Environment Survey (COLLES) domain is relevance (4.01). The lowest score can be seen in interactivity and teacher support. There are no significant differences in COLLES domains between graduates and re-taker groups. These findings also showed that the graduates' GPA significantly influences the student study success. It can be concluded that online learning during the pandemic did not influence pharmacists' achievement of minimum competency in Indonesia. [ABSTRACT FROM AUTHOR]

Diabetes mellitus (DM) is an endocrine system and metabolic disorder caused by defects in insulin secretion and action. Syzygium cumini (L.) Skeels (Myrtaceae) are often used in anti-diabetic medicine due to their high polyphenol contents. This study aims to provide a comprehensive review of the role of phytochemical compounds in S cumini as traditional antidiabetic medicinal plants. The review covers related articles on antidiabetic AND S cumini AND phytochemicals OR bioactive compounds. The examined articles were published from 2001 to January 2023. Pubmed, Science Direct, Scopus, and Google Scholar were utilized as the bibliographic databases in this systematic search. The inclusion criteria include articles written in English that describe experimental research, clinical trials, and randomized studies and articles containing phytochemical content profiling. The exclusion criteria were other types of reports such as literature reviews, conference articles, theses, dissertations, and cases that were irrelevant to the topic. The reporting item guidelines used for references in this review were the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) and the Center for Systematic Reviews for Laboratory Animal Experiments (SYRCLE) risk of bias (RoB) tool. By the systematic compensation used, 15 articles that meet the requirements were obtained and were further reviewed thoroughly. Seeds, leaves, and bark of plant parts were reported to be non-toxic in acute experiments on mice or rats. S. cumini contains flavonol glycosides, especially myricetin, myricitrin, quercetin, and kaempferol; phenolics, such as ellagic acid, tannins, and gallic acid; alkaloids; and saponins. These compounds contributions to the overall anti-diabetic activity were discussed by covering an increase of insulin sensitivity, secretion, and usage of glucose in tissues; thereby reducing insulin resistance, oxidative stress, gluconeogenesis, and absorption of carbohydrates and sucrose. In conclusion, the review confirmed that the compounds of S. cumini have a potential for treating diabetes mellitus. Specifically, the seeds and leaves of S. cumini have a high potential as antidiabetic herbal product, and thus making it crucial to find the research gap to support the development of this herbal compound by establishing preclinical and clinical trials and reliable analytical methods for phytochemical profiling. [ABSTRACT FROM AUTHOR]

The number of diabetes mellitus (DM) cases has increased, and Tinospora crispa (L.) Hook. f. & Thomson is recognized for treating DM. Despite publications on T. crispa as an antidiabetic, there were no bibliometric reports on this topic. Thus, this study aimed to conduct bibliometric studies of existing articles on the preclinical trials of T. crispa in DM management. We used Scopus to obtain a bibliographic database of primary research related to the topic. There were 24 selected publications between 1989 and 2019. We analyzed data with VOSviewer 1.6.16. Malaysia, John Radcliffe Hospital (United Kingdom), Journal of Ethnopharmacology, Hamdan Noor, and Stephen J.H. Ashcroft (John Radcliffe Hospital, United Kingdom) were the most impactful country, institution, source, and author, respectively. This plant is promising for treating DM, meanwhile, there were case studies of harmful effects on the gastrointestinal tract and liver. The majority and diverse fields of this topic were phytochemistry and pharmacology. Our findings strengthen research collaboration and identify research gaps required for herbal medicine applications. [ABSTRACT FROM AUTHOR]

