Articulating the Pharmacological and Nanotechnological Aspects of Genistein: Current and Future Prospectives.

Throughout the past several centuries, herbal constituents have been the subject of scientific interest and the latest research into their therapeutic potential is underway. Genistein is a soy-derived isoflavone found in huge amounts in soy, along with the plants of the Fabaceae family. Scientific studies have demonstrated the beneficial effects of genistein on various health conditions. Genistein presents a broad range of pharmacological activities, including anticancer, neuroprotective, cardioprotective, antiulcer, anti-diabetic, wound healing, anti-bacterial, antiviral, skin, and radioprotective effects. However, the hydrophobic nature of genistein results in constrained absorption and restricts its therapeutic potential. In this review, the number of nanocarriers for genistein delivery has been explored, such as polymeric nanoparticles, nanostructured lipid carriers, solid lipid nanoparticles, liposomes, micelles, transferosomes, and nanoemulsions and nanofibers. These nano-formulations of genistein have been utilized as a potential strategy for various disorders, employing a variety of ex vivo, in vitro, and in vivo models and various administration routes. This review concluded that genistein is a potential therapeutic agent for treating various diseases, including cancer, neurodegenerative disorders, cardiovascular disorders, obesity, diabetes, ulcers, etc., when formulated in suitable nanocarriers.

The classical D1 dopamine receptor antagonist SCH23390 is a functional sigma-1 receptor allosteric modulator.

SCH23390 is a widely used D1 dopamine receptor (D1R) antagonist that also elicits some D1R-independent effects. We previously found that the benzazepine, SKF83959, an analog of SCH23390, produces positive allosteric modulation of the Sigma-1 receptor (Sig1R). SCH23390 does not bind to the orthodoxic site of Sig1R but enhances the binding of 3H (+)-pentazocine to Sig1R. In this study, we investigated whether SCH23390 functions as an allosteric modulator of Sig1R. We detected increased Sig1R dissociation from binding immunoglobulin protein (BiP) and translocation of Sig1R to the plasma membrane in response to SCH23390 in transfected HEK293T and SH-SY5Y cells, respectively. Activation of Sig1R by SCH23390 was further confirmed by inhibition of GSK3ß activity in a time- and dose-dependent manner; this effect was blocked by pretreatment with the Sig1R antagonist, BD1047, and by knockdown of Sig1R. SCH23390 also inhibited GSK3ß in wild-type mice but not in Sig1R knockout mice. Finally, we showed that SCH23390 allosterically modulated the effect of the Sig1R agonist SKF10047 on inhibition of GSK3ß. This positive allosteric effect of SCH23390 was further confirmed via promotion of neuronal protection afforded by SKF10047 in primary cortical neurons challenged with MPP+. These results provide the first evidence that SCH23390 elicits functional allosteric modulation of Sig1R. Our findings not only reveal novel pharmacological effects of SCH23390 but also indicate a potential mechanism for SCH23390-mediated D1R-independent effects. Therefore, attention should be paid to these Sig1R-mediated effects when explaining pharmacological responses to SCH23390.

Unraveling Amentoflavone's Therapeutic Potential in Alzheimer's Disease: A Preclinical Assessment.

Alzheimer's disease is one of the neurodegenerative diseases which causes cognition deficit. There are currently few medications available to treat Alzheimer's disease, even though researchers have devoted a great deal of time studying the condition and offering many benefits. Thus, only a few drugs are available for the treatment of Alzheimer's disease. Amentoflavone is a dietary component found in many plants and herbs that has several health advantages. Amentoflavone has demonstrated strong protective benefits against a range of brain illnesses in preclinical trials, most frequently in Alzheimer's disease. Amentoflavone, a biflavonoid, can be identified in a variety of herbs upon isolation. Considering the beneficial properties of this compound, this review emphasizes the pharmacological effects and botanical sources of amentoflavone, as well as the compound's benefits and possible applications in the treatment of Alzheimer's disorders.

A Review on Bioactive Compounds, Ethnomedicinal Importance and Pharmacological Activities of Talinum triangulare (Jacq.) Willd.

