Natural Products Treat Atopic Dermatitis via NF-κB Signaling Pathway： A Review / 中国实验方剂学杂志

Atopic dermatitis （AD） is a chronic， recurrent， inflammatory， and pruritus skin disease caused by multiple internal and external factors， ranking first in the global burden of skin diseases. Due to the adverse reactions and high costs of conventional treatments and biologics， the development of natural products has attracted much attention. The nuclear factor-κB （NF-κB） signaling pathway is a key pathway for inhibiting inflammation and modulating immunity. This paper summarizes the pharmacological effects and molecular mechanisms of natural products such as flavonoids， alkaloids， phenols， terpenoids， coumarins， glycosides， and anthraquinones via NF-κB signaling pathway， aiming to provide guidance for the development of natural products. Basic studies have shown that natural products have high safety and efficacy. Oral or topical administration of natural products can regulate the phosphatidylinositol 3-kinase （PI3K）/protein kinase B （Akt）， mitogen-activated protein kinase （MAPK）， nuclear factor erythroid 2-related factor 2 （Nrf2）， high mobility group box 1 protein （HMGB1）/receptor for advanced glycation endproducts （RAGE）， and nucleotide-binding oligomerization domain-like receptor protein 3 （NLRP3） signaling pathways to exert anti-inflammatory， anti-allergy， antioxidant activities， thus reversing the pathological changes of AD. However， it is worth noting that the clinical application of natural products is still insufficient， and more rigorous clinical trials are still needed to verify their effects. The basic experiments and clinical evidence prove that natural products may play a role in alleviating AD， which provide a basis for evaluating the functioning mechanism of natural active substances and enrich the candidates for the development of potential drugs.

Genomics-driven derivatization of the bioactive fungal sesterterpenoid variecolin: Creation of an unnatural analogue with improved anticancer properties

A biosynthetic gene cluster for the bioactive fungal sesterterpenoids variecolin ( 1) and variecolactone ( 2) was identified in Aspergillus aculeatus ATCC 16872. Heterologous production of 1 and 2 was achieved in Aspergillus oryzae by expressing the sesterterpene synthase VrcA and the cytochrome P450 VrcB. Intriguingly, the replacement of VrcB with homologous P450s from other fungal terpenoid pathways yielded three new variecolin analogues ( 5- 7). Analysis of the compounds' anticancer activity in vitro and in vivo revealed that although 5 and 1 had comparable activities, 5 was associated with significantly reduced toxic side effects in cancer-bearing mice, indicating its potentially broader therapeutic window. Our study describes the first tests of variecolin and its analogues in animals and demonstrates the utility of synthetic biology for creating molecules with improved biological activities.

Strategies on biosynthesis and production of bioactive compounds in medicinal plants / 中草药·英文版

Medicinal plants are a valuable source of essential medicines and herbal products for healthcare and disease therapy. Compared with chemical synthesis and extraction, the biosynthesis of natural products is a very promising alternative for the successful conservation of medicinal plants, and its rapid development will greatly facilitate the conservation and sustainable utilization of medicinal plants. Here, we summarize the advances in strategies and methods concerning the biosynthesis and production of natural products of medicinal plants. The strategies and methods mainly include genetic engineering, plant cell culture engineering, metabolic engineering, and synthetic biology based on multiple "OMICS" technologies, with paradigms for the biosynthesis of terpenoids and alkaloids. We also highlight the biosynthetic approaches and discuss progress in the production of some valuable natural products, exemplifying compounds such as vindoline (alkaloid), artemisinin and paclitaxel (terpenoids), to illustrate the power of biotechnology in medicinal plants.

Research progress on the biological activity of pyrrole 1,2-α indole alkaloids / 中国基层医药

Pyrrole [1,2-α] indole is a novel fused heterocyclic skeleton, which is also the basic structural unit and synthetic intermediate of many natural active products and drugs. Pyrrole [1,2-α] indole heterocyclic derivatives have attracted much attention in organic synthesis and medicinal chemistry because of their extensive and marked biological activities. Plant extracts have always been an important source of active compounds. At present, the alkaloids based on the pyrrole [1,2-α] indole heterocyclic structure discovered and isolated from plant extracts include isatisine, isoborreverine, flinderoles, polyavolensin and yuremamine. This paper reviews the research progress on the biological activity of pyrrole [1,2-α] indole heterocyclic derivatives and has found that pyrrole [1,2-α] indole heterocyclic derivatives have a good development prospect in screening active compounds and developing candidate drugs.