The prevalence of diabetes mellitus has increased over time. Medicinal plants, including Andrographis paniculata (Burm.f) Nees, are recognized for their use to manage hyperglycemia. Nowadays, plenty of papers are published about A. paniculata as an antidiabetic; however, no bibliometric study about the topic exists. This study examines the existing papers about the preclinical trial of A. paniculata as an antidiabetic agent using bibliometric analysis focusing on countries, institutions, publishers, authors, documents, and keywords. Bibliographic information of relevant research and conference articles were obtained from the Scopus database. In total, 97 articles published between 1994 and 2021 were selected, covering 376 authors and 1270 keywords. Data were analyzed bibliometrically using Vosviewer 1.6.16. A total of 97 published papers occurred from 1994 to 2021 were selected. India, Universitas Gadjah Mada (Indonesia), Journal of Ethnopharmacology, and Agung Endro Nugroho (Universitas Gadjah Mada, Indonesia) were the most productive country, institution, publisher, and author, respectively. The analysis of the most influential papers, co-citation network of the most influential papers, bibliographical coupling network based on authors, and keyword co-occurrence network and overlay demonstrated that the abundance and variety of existing papers about preclinical trials of A. paniculata as an antidiabetic were from phytochemistry, pharmacology, and drug formulation. The findings of our analysis have implications for managerial and theoretical aspects on this topic, such as encouraging research collaborations by analyzing the contributions of countries, institutions, publishers, and authors and revealing research gaps (molecular mechanisms, toxicities and side effects, drug formulations, and clinical trials) to accept a phytomedicine as a therapeutic option. [Display omitted] • The abundance of preclinical trials of Andrographis paniculata as antidiabetic. • India, Universitas Gadjah Mada (Indonesia), Journal of Ethnopharmacology, and Agung Endro Nugroho were the most productive country, institution, publisher, and authors, respectively. • Research mapping is needed to determine the expansion of the research fields. • The related fields were phytochemistry, pharmacology, and drug formulation. [ABSTRACT FROM AUTHOR]

Co-administered medicinal herbs can modify a drug's pharmacokinetics (PK), effectiveness, and toxicity. Andrographis paniculata (Burm. f.) ethanolic extract (APE) and andrographolide (AND) (a potent CYP2C9 inducer/inhibitor) can alter the pharmacokinetic parameters of glipizide (GLZ). This study aimed to determine the potential pharmacokinetics of herb–drug interactions between GLZ and APE/AND in the plasma of normal and diabetic rats using the HPLC bioanalysis method. The glipizide bioanalytical method established with RP-HPLC/UV instrument was validated following the EMA guidelines. GLZ was administered alone and in combination with APE or AND to normal and diabetic rats. The GLZ pharmacokinetic parameters were estimated according to the correlation between concentration and sampling time using the PK solver program. A simple and rapid GLZ bioanalysis technique with a lower limit of quantitation of 25 ng/mL was developed and presented the following parameters: accuracy (error ≤ 15%), precision (CV ≤ 15%), selectivity, stability, and linearity (R2 = 0.998) at concentrations ranging 25–1500 ng/mL. APE administration significantly improved the Cmax and AUC0–t/AUC0–∞ GLZ values in normal and diabetic rats (p < 0.05). AND significantly reduced the bioavailability of GLZ in diabetic rats with small values of T 1/2, Cmax, and AUC0–t/AUC0–∞ (p < 0.05). This combination can be considered in administering medications because it can influence the pharmacological effects of GLZ. [ABSTRACT FROM AUTHOR]

• Indonesia has rich biodiversity and ethnic groups applying for traditional medicine as antidiabetic. • Numerous ethnopharmacological surveys were conducted on medicinal plants in Indonesia. • Ethnopharmacological studies of antidiabetic plants have prospects for further development. Indonesia is rich in biodiversity and ethnic groups, including those that use traditional medicine to treat diabetes mellitus (DM). Ethnopharmacological of antidiabetic medicinal plants is still an essential field of study to organize preclinical and clinical trials. This study presents a review of the ethnopharmacology of antidiabetic plants and their scientific information, focusing on highlighting gaps and direction for further studies. Data were obtained from online and offline sources to identify Indonesian medicinal plants used to lower blood glucose. Ethnopharmacological literature was searched from Google Scholar with keywords: ethnobotany AND medicinal plant AND diabetes AND Indonesia; an ancient book (Cabe Puyang Warisan Nenek Moyang), government reports on ethnopharmacological surveys, and BSc/MSc/PhD theses indexed and not indexed internationally. Subsequently, other sections regarding preclinical trials (in vitro and in vivo), phytochemical issues, clinical trials, and toxicological assessments were searched from Scopus with the relevant keywords. A total of 229 medicinal plant species belonging to 70 families and are used to treat DM were listed in this study. Among these plants, Asteraceae and Orthosiphon aristatus (Blume) Miq. were the most dominant plant family and species, respectively. Most of the herbal recipes were from North Sumatera (102 recipes). Leaf and boiling were the most applied plant part and mode of preparation, respectively. Furthermore, the top 10 highly cited antidiabetic medicinal plants from ethnopharmacological data were assessed in the preclinical (in vitro and in vivo), phytochemical issues, clinical trials, and toxicological tests. Pharmacological, phytochemical, clinical, and toxicological studies have been reported; meanwhile, many research opportunities can be explored, especially plants lacking scientific evidence. This study's application is expected to accelerate the drug discovery and development from natural resources to treat DM. Moreover, hopefully, medicinal plants can be one of the solutions to treat DM that is effective, safe, and sustainable. [ABSTRACT FROM AUTHOR]

