Gustavo P. Cosenza

Medicinal plants and other botanical products from the Brazilian Official Pharmacopoeia

In this paper, we describe the results of a thorough survey in the four editions of the Brazilian Official Pharmacopoeia (FBRAS), in a search for data about the plants and other botanical products included in them. The growth of the pharmaceutical industry since the second half of last century markedly affected the Brazilian official medicine. The paper analyses the transformation within the Pharmacopoeia, focusing on the presence of Monographs for Native medicinal plants. The result showed a strong substitution of Native American medicinal plants by industrialized medicine and foreign medicinal plants in FBRAS and confirms the necessity of investiments in research for the validation of Brazilian Native plants.

Traditional uses of American plant species from the 1st edition of Brazilian Official Pharmacopoeia.

The first edition of the Brazilian Official Pharmacopoeia (FBRAS), published in 1929, is a rich source of information about American medicinal plants, since it lists species used in both traditional and conventional medicine. In this study, we have performed a survey of the traditional uses of plants described in eighty-seven Monographs from the FBRAS in twenty bibliographies written from the 19th century to the 1970s. Eighty-six different traditional uses are described in three or more books; some of them were cited in ten or more books, illustrating their widespread use and importance in medicine. The species from the first edition of the FBRAS have a long tradition of medical utility, which is confirmed by historical records. In surveying these medically relevant species, we hope to encourage policy makers and the scientific public as a whole to engage in a strong debate in an attempt to improve and facilitate the pharmacological study of these species.

Medicinal Plants Recommended by the World Health Organization: DNA Barcode Identification Associated with Chemical Analyses Guarantees Their Quality

Medicinal plants are used throughout the world, and the regulations defining their proper use, such as identification of the correct species and verification of the presence, purity and concentration of the required chemical compounds, are widely recognized. Herbal medicines are made from vegetal drugs, the processed products of medicinal species. These processed materials present a number of challenges in terms of botanical identification, and according to the World Health Organization (WHO), the use of incorrect species is a threat to consumer safety. The samples used in this study consisted of the dried leaves, flowers and roots of 257 samples from 8 distinct species approved by the WHO for the production of medicinal herbs and sold in Brazilian markets. Identification of the samples in this study using DNA barcoding (matK, rbcL and ITS2 regions) revealed that the level of substitutions may be as high as 71%. Using qualitative and quantitative chemical analyses, this study identified situations in which the correct species was being sold, but the chemical compounds were not present. Even more troubling, some samples identified as substitutions using DNA barcoding contained the chemical compounds from the correct species at the minimum required concentration. This last situation may lead to the use of unknown species or species whose safety for human consumption remains unknown. This study concludes that DNA barcoding should be used in a complementary manner for species identification with chemical analyses to detect and quantify the required chemical compounds, thus improving the quality of this class of medicines.

Bitter plants used as substitute of Cinchona spp. (quina) in Brazilian traditional medicine.

ETHNOPHARMACOLOGICAL RELEVANCE Bitter tasting plant species are used as tonics and have been previously used to treat intermittent fevers in Brazil, the principal symptom of malaria. Many of these species were named quina and were used as substitutes of Cinchona spp., the source of quinine. AIM OF THE STUDY To present data on these bitter species named quina and to discuss their potential as sources of bioactive substances. MATERIALS AND METHODS Data about the plants were obtained from a survey of the literature and documents written by early naturalists and clinical doctors living in the 18th and 19th centuries in Brazil. Correlated pharmacological studies were obtained from different scientific databases. RESULTS A total of 29 species were recorded. The largest number of species belonged to the Rubiaceae family (14), being Remijia ferruginea (A. St.-Hil) DC. the most representative. Strychnos pseudoquina A. St.-Hil. (Loganiaceae), Hortia brasiliana Vand. ex DC. (Rutaceae) and Solanum pseudoquina A. St.-Hil. (Solanaceae) were also frequently mentioned in the historical bibliography. Pharmacological studies have shown the presence of bitter bioactive substances useful to treat digestive disorders and/or with antimalarial activities, in all of the recorded botanic families. CONCLUSION This study shows that several bitter species named quina were used in the past as substitute of Cinchona spp. and studying these plants can lead to the development of new products.

Effect of triterpene saponins from roots of Ampelozizyphus amazonicus Ducke on diuresis in rats

ETHNOPHARMACOLOGICAL RELEVANCE Ampelozizyphus amazonicus Ducke is a plant used in Brazilian folk medicine to both prevent malaria and act as a depurative. AIM OF THE STUDY We have investigated the effects of an ethanol crude extract of roots of Ampelozizyphus amazonicus (CEAaD), a chemically characterized saponin mixture (SAPAaD), as well as a saponin-free fraction (SAPAaD-free) obtained from CEAaD on diuresis in rats. MATERIALS AND METHODS Wistar rats under ad libitum water conditions or water deprivation for 12h prior to the start of the experiment were volume-expanded with 0.9% NaCl (4% body weight, by gavage) containing either CEAaD, SAPAaD, or SAPAaD-free at the doses indicated in the text. Rats were individually housed in metabolic cages, and urine volume was measured every 30 min throughout the experiment (3 h). RESULTS CEAaD increased urine volume in rats under conditions of both free access to water and under water deprivation. In the latter condition, CEAaD (150 mg/kg) increased the urine volume from zero to 0.9+/-0.1 ml/120 min, n=6). Similarly, the SAPAaD-free (50-200 mg/kg) mixture also increased the urine volume. In contrast, SAPAaD (12.5-1000 mg/kg) produced a significant reduction (p<0.01) in diuresis under conditions of both water deprivation and with free access to water prior to the start of the experiment. CONCLUSION Our data indicate that CEAaD contains compounds that cause both diuresis and antidiuresis and that the antidiuretic effect is due mainly to the presence of saponins.