P450-mediated dehydrotyrosine formation during WS9326 biosynthesis proceeds via dehydrogenation of a specific acylated dipeptide substrate

WS9326A is a peptide antibiotic containing a highly unusual N-methyl-E-2-3-dehydrotyrosine (NMet-Dht) residue that is incorporated during peptide assembly on a non-ribosomal peptide synthetase (NRPS). The cytochrome P450 encoded by sas16 (P450Sas) has been shown to be essential for the formation of the alkene moiety in NMet-Dht, but the timing and mechanism of the P450Sas-mediated α,β-dehydrogenation of Dht remained unclear. Here, we show that the substrate of P450Sas is the NRPS-associated peptidyl carrier protein (PCP)-bound dipeptide intermediate (Z)-2-pent-1'-enyl-cinnamoyl-Thr-N-Me-Tyr. We demonstrate that P450Sas-mediated incorporation of the double bond follows N-methylation of the Tyr by the N-methyl transferase domain found within the NRPS, and further that P450Sas appears to be specific for substrates containing the (Z)-2-pent-1'-enyl-cinnamoyl group. A crystal structure of P450Sas reveals differences between P450Sas and other P450s involved in the modification of NRPS-associated substrates, including the substitution of the canonical active site alcohol residue with a phenylalanine (F250), which in turn is critical to P450Sas activity and WS9326A biosynthesis. Together, our results suggest that P450Sas catalyses the direct dehydrogenation of the NRPS-bound dipeptide substrate, thus expanding the repertoire of P450 enzymes that can be used to produce biologically active peptides.

Identification of Bulbocodin D and C as novel STAT3 inhibitors and their anticancer activities in lung cancer cells / 中国天然药物

Cancer stands as one of the predominant causes of mortality globally, necessitating ongoing efforts to develop innovative therapeutics. Historically, natural products have been foundational in the quest for anticancer agents. Bulbocodin D (BD) and Bulbocodin C (BC), two bibenzyls derived from Pleione bulbocodioides (Franch.) Rolfe, have demonstrated notable in vitro anticancer activity. In human lung cancer A549 cells, the IC50s for BD and BC were 11.63 and 11.71 μmol·L-1, respectively. BD triggered apoptosis, as evidenced by an upsurge in Annexin V-positive cells and elevated protein expression of cleaved-PARP in cancer cells. Furthermore, BD and BC markedly inhibited the migratory and invasive potentials of A549 cells. The altered genes identified through RNA-sequencing analysis were integrated into the CMap dataset, suggesting BD's role as a potential signal transducer and activator of transcription 3 (STAT3) inhibitor. SwissDock and MOE analyses further revealed that both BD and BC exhibited a commendable binding affinity with STAT3. Additionally, a surface plasmon resonance assay confirmed the direct binding affinity between these compounds and STAT3. Notably, treatment with either BD or BC led to a significant reduction in p-STAT3 (Tyr 705) protein levels, regardless of interleukin-6 stimulation in A549 cells. In addition, the extracellular signal-regulated kinase (ERK) was activated after BD or BC treatment. An enhancement in cancer cell mortality was observed upon combined treatment of BD and U0126, the MEK1/2 inhibitor. In conclusion, BD and BC emerge as promising novel STAT3 inhibitors with potential implications in cancer therapy.

Anti-hepatitis B virus activities of natural products and their antiviral mechanisms / 中国天然药物

Chronic hepatitis B (CHB) infections caused by the hepatitis B virus (HBV) continue to pose a significant global public health challenge. Currently, the approved treatments for CHB are limited to interferon and nucleos(t)ide analogs, both of which have their limitations, and achieving a complete cure remains an elusive goal. Therefore, the identification of new therapeutic targets and the development of novel antiviral strategies are of utmost importance. Natural products (NPs) constitute a class of substances known for their diverse chemical structures, wide-ranging biological activities, and low toxicity profiles. They have shown promise as potential candidates for combating various diseases, with a substantial number demonstrating anti-HBV properties. This comprehensive review focuses on the current applications of NPs in the fight against HBV and provides a summary of their antiviral mechanisms, considering their impact on the viral life cycle and host hepatocytes. By offering insights into the world of anti-HBV NPs, this review aims to furnish valuable information to support the future development of antiviral drugs.