Diabetic Peripheral Neuropathy (DPN) is highly prevalent in diabetic patients, significantly diminishes the patient's quality of life, and has no definitive therapy currently. Based on the basic pathology of DPN, it's critical to restrict neuronal loss while also promoting neuron regeneration. As a peripheral regenerating cell, diabetic Schwann cells (SC) tend to have a low rate of cell proliferation and regeneration capacity. DLBS1033N, a protein hydrolysate obtained from Lumbricus rubellus, has been confirmed to promote Schwann cell line RSC96 growth and survival by inducting Nerve Growth Factor (NGF) expression via phosphatidylinositol-3-kinase (PI3K) pathway. This pathway primarily contributes to SC proliferation and migration during the peripheral regeneration process. Herein, the contribution of DLBS1033N to peripheral regeneration in high-glucose (50mM)-induced rat Schwann cell line RSC96 injury, a well-known DPN in vitro cell model, was evaluated. RSC96 were treated with high glucose (50mM) with or without DLBS1033N 25, 50, and 100 µg/mL for 24, 48, and 72 h. MTS assay kit were used to evaluate cell viability. The results showed that DLBS1033N significantly improved cell proliferation in 48 h incubation time in a dose-dependent manner (p < 0.05). Furthermore, the scratch assay confirmed that DLBS1033N significantly increased cell migration at a concentration of 100 µg/ml by 19% for 48 H incubation (p < 0.05). In conclusion, DLBS1033N enhanced peripheral regeneration which can be used as an effective and promising DPN treatment. [ABSTRACT FROM AUTHOR]

Cancer is one of the biggest causes of death after cardiovascular diseases. Alkaloid content of awar-awar leaf extract (Ficus septica Burm. f.) is reported to exhibit cytotoxic activity in several cancer cells. This research aimed to identify the antiangiogenesis potential of awar-awar leaf extract on chorioallantoic membrane (CAM) of chicken embryo induced by basic fibroblast growth factor (bFGF). Awar-awar leaf extract was obtained by the maceration method by using ethanol (70%). CAM was cultured in ex vivo and the angiogenesis was induced by bFGF. The CAM was treated with the extract at concentration of 13.00; 9.75; 6.50; and 3.25μg/mL. The observation was done macroscopically and microscopically. Macroscopic observation showed that the extract inhibited angiogenesis at the concentration of 13.00μg/mL (62.30%), 75 μg/mL (51.37%), 6.50 μg/mL (28.42%), and 3.25mg/mL (13.11%). At higher concentration of the extract, the growth of new blood vessels was decreased, indicated by the reduction in erythrocyte density, parallel blood vessel pattern, and cellular density of mesenchymal tissue. The statistical analysis showed that the inhibition of new blood vessels growth by the extract was in dose dependent manner (p<0.05). Here, we found that awar-awar leaf ethanolic extract showed antiangiogenesis activity in CAM of chicken embryo induced by bFGF. [ABSTRACT FROM AUTHOR]

Objectives: Andrographis paniculata (Burm. f.) Nees originates from India and grows widely in many areas in Southeast Asian countries. Andrographis paniculata (Burm. f.) Nees has shown an antidiabetic effect in type 1 DM rats. The present study investigates the purified extract of the plant and its active compound andrographolide for antidiabetic and antihyperlipidemic effects in high-fructose-fat-fed rats, a model of type 2 DM rats. Materials and Methods: Hyperglycemia in rats was induced by high-fructose-fat diet containing 36% fructose, 15% lard, and 5% egg yolks in 0.36 g/200 gb.wt. 55 days. The rats were treated with the extract or test compound on the 50th day. Antidiabetic activity was measured by estimating mainly the pre- and postprandial blood glucose levels and other parameters such as cholesterol, LDL, triglyceride, and body weight. Results: The purified extract and andrographolide significantly (P<0.05) decreased the levels of blood glucose, triglyceride, and LDL compared to controls. However, no changes were observed in serum cholesterol and rat body weight. Metformin also showed similar effects on these parameters. Conclusions: Andrographis paniculata (Burm. f.) Nees or its active compound andrographolide showed hypoglycemic and hypolipidemic effects in high-fat-fructose-fed rat. [ABSTRACT FROM AUTHOR]