Talinum triangulare (Jacq.) Willd. is a traditional leafy vegetable used by tribal communities for ethnomedicinal and ethnoculinary preparations. This article reviews the current knowledge of its multiple uses, including pharmacological activities and nutritional composition. The literature survey shows that it has been traditionally useful in the treatment of several diseases, such as anaemia, diabetes, measles, and ulcers and the preparation of various traditional foods. Analysis of the literature on its phytochemicals shows its richness in bioactive compounds. Further, research also shows that this plant has antidiabetic, antiobesity, antitumor, antiulcer, hepatoprotective, and neuroprotective activities besides anti-inflammatory and antioxidant properties. Nutrient analysis of the plant reveals the presence of Ca, Zn, Fe, vitamins C and E, dietary fibre and protein in considerable quantities. The results of the pharmacological studies on the antidiabetic, antiulcer and anti-anaemic activities provide support in favour of its ethnomedicinal uses. The presence of bioactive compounds and pharmacological activities show the usefulness of this plant as a functional food.

A Cross-Sectional Evaluation of Dental Professional's Knowledge of Locally Delivered Antimicrobial Agents and their Application in Periodontal Practice.

Introduction: Dentists must employ locally delivered antimicrobial agents (LDAs) in a way that is in line with current recommendations from the scientific literature and the guidelines set by professional organizations. Considering the dearth of research on this topic, it is not known what strategies are adapted when using LDAs in their periodontal practice. So, the purpose of this research was to investigate how LDAs are utilized by dental professionals in their distinct periodontal practices. Materials and Methods: This cross-sectional study used a closed-ended questionnaire. Dental professionals received electronic copies of the eight-item questionnaire. The questionnaire assessed the relevance of LDAs, how frequently they are used, which ones are used most, the number of patients who receive them, their understanding of pharmacological activities, and their knowledge of current treatment guidelines. The questionnaire's validity and reliability were evaluated before being presented to participants. Using the Statistical Package for the Social Sciences (SPSS), the input was analyzed. Results: A total of 120 dental professionals, with an average age of 34.7 years, answered the questionnaire. Half of these individuals have no history of ever using LDAs. The most frequent LDA used in its different forms was chlorhexidine gluconate (CHX), followed by tetracycline. The majority of participants placed LDAs (80%) in less than 10 patients. Less than half acknowledged the different LDAs and their pharmacological activities. Not even 70% of clinicians were up-to-date on the current European Federation of Periodontology (EFP) guidelines. None of the participants discounted the significance of LDAs in periodontal care. Conclusion: Dental professionals regard LDAs as essential to periodontal therapy. Yet, they lacked knowledge about general, pharmacological, and clinical aspects. The patient experience with LDAs was limited by an inappropriate deployment pattern.

Natto: A medicinal and edible food with health function.

Natto is a soybean product fermented by natto bacteria. It is rich in a variety of amino acids, vitamins, proteins and active enzymes. It has a number of biological activities, such as thrombolysis, prevention of osteoporosis, antibacterial, anticancer, antioxidant and so on. It is widely used in medicine, health-care food, biocatalysis and other fields. Natto is rich in many pharmacological active substances and has significant medicinal research value. This paper summarizes the pharmacological activities and applications of natto in and outside China, so as to provide references for further research and development of natto.

Guaiazulene and related compounds: A review of current perspective on biomedical applications.

