Industrial Scale Isolation, Structural and Spectroscopic Characterization of Epiisopiloturine from Pilocarpus microphyllus Stapf Leaves: A Promising Alkaloid against Schistosomiasis.

This paper presents an industrial scale process for extraction, purification, and isolation of epiisopiloturine (EPI) (2(3H)-Furanone,dihydro-3-(hydroxyphenylmethyl)-4-[(1-methyl-1H-imidazol-4-yl)methyl]-, [3S-[3a(R*),4b]]), which is an alkaloid from jaborandi leaves (Pilocarpus microphyllus Stapf). Additionally for the first time a set of structural and spectroscopic techniques were used to characterize this alkaloid. EPI has shown schistomicidal activity against adults and young forms, as well as the reduction of the egg laying adult worms and low toxicity to mammalian cells (in vitro). At first, the extraction of EPI was done with toluene and methylene chloride to obtain a solution that was alkalinized with ammonium carbonate. The remaining solution was treated in sequence by acidification, filtration and alkalinization. These industrial procedures are necessary in order to remove impurities and subsequent application of the high performance liquid chromatography (HPLC). The HPLC was employed also to remove other alkaloids, to obtain EPI purity higher than 98%. The viability of the method was confirmed through HPLC and electrospray mass spectrometry, that yielded a pseudo molecular ion of m/z equal to 287.1 Da. EPI structure was characterized by single crystal X-ray diffraction (XRD), (1)H and (13)C nuclear magnetic resonance (NMR) in deuterated methanol/chloroform solution, vibrational spectroscopy and mass coupled thermal analyses. EPI molecule presents a parallel alignment of the benzene and the methyl imidazol ring separated by an interplanar spacing of 3.758 Å indicating a π-π bond interaction. The imidazole alkaloid melts at 225°C and decomposes above 230°C under air. EPI structure was used in theoretical Density Functional Theory calculations, considering the single crystal XRD data in order to simulate the NMR, infrared and Raman spectra of the molecule, and performs the signals attribution.

[Prevalence of the use of anabolic agents among strength training apprentices in Porto Alegre, RS]. / Prevalência do uso de agentes anabólicos em praticantes de musculação de Porto Alegre.

This study aimed to determine through a questionnaire applied to interviewers, the current or past use of anabolic androgenic steroids (AAS), as well as other hormones (OH), and other medicines (OM), food supplement and illicit drugs among strength training apprentices in the city of Porto Alegre, RS. We interviewed 288 subjects draw from a sample of 13 gyms. The prevalence of current and past use of AAS was about 11.1% (32/288), OH 5.2% (16/288) and OM 4.2% (12/288). The most used AAS were nandrolone and stanozolol; the OH were gonadotropin, triiodothyronine (T3) and OM, like lipostabil, diuretics and veterinary medicines (Monovin E). The most frequent side-effects were behavioral such as humor oscillation, irritability and hostility, and endocrine disturbances such as acne and increased or decreased libido. When analyzed together with other hormones in a variable named "hormonal agents" (AH), AAS presented a statistical difference (p< 0.05) among genders considering that the most frequent use of AH occurred among men and those who consume food supplements. The comparison of these findings to other national and international results is difficult due to the epidemiological design. Even if it is considered, the observed prevalence suggests that preventive attitudes as well as special care in the orientation and education of this population must be taken.

Prevalência do uso de agentes anabólicos em praticantes de musculação de Porto Alegre / Prevalence of the use of anabolic agents among strength training apprentices in Porto Alegre, RS

Este estudo procura determinar, através de questionário realizado por entrevistadores, a prevalência do uso atual ou passado de esteróides anabólicos androgênicos (EAA), outros hormônios (OH), outros medicamentos (OM) e outras substâncias (suplementos alimentares e drogas ilícitas) em praticantes de musculação da cidade de Porto Alegre, entrevistando 288 indivíduos sorteados de uma amostra de 13 academias. A prevalência observada foi de 11,1 por cento (32/288) para EAA, 5,2 por cento (16/288) para OH e 4,2 por cento (12/288) para OM. Os EAA mais usados foram decanoato de nandrolona e estanozolol. Os OH foram gonadotrofina coriônica humana, triiodotironina e OM como lipostabil, diuréticos e medicamentos veterinários (ex.: Monovin E). Os efeitos colaterais mais freqüentes foram comportamentais (variação de humor, irritabilidade e agressividade) e endócrinos (acne e aumento/ diminuição da libido). Quando analisados os EAA juntamente aos OH na variável denominada "agentes hormonais" (AH), observamos diferença estatística (p< 0,05) entre os sexos, sendo o uso de AH mais prevalente em homens e entre os consumidores de suplementos alimentares. Comparar este estudo a outros é difícil, pois existe diferença no desenho epidemiológico. Entretanto, a alta prevalência observada sugere a necessidade de medidas preventivas, educativas e de cuidados na assistência desta população.

This study aimed to determine through a questionnaire applied to interviewers, the current or past use of anabolic androgenic steroids (AAS), as well as other hormones (OH), and other medicines (OM), food supplement and illicit drugs among strength training apprentices in the city of Porto Alegre, RS. We interviewed 288 subjects draw from a sample of 13 gyms. The prevalence of current and past use of AAS was about 11.1 percent (32/288), OH 5.2 percent (16/288) and OM 4.2 percent (12/288). The most used AAS were nandrolone and stanozolol; the OH were gonadotropin, triiodothyronine (T3) and OM, like lipostabil, diuretics and veterinary medicines (Monovin E). The most frequent side-effects were behavioral such as humor oscillation, irritability and hostility, and endocrine disturbances such as acne and increased or decreased libido. When analyzed together with other hormones in a variable named "hormonal agents" (AH), AAS presented a statistical difference (p< 0.05) among genders considering that the most frequent use of AH occurred among men and those who consume food supplements. The comparison of these findings to other national and international results is difficult due to the epidemiological design. Even if it is considered, the observed prevalence suggests that preventive attitudes as well as special care in the orientation and education of this population must be taken.