Neuroprotection of Natural Products Based on Keap1/Nrf2/ARE Signaling Pathway： A Review / 中国实验方剂学杂志

The pathological manifestations of neurodegenerative diseases， such as Alzheimer's disease， Parkinson's disease， and multiple sclerosis， are abnormal protein aggregation and accumulation， microglia activation， and mitochondrial dysfunction， which eventually lead to the gradual loss of neuronal structure or function and deteriorate over time. These pathological processes are related to the production of reactive oxygen species （ROS）， which can cause oxidative stress and damage proteins， lipids， and DNA， leading to cell and tissue injuries. The Kelch-like ECH-associated protein 1 （Keap1）/nuclear factor E2-related factor 2 （Nrf2）/antioxidant response element （ARE） signaling pathway is the main mechanism to maintain the redox balance of the body and defend against oxidative stress injury. Nrf2 activates the expression of a series of antioxidant genes related to ARE through the dissociation of Keap1 and nuclear transfer in the cytoplasm to protect the body from oxidative damage. Therefore， the discovery and study of the Keap1/Nrf2/ARE signaling pathway activator is of great significance for the prevention and treatment of neurodegenerative diseases. Because of the remarkable biological activity and slight side effects， natural products are a treasure trove for new drug research and development. Studies have shown that a variety of natural products can activate the Keap1/Nrf2/ARE signaling pathway and play a neuroprotective role. According to the structural characteristics， natural products can be divided into flavonoids， terpenoids， volatile oils， polyphenols， and phenylpropanoids. This study summarized the underlying mechanism of the Keap1/Nrf2/ARE signaling pathway in regulating diseases and reviewed the research progress on natural products based on this signaling pathway in neuroprotection to provide references for the development of clinical drugs for the prevention and treatment of neurodegenerative diseases.

Biosynthesis of natural products by non-conventional yeasts / 生物工程学报

Non-conventional yeasts such as Yarrowia lipolytica, Pichia pastoris, Kluyveromyces marxianus, Rhodosporidium toruloides and Hansenula polymorpha have proven to be efficient cell factories in producing a variety of natural products due to their wide substrate utilization spectrum, strong tolerance to environmental stresses and other merits. With the development of synthetic biology and gene editing technology, metabolic engineering tools and strategies for non-conventional yeasts are expanding. This review introduces the physiological characteristics, tool development and current application of several representative non-conventional yeasts, and summarizes the metabolic engineering strategies commonly used in the improvement of natural products biosynthesis. We also discuss the strengths and weaknesses of non-conventional yeasts as natural products cell factories at current stage, and prospects future research and development trends.

Modulation of type I interferon signaling by natural products in the treatment of immune-related diseases / 中国天然药物

Type I interferon (IFN) is considered as a bridge between innate and adaptive immunity. Proper activation or inhibition of type I IFN signaling is essential for host defense against pathogen invasion, tumor cell proliferation, and overactive immune responses. Due to intricate and diverse chemical structures, natural products and their derivatives have become an invaluable source inspiring innovative drug discovery. In addition, some natural products have been applied in clinical practice for infection, cancer, and autoimmunity over thousands of years and their promising curative effects and safety have been well-accepted. However, whether these natural products are primarily targeting type I IFN signaling and specific molecular targets involved are not fully elucidated. In the current review, we thoroughly summarize recent advances in the pharmacology researches of natural products for their type I IFN activity, including both agonism/activation and antagonism/inhibition, and their potential application as therapies. Furthermore, the source and chemical nature of natural products with type I IFN activity are highlighted and their specific molecular targets in the type I IFN pathway and mode of action are classified. In conclusion, natural products possessing type I IFN activity represent promising therapeutic strategies and have a bright prospect in the treatment of infection, cancer, and autoimmune diseases.

