Natural Products Chemistry and Pharmacognosy Commons^™

Percobaan Sintesis 4-(4-Metoksibenzilidena) 2-Metiloksazol-5-On Dari Asetilglisin Dan 4-Metoksibenzaldehid, Arif Arrahman, Hayun Hayun, Arry Yanuar

Majalah Ilmu Kefarmasian

Compound 4-(4-methoxybenzylidene)-2-methyloxazole-5-one was one of oxazolone moety derivative. Oxazolones had several different pharmacological activity depend on substituent which was bonded to oxazolone ring. Oxazolones was an important precursor for synthesizing several compounds which had pharmacological activity. For that reason, experiment to synthesize 4-(4-methoxybenzylidene)-2-methyloxazole-5-one from acetyl- glicine and 4-methoxybenzaldehyde as an oxazolone derivative become necessary. Com- pound 4-(4-methoxybenzylidene)-2-methyloxazole-5-one was synthesized over two step of reaction. First step was reacted glycine with acetic anhydride in acidic environment yielded acetylglycine. Second step was reacted acetylglycine with 4-methoxybenzaldehyde yielded 4-(4-methoxybenzylidene)-2-methyloxazole-5-one. The product, which was collected in every step, was purified by washing and recrystalization …

Efek Nefroprotektif Infus Daun Sukun (Artocarpus Altilis (Park.) Fsb.) Pada Tikus Jantan Yang Diinduksi Karbon Tetraklorida, Rianti Adi Cahyaningsih, Azizahwati Azizahwati, Dadang Kusmana

Majalah Ilmu Kefarmasian

Renal dysfunction can be caused by several factors, including hypertension, urinary tract obstruction, autoimmune disorders, urinary tract infection, diabetes mellitus, consumption of drugs that affect nephrotoxic and antibiotic from aminoglycoside class. Breadfruit leaves (Artocarpus altilis (Park.) Fsb.) is a traditional plant that hasbeen used empirically to treat kidney diseases. The research has been done to figure out the nephroprotective effect of breadfruit leaves infusion on white male rats strain Sprague-Dawley previously induced by carbon tetrachloride. There were 25 rats which were divided randomly into five groups. Group I which was the normal control group received CMC 0,5%. Group II which …

Uji Penghambatan Tirosinase Dan Stabilitas Fisik Sediaan Krim Pemutih Yang Mengandung Ekstrak Kulit Batang Nangka (Artocarpus Heterophyllus), Ninin Kartika Juwita, Joshita Djajadisastra, Azizahwati Azizahwati

Majalah Ilmu Kefarmasian

The cortex of jackfruit (Artocarpus heterophyllus) contains some flavonoids which have activity as tyrosinase inhibitors. This compound can inhibit the oxidation of l-tyrosine and levodopa in the mechanism of melanogenesis. The extract of jackfruit cortex formulated into creams differentiated by the extract concentration of 1,5% and 2,0%. Physical stability test was conducted with storing the creams at three different temperatures, 7 ± 2°, 27 ± 2°, and 40±2°C respectively. Centrifugal tests and cycling test was also performed on both cream. Tyrosinase inhibitory activity measurement was done by in vitro studies with measuring dopachrome. The result showed that both of formulations …

Formulasi Sediaan Granul Mukoadhesif Kombinasi Ekstrak Kulit Batang Mimba (Azadirachta Indica A. Juss) Dan Kunyit (Curcuma Domestica Val.), Sutriyo Sutriyo, Khairunnisya Khairunnisya, Abdul Mun’Im

Majalah Ilmu Kefarmasian

Neem bark (Azadirachta indica A.Juss) and turmeric (Curcuma domestica Val.) extracts have been found posses gastroprotective effect so that they are used in the treatment of gastric ulcer. Administration of combination of both extracts can give synergistic effect so that the administration dose can be reduced. In this research, combination of neem bark and turmeric extracts were formulated as mucoadhesive granules to improve their effectivenesses by increasing the residence time of dosage form in the stomach. Mucoadhesive granules were prepared by wet granulation method in six formulas using HPMC, Carbopol, and combination of HPMC and Carbopol as mucoadhesive polymers. Granules …

Analisis Kandungan Ion Fluorida Pada Sampel Air Tanah Dan Air Pam Secara Spektrofotometri, Yodifta Astriningrum, Herman Suryadi

Majalah Ilmu Kefarmasian

Fluoride ion is one of the compounds that are known to have benefits in the prevention of dental caries when used in certain concentrations, but also hasnegative effects that may cause the occurrence of dental and bone fluorosis when the intake was in excessive concentration. One of the fluoride intakes comes fromwater that is consumed. The aim of this research was to identify and measurefluoride ion levels in groundwater and piped water that used as drinking water consumption in the community. Measurement of fluoride ion concentration isdone by using visible spectrophotometry at the maximum wavelength of 586 nm using the …

