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The main objective of this review is to highlight the therapeutic potential of allicin, a defense molecule in garlic known for its diverse health benefits, and address the key challenges of its bioavailability and stability. The research further aims to evaluate various formulation strategies and nanotechnology-based delivery systems that can resolve these issues and improve allicin's clinical efficacy, especially in cancer therapy. We conducted a comprehensive review of the available literature and previous studies, focusing on the therapeutic properties of allicin, its bioavailability, stability issues, and novel formulation strategies. We assessed the mechanism of action of allicin in cancer, including its effects on signaling pathways, cell cycle, apoptosis, autophagy, and tumor development. We also evaluated the outcomes of both in vitro and in vivo studies on different types of cancers, such as breast, cervical, colon, lung, and gastric cancer. Despite allicin's significant therapeutic benefits, including cardiovascular, antihypertensive, cholesterol-lowering, antimicrobial, antifungal, anticancer, and immune-modulatory activity, its clinical utility is limited due to poor stability and unpredictable bioavailability. Allicin's bioavailability in the gastrointestinal tract is dependent on the activity of the enzyme alliinase, and its stability can be affected by various conditions like gastric acid and intestinal enzyme proteases. Recent advances in formulation strategies and nanotechnology-based drug delivery systems show promise in addressing these challenges, potentially improving allicin's solubility, stability, and bioavailability. Allicin offers substantial potential for cancer therapy, yet its application is hindered by its instability and poor bioavailability. Novel formulation strategies and nanotechnology-based delivery systems can significantly overcome these limitations, enhancing the therapeutic efficacy of allicin. Future research should focus on refining these formulation strategies and delivery systems, ensuring the safety and efficacy of these new allicin formulations. Clinical trials and long-term studies should be carried out to determine the optimal dosage, assess potential side effects, and evaluate their real-world applicability. The comparative analysis of different drug delivery approaches and the development of targeted delivery systems can also provide further insight into enhancing the therapeutic potential of allicin.

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Objectives: To evaluate the effectiveness and potential mechanism of traditional Chinese medicine Jiawei-Xiaoyao-San (JWXYS) as an adjunct or mono- therapy for antithyroid drugs (ATDs) in the treatment of hyperthyroidism. Methods: Eight databases and three trial registries were searched from inception until May 2023. Randomized controlled trials (RCTs) were included and meta-analysis was conducted using RevMan 5.4 and Stata 14.0. The Cochrane risk of bias (ROB) tool 1.0 and GRADE tool was used for quality appraisal. The findings from case reports using mono-JWXYS and pharmacological studies were summarized in tables. Results: Thirteen RCTs with 979 participants were included. The majority of the included studies were assessed as high risk of bias in one ROB domain. Compared with ATDs, JWXYS plus ATDs resulted in lower free triiodothyronine (FT3) (MD = -1.31 pmol/L, 95% CI [-1.85, -0.76]; low-certainty), lower free thyroxine (MD = -3.24 pmol/L, 95% CI [-5.06, -1.42]; low-certainty), higher thyroid stimulating hormone (MD = 0.42 mIU/L, 95% CI [0.26, 0.59]; low-certainty), higher effectiveness rate of traditional Chinese medicine syndrome (RR = 1.28, 95% CI [1.08, 1.52]; low-certainty), lower goiter score (MD = -0.66, 95% CI [-1.04, -0.29]; very low-certainty), lower thyrotrophin receptor antibody (SMD = -0.44, 95% CI [-0.73, -0.16]; low-certainty) and fewer adverse events (AEs) (RR = 0.34, 95% CI [0.18, 0.67]; moderate-certainty). Compared with regular dosage of ATDs, JWXYS plus half-dose ATDs resulted in fewer AEs (RR = 0.24, 95% CI [0.10, 0.59]; low-certainty). Compared with ATDs in 1 trial, JWXYS resulted in higher FT3, lower goiter score and fewer AEs. Three case reports showed that the reasons patients sought TCM-only treatment include severe AEs and multiple relapses. Three pharmacological studies demonstrated that JWXYS restored Th17/Treg balance, lowered deiodinases activity, regulated thyroid cell proliferation and apoptosis, and alleviated liver oxidative stress in mouse or rat models. Conclusion: JWXYS may enhance the effectiveness of ATDs for hyperthyroidism, particularly in relieving symptoms and reducing AEs. Mono-JWXYS is not recommended except in patients intolerant to ATDs. The findings should be interpreted with caution due to overall high risk of bias. Further pharmacological studies with more reliable models are needed. Systematic review registration: https://www.crd.york.ac.uk/prospero/, identifier CRD42023394923.

