UNIVERSIDAD DE GUAYAQUIL DEPARTMENT OF CHEMICAL SCIENCES



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CODE: 38/05 TITLE: Establishment of the potential anti-inflammatory effect of the product known as CUMANDA, originating from NutraMedix Laboratories, LLC, Florida OBJECTIVES: To study the possible anti-inflammatory effect of CUMANDA, measured by auricular 1 edemas 2 in laboratory mice. BACKGROUND: The auricular edema is achieved by applying 12-0- Tetradecanoil Forbol-13 Acetate (TPA), one of the components responsible for the irritating action of croton oil, into the auditory pavilion of the mouse. The inflammatory reaction consists of erythema 3, edema and infiltration by polymorphonuclear leukocytes 4. As such, eicosanoid 5 -type mediators are freed, inducing degranulation of the mast cell 6. This technique thus allows the evaluation of the inhibiting substances of the biosynthesis of prostaglandins 7 and leukotrienes 8. 1 Of or pertaining to the outer ear. 2 The swelling of soft tissues as a result of excess water accumulation 3 Redness of the skin. 4 A type of white blood cell with a nucleus that is so deeply lobated or divided that the cell looks to have multiple nuclei. Informally called a poly. 5 A lipid mediator of inflammation derived from the 20-carbon atom arachidonic acid or a similar fatty acid. The eicosanoids include the prostaglandins, prostacyclin, thromboxane, and leukotrienes. 6 A connective tissue cell whose normal function is unknown but which is frequently injured in allergic reactions, releasing chemicals including histamine that are very irritating and cause itching, swelling, and fluid leakage from cells. 7 One of a number of hormone-like substances that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation. Prostaglandins are derived from a chemical called arachidonic acid. 1

As discussed in numerous international works, the pharmacological study of the abovementioned effect is indispensable, and guarantees (within the margin of error associated with the technique) that the potential for producing anti-inflammatory effects in humans will be learned. The basis of this work is the pharmacological effect as an anti-inflammatory, as described in international literature (1, 2). TECHNICAL, SCIENTIFIC AND SOCIOECONOMIC BENEFITS: The demonstration of this product as an anti-inflammatory is important due to its potential as a new, plant-based medication, with its associated low toxicity. This was demonstrated by us in a previous work, allowing us to enter the product as a new medication in the appropriate Register. VARIABLES TO MEASURE: 1- Weight of the treated and untreated ears 2- % of Inflammation 3- % of inhibition PROCEDURES TO FOLLOW: TEST MATERIALS: Cumanda: The procedure followed was that described by CYTED (1996) and the Gerhard Voegel (1997). CHANGES IN THE CURRICULUM: Changes did not take place in protocol proposed to the Unity of Quality Guarantee, whose number is referred to on Page 1. 8 One of a group of hormones that cause the symptoms of hayfever and asthma. Derived from arachidonic acid, the leukotrienes act by mediating immediate hypersensitivity. Leukotriene modifiers that prevent the production or action of leukotrienes are used to treat hayfever and asthma. 2

DATA FROM THE SAMPLE: Organization soliciting services: NutraMedix Laboratories, LLC. Person in charge of the Organization s application: Jose Icaza Date of application: 4/20/05 Person in charge in the Executor Organization: MSc. Gastón Garcia Simón. Storage: The product was stored at room temperature with controlled access. Organization that carried out the work: University of Guayaquil, Department of Chemical Sciences. Address: Ciudadela Universitaria Dr. Salvador Allende Form of presentation of the product: amber glass drop bottle containing 30 milliliters Storage: The product was maintained at room temperature before and during the experiment, and as indicated was protected from light and kept in a locked cabinet. INFORMATION WITH RESPECT TO THE HANDLING: No special handling instructions were needed. COMPOSITION OF THE PRODUCT: Cumanda bark extract Mineral water Ethanol (20 25%) 3

EXPERIMENTAL PROCEDURE: INTRODUCTION This experiment was carried out with the intention of determining the possible anti-inflammatory effect of CUMANDA, utilizing croton oil as the inflammatory agent. DOSAGE USED IN THE TEST: 5 ml of Cumanda per kg of animal's body weight. PRINCIPAL TEST: METHODS AND TECHNIQUES: Study Material: Cumanda Animal Model: A single rodent species (mouse) was utilized, with a minimum of 5 animals of a single sex in each group. In this case, male mice with an average weight within ± 20% (3), belonging to the Swiss line and coming from the Chemistry Department of the University of Guayaquil were appropriate and were utilized in the experiment. The animals were maintained in quarantine conditions and were acclimated according to established procedures (4, 5), said period having a duration of five days minimum. Access to the water and the food was "ad libitum. (6, 7) 4

