Cyclodextrin inclusion complexes improving antibacterial drug profiles: an update systematic review.

Aim: The study aimed to review experimental models using cyclodextrins to improve antibacterial drugs' physicochemical characteristics and biological activities. Methods: The following terms and their combinations were used: cyclodextrins and antibacterial agents in title or abstract, and the total study search was conducted over a period up to October 2022. The review was carried out using PubMed, Scopus and Embase databases. A total of 1580 studies were identified, of which 27 articles were selected for discussion in this review. Results: The biological results revealed that the antibacterial effect of the inclusion complexes was extensively improved. Cyclodextrins can enhance the therapeutic effects of antibiotics already existing on the market, natural products and synthetic molecules. Conclusion: Overall, CDs as drug-delivery vehicles have been shown to improve antibiotics solubility, stability, and bioavailability, leading to enhanced antibacterial activity.

The overuse of drugs can cause bacteria to become less susceptible to them. This is known as resistance. One idea on how to tackle this resistance is by using cyclodextrins (CDs). CDs can change how drugs work, making them better at fighting bacteria. As CDs are already used in making drugs, they are a good choice for the basis of creating new drugs.

Antinociceptive Effect of a p-Cymene/ß-Cyclodextrin Inclusion Complex in a Murine Cancer Pain Model: Characterization Aided through a Docking Study.

Pain is one of the most prevalent and difficult to manage symptoms in cancer patients, and conventional drugs present a range of adverse reactions. The development of ß-cyclodextrins (ß-CD) complexes has been used to avoid physicochemical and pharmacological limitations due to the lipophilicity of compounds such as p-Cymene (PC), a monoterpene with antinociceptive effects. Our aim was to obtain, characterize, and measure the effect of the complex of p-cymene and ß-cyclodextrin (PC/ß-CD) in a cancer pain model. Initially, molecular docking was performed to predict the viability of complex formation. Afterward, PC/ß-CD was obtained by slurry complexation, characterized by HPLC and NMR. Finally, PC/ß-CD was tested in a Sarcoma 180 (S180)-induced pain model. Molecular docking indicated that the occurrence of interaction between PC and ß-CD is favorable. PC/ß-CD showed complexation efficiency of 82.61%, and NMR demonstrated PC complexation in the ß-CD cavity. In the S180 cancer pain model, PC/ß-CD significantly reduced the mechanical hyperalgesia, spontaneous nociception, and nociception induced by non-noxious palpation at the doses tested (p < 0.05) when compared to vehicle differently from free PC (p > 0.05). Therefore, the complexation of PC in ß-CD was shown to improve the pharmacological effect of the drug as well as reducing the required dose.

What do we have that is new in antifungal peptides? A patent review.

Drugs used to fight fungal infections may cause toxic or adverse drug interactions. For this reason, there is an increase in the development of natural, semisynthetic and synthetic antifungal peptides. This study aimed to perform a patent review to identify the advances in peptides to treat fungal infections. In a preliminary assessment, 597 patents were identified from the database. Then, duplicated patents (62) and those with titles in disagreement with the scope of this review (196) were excluded. Then, six patents were not in English or Spanish. Following the screening, 288 patents were outside the focus of this review, according to their abstract and description. The final selection covered 45 patents.

Currently, medications used to treat fungal infections may interact negatively with other drugs or be hazardous to the host. Scientists have been looking for novel, safe and efficient antifungal drugs since the enhancement of fungal resistance. Antimicrobial peptides, as opposed to traditional antibiotics, offer a variety of antibacterial activity against bacteria, fungi, parasites, viruses and cancer cells. The production of isolated natural, semisynthetic and synthetic antifungal peptides has increased. As a result, patents are a reliable and up-to-date source of innovation. As a result, their content analysis provides crucial information for identifying trends in new medications and targeted treatment plans.

Carvone and its pharmacological activities: A systematic review.