Plants, People, And Partnership In Madagascar: How Pharmaceutical Companies And Bioprospecting Ventures Must And May Positively Benefit The Communities Whose Resources They Use, Rebecca Slotkin

Independent Study Project (ISP) Collection

For centuries, traditional medical practitioners around the world have understood the tremendous wealth of medicinal power that can be found in the natural environment. In Madagascar, traditional practitioners have both used and cared for their natural environment, which in turn has given them a wide array of medical knowledge. According to the World Health Organization (WHO), “approximately 80% of the world’s inhabitants rely predominantly on traditional medicines for their primary health care” (Cao et al. 2009). Traditional medical knowledge has relatively recently come to the attention of the international medical market. This “recent ‘rediscovery’ of medicinally useful plants” (Sheldon et …

Pembuatan Sediaan Tablet Mengapung Famotidin Menggunakan Kompleks Polielektrolit Kitosan-Pektin Sebagai Bahan Matriks, Erny Sagita, Effionora Anwar, Silvia Surini

Majalah Ilmu Kefarmasian

Floating tablet is one of the drug delivery system retained in the stomach which aims to prolong the lag time of the drug in the stomach. This principle can be used to improve the efficacy of famotidine in treating diseases in the stomach The purpose of this research is to develop dosage form afloat by using Chitosan Pectin Electrolytes (PEC) as matrix then used as the matrix in tablet dosage form with famotidine as a drug model. PEC also combined with hydroxypropylmethylcellulose (HPMC) with different. PEC was also combined with hydroxypropilmethylcellulose (HPMC) in different concentrations. The results of the dissolution …

Pengembangan Sistem Penghantaran Obat Solid Self-Emulsifying Mikropartikel Gliklazid Untuk Meningkatkan Disolusi, Mega Suryani, Sutriyo Sutriyo

Majalah Ilmu Kefarmasian

Gliclazide is a Hypoglycemicdrug, second-generation sulfonylurea used in the treatment of non insulin dependent diabetes mellitus. Gliclazide exhibit poor aqueous solubility, so that their low bioavailability. Objectivesthis study is to develop solid self-emulsifying (SE) microparticles of poorly soluble gliclazide to dissolution enchancement. These microparticles were prepared by spray drying method, using three surfactant (acripol, tween 80 and sodium lauryl sulphate) with various concentration. SE microparticles characterized in terms of morphology (SEM), particle size distribution (PSA), x-ray diffraction (XRD), thermal analysis (DSC), functional group analysis (FTIR), solubility test, and dissolution test. The all gliclazide SE microparticlesexhibited particle size smaller than pure …

Analisis Adduct Dna Setelah Pemberian Natrium Nitrit Dan Dimetilamin Secara Berulang Pada Tikus, Sherly Meilianti, Yahdiana Harahap, Hayun Hayun

Majalah Ilmu Kefarmasian

Nitrosodimethylamine is a carcinogenic compound which can be formed from the reaction of nitrite and dimethylamine that is found in food. Nitrosodimethylamineis activated in liver and alkylates the DNA base and producing a DNA adductssuch as O6-methylguanine and N7-methylguanine that have a role incarcinogenesis. In this research, DNA was isolated from rat’s blood which waspreviously given nitrosodimethylamine’s precursor, sodium nitrite anddimethylamine. DNA adducts can be obtained from hydrolysis in hydrochloricacid 0.1 N for 30 minutes at 7000C. Then the adducts were analyzed using High Performance Liquid Chromatography (HPLC), with a strong cation exchangecolumn (Supelcosil LC-SCX, 5 μm, 250 x 4.6 …

Efek Antidiabetes Dan Identifikasi Senyawa Dominan Fraksi Kloroform Herba Ciplukan (Physalis Angulata L.), Sediarso Sediarso, Hadi Sunaryo, Nurul Amalia

Majalah Ilmu Kefarmasian

Antidiabetic activity of ciplukan (Physalis angulataL.) herb has a lot to do, as an extracts and infusions, proven to reduce blood sugar levels in rats or mice induced by alloxan. The research objective was to evaluate the antidiabetic effect and identify the content of the chloroform fraction ciplukan herb eluated with methanol-ammonia. Antidiabetic effects testing conducted using 30 male white mice (Mus musculus) ddY strain were divided into 6 groups, each consisting of 5 mice. K-1 is a negative control induced by alloxan, K-2, K-3 and K-4 induced by alloxan and treated with the test substance dose of 50 mg/kg …