Mucosal mast cells (MMCs) have an important role in allergic inflammation, and effective antagonists are required for their regulation. To discover a possible mechanism of controlling the activation of MMCs, we investigated the expression and function of syntaxin4, one of the soluble membrane N-ethylmaleimide-sensitive factor attachment protein receptor (SNARE) proteins, in RBL-2H3 cells, which is a rat mucosal mast cell line. Syntaxin4 silencing was induced by transfection of short interfering RNAs (siRNAs). Syntaxin4 was knocked down in mast cells at both the mRNA and protein levels. The release of granule contents that are involved in inflammation, such as histamine and hexosaminidase, was significantly suppressed by the gene silencing of syntaxin4. Silencing of this gene was also induced in the trachea and bronchi of rats by intratracheal application of the siRNAs using an atelocollagen delivery system. The activation of MMCs, which was monitored by the level of rat mast cell protease-II (RMCPII) in the bronchoalveolar lavage fluid (BALF), was inhibited, and asthmatic airway constriction was prevented by administration of the syntaxin/atelocollagen complex. These results indicate that siRNAs targeting syntaxin4 can stabilize mucosal mast cells and may have beneficial therapeutic effects on the asthmatic response. [ABSTRACT FROM AUTHOR]

Marmin or (7-(6′,7′-dihydroxygeranyl-oxy) coumarin is a compound isolated from Aegle marmelos Correa. In the study, we investigated the effects of marmin on the L-histidine decarboxylase (HDC), a rate-limiting histamine synthesizing enzyme, in rat mast cell. The study was performed by using rat basophilic leukemia (RBL-2H3) cell line, a tumor analog of mast cells. Dinitrophenylated bovine serum albumin (DNP24-BSA), a specific antigen for monoclonal IgE antibody, and phorbol myristate acetate (PMA), a protein kinase C (PKC) activator, were used as inducers for histamine release from mast cell. In the present study, marmin (10 and 100 μM) inhibited the histamine release from RBL-2H3 cells induced by DNP24-BSA by 17.0 ± 5.0% and 94.6 ± 1.0%, respectively. Besides, the compound at a concentration of 100 μM inhibited the synthesis of histamine in RBL-2H3 cells induced by DNP24-BSA by 62.37 ± 2.19%. However, marmin did not influence mRNA expression of HDC enzyme in these experiments. It indicates that the inhibitory effect of marmin on the synthesis of histamine in IRBL-2H3 cells is not related to mRNA transcription of HDC enzyme. However, it may involve in an inhibition process on the enzyme activity. The result of these studies may provide useful information in pharmaceutical science and an alternative anti-allergy drug. [ABSTRACT FROM AUTHOR]

2,5-Bis(4-hydroxy-3-methoxybenzylidene)cyclopentanone, known as pentagamavunon-0 (PGV-0), is a benzylidene cyclopentanone analog of curcumin. This compound posses stronger pharmacological activities such as anti-inflammatory, antioxidative and antibacterial effects in comparison to curcumin. PGV-0 was reported to also have antiallergic effect in rat basophilic leukemia cell line and rat peritoneal mast cell in vitro. This study will demonstrate the inhibitory effect of PGV-0 on the histamine release and edema formation stimulated by compound 48/80 in animal model. The study was conducted using an in vivo microdialysis technique implanted into rat hind paw, and histamine content in dialysate was quantified using HPLC-fluorometric method. In addition to the compound 48/80-induced edema formation, the skin histamine content was also evaluated. Intragastric administration of PGV-0 at 1 h prior to compound 48/80 subplantar injection inhibited the histamine release from the rat hind paw in a dose-dependent manner. PGV-0 at dose of 40 mg/kg body weight decreased the rat paw edema and inhibited the decrease of the histamine content and the degranulation of mast cell in skin tissue. These data demonstrated that the inhibition on the histamine release by PGV-0 resulted in the suppression of edema formation. These effects were suggested mainly due to inhibition of the histamine content and mast cell degranulation in rat skin tissue. [ABSTRACT FROM AUTHOR]