BACKGROUND: Thousands of people worldwide pass away yearly due to neurological disorders, cardiovascular illnesses, cancer, metabolic disorders, and microbial infections. Additionally, a sizable population has also been impacted by hepatotoxicity, ulcers, gastroesophageal reflux disease, and breast fissure. These ailments are likewise steadily increasing along with the increase in life expectancy. Finding innovative therapies to cure and consequently lessen the impact of these ailments is, therefore, a global concern. METHODS AND MATERIALS: All provided literature on Guaiazulene (GA) and its related compounds were searched using various electronic databases such as PubMed, Google Scholar, Web of Science, Elsevier, Springer, ACS, CNKI, and books via the keywords Guaiazulene, Matricaria chamomilla, GA-related compounds, and Guaiazulene analogous. RESULTS: The FDA has approved the bicyclic sesquiterpene GA, commonly referred to as azulon or 1,4-dimethyl-7-isopropylazulene, as a component in cosmetic colorants. The pleiotropic health advantages of GA and related substances, especially their antioxidant and anti-inflammatory effects, attracted a lot of research. Numerous studies have found that GA can help to manage various conditions, including bacterial infections, tumors, immunomodulation, expectorants, diuretics, diaphoresis, ulcers, dermatitis, proliferation, and gastritis. These conditions all involve lipid peroxidation and inflammatory response. In this review, we have covered the biomedical applications of GA. Moreover, we also emphasize the therapeutic potential of guaiazulene derivatives in pre-clinical and clinical settings, along with their underlying mechanism(s). CONCLUSION: GA and its related compounds exhibit therapeutic potential in several diseases. Still, it is necessary to investigate their potential in animal models for various other ailments and establish their safety profile. They might be a good candidate to advance to clinical trials.

Natto: A medicinal and edible food with health function / 中草药·英文版

Natto is a soybean product fermented by natto bacteria. It is rich in a variety of amino acids, vitamins, proteins and active enzymes. It has a number of biological activities, such as thrombolysis, prevention of osteoporosis, antibacterial, anticancer, antioxidant and so on. It is widely used in medicine, health-care food, biocatalysis and other fields. Natto is rich in many pharmacological active substances and has significant medicinal research value. This paper summarizes the pharmacological activities and applications of natto in and outside China, so as to provide references for further research and development of natto.

Research progress in chemical composition and pharmacological action of Astragali Radix and Atractylodis Macrocephalae Rhizoma / 国际中医中药杂志

After the compatibility of Astragali Radix and Atractylodis Macrocephalae Rhizoma, most of the effective components of Astragali Radix increase, and the bioavailability is improved. Compared with the application of the two drugs alone, it can enhance the effects of immune regulation, anti-tumor, diuresis, lung protection, regulation of flora, and intestinal protection. However, the optimal compatibility ratio of Astragali Radix- Atractylodis Macrocephalae Rhizoma pair to exert various pharmacological effects still needs to be clarified. The drug pair and related preparations are mostly used in the treatment of nephropathy, but its mechanism of action needs to be further elucidated.

Barbaloin: an amazing chemical from the 'wonder plant' with multidimensional pharmacological attributes.

Aloe vera (L.) Burm.f. is nicknamed the 'Miracle plant' or sometimes as the 'Wonder plant'. It is a plant that has been used since ancient times for the innumerable health benefits associated with it. It is one of the important plants that has its use in conventional medicinal treatments. It is a perennial succulent, drought-tolerant member of the family Asphodelaceae. There are scores of properties associated with the plant that help in curing various forms of human ailments. Extracts and gels obtained from plants have been shown to be wonderful healers of different conditions, mainly various skin problems. Also, this plant is popular in the cosmetics industry. The underlying properties of the plant are now mainly associated with the natural phytochemicals present in the plant. Diverse groups of phytoingredients are found in the plant, including various phenolics, amino acids, sugars, vitamins, and different other organic compounds, too. One of the primary ingredients found in the plant is the aloin molecule. It is an anthraquinone derivative and exists as an isomer of Aloin A and Aloin B. Barbaloin belonging to the first group is a glucoside of the aloe-emodin anthrone molecule. Various types of pharmacological properties exhibited by the plant can be attributed to this chemical. Few significant ones are antioxidant, anti-inflammatory, anti-diabetic, anti-cancer, anti-microbial, and anti-viral, along with their different immunity-boosting actions. Recently, molecular coupling studies have also found the role of these molecules as a potential cure against the ongoing COVID-19 disease. This study comprehensively focuses on the numerous pharmacological actions of the primary compound barbaloin obtained from the Aloe vera plant along with the mechanism of action and the potent application of these natural molecules under various conditions.

Xanthotoxin (8-methoxypsoralen): A review of its chemistry, pharmacology, pharmacokinetics, and toxicity.