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Eurycoma longifolia plant, the so called Tongkat Ali in Malaysia, is a well grown prominent tree in all Southeast Asia. It is well known among traditional medicine practitioners as a curative plant for many diseases and health conditions. The major quassinoid from the plant is eurycomanone, which exhibits many prominent effects on various cancer cell lines. Numerous studies have shown that eurycomanone inhibits cancerous cell growth and encourages cell death both in vitro and in vivo test. Even though analyses of safety and toxicity have been conducted, there is still a substantial knowledge barrier when it comes to providing a scientific foundation for the molecular mechanism as well as intervention strategy in the living people cancer cell. In a way to offer adequate baseline data for future investigations based on molecular mechanism and intervention, the present work seeks to review the researches conducted to date on this herbal plant.

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Woodfordia fruticosa (L.) Kurz is a woody medicinal shrub (Lythraceae) commonly known as the "fire flame bush." W. fruticosa plant parts either alone or whole plant have a long history of recommended use in the Indian medicine systems of Ayurveda, Unani, and Siddha (AUS). This plant is prominently known for its pharmacological properties, viz., antimicrobial, anti-inflammatory, anti-peptic ulcer, hepatoprotective, immunomodulatory, antitumor, cardioprotective, analgesic, and wound healing activities. Its important phyto-constituents, woodfordin C, woodfordin I, oenothein B, and isoschimacoalin-A, exhibit in vitro or in vivo physiological activities beneficial to human health. As the plant is a rich storehouse of phyto-constituents, it is indiscriminately used in its wild habitats. Moreover, due to very poor seed viability and difficult-to-root qualities, it is placed under IUCN list of endangered plant species. For W. fruticosa, biomass production or to its conservation by in vitro regeneration is the best feasible alternative. Till date, only few important in vitro regeneration methods are reported in W. fruticosa. ISSR molecular markers based clonal fidelity and Agrobacterium-mediated transformation has been demonstrated, indicating that W. fruticosa is amenable to genetic manipulation and genome editing studies. This review presents concise summary of updated reports on W. fruticosa phyto-constituents and their biological activities, while a critical appraisal of biotechnological interventions, shortcomings, and factors influencing such potential areas success was presented. The unexplored gaps addressed here are relevant for W. fruticosa scientific innovations yet to come. In this paper, for the first time, we have presented a simple and reproducible protocol for synthetic seed production in W. fruticosa. KEY POINTS: • Critical and updated records on W. fruticosa phytochemistry and its activities • In vitro propagation and elicitation of secondary metabolites in W. fruticosa • Key bottlenecks, in vitro flowering, value addition, and outlook in W. fruticosa.

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Diabetes mellitus is a metabolic disorder characterized by the presence of chronic hyper-glycemia that is accompanied, to a greater or lesser extent, by alterations in the metabolism of carbohydrates, proteins and lipids. It is the leading cause of death in developed countries. Current antidiabetic drug treatments present several adverse effects for which it has started searching for new oral hypoglycemic agents from vegetal species. This review presents the medicinal plants from the Peruvian Amazon used in the treatment of diabetes and a systematic review of their hypoglycemic properties reported in the literature in the last twenty years used in different bibliographic databases. Seventy seven medicinal plants are reported as being used for the treatment of diabetes by Amazonian indigenous people, which 46.75% of species report hypoglycemic activity, evidencing that traditional knowledge is a great source for to searching antidiabetic drugs and also an alternative for future research.