Natural products from plants have gained prominence in the search for therapeutic alternatives. Monoterpenes, such as carvone, are suggested as candidates for the treatment of several diseases. Therefore, the objective of this study is to review the pharmacological activities of carvone in experimental models in vitro and in vivo. For this, the searches were carried out in May 2020 (upgraded in July 2021) in the databases of PubMed, Web of Science and Scopus and gathered studies on the pharmacological activities of carvone. Two independent reviewers performed the selection of articles using the Rayyan application, extracted the relevant data and assessed the methodological quality of the selected studies using Syrcle's risk of bias tool. Ninety-one articles were selected that described 10 pharmacological activities of carvone, such as antimicrobial, antispasmodic, anti-inflammatory, antioxidant, antinociceptive, anticonvulsant, among others. The evaluation of the methodological quality presented an uncertain risk of bias for most studies. In light of that, carvone stands out as a viable and promising alternative in the treatment of several pathological conditions. However, carrying out studies to evaluate possible mechanisms of action and the safety of this monoterpene is recommended.

Cardiovascular effects of farnesol and its ß-cyclodextrin complex in normotensive and hypertensive rats.

Farnesol (FAR) is a sesquiterpene alcohol with a range of reported biological effects including cardioprotective, antioxidant and antiarrhythmic properties. However, due to its volatility, the use of drug incorporation systems, such as cyclodextrins, have been proposed to improve its pharmacological properties. Thus, the aim of this study was to evaluate and characterize the cardiovascular effects of FAR alone, and to investigate the antihypertensive effects of FAR complexed with ß-cyclodextrin (ßCD) in rats. Mean arterial pressure (MAP) and heart rate (HR) were measured before and after intravenous administration of FAR (0,5; 2,5; 5 and 7,5 mg/kg) in normotensive rats, and after oral acute administration (200 mg/kg) of FAR and FAR/ßCD complex in NG-nitro-L-arginine-methyl-ester (L-NAME) hypertensive rats. In normotensive animals, FAR induced dose-dependent hypotension associated with bradycardia. These effects were not affected by pre-treatment with L-NAME or indomethacin (INDO), but were partially attenuated by atropine. Pre-treatment with hexamethonium (HEXA) only affected hypotension. In the hypertensive rats, FAR/ßCD potentialized the antihypertensive effect when compared to FAR alone. Molecular docking experiments demonstrated for the first time that FAR has affinity to bind to the M3 and M2 muscarinic, and nicotinic receptors through hydrogen bonds in the same residues as known ligands. In conclusion, our results demonstrated that FAR induced hypotension associated with bradycardia, possibly through the muscarinic and nicotinic receptors. The inclusion complex with ßCD improved the antihypertensive effects of FAR, which can be relevant to improve current cardiovascular therapy using volatile natural components.

Mechanism of Action of Limonene in Tumor Cells: A Systematic Review and Meta-Analysis.

BACKGROUND: Cancer is a complex, multifactorial disease, and a major public health problem, as it is a leading cause of morbidity and mortality worldwide. Although treatments have significantly improved, still more effective drugs are searched. One source for these drugs is natural products (NPs). One NP that has shown anticancer activity is Limonene. However, the mechanisms of limonene's antiproliferative, anticancer and antineoplastic activity are not fully understood. OBJECTIVE: The objective of this study is to undertake a systematic review and meta-analysis of the literature on this subject. METHODS: A comprehensive literature search was performed using the Scopus, MEDLINE-PubMed, Web of Science, and Science Direct databases using the keywords: "limonene", "cancer", "neoplasm", and "tumor". The inclusion criteria were: in vivo and in vitro studies on the use of limonene in cancer published in English, Portuguese and Spanish until December 2019. Review articles, meta-analyses, abstracts, conference papers, editorials/ letters and case reports were excluded. RESULTS: The search identified 3568 articles, of which, 126 were selected for full reading, with 11 papers meeting the review criteria. Six more papers were added from the references of the initial 11 texts, giving a total of 17 papers. There was a high level of agreement in inclusion/exclusion (Kappa index > 80%). The risk of bias in the texts was shown to be high. CONCLUSION: The meta-analysis suggests that limonene acts mainly on tumor regression induced apoptosis and is a promising natural product for use in the treatment of several types of cancer.

Monoterpenes as a perspective for the treatment of seizures: A Systematic Review.

