Background: Traditional remedies are an integral part of Colombian culture. Here we present the results of a three-year study of ethnopharmacology and folk-medicine use among the population of the Atlantic Coast of Colombia, specifically in department of Bolívar. We collected information related to different herbal medicinal uses of the local flora in the treatment of the most common human diseases and health disorders in the area, and determined the relative importance of the species surveyed. Methods: Data on the use of medicinal plants were collected using structured interviews and through observations and conversations with local communities. A total of 1225 participants were interviewed. Results: Approximately 30 uses were reported for plants in traditional medicine. The plant species with the highest fidelity level (Fl) were Crescentia cujete L. (flu), Eucalyptus globulus Labill. (flu and cough), Euphorbia tithymaloides L. (inflammation), Gliricidia_sepium_(Jacq.) Kunth (pruritic ailments), Heliotropium indicum L. (intestinal parasites) Malachra alceifolia Jacq. (inflammation), Matricaria chamomilla L. (colic) Mentha sativa L. (nervousness), Momordica charantia L. (intestinal parasites), Origanum vulgare L. (earache), Plantago major L. (inflammation) and Terminalia catappa L. (inflammation). The most frequent ailments reported were skin affections, inflammation of the respiratory tract, and gastro-intestinal disorders. The majority of the remedies were prepared from freshly collected plant material from the wild and from a single species only. The preparation of remedies included boiling infusions, extraction of fresh or dry whole plants, leaves, flowers, roots, fruits, and seeds. The parts of the plants most frequently used were the leaves. In this study were identified 39 plant species, which belong to 26 families. There was a high degree of consensus from informants on the medical indications of the different species. Conclusions: This study presents new research efforts and perspectives on the search for new drugs based on local uses of medicinal plants. It also sheds light on the dependence of rural communities in Colombia on medicinal plants.

Physalis peruviana is a native plant from the South American Andes and is widely used in traditional Colombian medicine of as an anti-inflammatory medicinal plant, specifically the leaves, calyces, and small stems in poultice form. Previous studies performed by our group on P. peruviana calyces showed potent anti-inflammatory activity in an enriched fraction obtained from an ether total extract. The objective of the present study was to obtain and elucidate the active compounds from this fraction and evaluate their anti-inflammatory activity in vivo and in vitro. The enriched fraction of P. peruviana was purified by several chromatographic methods to obtain an inseparable mixture of two new sucrose esters named peruviose A (1) and peruviose B (2). Structures of the new compounds were elucidated using spectroscopic methods and chemical transformations. The anti-inflammatory activity of the peruvioses mixture was evaluated using λ-carrageenan-induced paw edema in rats and lipopolysaccharide-activated peritoneal macrophages. Results showed that the peruvioses did not produce side effects on the liver and kidneys and significantly attenuated the inflammation induced by λ-carrageenan in a dosage-dependent manner, probably due to an inhibition of nitric oxide and prostaglandin E2, which was demonstrated in vitro. To our knowledge, this is the first report of the presence of sucrose esters in P. peruviana that showed a potent anti-inflammatory effect. These results suggest the potential of sucrose esters from the Physalis genus as a novel natural alternative to treat inflammatory diseases.

Physalis peruviana [cape gooseberry] is highly appreciated for its commercial value. The Colombian ecotype is in great demand in the international market, particularly for the unique morphological characteristics of the calyx, which has extended use as a traditional herbal remedy in Colombia because of its anti-inflammatory properties. In this work, the anti-inflammatory activity of the total ethereal extract of Physalis peruviana calyces was evaluated in preventive and therapeutic protocols in a TNBS acid-induced colitis rat model. Colitis was induced by intrarectal administration of TNBS. An evaluation of macroscopic and histopathological parameters in colonic tissue was performed, along with the determination of myeloperoxidase enzyme activity, cytokine levels and gene expression. Additionally, effects on nitric oxide release by lipopolysaccharide [LPS]-stimulated RAW264.7 macrophages and the scavenging activity of DPPH and ABTS free radicals were determined. The treatment with the Physalis peruviana extract produced a significant improvement in the colonic tissue at both macroscopic and histological levels. IL-1β and TNF-α production was reduced by the extract in both experimental approaches. The groups treated with Physalis peruviana showed a tendency to MUC2 up-regulation and down-regulation of COX-2, iNOS, NLRP3, IL-1β, IL-6 and IL-10 expression. Nitric oxide release in RAW264.7 macrophages was significantly inhibited. The Physalis peruviana extract showed intestinal anti-inflammatory activity in the TNBS-induced colitis model, placing this species’ calyx, a natural derivative, as a promising source of metabolites that could be used in treatment for inflammatory bowel disease.