La diabetes mellitus es un trastorno metabólico caracterizado por la presencia de hiperglucemia crónica acompañada, en mayor o menor medida, de alteraciones en el metabolismo de carbohidratos, proteínas y lípidos, es la principal causa de muerte en los países desarrollados. Los tratamientos actuales con fármacos anti-diabéticos presentan varios efectos adversos, por lo que se ha iniciado una búsqueda de nuevos hipoglucemiantes orales a partir de especies vegetales. Esta revisión presenta las plantas medicinales de la amazonia peruana utilizadas en el tratamiento de la diabetes y una revisión sistemática de sus propiedades hipoglucémicas reportadas en la literatura en los últimos veinte años utilizando bases de datos bibliográficas. Se reportan 77 plantas medicinales utilizadas para el tratamiento de la diabetes por pobladores amazónicos, de las cuales el 46.75% reporta actividad hipoglucémica, evidenciando que el conocimiento tradicional es una fuente para la búsqueda de fármacos antidiabéticos y una alternativa para futuras investigaciones

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This report summarizes the chemical composition analysis of Nepeta cataria L. flower, leaf, and stem methanol extracts (FME, LME, SME, respectively) as well as their hepatoprotective and antigenotoxic features in vivo and in silico. Herein, Wistar rat liver intoxication with CCl4 resulted in the generation of trichloromethyl and trichloromethylperoxy radicals, causing lipid peroxidation within the hepatocyte membranes (viz. hepatotoxicity), as well as the subsequent formation of aberrant rDNA adducts and consequent double-strand break (namely genotoxicity). Examined FME, LME, and SME administered orally to Wistar rats before the injection of CCl4 exerted the most notable pharmacological properties in the concentrations of 200, 100, and 50 mg/kg of body weight, respectively. Thus, the extracts' hepatoprotective features were determined by monitoring the catalytic activities of enzymes and the concentrations of reactive oxidative species, modulating the liver redox status. Furthermore, the necrosis of hepatocytes was assessed by means of catalytic activities of liver toxicity markers. The extracts' antigenotoxic features were quantified using the comet assay. Distinct pharmacological property features may be attributed to quercitrin (8406.31 µg/g), chlorogenic acid (1647.32 µg/g), and quinic acid (536.11 µg/g), found within the FME, rosmarinic acid (1056.14 µg/g), and chlorogenic acid (648.52 µg/g), occurring within the LME, and chlorogenic acid (1408.43 µg/g), the most abundant in SME. Hence, the plant's secondary metabolites were individually administered similar to extracts, upon which their pharmacology in vivo was elucidated in silico by means of the structure-based studies within rat catalase, as a redox marker, and rat topoisomerase IIα, an enzyme catalyzing the rat DNA double-strand break. Conclusively, the examined N. cataria extracts in specified concentrations could be used in clinical therapy for the prevention of toxin-induced liver diseases.

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Cumulative evidence has pointed out cannabinoid CB2 receptors (CB2r) as a potential therapeutic key target for treating alcohol use disorder (AUD). This review provides the most relevant results obtained from rodent and human studies, including an integrative section focused on the involvement of CB2r in the neurobiology of alcohol addiction. A literature search was conducted using the electronic databases Medline and Scopus for articles. The search strategy was as follows: "Receptor, Cannabinoid, CB2" AND "Alcohol-Related Disorders" AND "human/or patients"; "Receptor, Cannabinoid, CB2" AND "Alcohol" OR "Ethanol" AND "rodents/or mice/or rats". Pharmacological approaches demonstrated that the activation or blockade of CB2r modulated different alcohol-addictive behaviors. Rodent models of alcoholism revealed significant alterations of CB2r in brain areas of the reward system. In addition, mice lacking CB2r (CB2KO) show increased alcohol consumption, motivation, and relapse alterations. It has been stressed that the potential neurobiological mechanisms underlying their behavioral effects involve critical elements of the alcohol reward system. Interestingly, recent postmortem studies showed CNR2 alterations in brain areas of alcoholic patients. Moreover, although the number of studies is limited, the results revealed an association between some genetic alterations of the CNR2 and an increased risk for developing AUD. This review provides evidence that CB2r may play a role in alcohol addiction. Clinical studies are necessary to figure out whether CB2r ligands may prove useful for the treatment of AUD in humans.