BACKGROUND: Epilepsy affects more than 65 million people worldwide. Treatment for epileptic seizures is ineffective and has many adverse effects. For this reason, the search for new therapeutic options capable of filling these limitations is necessary. HYPOTHESIS/PURPOSE: In this sense, natural products, such as monoterpenes, have been indicated as a new option to control neurological disorders such as epilepsy. STUDY DESIGN: Therefore, the objective of this study was to review the monoterpenes that have anticonvulsive activity in animal models. METHODS: The searches were performed in the PubMed, Web of Science and Scopus databases in September, 2020 and compiled studies using monoterpenes as an alternative to seizure. Two independent reviewers performed the study selection, data extraction and methodological quality assessment using the Syrcle tool. RESULTS: 51 articles that described the anticonvulsant activity of 35 monoterpenes were selected with action on the main pharmacological target, including GABAA receptors, glutamate, calcium channels, sodium and potassium. In addition, these compounds are capable of reducing neuronal inflammation and oxidative stress caused by seizure. CONCLUSION: These compounds stand out as a promising alternative for acting through different pharmacological mechanisms, which may not only reduce seizure, but also promote neuroprotective effect by reducing toxicity in brain regions. However, further studies are needed to determine the mechanism of action and safety assessment of these compounds.

Scenario of the Treatment of Arthritis with Natural Products.

BACKGROUND: Conventional treatments of arthritis use toxic and poorly tolerated drugs. Therefore, natural products are an alternative because they are important sources of bioactive substances with therapeutic potential. OBJECTIVE: To perform synthesis of patent applications associated with the use of natural products in the technological development of the invention for use in treating arthritis. METHODS: The search for patents was conducted using the following databases of World Intellectual Property Organization (WIPO), European Patent Office (EPO, Espacenet), United States Patents and Trademark Office (USPTO) and National Institute of Intellectual Property (INPI) using as keywords - arthritis, treatment and the International Patent Classification (IPC) A61K36 / 00. RESULTS: A total of 617 patents related to the subject were registered in the period available in patents databases during the study period from the years 2005 to 2017, of which 44 were analyzed based on the established inclusion criteria. The most important countries for protecting these inventions were China, followed by the United States of America, the Republic of Korea and Japan. As for the typology of depositors, that were identified by Educational Institutions and Public Institutes of Research (IEIPP) and Companies and Private Research Institutes (EIPP). CONCLUSION: The analysis of patents made it possible to characterize the natural products used in the treatment of arthritis, with emphasis on botanical extracts (71%), as a single component, as well as in association with other botanical extracts, isolated compounds and minerals.

Molecular mechanism underlying orofacial antinociceptive activity of Vanillosmopsis arborea Baker (Asteraceae) essential oil complexed with ß-cyclodextrin.

BACKGROUND: Vanillosmopsis arborea Baker has recognized economic value owing to the high content of (-)-α-bisabolol (BISA) in the essential oil of its stem (EOVA). The antinociceptive effect of EVOA has already been demonstrated, and ß-cyclodextrin (ßCD) is known to improve the analgesic effect of various substances. PURPOSE: Thus, we aimed to evaluate the orofacial antinociceptive effect of a complex containing EOVA-ßCD in rodents. METHODS: EOVA was obtained by simple hydrodistillation, and the essential oil was complexed with ßCD. The animals (n = 6/group) were treated orally with EOVA-ßCD (10 or 50 mg/kg), or vehicle (control), and subjected to cutaneous orofacial nociception (formalin, capsaicin, acidic saline or glutamate), corneal (hypertonic saline) or temporomandibular (formalin) tests. The expression of FOS protein was analyzed in the spinal cord. Molecular docking was performed using the 5-HT3 and M2 receptors and BISA. RESULTS: The oral administration of EOVA-ßCD reduced nociceptive behaviour. Moreover, EOVA-ßCD decreased FOS expression. The molecular docking study indicates that BISA interacts with 5-HT3 and M2 receptors, indicating the potential mechanism of action of the tested compound. CONCLUSIONS: Our results indicate that EOVA-ßCD possesses orofacial antinociceptive effect, indicating that this complex can be used in analgesic drug development.