A comprehensive review of natural products with anti-hypoxic activity / 中国天然药物

Natural products exhibit substantial impacts in the field of anti-hypoxic traetment. Hypoxia can cause altitude sickness and other negative effect on the body. Headache, coma, exhaustion, vomiting and, in severe cases, death are some of the clinical signs. Currently, hypoxia is no longer just a concern in plateau regions; it is also one of the issues that can not be ignored by urban residents. This review covered polysaccharides, alkaloids, saponins, flavonoids, peptides and traditional Chinese compound prescriptions as natural products to protect against hypoxia. The active ingredients, effectiveness and mechanisms were discussed. The related anti-hypoxic mechanisms involve increasing the hemoglobin (HB) content, glycogen content and adenosine triphosphate (ATP) content, removing excessive reactive oxygen species (ROS), reducing lipid peroxidation, regulating the levels of related enzymes in cells, protecting the structural and functional integrity of the mitochondria and regulating the expression of apoptosis-related genes. These comprehensive summaries are beneficial to anti-hypoxic research and provide useful information for the development of anti-hypoxic products.

Lysohexaenetides A and B, linear lipopeptides from Lysobacter sp. DSM 3655 identified by heterologous expression in Streptomyces / 中国天然药物

Lysobacter harbors a plethora of cryptic biosynthetic gene clusters (BGCs), albeit only a limited number have been analyzed to date. In this study, we described the activation of a cryptic polyketide synthase (PKS)/nonribosomal peptide synthetase (NRPS) gene cluster (lsh) in Lysobacter sp. DSM 3655 through promoter engineering and heterologous expression in Streptomyces sp. S001. As a result of this methodology, we were able to isolate two novel linear lipopeptides, lysohexaenetides A (1) and B (2), from the recombinant strain S001-lsh. Furthermore, we proposed the biosynthetic pathway for lysohexaenetides and identified LshA as another example of entirely iterative bacterial PKSs. This study highlights the potential of heterologous expression systems in uncovering cryptic biosynthetic pathways in Lysobacter genomes, particularly in the absence of genetic manipulation tools.

Heterologous production of bioactive xenoacremone analogs in Aspergillus nidulans / 中国天然药物

Tyrosine-decahydrofluorene derivatives are a class of hybrid compounds that integrate the properties of polyketides and nonribosomal peptides. These compounds feature a [6.5.6] tricarbocyclic core and a para-cyclophane ether moiety in their structures and exhibit anti-tumor and anti-microbial activities. In this study, we constructed the biosynthetic pathway of xenoacremones from Xenoacremonium sinensis ML-31 in the Aspergillus nidulans host, resulting in the identification of four novel tyrosine-decahydrofluorene analogs, xenoacremones I-L (1-4), along with two known analogs, xenoacremones A and B. Remarkably, compounds 3 and 4 contained a 12-membered para-cyclophane ring system, which is unprecedented among tyrosine-decahydrofluorene analogs in X. sinensis. The successful reconstruction of the biosynthetic pathway and the discovery of novel analogs demonstrate the utility of heterologous expression strategy for the generation of structurally diverse natural products with potential biological activities.

Neuroprotective potential of cannabidiol: Molecular mechanisms and clinical implications / 中西医结合学报

Cannabidiol (CBD), a nonpsychotropic phytocannabinoid that was once largely disregarded, is currently the subject of significant medicinal study. CBD is found in Cannabis sativa, and has a myriad of neuropharmacological impacts on the central nervous system, including the capacity to reduce neuroinflammation, protein misfolding and oxidative stress. On the other hand, it is well established that CBD generates its biological effects without exerting a large amount of intrinsic activity upon cannabinoid receptors. Because of this, CBD does not produce undesirable psychotropic effects that are typical of marijuana derivatives. Nonetheless, CBD displays the exceptional potential to become a supplementary medicine in various neurological diseases. Currently, many clinical trials are being conducted to investigate this possibility. This review focuses on the therapeutic effects of CBD in managing neurological disorders like Alzheimer's disease, Parkinson's disease and epilepsy. Overall, this review aims to build a stronger understanding of CBD and provide guidance for future fundamental scientific and clinical investigations, opening a new therapeutic window for neuroprotection. Please cite this article as: Tambe SM, Mali S, Amin PD, Oliveira M. Neuroprotective potential of Cannabidiol: Molecular mechanisms and clinical implications. J Integr Med. 2023; 21(3): 236-244.