Anthocyanins, Phenolics, And Antioxidant Capacity Of Vaccinium L. In Texas, Usa, Wei Yuan, Lijing Zhou, Guangrui Deng, Ping Wang, David Creech, Shiyou Li

Faculty Publications

Berries of Vaccinium spp. have long been an important source of food and pharmaceutical ingredients and are considered to have high antioxidant potential. Growing blueberries in Texas, United States is a substantial industry, but there is no report on their antioxidant capacity, total phenolics, and anthocyanins. This study evaluates antioxidant capacity and contents of total phenolics and anthocayanins in both fruits and leaves of 19 genotypes including five commercial cultivars and 11 selections of rabbiteye blueberry (V. ashei) and southern highbush (V. corymbosum hybrids), and three native species (V. darrowii, V. arboreum, and V. fuscatum) grown in Nacogdoches, Texas. Significant …

Preparation And Characterization Of A Standardized Anticonvulsant Ginseng Rb Extract From Panax Quinquefolius L., Xiao-Yuan Lian, Zhizhen Zhang

Faculty Publications

A ginseng Rb extract (GRbE) containing three major ingredients of ginsenoside Rb1 (G-Rb1), ginsenoside Rb3 (G-Rb3) and ginsenoside Rd (G-Rd) has been shown to have anticonvulsant and neuroprotective activity. As such, sufficient characterization and standardization of this active GRbE are demanded to facilitate an ongoing preclinical investigation on its potential for the treatment of epilepsy. In the investigation, the methods for generating the active GRbE and isolating G-Rb1, G-Rb3, and G-Rd in large scale from Panax quinquefolius are described. The chemical profile of GRbE was characterized by identifying the structure of the individual ingredients using NMR, and the concentration of …

Morinda Citrifolia L. (Noni) Improves The Quality Of Life In Adults With Osteoarthritis, Mian-Ying Wang, M. Nawal Lutfiyya, Vicki Weidenbacher-Hoper, Lin Peng, Martin S. Lipsky, Gary Anderson

Community Health Faculty Publications and Presentations

Background: Morinda citrifolia Linn (noni), as a “pain killer”, has been used as a traditional medicine by Polynesians for over 2000 years. It was reported to have a broad range of therapeutic effects including analgesic and anti-inflammation. The in-vitro and in vivoanti-inflammatory and analgesic properties of noni juice (NJ) suggest that NJ may be a useful adjunctive treatment for osteoarthritis (OA). In this pilot study we explored whether NJ improves the symptoms and Quality of Life (QoL) for adults with OA. We also sought to evaluate the tolerability and safety of NJ for patients with OA in …

Chemical Composition And Product Quality Control Of Turmeric (Curcuma Longa L.), Shiyou Li, Wei Yuan, Guangrui Deng, Ping Wang, Peiying Yang, Bharat Aggarwal

Faculty Publications

Chemical constituents of various tissues of turmeric (Curcuma longa L.) have been extensively investigated. To date, at least 235 compounds, primarily phenolic compounds and terpenoids have been identified from the species, including 22 diarylheptanoids and diarylpentanoids, eight phenylpropene and other phenolic compounds, 68 monoterpenes, 109 sesquiterpenes, five diterpenes, three triterpenoids, four sterols, two alkaloids, and 14 other compounds. Curcuminoids (diarylheptanoids) and essential oils are major bioactive ingredients showing various bioactivities in in vitro and in vivo bioassays. Curcuminoids in turmeric are primarily accumulated in rhizomes. The essential oils from leaves and flowers are usually dominated by monoterpenes while those from …

Development And Evaluation Of Therapeutics In The Setting Of Radiation Injury, Karin Emmons Thompson

Theses and Dissertations (ETD)

The possibility of an incident involving radiation exposure is at the forefront of public attention in the current global environment. With a greater number of entities possessing nuclear weapons and increased demand for nuclear power, the concern for uncontained exposure to radiation is increasing. In light of these developments, the need for treatments that may be easily stored and administered to large numbers of people who have been exposed to high doses of total body irradiation (TBI) is more urgent than ever before.