Nephroprotective Effect of Echinodorus macrophyllus Micheli on Gentamicin-Induced Nephrotoxicity in Rats

Background/Aims: Leaves of Echinodorus macrophyllus (EM), from the Alismataceae family, have been used in Brazilian folk medicine for their anti-inflammatory and diuretic properties. In this work, the diuretic and nephroprotective activities of crude extracts of EM were evaluated. Methods: Normal Wistar rats were given 0.9% NaCl containing either EM (10–300 mg/kg), furosemide (13 mg/kg) or arginine vasopressin (0.2 mg/kg). Thereafter, the rats were individually housed in metabolic cages, and urine volume was measured every 30 min for a total of 3 h. Acute kidney injury was induced by gentamicin (GM, 80 mg·kg–1·day–1, b.i.d., 5 days). Along with GM, 0.9% NaCl (control) or EM (30 mg/kg) was given to the rats by gavage. Results: EM produced a dose-dependent reduction in urine elimination. EM was effective in reversing all GM-induced alterations such as polyuria and glomerular filtration rate reduction. The GM-induced morphological alterations were not observed when EM was given concomitantly with GM. Conclusion: This study provides evidence that EM possesses nephroprotective effect which indicates that EM may have therapeutic applications in GM-induced acute kidney injury.

Morpho-anatomy and chemical profile of native species used as substitutes of quina (Cinchona spp.) in Brazilian traditional medicine. Part I: Polyouratea hexasperma

This research is part of a larger study of the Brazilian species that are commonly referred to as quinas and are usually used as substitute of Cinchona species. The purpose of the present study was the botanical characterization of the whole and powdered stem bark of Polyouratea hexasperma (A. St.-Hil.) Tiegh., Ochnaceae, by morphological and anatomical description, and the analysis of its chemical profile. The external texture of the bark, the whitened pit in the inner bark and the presence of cristarque cells, as well as the shape and arrangement of other lignified cells, are the most important macroscopic and microscopic features for the characterization of the bark. Chlorogenic and cafeic acids were detected in the chemical analysis and can also be used in the identification of the bark.

Euterpe oleracea pulp extract: Chemical analyses, antibiofilm activity against Staphylococcus aureus, cytotoxicity and interference on the activity of antimicrobial drugs

Euterpe oleracea (Açaí) fruit are widely consumed at the Brazilian Amazon region, and biological potentials such as immunomodulatory and antioxidant have been described for its extracts. However, its antimicrobial properties remain poorly investigated. Here, the antimicrobial and antibiofilm activities of the methanolic extract of an artisanally-manufactured açaí pulp (MEAP) were evaluated against clinical isolates of Staphylococcus aureus. Besides, MEAP interference on the activity of antimicrobial drugs of clinical relevance was explored, and its cytotoxicity against hepatocellular carcinoma cells (HepG2) was investigated. Biochemical and physicochemical properties of the pulp were investigated, and the presence of polyphenols on the extract was confirmed. For the first time, we report that the methanolic extract of açaí pulp is effective against planktonic cells and biofilms of S. aureus, and also decreased the proliferation of HepG2 cells. Statistically significant synergism was observed when the extract was combined to the tested antimicrobials except for erythromycin, and all biochemical and physicochemical parameters ranged within the accepted values established by the Brazilian legislation. Our data open doors for more studies on the antimicrobial activity of phytomolecules isolated from Euterpe oleracea extracts, and also for its combined use with antimicrobial drugs.

Influence of the preparation method on the low efficacy of multi-herb commercial products: the example of João da Costa e Associações

Native medicinal plants have been used for decades by Brazilian pharmaceutical companies to create commercial products. In this study, we have investigated the herb-combined product Joao da Costa e Associacoes® (JCA) commercialized for thirty years to treat dysmenorrhoea. JCA is prepared by decoction of Himatanthus lancifolius (Muell. Arg.) Woodson (Apocynaceae), Chondodendron platyphyllum Miers (Menispermaceae), Gossypium herbaceum L. (Malvaceae), Rosmarinus officinalis L. (Lamiaceae) and Echites peltata (Apocynaceae), followed by addition of sugar. The efficacy of JCA was verified by antinociceptive studies. The chemical composition was determined by fingerprint analysis in HPLC/ DAD. A weak inhibition of the second phase of the nociceptive effect induced by formalin indicated an activity similar to those steroids and not-steroids anti-inflammatories. Despite being prepared by decoction of five plants, the fingerprint analysis showed only two peaks. None of them corresponds to the chemical compounds observed in ethanol extracts prepared with the same plant material. We argue that the methods of preparation of the formulas should be considered in studies of multi-herbs products, since they can be the responsible for inefficacy or low activity of such products.