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One of the most important trends in chemotherapy is the development of green chemotropic drugs with maximal activity and minimal side effects. The nanoencapsulation of phytochemical oils with natural polymers has been documented as a promising approach to producing nanodrugs with sustainable bioactivity and prolonged stability. In this context, Syzygium aromaticum essential oil (SAEO) and ultrasound-assisted deacetylated chitosan (UCS3) were successfully extracted from clove buds and squid pens, respectively. Grafting of UCS3 by ρ-coumaric acid (ρCA) has been performed to fabricate the ρCACS nanogel which was used for nanoencapsulation of SAEO to yield SAEO-loaded nanogel (ρCACS@SAEO). The findings of spectral, thermal, and morphological analyses have confirmed the success of the formation of new materials and SAEO encapsulation, as well. Based on the findings of the in vitro antimicrobial, antioxidant, and anticancer studies, the nanoencapsulation of SAEO by ρCACS has significantly boosted its chemotherapeutic effects, compared to unencapsulated oil. Therefore, ρCACS@SAEO nanogel could be considered as a multifunctional chemotherapeutic/chemopreventive agent for prevention or therapy of pathologies induced by oxidative stress, microbial infection, and breast and skin cancer.

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Selective GluN2B/N-methyl-D-aspartate receptor (NMDAR) antagonists have exposed their clinical effectiveness in a cluster of neurodegenerative diseases, such as epilepsy, Alzheimer's disease, Parkinson's disease, pain, and depression. Hence, GluN2B/NMDARs are considered to be a prospective target for the management of neurodegenerative diseases. Here, we have discussed the current results and significance of subunit selective GluN2B/NMDAR antagonists to pave the way for the establishment of new, safe, and economical drug candidates in the near future. By using summarized data of selective GluN2B/NMDAR antagonists, medicinal chemists are certainly a step closer to the goal of improving the therapeutic and side effect profile of selective antagonists. Outlined summary of designing strategies, synthetic schemes, and pharmacological evaluation studies reinvigorate efforts to identify, modify, and synthesize novel GluN2B/NMDAR antagonists for treating neurodegenerative diseases.

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Uapaca bojeri is an endemic Malagasy plant used by the local population. This work aimed to evaluate antioxidant, anti-inflammatory, and antidiabetic activities of the methanol extracts of U. bojeri leaves and stems and to report their total phenolic content and the bioactive compound content by HPLC methods. Antioxidant capacity was determined by DPPH and ferric reducing antioxidant power (FRAP) assays. An in vivo carrageenan-induced paw oedema and acetic acid-induced writhing test in mice were used for anti-inflammatory activity evaluation. An oral glucose tolerance test was performed in mice to evaluate antidiabetic activity. The total bioactive compound content of leaves was higher than that of stems. Stem methanol extract inhibited the free radical DPPH more than the leaf methanol extract. Leaf methanol extract inhibited, in a dose-dependent manner, the carrageenan-induced paw oedema more than the stem extract, but their inhibition of the pain symptoms caused an acetic acid-induced decrease similar to the number of writhes in the dose-dependent case. The leaf and stem methanol extracts significantly reduced blood glucose levels after 30 min of glucose loading in mice compared to the control group blood glucose reduction. The presence of several bioactive compounds in U. bojeri contributed to the different biological activities, but isolation and identification of these bioactive molecules are necessary to confirm these pharmacological properties.

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ETHNOPHARMACOLOGICAL RELEVANCE: The genus Polygala, the most representative genus of the Polygalaceae family, comprises more than 600 species from all over the world of which around 40 are distributed in China, some of them, being used in the Traditional Chinese Medicine system. AIM OF THE REVIEW: We intend to discuss the current knowledge about the traditional uses, and the newest phytochemical and pharmacological achievements with tentative elucidation of the mechanism of action on the genus Polygala covering the period 2013-2019 to provide a scientific support to the traditional uses, and to critically analyze the reported studies to obtain new insights for further researches. MATERIALS AND METHODS: The data were systematically collected from the scientific electronic data bases including SciFinder, Scopus, Elsevier, PubMed and Google Scholar. RESULTS: This literature overview reported several traditional uses of different species of Polygala, mainly against wounds, inflammation, cardiovascular and central nervous system disorders. P. altomontana, P caudata, P. flavescens, P. glomerata, P. japonica, P. molluginifolia, P. sibirica, P. tenuifolia are the main species which have been studied in the last few years. Phytochemical studies showed that they contain triterpene saponins, triterpenes, terpenoids, xanthones, flavonoids, coumarins, oligosaccharide esters, styryl-pyrones, benzophenones, and polysaccharides. Pharmacological in vitro and in vivo studies and proposal of the mechanisms of action indicated that pure constituents and extracts of Polygala ssp exhibited significant anti-inflammatory, neuroprotective, antiischemic, antidepressant, sedative, analgesic, antiatherosclerosis, antitumor and enzyme inhibitory properties. CONCLUSION: This review on traditional uses and phytopharmacological potential of the genus Polygala revealed updated insights which can be explored for further mechanism-based pharmacological activities and structure/activity relationships studies and a better comprehension of the development of Chinese medicine preparations. However some pharmacological studies showed several gaps such as incomplete methodologies and ambiguous findings. More high scientific quality preclinical studies with pharmacokinetic considerations will be required in the future to assess the traditional uses of some species of this genus. This might lead to efficacy and safety issues in clinical trials and to potential medicinal applications.