Introduction: Metformin given together with herbs in order to optimizing its mechanism of actions. The effect might be positive and vice versa. Interaction might occur pharmacokinetics or pharmacodynamically. The study aimed to review potential interaction of metformin and some herbs with various pharmacological activities. Methods: This literature review was conducted by collecting articles with keywords Metformin, Herb-drug Interaction, drug interaction, pharmacokinetics, pharmacodynamics, and pharmacology from international databases such as Science Direct, PubMed, Springer Link, and Scopus up to 2021. Results: Metformin with its various uses such as antidiabetic agent, an agent for reducing weight for patients that sensitive or even resistant to insulin, patients with obesity, anti-tumor agent, anti-cancer potential agent, and also has anti-aging potential. Metformin could interacted with drugs, herbs, and also some bioactive isolate. The interaction might occurs pharmacokinetically or pharmacodynamically. Pharmacokinetics interactions occurred during distribution and also excretion via transporters that metformin transported with. This was shown as the elevated or lowered metformin levels in blood. Pharmacodynamic interactions can be seen as the lowering or elevated levels of glucose, HbA1c and even the lipid profile in blood or plasma. Conclusion: According to this literature review, Metformin have potential interaction with drugs, herbs, and also some bioactive isolate. The interactions occur pharmacokinetically or pharmacodynamically. This study can be used as a established familiarity with and understanding the potential HDIs from Metformin and herbal products. [ABSTRACT FROM AUTHOR]

In silico data revealed that the active compound of ginger (Zingiber officinale Roscoe), 6-shogaol, has strong affinity toward transient receptor potential vanilloid-1 (TRPV-1). TRPV-1 is expressed in nervous tissue and pancreatic β-cells. Prolonged induction of TRPV-1 is related to the expression of N-methyl-D-aspartate receptor subunit 2B (NMDAR2B). However, there are no data on TRPV-1 and NMDAR2B expressions in nervous tissue after 6-shogaol or ginger extract treatment nor pancreatic islet morphology and insulin expression in mice model of painful diabetic neuropathy (PDN). This study aimed to investigate the mechanism of action of ginger extract and its compound, 6-shogaol, on pancreatic islets as well as on expressions of TRPV-1 and NMDAR2B in the spinal cord of streptozotocin (STZ)-induced mice model of PDN. Sixty-four 5–6 weeks old male-Balb/C mice were induced with 110 mg/kgBW STZ i.p., while eight mice were used as control group. Mice with blood glucose level ≥200 mg/d, that suffered hyperalgesia and allodynia were classified as PDN mice. Hot plate and von Frey filament tests were performed once a week until termination. At day 28 after considered as PDN, ginger extracts, 6-shogaol or gabapentin as control treatment were given once daily for 21 days until day 49, except for the diabetic control group. Upon termination, mice' pancreas were fixed, processed as paraffin sections and stained with hematoxylin eosin. Total volume of pancreatic islets was estimated using Cavalieri methods. Immunohistochemistry on pancreatic sections were performed to observe insulin expression. mRNA was extracted from lumbar segments of the spinal cord, followed by cDNA preparation and quantitative Real-Time Polymerase Chain Reaction (qRT-PCR) to measure the expressions of TRPV1 and NMDAR2B. The mean differences between groups were analyzed using one-way analysis of variance (ANOVA) with p < 0.05 considered statistically significant. Ginger extracts and 6-shogaol alleviated hyperalgesia and allodynia. The groups that received ginger extract 400 mg/kgBW or 6-shogaol 15 mg/kgBW had significantly lower TRPV1 and NMDAR2B expressions in the spinal cord compared to the diabetic control group (p < 0.001; p < 0.05). However, no differences in volume of pancreatic islets (p > 0.05) nor insulin expression were observed in all PDN groups. Ginger extracts and its compound, 6-shogaol, reduced pain symptoms in PDN via its effect on decreasing TRPV1 and NMDAR2B expressions in the spinal cord, with very limited effect on pancreatic islets. Image 1 [ABSTRACT FROM AUTHOR]