Xanthotoxin (XAT) is a natural furanocoumarins, a bioactive psoralen isolated from the fruit of the Rutaceae plant Pepper, which has received increasing attention in recent years due to its wide source and low cost. By collecting and compiling literature on XAT, the results show that XAT exhibits significant activity in the treatment of various diseases, including neuroprotection, skin repair, osteoprotection, organ protection, anticancer, antiinflammatory, antioxidative stress and antibacterial. In this paper, we review the pharmacological activity and potential molecular mechanisms of XAT for the treatment of related diseases. The data suggest that XAT can mechanistically induce ROS production and promote apoptosis through mitochondrial or endoplasmic reticulum pathways, regulate NF-κB, MAPK, JAK/STAT, Nrf2/HO-1, MAPK, AKT/mTOR, and ERK1/2 signaling pathways to exert pharmacological effects. In addition, the pharmacokinetics properties and toxicity of XAT are discussed in this paper, further elucidating the relationship between structure and efficacy. It is worth noting that data from clinical studies of XAT are still scarce, limiting the use of XAT in the clinic, and in the future, more in-depth studies are needed to determine the clinical efficacy of XAT.

Ginsenosides in central nervous system diseases: Pharmacological actions, mechanisms, and therapeutics.

The nervous system is one of the most complex physiological systems, and central nervous system diseases (CNSDs) are serious diseases that affect human health. Ginseng (Panax L.), the root of Panax species, are famous Chinese herbs that have been used for various diseases in China, Japan, and Korea since ancient times, and remain a popular natural medicine used worldwide in modern times. Ginsenosides are the main active components of ginseng, and increasing evidence has demonstrated that ginsenosides can prevent CNSDs, including neurodegenerative diseases, memory and cognitive impairment, cerebral ischemia injury, depression, brain glioma, multiple sclerosis, which has been confirmed in numerous studies. Therefore, this review summarizes the potential pathways by which ginsenosides affect the pathogenesis of CNSDs mainly including antioxidant effects, anti-inflammatory effects, anti-apoptotic effects, and nerve protection, which provides novel ideas for the treatment of CNSDs.

Effects of turmeric (Curcuma longa) on oral health.

The turmeric plant was used in ancient medicine to cure a wide range of diseases, including cough, diabetes, and liver disease. Data shows that the principal chemical component of turmeric, curcumin, has a variety of beneficial effects on the body. Therefore, it is of interest to document data on the therapeutic activities of turmeric, including its extracts and possible medical uses, as well as its oral and dental uses and a safety assessment of those uses. Curcumin, the most pure form of turmeric, has shown promise in dentistry.

A Network Pharmacological Approach to Explore the Mechanisms of TongXieYaoFang in Inflammatory Bowel Disease

Abstract Inflammatory bowel disease (IBD) is a chronic inflammatory disorder of the intestine, demonstrating an increasing incidence every year. TongXieYaoFang (TXYF) has been used widely in China as a complementary therapy to relieve the symptoms of IBD for hundreds of years. In the present research, a network pharmacology-based approach was used to systematically explore the intrinsic mechanisms of TXYF in IBD at the molecular level. Network pharmacology-based methods, which mainly included database mining, screening of bioactive compounds, target prediction, collection of IBD-related targets, gene enrichment analysis, network construction, and molecular docking, were employed in the present study. Network analysis revealed a total of 108 potential targets derived from 22 component compounds of TXYF, among which 34 targets were common with the IBD-related targets. In the protein-protein interaction (PPI) network, 10 key targets were identified. The gene enrichment analysis suggested that anti-inflammatory processes, such as NF-kappa B signaling pathway and Toll-like receptor signaling pathway, could be the core processes involved in the action of TXYF in IBD. Molecular docking results revealed that three compounds present in TXYF exhibited strong binding affinity for PTGS2. The present study provides novel insights into the molecular mechanisms and network approaches of TXYF action in IBD from a systemic perspective. The potential targets and pathways identified in the present study would assist in further research on the clinical application of TXYF in IBD therapy.

Medicinal Properties and In Vitro Biological Activities of Selected Helichrysum Species from South Africa: A Review.