Inclusion complex between ß-cyclodextrin and hecogenin acetate produces superior analgesic effect in animal models for orofacial pain.

Hecogenin acetate (HA) is a steroidal sapogenin-acetylated with pharmacological properties which have already been described in the literature such as, anti-inflammatory, anti-hyperalgesic and antinociceptive, but it has low solubility in aqueous media. Therefore, in an attempt to overcome this, we set out to create inclusion complexes between HA and b-cyclodextrin (b-CD) and evaluate the antinociceptive effects in the orofacial nociception in mice. The complexes were prepared using different methods in the molar ratios 1:1 and 1:2 and characterized physicochemically. The results of the physicochemical characterization elucidated inclusion complexes formation between b-CD and HA by freeze drying method in the molar ratio 1:2, which obtained a complexation efficiency of 92% and produced superior analgesic effect in animal models for orofacial pain at a lower dose when compared to HA alone.

Physico-chemical characterization and antibacterial activity of inclusion complexes of Hyptis martiusii Benth essential oil in ß-cyclodextrin.

Cyclodextrins (CDs) have been used as important pharmaceutical excipients for improve the physicochemical properties of the drugs of low solubility as the essential oil of Hyptis martiusii. This oil is important therapeutically, but the low solubility and bioavailability compromises your use. Therein, the aim of this study was to obtain and to characterize physico-chemically the samples obtained by physical mixture (PM), paste complexation (PC) and slurry complexation (SC) of the essential oil Hyptis martiusii (EOHM) in ß-CD, and to compare the antibacterial and modulatory-antibiotic activity of products obtained and oil free. The physicochemical characterization was performed by differential scanning calorimetry (DSC), thermogravimetry/derivative thermogravimetry (TG/DTG), scanning electron microscopy (SEM), X-ray diffraction (XRD) and Karl Fischer titration. Additionally, the antibacterial tests were performed by microdilution technique. Thus, it was observed that the PM method showed low complexing capacity, unlike PC and SC in which it was observed the formation of inclusion complexes. In addition, the second stage of the TG/DTG curves showed that SC was the best method inclusion with mass loss of 6.9% over the PC that was 6.0%. The XRD results corroborate with the results above suggesting the formation of new solid phase and the SEM photomicrographs showed the porous surface of the samples PC and SC. The essential oil alone demonstrated an antibacterial and modulatory effect against the S. aureus and the Gram negative strain, respectively. However, the ß-CD and the inclusion complex did not demonstrate any biological activity in the performed antibacterial assays.

Docking, characterization and investigation of ß-cyclodextrin complexed with citronellal, a monoterpene present in the essential oil of Cymbopogon species, as an anti-hyperalgesic agent in chronic muscle pain model.

BACKGROUND: Citronellal (CT) is a monoterpene with antinociceptive acute effect. ß-Cyclodextrin (ßCD) has enhanced the analgesic effect of various substances. HYPOTHESIS/PURPOSE: To evaluate the effect of CT both complexed in ß-cyclodextrin (CT-ßCD) and non-complexed, in a chronic muscle pain model (CMP) in mice. STUDY DESIGN: The complex containing CT in ßCD was obtained and characterized in the laboratory. The anti-hyperalgesic effect of CT and CT-ßCD was evaluated in a pre-clinical in vivo study in a murine CMP. METHODS: The complex was characterized through differential scanning calorimetry, derivative thermogravimetry, moisture determination, infrared spectroscopy and scanning electron microscopy. Male Swiss mice were pre-treated with CT (50mg/kg, po), CT-ßCD (50mg/kg, po), vehicle (isotonic saline, po) or standard drug (tramadol4 mg/kg, ip). 60 min after the treatment and then each 1h, the mechanic hyperalgesia was evaluated to obtain the time effect. In addition, the muscle strength using grip strength meter and hyperalgesia were also performed daily, for 7 days. We assessed by immunofluorescence for Fos protein on brains and spinal cords of mice. The involvement of the CT with the glutamatergic system was studied with molecular docking. RESULTS: All characterization methods showed the CT-ßCD complexation. CT-induced anti-hyperalgesic effect lasted until 6h (p <0.001) while CT-ßCD lasted until 8h (p <0.001vs vehicle and p <0.001vs CT from the 6th h). CT-ßCD reduced mechanical hyperalgesia on all days of treatment (p <0.05), without changing muscle strength. Periaqueductal gray (p <0.01) and rostroventromedular area (p <0.05) showed significant increase in the Fos protein expression while in the spinal cord, there was a reduction (p <0.001). CT showed favorable energy binding (-5.6 and -6.1) to GluR2-S1S2J protein based in the docking score function. CONCLUSION: We can suggest that ßCD improved the anti-hyperalgesic effect of CT, and that effect seems to involve the descending pain-inhibitory mechanisms, with a possible interaction of the glutamate receptors, which are considered as promising molecules for the management of chronic pain such as CMP.