The solubility of ketoconazole is highly dependent on the pH of the medium. Solubility is an important physicochemical parameter needed to consider and predict to obtain the drug behavior in a physiological environment. Determination of solubility of ketoconazole in pH of intestine fluid (6-7.4) is not easy due to ketoconazole poor soluble in intestine fluid pH. The aim of this study was to validate an assay for the solubility of ketoconazole in phosphate buffer pH 6.8 using the RP-HPLC method. In addition to representing intestinal pH, phosphate buffer pH 6.8 is also generally used as an alkaline medium for the dissolution testing of several drugs. The method to analyze the solubility of ketoconazole has been developed and validated. The method was used an isocratic Reverse Phase-High Performance Liquid Chromatography (RP-HPLC) using Phenomenex Luna (250 x 4.6 mm, 5 µm) column with a mobile phase consisting of acetonitrile: water with TEA 0.15% pH 3.3 in ratio 50:50, at the flow rate of 1 mL/min and UV detection at wavelength 232 nm. The correlation coefficients were obtained at r2=0.9997 in the range of 0.5-12 µg/mL. The recovery % ranged within 100-101%. The intra and interday RSD% were less than 1.74%. LoD was 0.15 µg/mL and LoQ was 0.45 µg/mL. According to ICH guidelines, the method was validated for selectivity, linearity, accuracy, precision, LoQ, and LoD. The proposed method is suitable for determining the solubility of ketoconazole in phosphate buffer pH 6.8. [ABSTRACT FROM AUTHOR]

Naringenin (NAR), a natural flavonoid aglycone of naringin has been extensively investigated for its pharmacological activities, including anti-tumor effects. However, its poor bioavailability has been identified as the single most important challenge in oral drug delivery. Based in this condition, it is used nanoencapsulation to increase the effectiveness of NAR as anticancer. The objectives of this research were to develop the formulation of NAR-loaded nanoparticles (NARNPs) as well as to evaluate its potential as anti-cancer against T47D breast cancer cells line. NARNPs is prepared through the method of ionic gelation, meanwhile its characteristic is evaluated through photon correlation spectroscopy (PCS), transmission electron microscopy (TEM), fourier transform infra-red spectroscopy (FTIR), and different scanning calorimeter (DSC). The result of MTT test and cellular uptake indicate that NARNPs increase cytotoxicity and internalization of NAR to the cells compared to that of free NAR. The result of qualitative apoptosis study using fluorescence microscope indicates that both free NAR and NARNPs were able to induce apoptosis. It can be conclude that Chitosan nanoparticles- TPP conjugates have the capability to encapsulate naringenin hence increase the cellular uptake and cytotoxcicity of naringenin against T47D cell line. NARNPs also could induce the apoptosis effect. [ABSTRACT FROM AUTHOR]

A previous study has shown that ethanolic extract of leaves of A. marmelos Correa on isolated ileum had an antagonistic effect on the contraction induced by histamine. Apart from H1 receptors, muscarinic acetylcholine (AChM) receptors are also involved in the mechanism of ileum contraction. Marmin is predicted to antagonize the AChM3 receptors. This study was aimed at determining the effect of marmin on smooth muscle contraction of isolated guinea pig ileum induced by metacholine, an AChM3 agonist. The methods used were in vitro (isolated organ) and in silico (docking PLANTS) studies. In the in vitro study, marmin exhibited a competitive antagonistic effect at a concentration of 100 μM (pA2 = 1,728) on the AChM3 receptors. A reversibility assay of the AChM3 receptors showed that by washing the ileum with Tyrode's buffer every 6 minutes for 30 minutes, the bond of marmin to the receptors was still not completely detached. In the in silico study, marmin was observed to be bound to the AchM3 receptors (docking score: -102.086). The marmin bond was weaker than that of the native ligand of the AChM3 receptors (tiotropium, docking score: -115.107), but stronger than that of the AChM3 receptor agonist and antagonist. Based on the results, we conclude that marmin has competitive antagonist activity on AChM3 receptors. [ABSTRACT FROM AUTHOR]

Purpose: Exploration of plant combinations could be an alternative approach for diabetes treatment. The aim of this study is to evaluate the hypoglycemic effect of combination of A. indica and G. procumbens ethanolic extracts in alloxan-induced diabetic rats. Methods: Powder of A. indica and G. procumbens leaves were macerated with ethanol 70%. Determination of rutin in A. indica and quercetin in G. procumbens were performed by TLCdensitometry. Hyperglycemia in rats was induced by an intraperitoneal injection of alloxan monohydrate at a single dose of 150 mg/kgBW. The rats were treated with 3 dosage variation of combinations for 15 days. Hypoglycemic effect was evaluated by estimating the blood glucose levels and the rats pancreas histological study. Results: A. indica contained 2.90±0.15% of rutin and G. procumbens contained 18.86±0.86% of quercetin. Combination at the ratio of 50mg/kgBW A. indica:112.5mg/kgBW G. procumbens showed the highest hypoglycemic effect: 68.74±4.83% (preprandial) and 73.91±3.18% (postprandial). Histological studies indicated that this combination improved the morphology of the islets of Langerhans and β cells. It also increased insulin expression and decreased the elevated-glucose concentrations. Conclusion: This study showed that combination of both extracts has better hypoglycemic effect than the single treatment of A. indica or G. procumbens. Combination of both extracts was potential to develop as a blood glucose-lowering agent for diabetic patients. [ABSTRACT FROM AUTHOR]