In vitro effects of lapachol and β-lapachone against Leishmania amazonensis

Leishmaniasis is a neglected disease that affects millions of people worldwide, and special attention should be given to treatment because the available drugs have limitations, which can lead to low therapeutic adherence and parasitic resistance. This study evaluated the activity of the bioactive naphthoquinones, lapachol and β-lapachone, against Leishmania amazonensis. The cell alterations were evaluated in vitro on promastigote and amastigote forms. The lethal dose (LD50) at 24, 48, and 72 h on the promastigote's forms using lapachol was 75.60, 72.82, and 58.85 μg/mL and for β-lapachone was 0.65, 1.24, and 0.71 μg/mL, respectively. The naphthoquinones significantly inhibited the survival rate of L. amazonensis amastigotes at 83.11, 57.59, and 34.95% for lapachol (82.28, 41.14, and 20.57 µg/mL), and 78.49, 83.25, and 80.22% for β-lapachone (3.26, 1.63, and 0.815 µg/mL). The compounds on the promastigote's forms led to the loss of mitochondrial membrane potential, induced changes in the integrity of the membrane, caused damage to cells suggestive of the apoptotic process, and showed inhibition of tumor necrosis factor (TNF)-α and interleukin (IL)-6 production. The results showed that these naphthoquinones are promising candidates for research on new drugs with anti-Leishmania activity derived from natural products.

Aplicación de la medicina natural y tradicional por profesionales de la salud en el nivel primario de atención / Use of natural and traditional medicine by health professionals in the primary care level i: en

Introducción: La medicina natural y tradicional es una alternativa terapéutica inocua, económica y de fácil aplicación; sin embargo, aún persiste el poco empleo de sus modalidades. Objetivo: Describir el uso de la medicina natural y tradicional por profesionales de la salud en el nivel primario de atención. Métodos: Se efectuó un estudio observacional, descriptivo y transversal, desde enero hasta marzo de 2022, que incluyó a los 167 médicos y enfermeros que laboraban en los 42 consultorios pertenecientes al Policlínico Docente Ernesto Guevara de la Serna del municipio de Niquero, provincia de Granma. Entre las variables analizadas figuraron: perfil profesional de los integrantes del equipo básico de salud, frecuencia de aplicación de la medicina natural y tradicional, modalidades más empleadas, prescripción según afecciones y fortalezas para garantizar la práctica de este tratamiento. Resultados: Predominaron los residentes de medicina general integral (34,8 %), el uso frecuente del tratamiento (43,1 %), así como la fitoterapia (86,8 %) y la apiterapia (73,6 %) como modalidades más empleadas; asimismo, la mayoría de las prescripciones fueron para los pacientes con enfermedades osteomioarticulares y cardiovasculares (55,7 y 37,1 %, respectivamente). Conclusiones: El empleo de la medicina natural y tradicional en la atención primaria de salud en el municipio de Niquero proporcionó la información necesaria a los profesionales de la salud para confeccionar planes futuros y trazar estrategias relacionadas con las variantes de tratamiento.

Introduction: The natural and traditional medicine is an innocuous, economic therapeutic alternative of easy application; however, the little use of its modalities still persists. Objective: To describe the use of natural and traditional medicine by health professionals in the primary care level. Methods: An observational, descriptive and cross-sectional study was carried out from January to March, 2022, that included the 167 doctors and male nurses that worked in the 42 family doctor offices belonging to Ernesto Guevara de la Serna Teaching Polyclinic of Niquero municipality in Granma. Among the analyzed variables were the following: professional profile of the health basic team, frequency of natural and traditional medicine use, most used modalities, prescription according to affections and strengths to guarantee the practice of this treatment. Results: There was a prevalence of residents in comprehensive general medicine (34.8 %), the frequent use of the treatment (43.1 %), as well as fitotherapy (86.8 %) and apitherapy (73.6 %) as most used modalities; also, most of the prescriptions were for the patients with osteomioarticular and cardiovascular diseases (55.7 and 37.1 %, respectively). Conclusions: The use of natural and traditional medicine in primary health care in Niquero municipality provided the health professionals with the necessary information to make future plans and trace strategies related to the treatment variants.