The genus Helichrysum Mill comprises hundreds of species that are mostly flowering perennial shrubs. Some of these plants that belong to the Helichrysum species are used in traditional medicine to treat cough, back pain, diabetes, asthma, digestive problems, menstrual pain, chest pain, kidney disorders, skin disorders, wounds, open sores, among other conditions, but, only a few scientific studies are reported in the literature with sufficient information that validates the acclaimed folkloric benefits of these plants. This review, therefore, provides a comprehensive update of the available information on the cytotoxicity, genotoxicity, anti-proliferative, anti-bacterial, anti-fungal, anti-viral, anti-HIV, anti-malarial, anti-ulcerogenic, anti-tyrosinase, anti-inflammatory, and anti-oxidant activities of selected Helichrysum species of interest: H. petiolare, H. cymocum, H. foetidum, and H. pandurifolium Schrank, using scientific databases as well as electronic and print sources. The ethnobotanical and morphological characteristics as well as the phytochemical composition and biological activities of these plants are elucidated. The scientific rationale for their current use is discussed based on the evidence in the literature. This review highlights the putative use of the Helichrysum species as a reliable source of bioactive compounds for the production of standard commercial drugs to treat many ailments, including those reported in folkloric uses. Further research on the many plants in the genus Helichrysum is recommended to explore their economic importance both as edible crops and medicinal botanicals.

Borneol in cardio-cerebrovascular diseases: Pharmacological actions, mechanisms, and therapeutics.

With the coming acceleration of global population aging, the incidence rate of cardio-cerebrovascular diseases (CVDs) is increasing. It has become the leading cause of human mortality. As a natural drug, borneol (BO) not only has anti-inflammatory, anti-oxidant, anti-apoptotic, anti-coagulant activities and improves energy metabolism but can also promote drugs to enter the target organs or tissues through various physiological barriers, such as the blood-brain barrier (BBB), mucous membrane, skin. Thus, it has a significant therapeutic effect on various CVDs, which has been confirmed in a large number of studies. However, the pharmacological actions and mechanisms of BO on CVDs have not been fully investigated. Hence, this review summarizes the pharmacological actions and possible mechanisms of BO, which provides novel ideas for the treatment of CVDs.

Traditional use, phytochemistry, toxicology, and pharmacology of Origanum majorana L.

ETHNOPHARMACOLOGICAL RELEVANCE: Origanum majorana L., is an aromatic and medicinal plant distributed in different parts of Mediterranean countries. This species is widely used in traditional medicine for the treatment of many diseases such as allergies, hypertension, respiratory infections, diabetes, stomach pain, and intestinal antispasmodic. AIM OF THE REVIEW: This work reports previous studies on O. majorana concerning its taxonomy, botanical description, geographical distribution, traditional use, bioactive compounds, toxicology, and biological effects. MATERIALS AND METHODS: Different scientific data bases such as Web of Science, Scopus, Wiley Online, SciFinder, Google Scholar, PubMed, ScienceDirect, and SpringerLink were consulted to collect data about O. majorana. The presented data emphasis bioactive compounds, traditional uses, toxicological investigations, and biological activities of O. majorana. RESULTS: The findings of this work marked an important correlation between the traditional use of O. majorana as an anti-allergic, antihypertensive, anti-diabetic agent, and its biological effects. Indeed, pharmacological investigations showed that essential oils and extracts from O. majorana exhibit different biological properties, particularly; antibacterial, antifungal, antioxidant, antiparasitic, antidiabetic, anticancer, nephrotoxicity protective, anti-inflammatory, analgesic and anti-pyretic, hepatoprotective, and antimutagenic effects. Toxicological evaluation confirmed the safety and innocuity of this species and supported its medicinal uses. Several bioactive compounds belonging to different chemical family such as terpenoids, flavonoids, and phenolic acids were also identified in O. majorana. CONCLUSIONS: The results suggest that the pharmacological properties of O. majorana confirm its traditional uses. Indeed, O. majorana essential oils showed remarkable antimicrobial, antioxidant, anticancer, anti-inflammatory, antimutagenic, nephroprotective, and hepatoprotective activities. However, further investigations regarding the evaluation of molecular mechanisms of identified compounds against human cancer cell lines, inflammatory process, and microbial infections are needed to validate pharmacodynamic targets. The toxicological investigation of O. Majorana confirmed its safety and therefore encouraged pharmacokinetic evaluation tests to validate its bioavailability.