α-Terpineol, a monoterpene alcohol, complexed with ß-cyclodextrin exerts antihyperalgesic effect in animal model for fibromyalgia aided with docking study.

The anti-hyperalgesic effect of the complex containing α-terpineol (αTPN) and ß-cyclodextrin (ßCD) was analyzed in a non-inflammatory chronic muscle pain model, as well as its mechanism of action through docking study for a possible interaction with receptors. The αTPN-ßCD complex was prepared and characterized through the thermogravimetry/derivate thermogravimetry (TG/DTG), Fourier transform infrared spectroscopy (FTIR) and scanning electron microscope (SEM). The model of chronic muscle pain was induced by two injections of pH 4.0 saline (20 µl) into the left gastrocnemius 5 days apart. After confirming hyperalgesia, male mice were treated with αTPN-ßCD (25, 50 or 100 mg/kg; p.o.) or vehicle (saline 0.9%, p.o.) daily for 10 days. 1 h after the mechanical hyperalgesia, motor performance was evaluated. In addition, the systemic administration of naloxone and ondansetron tested the analgesic effect on the active opioid and serotonin receptors, respectively. The characterization tests indicated that αTPN was efficiently incorporated into ßCD. The oral treatment with αTPN-ßCD, at all doses tested, produced a significant (p < 0.001) decrease in the mechanical hyperalgesia, without causing any alteration in the force and in motor performance. This analgesic effect was reversed by the systemic administration of naloxone or ondansetron. These findings are corroborated by the docking study described in the present study, which verified a possible interaction of αTPN-ßCD with opioid (MU, Kappa, Delta) and 5-HT receptors. Thus, it can be concluded that αTPN-ßCD reduced the hyperalgesia followed by the chronic muscle pain model, probably evoked by the descending inhibitory pain system, specifically by opioid and serotoninergic receptors.

Characterization and Antihypertensive Effect of the Complex of (-)-ß- pinene in ß-cyclodextrin.

This work aimed to characterize and evaluate the antihypertensive effect of the (-)-ß-pinene/ß-cyclodextrin (ßP/ß-CD) complex. The complex was prepared through physical mixture and slurry complexation methods and was analyzed through differential scanning calorimetry, thermogravimetry/derivative thermogravimetry, fourier transform infrared spectroscopy, diffraction X-ray, docking and scanning electron microscopy. Normotensive or L-NAME-induced hypertensive rats were used in pharmacological experiments. Mean arterial pressure (MAP) was determined with direct blood pressure measurements from the abdominal aorta. The drugs were orally administrated and their effects were recorded during 48 hours. Vascular effects of ßP were evaluated in isolated ring of mesenteric artery. The physicochemical characterization showed ßP/ß-CD complex formation. In hypertensive rats (MAP = 156±16 mmHg), the complex, but not ßP alone, promoted hypotension at 36 and 48 hours after administration (MAP = 124±3 and 110±5 mmHg, respectively). In arterial rings, ßP vasorelaxed rings precontracted with phenylephrine (Emax = 105±6%), which was not changed after the removal of the vascular endothelium (Emax = 108±4%), after the pre-contraction with KCl 80 mM (Emax = 107±8%) or S(-)-BayK8644 (Emax = 107±5%), or after incubation with TEA (Emax = 113±4%). Finally, ßP inhibited CaCl2- and sodium-orthovanadate-induced contractions. In conclusion, the slurry complexation method was the best among them. Pharmacological results demonstrated that the complex promoted antihypertensive effect. Furthermore, ßP induced endothelium- independent vasorelaxation possibly caused by the inhibition of the Ca2+ influx through L-type Ca2+ channel associated to a decrease in calcium sensitivity.

