Medicinal Plants and Other Living Organisms with Antitumor Potential against Lung Cancer

Lung cancer is a disease with high morbidity and mortality rates. As a result, it is often associated with a significant amount of suffering and a general decrease in the quality of life. Herbal medicines are recognized as an attractive approach to lung cancer therapy with little side effects and are a major source of new drugs. The aim of this work was to review the medicinal plants and other living organisms with antitumor potential against lung cancer. The assays were conducted with animals and humans, and Lewis lung carcinoma was the most used experimental model. China, Japan, South Korea, and Ethiopia were the countries that most published studies of species with antitumor activity. Of the 38 plants evaluated, 27 demonstrated antitumor activity. In addition, six other living organisms were cited for antitumor activity against lung cancer. Mechanisms of action, combination with chemotherapeutic drugs, and new technologies to increase activity and reduce the toxicity of the treatment are discussed. This review was based on the NAPRALERT databank, Web of Science, and Chemical Abstracts. This work shows that natural products from plants continue to be a rich source of herbal medicines or biologically active compounds against cancer

SYNTHESIS, IN SILICO CHARACTERIZATION AND EX VIVO EVALUATION OF THE NOVEL ORGANIC NITRATE NDIBP AS A POTENTIAL VASORELAXANT AGENT

Objective: This study aimed to describe the synthesis and biological/pharmacokinetic potential of the 1,3-diisobutoxypropan-2-yl nitrate (NDIBP) using in silico and ex vivo approaches. Methods: The compound was characterized by Fourier-transform infrared spectroscopy and 1H and 13C- nuclear magnetic resonance spectra. NDIBP biological activity spectrum was obtained by Prediction of Activity Spectra for Substances (PASS). The pharmacological effect was validated in ex vivo studies using mesenteric artery. Drug-like properties and Absorption Distribution Metabolism Excretion and Toxicity (ADMET) studies were carried out by pkCSM (Predicting Small-Molecule Pharmacokinetic Properties Using Graph-Based Signatures) software. Results: PASS prediction indicated NDIBP as nitric oxide (NO) donor with vasodilator effect. Ex vivo studies validated PASS analysis and showed the NDIBP vasorelaxant activity in mesenteric arteries. Physicochemical parameters and ADMET prediction suggested that NDIBP is a drug-like molecule with a good theoretical oral bioavailability, good absorption in the gastrointestinal tract, and a low distribution in the tissues. Conclusion: All the data indicated that NDIBP possesses biological activities and drug-like properties to be considered as a vasorelaxant agent and a good candidate for further investigation in the treatment of arterial hypertension and drug development studies

Neolignans from Licaria chrysophylla and Licaria aurea with DNA topoisomerase II-α inhibitory activity

Seven natural neolignans isolated from Licaria chrysophylla and Licaria aurea along with five semisynthetic derivatives were tested for their inhibitory action on DNA-topoisomerase by relaxation assays on pBR322 plasmid DNA. All compounds tested showed strong inhibition at a concentration of 100 µM, while none showed activity between 5 and 70 µM. These results indicate that no obvious correlation can be derived between the structure of these compounds and their inhibitory effect on the DNA relaxation activity of topoisomerase II. This is the first report on DNA topoisomerase II inhibitors from Licaria chrysophylla and Licaria aurea leading to the identification of lignoids as topoisomerase II-α inhibitors

Traditional Uses, Chemical Constituents, and Biological Activities of Bixa orellana

Bixa orellana L., popularly known as “urucum,” has been used by indigenous communities in Brazil and other tropical countries for several biological applications, which indicates its potential use as an active ingredient in pharmaceutical products. The aim of this work was to report the main evidence found in the literature, concerning the ethnopharmacology, the biological activity, and the phytochemistry studies related to Bixa orellana L. Therefore, this work comprises a systematic review about the use of Bixa orellana in the American continent and analysis of the data collected. This study shows the well-characterized pharmacological actions that may be considered relevant for the future development of an innovative therapeutic agent

Tannins, Peptic Ulcers and Related Mechanisms

This review of the current literature aims to study correlations between the chemical structure and gastric anti-ulcer activity of tannins. Tannins are used in medicine primarily because of their astringent properties. These properties are due to the fact that tannins react with the tissue proteins with which they come into contact. In gastric ulcers, this tannin-protein complex layer protects the stomach by promoting greater resistance to chemical and mechanical injury or irritation. Moreover, in several experimental models of gastric ulcer, tannins have been shown to present antioxidant activity, promote tissue repair, exhibit anti Helicobacter pylori effects, and they are involved in gastrointestinal tract anti-inflammatory processes. The presence of tannins explains the anti-ulcer effects of many natural products

The Antinociceptive and Anti-Inflammatory Activities of Caulerpin, a Bisindole Alkaloid Isolated from Seaweeds of the Genus Caulerpa