Multifunctional epiberberine mediates multi-therapeutic effects.

Epiberberine, a natural protoberberine from Coptis chinensis Franch., is a potential alkaloid for the treatment of a variety of chronic diseases. The aim of this study is to summarize recent advances in the multiple and potential therapeutic effects of epiberberine. High-quality researches published in last two decades were retrieved from Web of science, ScienceDirect, PubMed and Springer with keywords namely 'epiberberine', 'protoberberine', 'coptis', 'huanglian', 'Coptidis rhizoma' and vital targets of some pathways in anti-adipogenesis, anti-dyslipidemia and anti-cancer activities. All the available research studies indicated that epiberberine is a multi-target small molecule with a low toxicity and exerts many activities including anti-adipogenesis via Akt and ERK pathways, anti-dyslipidemia via inhibition on cholesterol synthesis, anti-cancer via p53/Bax apoptosis pathway, anti-bacterial, improvement in diabetes and Alzheimer's disease. The present work will shed light on the direction for future investigations. Undoubtedly, C. chinensis and epiberberine are expected to exert beneficial effects in various diseases. However, there is a lack of evaluation of clinical applications and underlying molecular mechanisms of epiberberine in diabetes and dementia.

Efficacy, Chemical Constituents, and Pharmacological Actions of Radix Paeoniae Rubra and Radix Paeoniae Alba.

Radix Paeoniae Rubra and Radix Paeoniae Alba are the different characteristic forms of Paeonia lactiflora Pall. They are widely used as traditional Chinese medicines in clinical practices. This study analyzes the development history, efficacy, chemical compositions, and pharmacological effects of Radix Paeoniae Rubra and Radix Paeoniae Alba, and explores the causes of the similarities and differences of these two amalgams. It provides a basis for the clinical application of these two Chinese medicinal materials, and lays a foundation for further study of the pharmacological effects and the quality identification of Paeonia lactiflora Pall as it applies to traditional Chinese medicine.

Chemistry, pharmacokinetics, pharmacology and recent novel drug delivery systems of paeonol.

Paeonol is a bioactive phenol present in Dioscorea japonica, Paeonia suffruticosa and Paeonia lactiflora. It is reported for various pharmacological activities. AIM: To review chemistry, pharmacokinetics, pharmacological activities as well as various formulations of paeonol. MATERIALS AND METHODS: A literature search was done using different search terms for paeonol by using different scientific databases like PubMed, Scopus and ProQuest. Scientific papers published during the period 1969 to 2019 were comprehensively reviewed. KEY FINDINGS: Researchers have synthesized methoxy, ethoxy, piperazine, chromonylthiazolidine, phenol-phenylsulfonyl, alkyl ether, aminothiazole, tryptamine hybrids and paeononlsilatie derivatives to enhance the stability of paeonol. These derivatives were synthesized and evaluated for in vitro series of biological activities like anti-inflammatory, tyrosinase inhibitory, neuroprotective, anticancer and antiviral activity. Regardless of valuable therapeutic potential, the clinical use of paeonol is restricted due to poor water solubility, low oral bioavailability, low stability and high volatility at room temperature. To enhance the bioavailability of paeonol various formulations are prepared and evaluated for its activity. Paeonol formulations can be categorized as conventional-tablets, topical gel and hydrogel; polymeric delivery system-microparticles, microsponges, dendrimers, nanocapsules, polymeric nanoparticles, nanospheres; lipid-based delivery systems-microemulsion, self-micro-emulsifying drug delivery, liposome, transethosomes, ethosomes, niosomes, proniosomes, lipid-based nanoparticles and nanoemulsion of paeonol. SIGNIFICANCE: Paeonol has a potential to be developed as a techno-commercial product with respect to its multi-faceted pharmacological properties. Even though in vitro and in vivo studies have been reported the important activities of paeonol, its commercial utilization requires extensive safety and efficacy data.