ß-caryophyllene, a dietary cannabinoid, complexed with ß-cyclodextrin produced anti-hyperalgesic effect involving the inhibition of Fos expression in superficial dorsal horn.

AIMS: Evaluate the anti-hyperalgesic effect of the complex containing ß-caryophyllene (ßCP) and ß-cyclodextrin (ßCD) in a non-inflammatory chronic muscle pain mice model and investigated its action on superficial dorsal horn of the lumbar spinal cord. MAIN METHODS: The ßCP-ßCD complex were prepared and characterized through the DSC, TG/DTG, FTIR, XRD and SEM. The model of chronic muscle pain was induced by two injections of pH4.0 saline (20µL) into left gastrocnemius 5days apart. After confirming hyperalgesia, male mice were treated with ßCP-ßCD (10 or 20mg/kg; p.o.) or vehicle (saline 0.9%, p.o.) daily for 9days. 1h after, the mechanical hyperalgesia, muscle withdrawal thresholds and motor performance were evaluated. To evaluate the ßCP-ßCD action on spinal cord, animals induced with chronic muscle pain were treated with ßCP-ßCD (20mg/kg; p.o.) or vehicle (saline 0.9%, p.o.) and 90min. after, were perfused, the lumbar spinal cord collected, crioprotected, cut and submitted in an immunofluorescence protocol for Fos protein. KEY FINDINGS: The characterization tests indicated that ßCP were efficiently incorporated into ßCD. The oral treatment with ßCP-ßCD, at all doses tested, produced a significant (p<0.05) reduction on mechanical hyperalgesia and a significant (p<0.05) increase in muscle withdrawal thresholds, without produce any alteration in force. In addition, ßCP-ßCD was able to significantly (p<0.05) decrease Fos expression in the superficial dorsal horn. SIGNIFICANCE: Thus, ßCP-ßCD attenuates the non-inflammatory chronic muscle pain in mice and inhibits the Fos expression in the lumbar spinal cord.

A review of recent patents on the ASICs as a key drug target.

Acid-sensing ion channels (ASICs) are scattered various cells of human body. Drugs like amiloride has demonstrated nonspecific antagonism ASICs. Toxins, such as Psalmotoxin-1, have been used in animal models. There are no drugs available in the market whose action mechanism acts through these channels. We revised all patents relating to pharmaceutical formulations of applicability in ASICs. Drugs acting as antagonist in ASIC1 or ASIC3 channels seem to be the most promising targets. Patent data have suggested a variety of approaches for selective ASICs drugs, such as neuroprotective and analgesic. Studies analysis suggested that ASICs are promising targets for new drugs.

Preparation, Characterization, and Pharmacological Activity of Cymbopogon winterianus Jowitt ex Bor (Poaceae) Leaf Essential Oil of ß-Cyclodextrin Inclusion Complexes.

This study aimed to evaluate the orofacial antinociceptive effect of the Cymbopogon winterianus essential oil (LEO) complexed in ß-cyclodextrin (LEO-CD) and to assess the possible involvement of the central nervous system (CNS). The LEO was extracted, chromatographed, and complexed in ß-cyclodextrin. The complex was characterized by differential scanning calorimetry (DSC) and thermogravimetry derivative (TG/DTG). Male Swiss mice (2-3 months) were treated with LEO-CD (50-200 mg/kg, p.o.), vehicle (distilled water, p.o.), or standard drug (i.p.) and subjected to the orofacial nociception formalin-, capsaicin-, and glutamate-induced. After the formalin test, the animals were perfused and the brains subjected to immunofluorescence for Fos. The rota-rod test (7 rpm/min) was carried out. Geraniol (37.57%) was the main compound of LEO. DSC and TG/DTG proved the complexation. The orofacial nociceptive behavior was significantly (p < 0.05) reduced. The number of Fos-positive cells was significantly changed in the dorsal raphe nucleus (p < 0.01), locus coeruleus (p < 0.001), trigeminal nucleus (p < 0.05), and trigeminal thalamic tract (p < 0.05). LEO-CD did not cause changes in motor coordination in the rota-rod test. Thus, our results suggested that LEO-CD has an orofacial antinociceptive profile, probably mediated by the activation of the CNS without changing the motor coordination.

