Pharmaceutical activity of sappan wood extract (Caesalpinia sappan L.) for treating Escherichia coli infection in piglets.

Background: Escherichia coli infection is one of the major diarrheal diseases resulting in the loss of pigs at a young age. Aim: This research investigated the antimicrobial activity of Caesalpinia sappan wood extract against E. coli infection as an antibiotic replacement. Methods: E. coli was cultured from diarrheal piglets and then used to find the minimal inhibition concentration (MIC). Caesalpinia sappan wood extract (500 mg/kg) was used for the treatment of diarrheal piglets compared to antibiotics (enrofloxacin 5 mg/kg) by oral administration. Another three groups of diarrheal piglets were used supplemented feed with 1% and 2% extract compared with commercial feed. Subsequently, E. coli enumeration, fecal shape, fecal color, and growth rate were recorded from day 1 to 7. Results: Based on the results, C. sappan wood extract could inhibit E. coli growth at a MIC of 16-34 mg/ml. The number of colonies did not significantly differ between C. sappan wood extract and enrofloxacin treatment groups. A supplemented feed with 1% and 2% C. sappan wood extract could improve the fecal shape and fecal score compared to the control group, albeit only in suckling pigs. There were significant differences from the control group on days 4, 5, 6, and 7 (p < 0.05). However, the average daily gain did not significantly differ among the three groups. Conclusion: The results indicate that C. sappan wood extract could improve diarrheal signs in suckling pigs and can be used as a replacement for antibiotics for organic pig production.

Quinoxaline 1,4-Dioxides: Advances in Chemistry and Chemotherapeutic Drug Development.

N-Oxides of heterocyclic compounds are the focus of medical chemistry due to their diverse biological properties. The high reactivity and tendency to undergo various rearrangements have piqued the interest of synthetic chemists in heterocycles with N-oxide fragments. Quinoxaline 1,4-dioxides are an example of an important class of heterocyclic N-oxides, whose wide range of biological activity determines the prospects of their practical use in the development of drugs of various pharmaceutical groups. Derivatives from this series have found application in the clinic as antibacterial drugs and are used in agriculture. Quinoxaline 1,4-dioxides present a promising class for the development of new drugs targeting bacterial infections, oncological diseases, malaria, trypanosomiasis, leishmaniasis, and amoebiasis. The review considers the most important methods for the synthesis and key directions in the chemical modification of quinoxaline 1,4-dioxide derivatives, analyzes their biological properties, and evaluates the prospects for the practical application of the most interesting compounds.

Recent Advances in the Green Synthesis of Active N-Heterocycles and Their Biological Activities.

N-heterocyclic scaffolds represent a privileged architecture in the process of drug design and development. It has widespread occurrence in synthetic and natural products, either those that are established or progressing as potent drug candidates. Additionally, numerous novel N-heterocyclic analogues with remarkable physiological significance and extended pharmaceutical applications are escalating progressively. Hence, the classical synthetic protocols need to be improvised according to modern requirements for efficient and eco-friendly approaches. Numerous methodologies and technologies emerged to address the green and sustainable production of various pharmaceutically and medicinally important N-heterocyclic compounds in last few years. In this context, the current review unveils greener alternatives for direct access to categorically differentiated N-heterocyclic derivatives and its application in the establishment of biologically active potent molecules for drug design. The green and sustainable methods accentuated in this review includes microwave-assisted reactions, solvent-free approaches, heterogeneous catalysis, ultrasound reactions, and biocatalysis.

Una profesión, una (bio)ética. Una visión conceptual / A profession, a (bio)ethics. A conceptual vision

La profesión farmacéutica tiene un ámbito de intervención único en el área de la salud, donde el farmacéutico se pude encontrar en todos los dominios relacionados con el acceso a la atención sanitaria, en sus más variados niveles. Todo este alcance se basa en una formación académica amplia, donde el conocimiento científico y los saberes confieren habilidades que se reflejan de manera directa sobre la profesión y la práctica farmacéutica. La práctica profesional del farmacéutico es muy diversa y se puede observar en diversas circunstancias, desde el contacto directo con el paciente, con la persona, como en la farmacia comunitaria, farmacia hospitalaria, laboratorio de análisis clínicos, en residencias de ancianos, hasta en situaciones de mayor resguardo, como en el laboratorio o en la investigación científica y clínica. Esta amplia gama de actividad del farmacéutico, apoyada en relaciones laborales individuales o integrada en equipos de salud multidisciplinares, requiere de él un comportamiento asertivo y una conciencia (bio)ética que le permita responder a las diferentes demandas que enfrenta en su vida diaria. Es importante, pues, reflexionar sobre los conceptos y presupuestos que la ética o la bioética tienen en su vida profesional, en el área de la salud y las ciencias de la vida, y, por qué no, en la vida personal de cada uno. (AU)

