Chemical Composition and Antiproliferative Activity of the Ethanolic Extract of Cyperus articulatus L. (Cyperaceae).

Cyperus articulatus L. (Priprioca) is a plant of the Cyperaceae family traditionally used in traditional medicine in the Amazon region. Studies of the essential oil of this species have identified many terpene compounds. However, little is known about the possible uses of solid waste generated by the extraction of essential oils. This study aimed to investigate the chemical composition of volatile compounds and to evaluate the antiproliferative activity of the ethanolic extract of solid residues generated by the extraction of the essential oil of C. articulatus L. rizhomes in experimental models in vitro using peritoneal macrophages of mice and human tumor cell lines. The analysis of the chemical composition of volatile compounds indicated the presence of sesquiterpenes and particularly sequiterpenic ketones as main constituents. The results showed that the treatment with ethanolic extract of C. articulatus L. reduced the activity of the enzyme arginase and proliferation of cancer cells (p < 0.0001). The extract also showed no cytotoxicity in macrophages in concentrations between 12.5; 25 and 50 mg/mL (p < 0.0001). The results indicated that the extract of C. articulatus L. exerts antiproliferative activity (p < 0.0001) with low toxicity on healthy cells in experimental models in vitro.

Efficacy of Phytopharmaceuticals From the Amazonian Plant Libidibia ferrea for Wound Healing in Dogs.

We comparatively evaluate two distinct formulations containing 5% of Jucá (Libidibia ferrea) for wound healing in dogs. An excision model study was performed in 11 dogs with three dermal wounds in each animal, which were treated with: (1) topical phytopharmaceutical based on Carbopol (PyC) containing 5% Jucá ethanolic extract; (2) topical phytopharmaceutical based on Astrocaryum murumuru butter (PyM) containing 5% Jucá ethanolic extract; and (3) commercial ointment (control). Wound treatment was carried out on alternated days starting at day (D) one until D21. Macroscopic (all time-points) and histological (D0 and D21) analyses were performed. The antimicrobial activity of Jucá was evaluated through Minimal Inhibitory Concentration (MIC). Phytochemical analysis of Jucá revealed 3.1% phenolic compound content expressed in rutin and the presence of hydrolyzable tannins and flavonoids. The mean wound retraction was 33.7 ± 5.5, 34.0 ± 4.7, and 28.4 ± 4.9 % for PyC, PyM, and control groups, respectively, with higher wound retraction for both herbal-treated groups compared to the control (P < 0.05). Alcoholic extract of Jucá had antimicrobial activity against the microorganisms Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Candida krusei at different degrees, with MIC ranging from 250 to 16.625 µg/ml. Microscopic evaluation showed that the phytotherapic formulations contributed to better dermal wound healing through wound fibroplasia. The alcoholic extract of Jucá pods has great potential for wound healing in dogs and can be used in the development of commercially viable phytotherapic formulations.

Leishmanicidal activity of Piper marginatum Jacq. from Santarém-PA against Leishmania amazonensis.

Leishmaniasis is an infectious disease that has high endemicity and is among the six parasitic diseases of higher occurrence in the world. The current treatments are limited due to their toxicity, treatment resistance and high cost which have increased the search for new substances of natural origin for its therapy. Based on this, an in vitro biological and chemical investigation was carried out to evaluate the potential of Piper marginatum against Leishmania amazonesis. P. marginatum leaves were collected to obtain the essential oil (EO) and the ethanolic extract (CE). The chemical profile of the CE and fractions was obtained by 1H NMR. The analysis of the EO chemical composition was performed by GC-MS. EO, CE and fractions were submitted to antileishmanial and cytotoxicity assays against macrophages. The chromatographic profiles of EO, CE and fractions showed the presence of phenolic compounds and terpenoids, having 3,4-Methylenedioxypropiophenone as a major compound. All P. marginatum samples showed low toxicity to macrophages. The CE and the methanolic, hexane and ethyl acetate fractions had low cytotoxicity when compared to Pentamidine. All tested samples inhibited growth of L. amazonensis promastigotes. The antileishmanial activity of EO, CE and fractions were evaluated in macrophages infected with L. (L.) amazonensis and treated with the concentrations 1, 10 and 100 µg/mL for 48 h. All samples were active, but EO and CE showed superior activity against amastigote forms when compared to the promastigote forms of L. amazonensis. This work describes for the first time the antileishmanial activity of the species P. marginatum and its cytotoxicity against macrophages, suggesting that it can be an alternative source of natural products in the phytotherapeutic treatment of leishmaniasis.

In vitro and in vivo antimalarial activity of the volatile oil of Cyperus articulatus (Cyperaceae)

Malaria is a disease of global tropical distribution, being endemic in more than 90 countries and responsible for about 212 million cases worldwide in 2016. To date, the strategies used to eradicate this disease have been ineffective, without specific preventive measures such as vaccines. Currently, the existing therapeutic arsenal is limited and has become ineffective against the expansion of artemisinin-resistant Plasmodium, demonstrating the need for studies that would allow the development of new compounds against this disease. In this context, we studied the volatile oil obtained from rhizomes of Cyperus articulatus (VOCA), a plant species commonly found in the Amazon region and popularly used as a therapeutic alternative for the treatment of malaria, in order to confirm its potential as an antimalarial agent by in vitro and in vivo assays. We cultured Plasmodium falciparum W2 (chloroquine-resistant) and 3D7 (chloroquine-sensitive) strains in erythrocytes and exposed them to VOCA at different concentrations in 96-well microplates. In vivo antimalarial activity was tested in BALB/c mice inoculated with approximately 106 erythrocytes infected with Plasmodium berghei. VOCA showed a high antimalarial potential against the two P. falciparum strains, with IC50 = 1.21 µg mL-1 for W2 and 2.30 µg mL-1 for 3D7. VOCA also significantly reduced the parasitemia and anemia induced by P. berghei in mice. Our results confirmed the antimalarial potential of the volatile oil of Cyperus articulatus. (AU)