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Chalcones are among the leading bioactive flavonoids with a therapeutic potential implicated to an array of bioactivities investigated by a series of preclinical and clinical studies. In this article, different scientific databases were searched to retrieve studies depicting the biological activities of chalcones and their derivatives. This review comprehensively describes preclinical studies on chalcones and their derivatives describing their immense significance as antidiabetic, anticancer, anti-inflammatory, antimicrobial, antioxidant, antiparasitic, psychoactive, and neuroprotective agents. Besides, clinical trials revealed their use in the treatment of chronic venous insufficiency, skin conditions, and cancer. Bioavailability studies on chalcones and derivatives indicate possible hindrance and improvement in relation to its nutraceutical and pharmaceutical applications. Multifaceted and complex underlying mechanisms of chalcone actions demonstrated their ability to modulate a number of cancer cell lines, to inhibit a number of pathological microorganisms and parasites, and to control a number of signaling molecules and cascades related to disease modification. Clinical studies on chalcones revealed general absence of adverse effects besides reducing the clinical signs and symptoms with decent bioavailability. Further studies are needed to elucidate their structure activity, toxicity concerns, cellular basis of mode of action, and interactions with other molecules.

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ETHNOPHARMACOLOGICAL RELEVANCE: The prescription of Shenling Baizhu San (SLBZS) was derived from the Song Dynasty "Taiping Huimin Heji Ju Fang", which was a representative prescription for treating spleen asthenic diarrhea. The prescription comprised of 10 herbs for treating weak spleen and stomach. It describes symptoms like eating less, loose stools, cough, shortness of breath and tired limbs. SLBZS has been reported to be capable of eliminating discomfort when it is administered for treating irritable bowel syndrome and diarrhea. This traditional Chinese medicine (TCM) formula has been widely used for improving gastrointestinal dysfunction and modifying the immune response to inflammation. AIM OF THE STUDY: This review is aimed to provide the up-to-date information on the pharmacology and clinical research of SLBZS in the treatment of ulcerative colitis (UC), and to discuss the research findings and possible deficiencies, hoping to better guide the clinical application and scientific research of SLBZS in the treatment of UC. MATERIALS AND METHODS: Relevant studies from 2004 to 2018 on SLBZS in the treatment of UC mechanism and curative effect were collected from ancient books, pharmacopoeia, reports, thesis via library and Digital databases (PubMed, CNKI, Google Scholar, Web of Science, SciFinder, Springer, Elsevier, etc). RESULTS: SLBZS could regulate inflammatory factors and intestinal flora, and ERK/p38 MAPK signaling pathway may be one of its targets. In addition, clinical research results show that SLBZS has a good therapeutic effect on UC, and the adverse reactions are small. CONCLUSION: Although SLBZS has achieved some success in the treatment of UC, there are still some scientific gaps. There is a lack of uniform standards for constructing UC animal models, and some methods of modeling through environmental and dietary interventions are not reproducible, and there is a lack of uniform dosing regimen standards. SLBZS doses follow the tradition and lack toxicological validation. Therefore, more specific toxicological research models are essential. The clinical application of SLBZS requires reassessment and standardization. Although all clinical research reports randomly assigned patients to different groups, most did not describe a detailed method of randomization and no description of the analysis data. In addition, extensive in vitro studies and further in-depth molecular studies are essential for the determination of mechanisms that have been performed in all in vivo experiments on animal models and patients.