Development of standardized extractive solution from Lippia sidoides by factorial design and their redox active profile

AbstractThe aim of this study was to evaluate the influences of variables of preparation on total flavonoids content from extractive solution of Lippia sidoides Cham., Verbenaceae. Thus a 23 factorial design was used to study the importance of plant proportion, the extraction method and solvent on the extraction of flavonoid. The methodology of determination of chemicals in factorial design was validated according to the parameters required by Brazilian Health Agency. The extraction solution was selected through a full factorial design where the best conditions to achieve the highest content of flavonoids were: 7.5% (w/v) of plant with ethanol 50% (v/v) as solvent. The polyphenols content was determined by LC method and its relationship with the antioxidant and free radical scavenging activities was evaluated. The free radical scavenging activities and antioxidant potentials were determined for different concentrations using various in vitro models. Our results indicate that extracts exhibited a significant dose-dependent antioxidant effect as evaluated by TRAP/TAR assays. Besides, we observed an antioxidant activity against hydroxyl radicals and nitric oxide, and protection against lipid peroxidation in vitro. Our results suggest that the extract presents significant in vitro antioxidant potential indicating promising perspectives for its use as pharmaceutical/or food additive.

Natural compounds for solar photoprotection: a patent review.

INTRODUCTION: Ultraviolet irradiation has deleterious effects on human skin, including tanning, sunburn, cancer and connective tissue degradation (photoaging). Botanical antioxidants have been shown to be associated with reduced incidence of photocarcinogenesis and photoaging through their photoprotective profile. AREAS COVERED: Here, the authors summarized therapeutic patent applications concerning the employment of medicinal plants on the technological development of a formulation with photoprotective or photoaging application. So, the patent search was conducted in the databases WIPO, Espacenet, USPTO and Derwent, using the keywords - photoaging, photoprotection and the IPC A61K 8/97 (cosmetics or similar cleaning supplies obtained from vegetable origin, for example, plant extracts) and A61K 36/00 (medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, for example, traditional herbal medicines). We found 180 patents, out of which 25 were evaluated using inclusion criteria as application of natural products with photoprotective or photoaging application. EXPERT OPINION: We found that some patents related to the cosmetic compositions for improving skin wrinkle and either preventing or reducing the signs of photoaging and sunburn. The cosmetic compositions are manufactured in the form of a lotion, gel, soluble liquid, cream, essence, oil-in-water-type or water-in-oil-type formulation, containing the vegetal extracts as an active ingredient.

Physicochemical characterization and analgesic effect of inclusion complexes of essential oil from Hyptis pectinata L. Poit leaves with ß-cyclodextrin.

The formation of inclusion complexes of Hyptis pectinata essential oil (EOHP), with potent activities such as anti-nociceptive, anti-inflammatory, among others, with ß -cyclodextrin (ß-CD), was obtained by slurry (SC) and paste procedures (PC). The gas chromatography coupled to the mass spectrometry (GC/MS) analysis demonstrated a total of 36.4% monoterpenes and 63.6% sesquiterpenes in the EOHP. The major components of EOHP were identified as (E)- caryophyllene (54.07%). The analysis of samples (PM, PC and SC) by GC/MS involved the surface and the total extracted oils. The GC/MS results suggested important differences between in SC and PC methods indicating the complexation of mono and sesquiterpenoids in different ratios. Furthermore, the thermal analysis techniques suggests the complexation, especially in SC, which show a thermogravimetry/derivative thermogravimetry (TG/DTG) peak at 140-270ºC, probably related to oil loss. Scanning electron microscopy (SEM) images showed reduction size of the samples mainly in the SC product. Additionally, EOHP/ ß-CD improves pharmacological profile of EOHP alone in formalin-induced pain protocol in mice.