Achyrocline satureioides review: From the pharmacochemical diversity to the technological development of products.

Achyrocline satureioides (Lam.) DC (Asteraceae) is a native species of the southeastern subtropical and temperate region of South America, popularly known as "marcela" or "macela". This species is recognized, in traditional medicine, by diverse biological activities such as digestive, antispasmodic, anti-inflammatory, antiviral, sedative, hepatoprotective, among others. Some of these activities have been related to the presence of phenolic compounds, including flavonoids, phenolic acids, terpenoids in the essential oils, coumarins and phloroglucinol derivatives reported to the species. The approaches on the technological development of phytopharmaceutical products of this species provided relevant advances in the optimization of the extraction and product obtention, especially spray-dried powders, hydrogels, ointments, granules, films, nanoemulsions and nanocapsules. The most relevant biological activities described for the extracts or derivative products from A. satureioides were antioxidant, neuroprotective, antidiabetic, antiobesity, antimicrobial, anticancer effects, and obstructive sleep apnea syndrome. The scientific and technological findings reported for the species, in conjunction with its traditional use and cultivation, reveal the high potential of the species for diverse industrial applications.

The challenge of improving pterostilbene (PTS) solubility for solid and semi-solid dosage forms: The obtention of binary and ternary systems.

Pterostilbene (PTS) is a drug candidate with low water solubility and poor bioavailability. On the other hand, drug:cyclodextrins complexes frequently provide bulk powders with low drug concentrations, which is crucial for obtention solid or semi-solid pharmaceutical dosage forms. In order to determine the optimal conditions for enhancing the solubility of PTS:BCD (ß-cyclodextrin) complex, a Box-Behnken design was performed. Although the optimal conditions have been applied, low complexation efficiency (0.127) and the bulk powder remained. A PTS:BCD:HPMC (HPMC, hydroxypropyl methylcellulose) ternary system was developed to overcome this limitation, comparing two media, water and a mixture of ethanol-water. When ethanol was used as a co-solvent, the PTS:BCD:HPMC ternary system (freeze-dried) contained 116.65 ± 1.40 mg/g of PTS. This value was 3.4-fold higher than the PTS content observed when the same ternary system was obtained in aqueous media (34.8 mg/g) and 2.8-fold higher than the PTS content observed for PTS:BCD complex (freeze-dried) obtained using ethanol as a co-solvent. Dissolution tests revealed that after 120 min, in a buffer with a pH value of 1.2, only 43% of PTS dissolved. In contrast, 80% and 90% of PTS were dissolved from the PTS:BCD complex and PTS:BCD:HPMC ternary system, respectively. Moreover, the dissolution was fast in a buffer with a pH value of 6.8. PTS:BCD complex reached the maximum PTS dissolution at 75 min and PTS:BCD:HPMC at 45 min. In summary, the results of this study demonstrated, for the first time, that low-bulk powders with a high content of PTS can be obtained from PTS:BCD:HPMC ternary systems using ethanol as a co-solvent. This new finding offers a valuable alternative for producing solid or semi-solid formulations containing highly soluble PTS.

Iridoids as a Potential Hepatoprotective Class: A Review.

BACKGROUND: Liver disease rates are gradually increasing over the years, becoming a severe public health problem. The indiscriminate use of drugs associated with a rich fat diet, high consumption of alcoholic beverages, and exposure to viral infections and lipid peroxidative products are considered the chief factors for developing hepatic disorders. Owing to the absence of reliable hepatoprotective drugs in the therapeutic arsenal, since they present a high incidence of adverse reactions and/or lack of efficacy in some cases, liver diseases are widely treated with medicinal plants. Among them are the plants producing iridoids, which are believed to be good remedies for liver disease due to their bitter taste. The hepatoprotective effect of iridoids and extracts, rich in these compounds, has been demonstrated, both in vitro and in vivo. OBJECTIVE: This review aims to scrutinize the available literature related to the hepatoprotective activity of iridoids. METHODS: The information was obtained from scientific databases (Science Direct, PubMed, Web of Science, Scopus, ACS Publications, Wiley Online Library) until December, 2021. RESULTS AND CONCLUSION: A total of 63 hepatoprotective iridoids were found, including aucubin, catalpol and picroliv, a mixture of two iridoids. They are the target of a high number of studies, which revealed their protective action against different hepatotoxic agents and detailed action mechanisms.

Subtribe Hyptidinae (Lamiaceae): A promising source of bioactive metabolites.