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Dioscorea nipponica Makino is a perennial twining herbs belonging to the family Dioscoreaceae, which is mainly distributed in the northeastern, northern, eastern and central regions of China. Traditionally, the rhizome of this herb has been commonly used by Miao and Meng ethnic groups of China to treat rheumatoid arthritis, pain in the legs and lumbar area, Kashin Beck disease, bruises, sprains, chronic bronchitis, cough and asthma. Modern pharmacological studies have discovered that this herb possesses anti-tumor, anti-inflammatory, anti-diuretic, analgesic, anti-tussive, panting-calming and phlegm-dispelling activities, along with enhancing immune function and improving cardiovascular health. In recent years, both fat-soluble and water-soluble steroidal saponins were isolated from the rhizomes of D. nipponica using silica gel column chromatography, thin layer chromatography and high performance liquid chromatography methods. Saponin and sapogenins are mainly responsible for most of the pharmacological effects of this plant. Further, the chemical components of the aboveground parts contain more than 10 kinds of phenanthrene derivatives. The present review summarizes the knowledge concerning the geographical distribution, chemical composition, pharmacological effects, toxicology studies and clinical applications of D. nipponica.

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Primary human hepatocytes represent an important cell source for in vitro investigation of hepatic drug metabolism and disposition. In this study, a multi-compartment capillary membrane-based bioreactor technology for three-dimensional (3D) perfusion culture was further developed and miniaturized to a volume of less than 0.5 ml to reduce demand for cells. The miniaturized bioreactor was composed of two capillary layers, each made of alternately arranged oxygen and medium capillaries serving as a 3D culture for the cells. Metabolic activity and stability of primary human hepatocytes was studied in this bioreactor in the presence of 2.5% fetal calf serum (FCS) under serum-free conditions over a culture period of 10 days. The miniaturized bioreactor showed functions comparable to previously reported data for larger variants. Glucose and lactate metabolism, urea production, albumin synthesis and release of intracellular enzymes (AST, ALT, GLDH) showed no significant differences between serum-free and serum-supplemented bioreactors. Activities of human-relevant cytochrome P450 (CYP) isoenzymes (CYP1A2, CYP3A4/5, CYP2C9, CYP2D6, CYP2B6) analyzed by determination of product formation rates from selective probe substrates were also comparable in both groups. Gene expression analysis showed moderately higher expression in the majority of CYP enzymes, transport proteins and enzymes of Phase II metabolism in the serum-free bioreactors compared to those maintained with FCS. In conclusion, the miniaturized bioreactor maintained stable function over the investigated period and thus provides a suitable system for pharmacological studies on primary human hepatocytes under defined serum-free conditions.

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ETHNOPHARMACOLOGICAL RELEVANCE: This is an extensive review of plants used traditionally for women's healthcare in Southeast Asia and surrounding countries. Medicinal plants have a significant role in women's healthcare in many rural areas of the world. Plants with numerous efficacious observations have historically been used as a starting point in the development of new drugs, and a large percentage of modern pharmaceuticals have been derived from medicinal plants. MATERIALS AND METHODS: A review was conducted for all plant use mentioned specifically for female healthcare, such as medicine to increase fertility, induce menstruation or abortion, ease pregnancy and parturition, reduce menstrual bleeding and postpartum hemorrhage, alleviate menstrual, parturition and postpartum pain, increase or inhibit lactation, and treat mastitis and uterine prolapse, in 200 studies focusing on medicinal plant use, either general studies or studies focusing specifically on women's healthcare. RESULTS: Nearly 2000 different plant species are reported to be used in over 5000 combinations. Most common are Achyranthes aspera, Artemisia vulgaris, Blumea balsamifera, Carica papaya, Curcuma longa, Hibiscus rosa-sinensis, Leonurus japonicus, Psidium guajava and Ricinus communis, and each of these species had been reported in more than 10 different scientific articles. CONCLUSIONS: This review provides a basis for traditional plant use in women's healthcare, and these species can be used as the starting point in the discovery of new drugs.