Plants with antioxidant activity and their potential use as sun protector agents in Costa Rica

SUMMARY Aims: To carry out a bibliographic review related to plants available in Costa Rica that have demonstrated antioxidant power and a sun protection factor (SPF) suitable to be used in sunscreen products. Methods: The bibliographic review was carried out using different descriptors and by consulting different databases. Results: Information about antioxidant power about acerola, avocado, carrots, passion fruit, moringa, banana, pumpkin and amaranth, guava, matico, ginkgo, blackberry, mango, coffee was obtained. The information obtained suggests that the mentioned plants could be used for the formulation of sunscreens. Conclusion: Sun protection products should be used every day to prevent skin damage; some sunscreens produce allergic reactions, so it is necessary to investigate natural options to be used in sun protection products. Some natural products exhibit SPF values that allow their incorporation as sun protection agents, adjuvants, or enhancers in sunscreens.

Objetivo: llevar a cabo una investigación bibliográfica sobre plantas disponibles en Costa Rica que han demostrado su poder antioxidante y un factor de protector solar (SPF) apto para ser utilizados en protectores solares. Métodos: la revisión bibliográfica se realizó utilizando diferentes descriptores y mediante la consulta en diferentes bases de datos. Resultados: se obtuvo información sobre el poder antioxidante de las plantas: acerola, aguacate, zanahoria, maracuyá, moringa, banano, calabaza y amaranto, guayaba, matico, ginkgo, mora, mango, café. La información obtenida sugiere que las plantas mencionadas podrían ser utilizadas para la formulación de protectores solares. Conclusiones: los protectores solares deben ser utilizados diariamente para prevenir el daño sobre la piel. Algunos de estos productos generan reacciones alérgicas y por esta razón es necesario investigar posibles opciones naturales para ser incorporadas en bloqueadores solares. Algunos productos naturales exhiben valores de SPF que permiten su uso como agentes protectores solares, adyuvantes o potenciadores en los bloqueadores solares.

Objetivo: realizar uma pesquisa bibliográfica sobre plantas disponíveis na Costa Rica que demonstraram poder antioxidante e um fator de proteção solar (FPS) adequado para uso em protetores solares. Métodos: a revisão bibliográfica foi realizada usando diferentes descritores e consultando diferentes bases de dados. Resultados: foram obtidas informações sobre o poder antioxidante das plantas: acerola, abacate, cenoura, maracujá, moringa, banana, abóbora e amaranto, goiaba, matico, ginkgo, amora, manga, café. As informações sugerem que as referidas plantas poderiam ser utilizadas para a formulação de protetores solares. Conclusões: protetores solares devem ser usados diariamente para prevenir danos à pele. Alguns desses produtos geram reações alérgicas e por isso é necessário investigar possíveis opções naturais para serem incorporadas aos protetores solares. Alguns produtos naturais apresentam valores de FPS que permitem seu uso como protetores solares, adjuvantes ou potencializadores em protetores solares.

Amoebicidal and trichomonicidal capacity of polymeric nanoparticles loaded with extracts of the plants Curcuma longa (Zingiberaceae) and Berberis vulgaris (Berberidaceae) / Capacidad amebicida y tricomonicida de nanopartículas poliméricas cargadas con extractos de las plantas Curcuma longa (Zingiberaceae) y Berberis vulgaris (Berberidaceae)

Abstract Introduction: Pathogenic protozoans, like Entamoeba histolytica and Trichomonas vaginalis, represent a major health problem in tropical countries; and polymeric nanoparticles could be used to apply plant extracts against those parasites. Objective: To test Curcuma longa ethanolic extract and Berberis vulgaris methanolic extracts, and their main constituents, against two species of protozoans. Methods: We tested the extracts, as well as their main constituents, curcumin (Cur) and berberine (Ber), both non-encapsulated and encapsulated in polymeric nanoparticles (NPs), in vitro. We also determined nanoparticle characteristics by photon correlation spectroscopy and scanning electron microscopy, and hemolytic capacity by hemolysis in healthy erythrocytes. Results: C. longa consisted mainly of tannins, phenols, and flavonoids; and B. vulgaris in alkaloids. Encapsulated particles were more effective (P < 0.001); however, curcumin and berberine nanoparticles were the most effective treatments. CurNPs had IC50 values (µg/mL) of 9.48 and 4.25, against E. histolytica and T. vaginalis, respectively, and BerNPs 0.24 and 0.71. The particle size and encapsulation percentage for CurNPs and BerNPs were 66.5 and 73.4 nm, and 83.59 and 76.48 %, respectively. The NPs were spherical and significantly reduced hemolysis when compared to non-encapsulated extracts. Conclusions: NPs represent a useful and novel bioactive compound delivery system for therapy in diseases caused by protozoans.