ETHNOPHARMACOLOGICAL RELEVANCE: The subtribe Hyptidinae contains approximately 400 accepted species distributed in 19 genera (Hyptis, Eriope, Condea, Cantinoa, Mesosphaerum, Cyanocephalus, Hypenia, Hyptidendron, Oocephalus, Medusantha, Gymneia, Marsypianthes, Leptohyptis, Martianthus, Asterohyptis, Eplingiella, Physominthe, Eriopidion and Rhaphiodon). This is the Lamiaceae clade with the largest number of species in Brazil and high rates of endemism. Some species have been used in different parts of the world mainly as insecticides/pest repellents, wound healing and pain-relief agents, as well as for the treatment of respiratory and gastrointestinal disorders. AIM OF THE REVIEW: This review aims to discuss the current status concerning the taxonomy, ethnobotanical uses, phytochemistry and biological properties of species which compose the subtribe Hyptidinae. MATERIALS AND METHODS: The available information was collected from scientific databases (ScienceDirect, Pubmed, Web of Science, Scopus, Google Scholar, ChemSpider, SciFinder ACS Publications, Wiley Online Library), as well as other literature sources (e.g. books, theses). RESULTS: The phytochemical investigations of plants of this subtribe have led to the identification of almost 300 chemical constituents of different classes such as diterpenes, triterpenes, lignans, α-pyrones, flavonoids, phenolic acids and monoterpenes and sesquiterpenes, as components of essential oils. Extracts, essential oils and isolated compounds showed a series of biological activities such as insecticide/repellent, antimicrobial and antinociceptive, justifying some of the popular uses of the plants. In addition, a very relevant fact is that several species produce podophyllotoxin and related lignans. CONCLUSION: Several species of Hyptidinae are used in folk medicine for treating many diseases but only a small fraction of the species has been explored and most of the traditional uses have not been validated by current investigations. In addition, the species of the subtribe appear to be very promising as alternative sources of podophyllotoxin-like lignans which are the lead compounds for the semi-synthesis of teniposide and etoposide, important antineoplastic agents. Thus, there is a wide-open door for future studies, both to support the popular uses of the plants and to find new biologically active compounds in this large number of species not yet explored.

In vitro protective effect of topical nanoemulgels containing Brazilian red propolis benzophenones against UV-induced skin damage.

The overexposure of the skin to ultraviolet (UV) radiation may lead to oxidative stress, resulting in severe damage. The prevention of skin injuries through the topical application of natural compounds rich in antioxidants, such as propolis extracts, has shown promising results. In Brazil, the "red propolis" extract has stood out due to its complex constitution, based mainly on polyprenylated benzophenones (BZP). However, although the use of red propolis extracts has been shown to be encouraging, their addition in topical formulations is limited by the low solubility of BZP. For this reason, this study aimed to develop topical nanoemulgels containing Brazilian red propolis (BRP) extract to increase the potential of topical application, and the evaluation of skin protection against UVA/UVB radiation damage by means of protein carbonylation, protein thiol content and TBARS assays. The nanoemulgels were obtained by adding gelling polymer to nanoemulsions that were previously prepared by spontaneous emulsification. In this sense, a nanoemulgel containing BRP extract-loaded nanoemulsions (H-NE) and a nanoemulgel containing BRP extract-loaded nanoemulsions with DOTAP (H-NE/DT) were prepared. The physicochemical characterization of nanoemulgels showed monodisperse populations of 200-300 nm. The H-NE zeta potential was -38 mV, while that of H-NE/DT was +36 mV. BZP content in the formulations was around 0.86 mg g-1. These parameters remained stable for 90 days under cold storage. H/NE and H-NE/DT presented a non-Newtonian pseudoplastic rheological behavior. Permeation/retention studies, through porcine ear skin, showed the highest BZP retention (18.11 µg cm-2 after 8 h) for H-NE/DT, which also demonstrated, in an in vitro study, the highest ability to protect skin against oxidative damage after UVA/UVB radiation exposure. The results concerning the antioxidant activity revealed that formulations containing the BRP n-hexane extract were the most promising in combating oxidative stress, probable due to the presence of polyprenylated BZP. Altogether, the outcomes of this study suggest that nanoemulgels have suitable characteristics for topical application, and may be an alternative for the prevention of oxidative skin damage caused by UVA/UVB radiation.

Hypericum species: An analysis on the patent technologies.

Hypericum (Hypericaceae) is a genus that comprises approximately 500 species around the world. The industrial relevance of these plants is based on the occurence of specialized metabolites that exhibit a range of pharmaceutical potential. Besides that, several species are relevant due to their ornamental value. Taking to account the vast market worth of products and processes involving Hypericum, the present study aims to provide a comprehensive overview of patents concerning this subject between 2007and 2017. For this purpose, a survey was performed in free databases (Espacenet®, PatentScope® and Google Patents®) using the keyword Hypericum in the patents title or title plus abstract. The documents were then organized by groups (medicinal and non-medicinal approaches), subgroups, type of applicants and countries. Espacenet® was chosen to data analysis, and a total of 174 patents were found. The majority of the applicants are from China and companies appear as the principal owners of patents. Several technologies are not intended for medicinal purposes, being mainly related to the development of new cultivars for ornamental uses. Concerning the medicinal approaches, the chief subject is related to extraction and incorporation into formulations. The main species cited in the documents is H. perforatum and the therapeutic use is for central nervous system diseases. In general, this study covers the patents published in recent years hoping to boost the scientists and companies that invest in Hypericum researches to visualize the state of art, opportunities and challenges for innovation in this area.