The animals were randomly distributed from within the different groups. (8) Food was denied 4 hours before exposure to the test material. The experiment lasted 6 days (5 of acclimation and 1 of test) DEVELOPMENT OF THE METHOD: The following three groups were constructed for the test: TEST GROUPS 1 Oil of croton 20L 2 Oil of croton 20L + Feldene 9 that covered the two sides of the auditory pavilion. 3 Oil of croton 20L + 5 ml of Cumanda per kilo of mouse body weight The mice were denied food for four hours then weighed, after which began the experiment. 9 Feldene (generic name Piroxicam) is a nonsteroidal anti-inflammatory drug (NSAID) effective in treating fever, pain, and inflammation in the body. 5

The irritant solution of 5% croton oil in acetone was applied topically in the right ear, at the indicated volume, using an automatic pipette. The composite solution of Feldene and Croton was administered topically in the right ear immediately after the irritant, in the indicated volume, while Cumanda was administered orally. One hour after the application of the irritant, the animals are euthanized in a saturated ether atmosphere, and their ears are cut along the edge. 6 mm discs were cut with a punch then weighed. RESULTS CALCULATIONS: Outcomes are rated by calculating the weight of each mouse s ears, both the treated and untreated. The percentage of inflammation of the treated as opposed to the untreated ear is calculated using the following formula: % Inflammation = T x 100-100 ST Where T is the average of the weights of the treated ears (right) and ST is the average of the weights of the untreated ears (left). % Inhibition of inflammation = C - T x 100 C Where C is the average value of % of inflammation of the animals of the control group and T is the average value of % of inflammation of the animals of the control problem group or control. 6

DESCRIPTION OF THE DOSAGE, METHOD OF ADMINISTRATION AND DURATION OF THE TEST: The test was achieved by following the method established by CYTED and using the dose of 50L each mouse. The Cumanda was administered orally: 0.1mL per 20 g of mouse body weight using a intragastric canula. The irritant and the composite solution of Feldene and the irritant were applied in the right auditory pavilion of the study animals, the left auditory pavilion being the control. ANALITICAL RESULTS: The results of the average value of the weights of the right and left ears are found in Table #1. 7

DEPARTMENT OF CHEMICAL SCIENCIES TABLE # 1. STUDY OF THE POSSIBLE ANTI-INFLAMMATORY EFFECT OF CUMANDA. Weight Of Ears In mg Group Right Ear Left Ear Control group treated with oil of croton Mean ± standard deviation 15.5 ±1.06 9.06 ± 0.9 Croton + Feldene Mean ± standard deviation 9.42 ± 0.3 9.3 ± 0.4 Croton + Cumanda Mean ± standard deviation 9.88 ± 1.06 9.70 ± 0.71 The percentages of inflammation and of inhibition of inflammation which appear in Table 2 were calculated with these values. 8

DEPARTMENT OF CHEMICAL SCIENCIES TABLE # 2. STUDY OF THE POSSIBLE ANTI-INFLAMMATORY EFFECT OF CUMANDA. Inflammation and Inhibition Percentages (%) Group % Inflammation % Inhibition Croton 72 - Croton + Feldene 1.29 98 Croton + CUMANDA 1.8 97 As can be seen from the table, Feldene 0.5% (Piroxicam) demonstrated a marked anti-inflammatory effect, as did the Cumanda which showed a similar effect. 9

CONCLUSIONS: 1- Cumanda was demonstrated to have a marked anti-inflammatory effect in the animal subjects, in that it is capable of diminishing inflammation from Croton oil. 2- Feldene was also shown to have the effect for which it is sold. GENERAL CONCLUSIONS: Cumanda was demonstrated to have anti-inflammatory effect similar to Feldene and can be used to address inflammation from inflammatory agents such as Croton oil, as observed in animal testing and as appears in specialized literature. PERSONNEL RESPONSIBLE FOR THE STUDY: Responsible Professional: MSc. Gastón García Simón Date: 05/27/05 Signature: 10

BIBLIOGRAPHY: 1- CYTED course for Researchers in the Discovery of new medicines, Lima November 1996, Edema Earpiece pp 83. 2- Drugs Discovery, Gerhard Voegel (1997). 3- Procedure. Bodily weight of mice 4- Procedure. Guide for the care of laboratory animals 5- Procedure. Quarantine 6- Procedure. Sub-minister of Water, Usage Manual. 7- Procedure. Random Allocation of rodent species 8- Procedure. Euthanesia 9- Pink W. Statistics for toxicology, in Principles and methods of Toxicology, W. Hayes, ed. Raven Press, N:Y: 1994 11