Resumen Introducción: Los protozoos patógenos, como Entamoeba histolytica y Trichomonas vaginalis, representan un importante problema de salud en los países tropicales; y se podrían usar nanopartículas poliméricas para aplicar extractos de plantas contra esos parásitos. Objetivo: Probar los extractos etanólicos de Curcuma longa y Berberis vulgaris, y sus principales constituyentes, contra dos especies de protozoos. Métodos: Probamos los extractos, así como sus principales constituyentes, curcumina (Cur) y berberina (Ber), tanto no encapsulados como encapsulados en nanopartículas poliméricas (NPs), in vitro. También determinamos las características de las nanopartículas por espectroscopía de correlación de fotones y microscopía electrónica de barrido, y la capacidad hemolítica por hemólisis en eritrocitos sanos. Resultados: C. longa tenía principalmente: taninos, fenoles y flavonoides; y B. vulgaris, alcaloides. Las partículas encapsuladas fueron más efectivas (P < 0.001); sin embargo, las nanopartículas de curcumina y berberina fueron los tratamientos más efectivos. CurNPs tenía valores IC50 (µg/mL) de 9.48 y 4.25, contra E. histolytica y T. vaginalis, respectivamente, y BerNPs 0.24 y 0.71. El tamaño de partícula y el porcentaje de encapsulación para CurNPs y BerNPs fueron: 66.5 y 73.4 nm, y 83.59 y 76.48 %, respectivamente. Los NP son esféricos y redujeron significativamente la hemólisis en comparación con los extractos no encapsulados. Conclusiones: Las NP representan un sistema de administración de compuestos bioactivos útil y novedoso para la terapia enfermedades causadas por protozoos.

Exposing the Hepatotoxicity of Medicinal Plants: A Review of Copalchi Stem Bark (Hintonia latiflora) / Exponiendo la hepatotoxicidad de las plantas medicinales: una revisión de palo amargo (Hintonia latiflora)

Resumen Se estima que el 80% de la población mundial utiliza diversas plantas medicinales para el tratamiento o control de diversas enfermedades, ya sean agudas o crónicas, debido a su accesibilidad y bajo costo, observándose en los últimos años un aumento en el consumo sin una observación médica adecuada. México es considerado como el segundo país más importante del mundo en cuanto al conocimiento de la medicina tradicional, solo después de china. El uso de las plantas medicinales se ha reportado desde tiempos prehispánicos como una opción terapéutica, sin embargo, el único enfoque que se tiene es la parte curativa y no se ha reflexionado en que las plantas poseen metabolitos secundarios (compuestos químicos producidos por las plantas con actividad biológica en los seres vivos) que, además de tener efectos terapéuticos poseen efectos tóxicos en las personas que las consumen, observándose en algunos casos efectos reversibles después de suspender su consumo. El copalchi o palo amargo es una planta medicinal que proviene de la corteza del árbol de Hintonia latiflora (sin. Coutarea latiflora), la cual ha sido utilizada principalmente como tratamiento alternativo para pacientes con diabetes tipo 2, ya que se ha demostrado que tiene efecto hipoglucemiante. Sin embargo, se han reportado casos de hepatotoxicidad aguda con un incremento en las transaminasas hepáticas (ALT y AST) por el consumo continuo de dicha corteza, no obstante el procesamiento de las plantas medicinales utilizando medios físicos (calentar o hervir) puede alterar la actividad farmacológica de los constituyentes orgánicos, los cuales pueden verse también afectados en su concentración dependiendo de los factores ambientales de cultivo, localización del suelo, humedad y temperatura ambiental, así como la temporada de cosecha (tallos, hojas, flores, raíces, semillas). El consumo de esta planta medicinal es por medio de infusiones calientes o en cápsulas con extracto.