The antinociceptive and anti-inflammatory activity of caulerpin was investigated. This bisindole alkaloid was isolated from the lipoid extract of Caulerpa racemosa and its structure was identified by spectroscopic methods, including IR and NMR techniques. The pharmacological assays used were the writhing and the hot plate tests, the formalin-induced pain, the capsaicin-induced ear edema and the carrageenan-induced peritonitis. Caulerpin was given orally at a concentration of 100 μmol/kg. In the abdominal constriction test caulerpin showed reduction in the acetic acid-induced nociception at 0.0945 μmol (0.0103–1.0984) and for dypirone it was 0.0426 μmol (0.0092–0.1972). In the hot plate test in vivo the inhibition of nociception by caulerpin (100 μmol/kg, p.o.) was also favorable. This result suggests that this compound exhibits a central activity, without changing the motor activity (seen in the rotarod test). Caulerpin (100 μmol/kg, p.o.) reduced the formalin effects in both phases by 35.4% and 45.6%, respectively. The possible anti-inflammatory activity observed in the second phase in the formalin test of caulerpin (100 μmol/kg, p.o.) was confirmed on the capsaicin-induced ear edema model, where an inhibition of 55.8% was presented. Indeed, it was also observed in the carrageenan-induced peritonitis that caulerpin (100 μmol/kg, p.o.) exhibited anti-inflammatory activity, reducing significantly the number of recruit cells by 48.3%. Pharmacological studies are continuing in order to characterize the mechanism(s) responsible for the antinociceptive and anti-inflammatory actions and also to identify other active principles present in Caulerpa racemosa

Database Survey of Anti-Inflammatory Plants in South America: A Review

Inflammation is a complex event linked to tissue damage whether by bacteria, physical trauma, chemical, heat or any other phenomenon. This physiological response is coordinated largely by a variety of chemical mediators that are released from the epithelium, the immunocytes and nerves of the lamina propria. However, if the factor that triggers the inflammation persists, the inflammation can become relentless, leading to an intensification of the lesion. The present work is a literature survey of plant extracts from the South American continent that have been reported to show anti-inflammatory activity. This review refers to 63 bacterial families of which the following stood out: Asteraceae, Fabaceae, Euphorbiaceae, Apocynaceae and Celastraceae, with their countries, parts used, types of extract used, model bioassays, organisms tested and their activity

Synthesis, characterization and evaluation of the activity of ten mesoionic compounds against microorganisms

Tres mesoiónicos 1,3,4-tiadiazolio-2-tiolato siete cloruros 1,3,4-triazolio-2-tiol se han sintetizado y se ha probado su actividad contra distintos microoganismos. Las estructuras químicas se determinaron por Análisis Elemental, IR, Masa y espectrometría de RMN 1H e 13C. Las pruebas biológicas indican que los compuestos tienen actividad sustancial contra bacterias Gram positivas y alcohol-ácido-resistentes, actividad moderada contra levaduras, escasa actividad contra otros hongos y son inactivos contra las bacterias Gram negativas ensayadas.Three mesoionic 1,3,4-thiadiazoliuin-2-thiolates and seven 1,3,4-triazolium-2-thiol chlorides have been synthesised and tested for activity against a range of microorganisms. The chemical structures were confirmed by Elemental Analysis, IK, Mass, 1H and 13C NMR spectrometry. The biological tests indicate that the compounds have substantial activity against Gram-positive and alcohol-acid-resistant bacteria; moderate activity against yeasts and little activity against other fungi and are inactive against Gram-negative bacteria.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Synthesis, characterization and evaluation of the activity of ten mesoionic compounds against microorganisms

Tres mesoiónicos 1,3,4-tiadiazolio-2-tiolato siete cloruros 1,3,4-triazolio-2-tiol se han sintetizado y se ha probado su actividad contra distintos microoganismos. Las estructuras químicas se determinaron por Análisis Elemental, IR, Masa y espectrometría de RMN 1H e 13C. Las pruebas biológicas indican que los compuestos tienen actividad sustancial contra bacterias Gram positivas y alcohol-ácido-resistentes, actividad moderada contra levaduras, escasa actividad contra otros hongos y son inactivos contra las bacterias Gram negativas ensayadas.Three mesoionic 1,3,4-thiadiazoliuin-2-thiolates and seven 1,3,4-triazolium-2-thiol chlorides have been synthesised and tested for activity against a range of microorganisms. The chemical structures were confirmed by Elemental Analysis, IK, Mass, 1H and 13C NMR spectrometry. The biological tests indicate that the compounds have substantial activity against Gram-positive and alcohol-acid-resistant bacteria; moderate activity against yeasts and little activity against other fungi and are inactive against Gram-negative bacteria.Colegio de Farmacéuticos de la Provincia de Buenos Aire