Our goal was to identify and develop novel, drug-like small molecules that would exhibit radiomitigating activity for …

Studies On Antidyslipidemic Effects Of Morinda Citrifolia (Noni) Fruit, Leaves And Root Extracts., Saf-Ur Rehman Mandukhail, Nauman Aziz, Anwar Gilani

Department of Biological & Biomedical Sciences

Background: The objective of present study was to provide the pharmacological basis for the medicinal use of Morinda citrifolia Linn in dyslipidemia using the aqueous-ethanolic extracts of its fruits (Mc.Cr.F), leaves (Mc.Cr.L) and roots (Mc.Cr.R). Results: Mc.Cr.F, Mc.Cr.L and Mc.Cr.R showed antidyslipidemic effects in both triton (WR-1339) and high fat diet-induced dyslipidemic rat models to variable extents. All three extracts caused reduction in total cholesterol and triglyceride levels in triton-induced dyslipidemia. In high fat diet-induced dyslipidemia all these extracts caused significant reduction in total cholesterol, triglyceride, low density lipoprotein-cholesterol (LDL-C), atherogenic index and TC/HDL ratio. Mc.Cr.R extract also caused increase …

The Marine Sponge Metabolite Mycothiazole: A Novel Prototype Mitochondrial Complex I Inhibitor., J Brian Morgan, Fakhri Mahdi, Yang Liu, Veena Coothankandaswamy, Mika B. Jekabsons, Tyler A. Johnson, Koneni V. Sashidhara, Phillip Crews, Dale G. Nagle, Yu-Dong Zhou

Natural Sciences and Mathematics | Faculty Scholarship

A natural product chemistry-based approach was applied to discover small-molecule inhibitors of hypoxia-inducible factor-1 (HIF-1). A Petrosaspongia mycofijiensis marine sponge extract yielded mycothiazole (1), a solid tumor selective compound with no known mechanism for its cell line-dependent cytotoxic activity. Compound 1 inhibited hypoxic HIF-1 signaling in tumor cells (IC(50) 1nM) that correlated with the suppression of hypoxia-stimulated tumor angiogenesis in vitro. However, 1 exhibited pronounced neurotoxicity in vitro. Mechanistic studies revealed that 1 selectively suppresses mitochondrial respiration at complex I (NADH-ubiquinone oxidoreductase). Unlike rotenone, MPP(+), annonaceous acetogenins, piericidin A, and other complex I inhibitors, mycothiazole is a mixed polyketide/peptide-derived compound …

Antispasmodic, Bronchodilator And Blood Pressure Lowering Properties Of Hypericum Oblongifolium - Possible Mechanism Of Action, Arif-Ullah Khan, Munasib Khan, Fazal Subhan, Anwar Gilani

Department of Biological & Biomedical Sciences

The crude extract of Hypericum oblongifolium (Ho.Cr), which tested positive for flavonoids, saponins and tannins caused concentration-dependent (0.1-1.0 mg/mL) relaxation of spontaneous and high K(+) (80 mM)-induced contractions in isolated rabbit jejunum preparations, suggesting a Ca(++) antagonistic effect, which was confirmed when pretreatment of the tissue with Ho.Cr produced a rightward shift in the Ca(++) concentration-response curves, like that caused by verapamil. Ho.Cr relaxed carbachol (1 mu M) and high K(+)-induced contractions in guinea pig tracheal preparations. It caused a dose-dependent (3-100 mg/kg) fall in arterial blood pressure of rats under anesthesia. In isolated guinea pig atria, Ho.Cr caused inhibition …

Discovery Of Quinic Acid Derivatives As Oral Anti-Inflammatory Agents, Kui Zeng

Theses and Dissertations (ETD)

Quinic acid (QA) esters found in hot water extracts of Uncaria tomentosa (a.k.a. Cat’s claw) exert anti-inflammatory activity through mechanisms involving inhibition of the pro-inflammatory transcription factor nuclear factor kappa B (NF-κB). Herein, we described the synthesis and biological testing of novel QA derivatives. Inhibition of NF-κB was assessed using A549 (Type II alveolar epithelial-like) cells that stably express a secreted alkaline phosphatase (SEAP) reporter driven by an NF-κB response element. A549- NF-κB cells were stimulated with TNF-α (10 ng/mL) in the presence or absence of QA derivative for 18 hours followed by measurement of SEAP activity. Amide substitution at …

Development And Validation Of A Rapid Method For The Detection Of Latrunculol A In Plasma., Jiajiu Shaw, Frederick A. Valeriote, Joseph Media, Tyler A. Johnson, Taro Amagata, Karen Tenney, Phillip Crews

Natural Sciences and Mathematics | Faculty Scholarship

Latrunculol A is a recently discovered 6,7-dihydroxy analog of the potent actin inhibitor latrunculin A. Latrunculol A has exhibited greater cytotoxicity than latrunculin A against both murine and human colon tumor cell lines in vitro. Currently, there are no reports regarding the bioavailability of latrunculol A in vivo. This study was undertaken as a prelude to pharmacokinetic assessments and it is the first work where bioavailability of latrunculol A was studied. In the present work, a simple plasma preparation and a rapid HPLC method have been developed. Mouse plasma containing latrunculol A was first treated by acetonitrile and then centrifuged …