Abstract Approximately 80% of the world's population uses various medicinal plants for the treatment or control of various diseases, whether acute or chronic, due to their accessibility and low cost, observing in recent years an increase in consumption without proper medical observation. Mexico is considered the second most important country in the world in terms of traditional medicine knowledge, only after China. The use of medicinal plants has been reported since pre-Hispanic times as a therapeutic option; however, the only focus is on the curative part and it has not been considered that plants have secondary metabolites (chemical compounds produced by plants with biological activity in living beings) that, besides having therapeutic effects, have toxic effects in people who consume them, and in some cases reversible effects are observed after suspending their consumption. Copalchi or palo amargo is a medicinal plant obtained from the bark of the Hintonia latiflora tree (syn. Coutarea latiflora), which has been used mainly as an alternative treatment for patients with type 2 diabetes, since it has been shown to have a hypoglycemic effect. However, cases of acute hepatotoxicity have been reported with an increase in hepatic transaminases (ALT and AST) by the continuous consumption of this bark. However, the processing of medicinal plants using physical means (heating or boiling) can alter the pharmacological activity of the organic constituents, which can also be affected in their concentration depending on the environmental factors of cultivation, soil location, humidity, and environmental temperature, as well as the harvesting season (stems, leaves, flowers, roots, seeds). The consumption of this medicinal plant is by means of hot infusions or in capsules with extract.

Whitening efficacy of popular natural products on dental enamel

Abstract The objective of this study was to evaluate the effect of natural bleaching products on the color, whiteness, and superficial properties of dental enamel. Seventy fragments of bovine teeth were obtained (6mm x 6mm x 2mm). Initial surface roughness (Surfcorder SE1700, Kosakalab), microhardness (HMV-2, Shimadzu), color (EasyShade, VITA), and surface gloss (Micro-Gloss 45º BYK, Gardner) readings were done. Samples were separated into five groups (n=14) according to the treatments used: CT-conventional toothpaste (negative control); CH-charcoal; TU-turmeric; BP-banana peel, and CP16%-16% carbamide peroxide gel (positive control, 4 h/day for 14 days), and then brushed for 560 cycles (T1) and 1200 cycles (T2), equivalent to 14 and 30 days of brushing. New measurements were performed after T1 and T2. The whiteness index for dentistry change (∆WID) and Weight loss (Wl) were calculated. CP16% demonstrated the highest (p<.05) color change (ΔE00) and ∆WID (2-way ANOVA, Bonferroni, p<.05). Surface gloss alterations were lower for TU, CP16%, and BP. CT and CH increased surface roughness (p<.05). CP16% decreased enamel microhardness. CH presented medium abrasiveness, and CT and TU, low abrasiveness. The popular bleaching products were not efficient for tooth whitening. Furthermore, brushing with charcoal increased the enamel surface roughness, and CP16% decreased enamel microhardness over time

Resumo O objetivo deste estudo foi avaliar o efeito de produtos clareadores naturais na cor, efeito clareador e propriedades superficiais do esmalte dentário. Setenta fragmentos de dente bovino foram obtidos (6mm x 6mm x 2mm). Foram realizadas leituras iniciais de rugosidade de superfície (Surfcorder SE1700, Kosakalab), microdureza (HMV-2, Shimadzu), cor (EasyShade, VITA) e brilho (Micro-Gloss 45º BYK, Gardner). As amostras foram separadas em cinco grupos (n=14), de acordo com os tratamentos utilizados: DC - dentifrício convencional (controle negativo); CA - carvão ativado; CM - cúrcuma; CB - casca de banana e PC16% - gel de peróxido de carbamida a 16% (controle positivo, 4h/dia por 14 dias), foram então escovadas por 560 ciclos (T1) e 1200 ciclos (T2), equivalente a 14 e 30 dias de escovação. Novas leituras foram realizadas após T1 e T2. A alteração do whiteness index for dentistry (∆WID) e perda de massa (Pm) foram calculadas. PC16% demonstrou a maior (p<0,05) alteração de cor (ΔE00) e ∆WID (2-way ANOVA, Bonferroni, p<0,05). A alteração de brilho foi menor para CM, PC16% e CB. DC e CA aumentaram a rugosidade de superfície (p<0,05). PC16% diminuiu a microdureza do esmalte. CA apresentou abrasividade média, e DC e CM, baixa abrasividade. Os produtos clareadores populares não foram eficientes para clareamento dental. Ademais, a escovação com carvão ativado aumentou a rugosidade de superfície do esmalte dentário, e com maior tempo PC16% diminuiu a microdureza do esmalte.