Green nanoarchitectonics of carbon quantum dots from Cinchona Pubescens Vahl as targeted and controlled drug cancer nanocarrier.

Carbon quantum dots (CQDs) are a new carbon-based nanomaterial that has attracted tremendous attention due to their excellent fluorescent properties, chemical stability, water solubility, and biocompatibility features. Here, fluorescent CQDs synthesized by a green nanoarchitectonic method using Cinchona Pubescens Vahl extract were evaluated as drug nanocarriers for carboplatin (CBP) delivery. The characterization methods showed CQDs with semispherical shapes and sizes around 5 nm, temperature- and pH-dependent functional groups that interact with the CBP molecule adding specificity to the drug-delivery system. Based on the load efficiency results, it seems that the CQDs can carry almost 100 µg of carboplatin for every 1 mg of CQDs. This is possible due to the self-assembly process that takes place through the interaction between the protonation/deprotonation functional groups of CQDs and the hydrolyzed CBP molecule. Through this process, it is created spherical nanoparticles with an average size of 77.44 nm. The CQDs-CBP nanoparticles release the drug through a diffusion-controlled release mechanism where the acidic media is preferred, and the EPR effect also plays a helpful role. Besides, the viability test shows that the CQDs have almost null cytotoxicity suggesting that they could be used as a promising cancer treatment, improving the efficiency of cell internalization and significantly increasing their drug delivery.

Familiar Dermatologic Drugs as Therapies for COVID-19. / Fármacos de uso frecuente en dermatología como terapia para COVID-19.

Researchers the world over are working to find the treatments needed to reduce the negative effects of coronavirus disease 2019 (COVID-19) and improve the current prognosis of patients. Several drugs that are often used in dermatology are among the potentially useful treatments: ivermectin, antiandrogenic agents, melatonin, and the antimalarial drugs chloroquine and hydroxychloroquine. These and other agents, some of which have proven controversial, are being scrutinized by the scientific community. We briefly review the aforementioned dermatologic drugs and describe the most recent findings relevant to their use against COVID-19.

The use of an integrated molecular-, chemical- and biological-based approach for promoting the better use and conservation of medicinal species: a case study of Brazilian quinas.

ETHNOPHARMACOLOGICAL RELEVANCE: Quina is a popular name originally attributed to Cinchona pubescens Vahl (=Cinchona succirubra) and Cinchona. calisaya Wedd., species native from Peru that have the antimalarial alkaloid quinine. In Brazil, bitter barks substitutes for the Peruvian species began to be used centuries ago, and they still are sold in popular markets. To assess the authenticity and the conditions on which samples of quinas have been commercialized, using the DNA barcode, chemical and biological assays. MATERIALS AND METHODS: Starting with 28 samples of barks acquired on a popular market, 23 had their DNA extracted successfully. The regions matK and rbcL were amplified and sequenced for 15 and 23 samples, respectively. Phytochemical analyses were performed by chromatographic methods, and biological essays were done by antimalarial tests in vitro. RESULTS: The identified species belonged to six different families, many of them endangered or with no correlation with use in traditional medicine as a Brazilian quina. The absence of typical bitter chemical substances indicated that barks have been collected from other species or from very young trees. The results of biological essays confirm the lack of standardization of the sold materials. CONCLUSION: The integrated approaches proved to be efficient to evaluate medicinal plants sold in popular markets and can be useful for promoting their better use and conservation.