Precipitation due to supersaturation phenomenon and intraluminal solubilization behavior is mainly faced on reducing bioavailability, particularly for weak base drugs. Incomplete and extend of absorption can be avoided by modification of drug-excipient interaction namely polymers. This interaction is proposed to stabilize the amorphous form of drug through reducing nucleation followed by crystal growth. Therefore, polymers can be utilized to inhibit the precipitation phenomenon through their interaction with poorly water-soluble and weak base drugs. However, until to date, there was no recent updates on the use of polymer for precipitation inhibitor of weak base drug. This review discussed the brief and recent updates on polymer as precipitation inhibitor of weak base drug during intraluminal solubilization behavior namely mechanism, factors, and polymer application. [ABSTRACT FROM AUTHOR]

Bengkoang (Pachyrhizus erosus (L.) Urban) contains phytosterol and the isoflavone daidzein, which are thought to have immunomodulatory activity. There have been no studies reporting on the immunomodulatory effects of bengkoang extract containing polar and semi-polar compounds, such as phytosterols and isoflavone-like compounds. The objective of this study was to evaluate the immunomodulatory effects of bengkoang extracts, including petroleum ether extract (PEE), methanol extract (ME), and the ethyl acetate fraction (EAF) of bengkoang, in vitro. The immunomodulatory effects of PEE, ME, and EAF of bengkoang were determined according to the phagocytic activity of macrophages based on phagocytosis of latex beads, lymphocyte proliferation, and detection of cytokine production of tumor necrosis factor-α (TNF-α) interleukin-6 (IL-6), and interleukin-10 (IL-10) levels. Results: The phagocytic index and phagocytic capacity of ME, PEE, and EAF of bengkoang on macrophage cells were significantly increased (p < 0.05), whereas on lymphocyte proliferation, ME showed a trend of increasing activity (p < 0.05). On the other hand, the PEE effect showed a decreasing trend of activity, and the others had no significant effect on lymphocyte proliferation (p > 0.05), and ME of bengkoang enhanced the levels of the cytokines TNF-α and IL-6. In contrast, PEE and EAF of bengkoang decreased TNF-α and IL-6 levels compared with the control group. All of the bengkoang extracts decrease the production of the anti-inflammatory cytokine IL-10. In conclusion, this study showed that PEE, ME, and EAF of bengkoang could increase the non-specific immune response (phagocytic activity) but had a lesser effect on the specific immune response (lymphocyte proliferation). The ME of bengkoang acts as an immunostimulant by increasing the levels of the inflammatory cytokines TNF-α and IL-6 and decreasing those of the antiinflammatory cytokine IL-10. Further investigation of in vivo immunomodulatory effects is needed to determine its effect on systemically innate and adaptive immune responses. [ABSTRACT FROM AUTHOR]

Non Steroid Anti-Inflammatory (NSAID) is one type of Anti- Inflammatory drug that is used to treat pain in patients of osteoarthritis (OA) and rheumatoid arthritis (RA). The use of NSAIDs can cause gastrointestinal side effects. To prevent the side effects, NSAIDs are prescribed in combination with gastroprotective agent (GPA). The aim of the study is to determine the factors considered in the GPA prescription by the doctors in patients who have risk factors for gastric disorder due to NSAIDs use. This study was performed using a cross-sectional observational design. The data were collected retrospectively during a period of January to December 2010. The subjects were OA and RA patients considering the inclusion and exclusion criteria. The data included patient characteristics (gender, age, occupation, payment method, the primary diagnosis), prescription of NSAID, prescription of GPA, history of gastrointestinal disease, NSAID prescription with corticosteroids, prescription with antiplatelet. The data were processed descriptively and quantitatively, and analyzed statistically using chi-square and log. regression with 95% Confidence Interval. The results showed that there were correlation between some predictor factors with prescription of gastroprotective agent. These factors were women patient, patient age of ≥65 years, oxicam prescribing, diclofenac sodium prescribing, prescribing >1 type of NSAIDs, prescription of NSAID concomitant with corticosteroids, prescription of NSAID concomitant with antiplatelet, patients with history of gastrointestinal, prescribing NSAIDs with duration of = 3 months. Patient with a history of gastrointestinal disease was the most predictor influential factor, with OR (odds ratio) of 3.6 (95% CI: 2.79 - 4.66). Predictor factor of patients with a history of dyspepsia possessed the highest OR {OR=4,29 (CI 95%: 3.23– 5.7)}. It means that patients with a history of dyspepsia prescribed NSAIDs would have greater risk of 4.29 times to get GPA prescription than patients without a history of dyspepsia. Prescribing NSAIDs >1 DDD (defined daily dose) had p value of 0.777, which means there was no relationship between GPA prescription with NSAIDs >1 DDD prescription. [ABSTRACT FROM AUTHOR]