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La realización de estudios farmacocinéticos es una actividad que se efectúa en algunos centros investigativos del país. Para llevarlos a cabo se hizo necesario procesar los datos obtenidos de los análisis que se realizan a las especies de laboratorio, ya que actualmente es una labor engorrosa que demanda la utilización de medios de cómputo. En el Centro de Isótopos se usan dos software que además de ser obsoletos, no satisfacen las necesidades de los especialistas, por lo que el objetivo del trabajo se enmarca en realizar una aplicación Web que integre las funcionalidades de los software existentes en esta actividad e incluya otras nuevas que faciliten el proceso investigativo. Anteriormente, se implementó una aplicación web para estudios farmacocinéticos, dicha aplicación permite gestionar y almacenar la información obtenida al realizar un estudio farmacocinético, así como el cálculo de parámetros, pero esta primera versión del software está muy lejos de cumplir las expectativas de los especialistas, por lo que se decide trabajar en una segunda versión del software PK-Web, la versión 2.0 a la cual se le agregarán nuevas funcionalidades a implementar como son: la gestión de archivos referentes al plan de estudio, la implementación de un Web Service y el ajuste de curva, entre otras(AU)

In Cuba the studies of pharmacokinetic is an activity which takes place at some research centers of the country. In order to do so it is necessary to process the data obtained from the analysis that are performed to laboratory species, which currently is a cumbersome task that requires the use of computing resources. The researchers at Isotopes Center uses two software which, besides being obsolete, do not meet the needs of specialists, so the goal of this project is making a web application that integrates the functionality of existing software in this activity and include other new to facilitate the research process. Previously, we implemented a web application for pharmacokinetic studies, this application allows researchers to manage and store the information obtained from a pharmacokinetic study, as well as calculation of parameters, but this first version of the software is far from meeting the expectations of specialists, so it was decided to work on a second version of the PK-Web software, version 2.0 which will add new features to implement, such as: file management regarding the curriculum, the implementation of a web Service and curve fitting, among others(AU)

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Two recent health technology assessment (HTA) reports published in Germany focused on non-pharmacological interventions for patients with dementia. One of the major results was the poor methodological quality of the studies in this field. This paper concisely presents the main quantitative and qualitative findings of the HTA report published by the German Agency for HTA at the Institute of Medical Information and Documentation (dahta@DIMDI), followed by a detailed discussion of the major methodological problems observed for the inclusion criteria, interventions, the setting, number of patients included, duration of observation, comparators, clinical endpoints, health economics, and, most obvious, the impossibility of blinding and eliminating placebo effects for future clinical studies. We conclude with several suggestions addressing these challenges for future research in this field.

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We describe structure-activity relationship and optimization studies of RN-18, an HIV-1 Vif-APOBEC3G axis inhibitor. Targeted modifications of RN-18 ring-C, ring-B, ring-A, bridge A-B, and bridge B-C were performed to identify the crucial structural features, which generated new inhibitors with similar (4g and 4i) and improved (5, 8b, and 11) activities. Two potent water-soluble RN-18 analogues, 17 and 19, are also disclosed, and we describe the results of pharmacological studies with compound 19. The findings described here will be useful in the development of more potent Vif inhibitors and in the design of probes to identify the target protein of RN-18 and its analogues.

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Objective To compare the efficacy for phytochemical, antibacterial and antioxidant activities of petroleum ether, chloroform, ethanol, and aqueous extracts of in vitro propagated plants and field grown plants of Crotalaria sps., for against five human pathogens. Methods The preliminary phytochemistry, antimicrobial and antioxidant activities were evaluated using disc diffusion and DPPH radical scavenging methods. Results The ethanolic extract of in vitro raised Crotalaria retusa (C. retusa) was effective on tested microorganisms and optimal ZOI values of 38 mm was obtained against Pseudomonas aeruginosa (P. aeruginosa). The optimal concentration (IC50) required for 50% inhibition of the DPPH radical scavenging was 57.6 μ g/mL obtained for ethanolic extract of in vitro propagated C. retusa. The in vitro propagated C. retusa has significant pharmacological activities while the Crotalaria prostrate (C. prostrate) and Crotalaria medicaginea (C. medicaginea) has low pharmacological activites. It was cleared that ethanolic extract of in vitro regenerated plants was most effective. Conclusions These findings indicate compounds isolated from ethanolic extracts of Crotalaria sps., possesses pharmacological properties and potential to develop natural compounds based pharmaceutical products. The IC