Cuantificación de quinina en extractos de Cinchona pubescens y evaluación de la actividad antiplasmodial y citotóxica / Quantification of quinine in extracts from stems Cinchona pubescens and evaluation of antiplasmodial and cytotoxic activity

Plants belonging to the genus Cinchona L. (Rubiaceae), whose active ingredient is quinine, was used for centuries to treat malaria. Plants of this genus are a potential source of new structural templates in the search for new antimalarial candidates. This study aimed to the identification, quantification of quinine and other metabolites present in extracts of different polarity of the stems of Cinchona pubescens Vahl. , oxoquinovic acid isolation, antiplasmodial activity, and measuring its cytotoxic effect. The results show a high activity to antiplasmodial alkaloids extract (IC50 = 2.20 +/- 0.0325 ug/mL), cytotoxicity (CC50 = 80.2 +/- 12.2 ug/mL), and a quinine content of 21.3+/-0.0247 ppm. The compound known as acid antiplasmodial activity oxoquinovic presented in IC50 = 11.3 +/- 0.741 ug/mL, and cytotoxicity CC50 = 72.4 +/- 3.85 ug/mL. These results motivate phytochemical studies in the search for active structural analogues quinine and quinolinic core as a source of new antimalarial agents.

Las plantas pertenecientes al género Cinchona L. (familia Rubiaceae), cuyo principio activo es la quinina, fueron utilizadas durante siglos para tratar la malaria. Este género es una fuente potencial de nuevas plantillas estructurales en la búsqueda de nuevos candidatos antimaláricos. El presente trabajo tuvo como objetivo la identificación y, cuantificación de la quinina y de otros metabolitos presentes en los extractos de diferente polaridad, de los tallos de Cinchona pubescens Vahl. , el aislamiento del ácido oxoquinóvico, la actividad antiplasmodial y, además, la medición de su efecto citotóxico. Los resultados muestran una alta actividad antiplasmodial para el extracto de los alcaloides (IC50 = 2,20 +/- 0,0325 ug/mL), una baja citotoxicidad (CC50 = 80,2 +/- 12,2 ug/mL), y un alto contenido de quinina el cual fue 21,3+/-0,0247 ppm. El compuesto ácido oxoquinóvico presentó una actividad antiplasmodial de IC50 = 11,3 +/- 0.741 ug/mL, y una citotoxicidad de CC50 = 72,4 +/- 3,85 ug/mL. Estos resultados motivan los estudios fitoquímicos en la búsqueda de principios activos y análogos estructurales en diferentes especies de Cinchonas como una fuente de nuevos agentes antimaláricos.

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.

Estudio químico de los tallos de Cinchona Pubescens / Chemical study of Cinchona Pubescens stems

De los tallos de Cinchona pubescens que fueron colectados en la localidad de Yuracmallo (a 1 380 msnm, distrito de San Juan de Oro, Provincia de Sandia, Dpto. Puno) se aisló la quinina, que fue identificada mediante sus espectros de Masas, RMN1H, RMN13C y 1H-1H COSY. Además, se realizó el análisis cualitativo de sus metabolitos secundarios.

From the stems of the Cinchona pubescens, wich were collected in the locality Yuracmallo (Province of Sandia, Puno), quinine was obtained, wich was identified by the mass spectra, RMN1H, RMN13C and 1H-1H COSY. Furthermore, the qualitative analysis of the secondary metabolites was done.

Antimalarial activity of Cinchona-like plants used to treat fever and malaria in Brazil.

For centuries, malaria was treated with the bark of Cinchona calisaya and Cinchona succirubra plants named "quinas" in Brazil, from which the quinine molecule was isolated. Other plant species known also as "quinas" are used to treat fever and malaria, like Deianira erubescens (roots and leaves), Strychnos pseudoquina (bark), and Remijia ferruginea (bark). Based on this popular knowledge, we evaluated the in vivo antimalarial activity of the ethanol crude extracts of these plant species in mice infected with Plasmodium berghei. Only Remijia ferruginea showed antimalarial activity, reducing parasitaemia and mortality at the highest dose tested. Its phytochemical analysis showed the presence of alkaloids but not quinine. The other two plant species were inactive.

Voto de un ministro togado de la Audiencia de Quito / Vote of a minister magistrate of the Hearing of Quito

Contiene la edición facsimilar de un documento escrito por Eugenio Espejo sobre si es conveniente o no el uso terapéutico de la quina. Presenta también el facsímil del proyecto para la estanco de la quina y una carta de José Celestino Mutis a Espejo acerca del tema...