Purpose: Insulin resistance is a characteristic of non-insulin-dependent diabetes mellitus associated with obesity and caused by the failure of pancreatic beta cells to secrete sufficient amount of insulin. Andrographolide (AND) improves beta-cell reconstruction and inhibits fat-cell formation. This research aimed to improve the delivery of water-insoluble AND in self-nanoemulsifying (ASNE) formulation, tested in streptozotocin (STZ)-induced diabetic rats and 3T3-L1 preadipocyte cells. Methods: A conventional formulation of AND in suspension was used as a control. The experimental rats were orally administered with self-nanoemulsifying (SNE) and suspension of AND for 8 days. Measurements were performed to evaluate blood glucose levels in preprandial and postprandial conditions. Immunohistochemistry was used to assess the process of islet beta cell reconstruction. In vitro study was performed using cell viability and adipocyte differentiation assay to determine the delivery of AND in the formulation. Results: ASNE lowered blood glucose levels (day 4) faster than AND suspension (day 6). The histological testing showed that ASNE could regenerate pancreatic beta cells. Therefore, ASNE ameliorated pancreatic beta cells. The in vitro evaluation indicated the inhibition of adipocyte differentiation by both AND and ASNE, which occurred in a time-dependent manner. ASNE formulation had better delivery than AND. Conclusion: ASNE could improve the antidiabetic activity by lowering blood glucose levels, enhancing pancreatic beta cells, and inhibiting lipid formation in adipocyte cells. [ABSTRACT FROM AUTHOR]

The recent work focuses on the physical characterization and dissolution study of PGV-0 loaded self-nanoemulsifying drug delivery system (SNEDDS). The PGV-0 SNEDDS was prepared by spontaneous emulsification method using oleic acid, tween 20:labrasol (1:1) and polyethylene glycol 400. The zeta potential of the PGV-0 SNEDDS was -34.4±7.66 mv. The nanoemulsion of PGV-0 SNEDDS was thermodynamically stable with forming droplet oil containing PGV-0 in it and spherical. The dissolution result showed that the dissolution profile of SNEDDS PGV-0 was dissimilar with the PGV-0 powder in AGF and AIF. The PGV-0 SNEDDS was able to increase the dissolution significantly (p <0.05) compared with PGV-0 powder of 44.13% in AGF medium and 30.37% in AIF medium. It is concluded that SNEDDS formulation was able to improve the dissolution profile of PGV-0. [ABSTRACT FROM AUTHOR]

A white-rot fungus of Polyporus sp. S133 was isolated from an oil-polluted soil. The metabolism of pyrene by this fungus was investigated in liquid medium with 5 mg of the compound. Depletion of pyrene was evident during the 30-day growth period and was 21% and 90%, respectively, in cometabolism and metabolism of pyrene alone. Pyrene was absorbed to fungal cells or biodegraded to form simpler structural compounds. Seventy-one percent of eliminated pyrene was transformed by Polyporus sp. S133 into other compounds, whereas only 18% was absorbed in the fungal cell. The effects of pH and temperature on biomass production of Polyporus sp. S133 for pyrene were examined; the properties of laccase and 1,2-dioxygenase produced by Polyporus sp. S133 during pyrene degradation were investigated. The optimal values of pH were 3, 5, and 4 for laccase, 1,2-dioxygenase, and biomass production, respectively, whereas the optimal values of temperature were 25 °C for laccase and 50 °C for 1,2-dioxygenase and biomass production. Under optimal conditions, pyrene was mainly metabolized to 1-hydroxypyrene and gentisic acid. The structure of 1-hydroxypyrene and gentisic acid was determined by gas chromatography-mass spectrometry after identification using thin-layer chromatography. [ABSTRACT FROM AUTHOR]