Despite Cryptostegia grandiflora Roxb. ex R. Br. (Apocynaceae) leaves are widely used in folk Caribbean Colombian medicine for their anti-inflammatory effects, there are no studies that support this traditional use. Therefore, this work aimed to evaluate the effect of the total extract and primary fractions obtained from Cryptostegia grandiflora leaves, using in vivo and in vitro models of inflammation, and further get new insights on the mechanisms involved in this activity. Ethanolic extract of Cryptostegia grandiflora leaves, and its corresponding ether and dichloromethane fractions, significantly reduced inflammation and myeloperoxidase activity (MPO) in ear tissue of mice treated with 12-O-tetradecanoyl-phorbol-13-acetate (TPA). Histological analysis revealed a reduction of edema and leukocyte infiltration. Complementarily, we demonstrated that extract and fractions reduced nitric oxide (NO•) and prostaglandin E2 (PGE2) production in LPS-stimulated RAW 264.7 macrophages, as well as scavenging activity on DPPH and ABTS radicals. Our results demonstrated for the first time the anti-inflammatory activity of Cryptostegia grandiflora leaves, supporting its traditional use. This activity was related to inhibition of MPO activity, and PGE2 and NO• production. These mechanisms and its antioxidant activity could contribute, at least in part, to the anti-inflammatory effect showed by this plant.

Colorectal cancer (CRC) is a disease with high incidence and mortality, constituting the fourth most common cause of death from cancer worldwide. Naphthoquinones are attractive compounds due to their biological and structural properties. In this work, 36 naphthoquinone derivatives were synthesized and their activity evaluated against HT-29 cells. Overall, high to moderate anti-proliferative activity was observed in most members of the series, with 15 compounds classified as active (1.73 < IC₅₀ < 18.11 μM). The naphtho[2,3-b]thiophene-4,9-dione analogs showed potent cytotoxicity, 8-hydroxy-2-(thiophen-2-ylcarbonyl)naphtho[2,3-b]thiophene-4,9-dione being the compound with the highest potency and selectivity. Our results suggest that the toxicity is improved in molecules with tricyclic naphtho[2,3-b]furan-4,9-dione and naphtho[2,3-b]thiophene-4,9-dione systems 2-substituted with an electron-withdrawing group. A 3D-QSAR study of comparative molecular field analysis (CoMFA) was carried out, resulting in the generation of a reliable model (r² = 0.99 and q² = 0.625). This model allowed proposing five new compounds with two-fold higher theoretical anti-proliferative activity, which would be worthwhile to synthesize and evaluate. Further investigations will be needed to determine the mechanism involved in the effect of most active compounds which are potential candidates for new anticancer agents.

Anxiety disorders are highly prevalent, chronic, and disabling conditions that impose enormous health and economic costs both on individuals and on society. Medicinal plants are an invaluable source of bioactive metabolites that can be useful as new pharmacological treatment. Teas fromMentha spicataandPlantago majorare employed by Colombian populations to treat stress and insomnia. This work was conducted to evaluate their anxiolytic and hypnotic properties. For this, we employed the Elevated Plus‐Maze test and the sodium pentobarbital‐induced hypnosis method using Wistar rats. Oral administration ofM. spicataextract (1000 mg/Kg) significantly increased the exploration and time spent in the open arms, which indicates its anxiolytic activity. On the other hand, bothM. spicataandP. majorextracts (1000 mg/Kg) remarkably augmented the sleeping time induced by pentobarbital, suggesting a sedative and hypnotic effect of the plants extracts. In addition, the acute toxicological study demonstrated that the doses used did not induce mortality or toxicity effects at hepatic or renal level. The bioactivity seems to be related to several kinds of constituents, mainly phenolic compounds such as flavonoids and tannins. In conclusion, these results reinforce the potential use of these species in the therapy of anxiety.