The pharmaceutical profession has a unique scope of intervention in the area of health, where the pharmacist can be found in all domains related to access to health care, at its most varied levels. All this scope is based on a broad academic training, where scientific knowledge and expertise confer skills that are directly reflected on the pharmaceutical profession and practice. The professional practice of the pharmacist is very diverse and can be observed in various circumstances, from direct contact with the patient, with the person, as in community pharmacy, hospital pharmacy, clinical analysis laboratory, palliative or continuous care, in nursing homes, to in more reserved situations, such as in the laboratory or in scientific and clinical research. This wide range of activity of the pharmacist, supported by individual labor relations or integrated into multidisciplinary health teams, requires from him an assertive behavior and a (bio)ethical awareness that allows him to respond to the different demands he faces in his daily life. It is important, therefore, to reflect on the concepts and assumptions that ethics or bioethics have in the professional life of pharmacist, in the area of health and life sciences, and in the personal life of each one. (AU)

Myrtle: a versatile medicinal plant.

Myrtus, commonly called myrtle, is a genus of flowering plants in the Myrtaceae family. This study aimed to review myrtle's pharmaceutical, food, and other uses. The pharmacological effects of myrtle for antioxidant, antibacterial, and anti-inflammatory activities, reduction of COVID-19 symptoms, anti-diabetic in the animal model, hepatoprotective in the rat model, antihypertensive, control of intestinal helminthiasis in mice model, inhibition of glucosyltransferase activity, protective effect on oxidative metabolism in the hypothyroidism model, and reducing the damage caused by skin burns are reviewed. In addition, the food uses of this plant such as improving the oxidative and microbial stability of products containing salmon, antimicrobial activity in meat and dairy products, flavoring in sea salt, microbial improvement of fresh fruits during post-harvest storage, animal nutrition, and bio-oil production are summarized. Supplementary Information: The online version contains supplementary material available at 10.1186/s41110-023-00194-y.

Advances in biochemistry and the biotechnological production of taxifolin and its derivatives.

Taxifolin (dihydroquercetin) and its derivatives are medicinally important flavanonols with a wide distribution in plants. These compounds have been isolated from various plants, such as milk thistle, onions, french maritime, and tamarind. In general, they are commercially generated in semisynthetic forms. Taxifolin and related compounds are biosynthesized via the phenylpropanoid pathway, and most of the biosynthetic steps have been functionally characterized. The knowledge gained through the detailed investigation of their biosynthesis has provided the foundation for the reconstruction of biosynthetic pathways. Plant- and microbial-based platforms are utilized for the expression of such pathways for generating taxifolin-related compounds, either by whole-cell biotransformation or through reconfiguration of the genetic circuits. In this review, we summarize recent advances in the biotechnological production of taxifolin and its derivatives.

CORRUPTION OFFENCES IN MEDICATIONS CIRCULATION: INVESTIGATION PROBLEMS.

OBJECTIVE: The aim: The article aims to focus attention on the pressing problems of corruption in the field of pharmaceutical activities at the stage of medicines sale. Possible ways to solve the problems are elucidated. PATIENTS AND METHODS: Materials and methods: The research has been carried out using the results of analysis and generalization of different countries' regulation acts governing pharmaceutical activity implementation, also of legal practice, including author's private practice, interviewing investigators, interviews, and questionnaires of pharmaceutical companies and professionals. General scientific and special scientific methods (dialectical, logical-normative, system-structural, comparative-legal, etc.) were used. RESULTS: Results: As a result of the study, the main problems of corruption that exist in the pharmaceutical activity sphere at the stage of medicines sale have been outlined. One of the most widespread corrupt manifestation are a relationships between a doctor and a pharmacist and sale medicine which contain drugs without doctors prescription. Proposals are formulated regarding possible ways to solve the problems, including other countries experience such as introduce digital control tools when concluding contracts. CONCLUSION: Conclusions: Investigation problems of pharmaceutical corruption offences deals with the absence of forensic investigation methodic of such crimes. It is caused by high latency of this category of criminal offenses. Among the main problems of the existence of corruption in the field of pharmaceutical activities at the stage of medicines' sale can be those: insufficiency and imperfection of the legislative regulation of medicines circulation; lack of professional relations regulation between medical institutions, doctors, and pharmaceutical entities; lack of an electronic database of prescribed prescriptions, etc.

Hemp in Veterinary Medicine: From Feed to Drug.

Hemp (Cannabis sativa) is an angiosperm plant belonging to the Cannabaceae family. Its cultivation dates back to centuries. It has always been cultivated due to the possibility of exploiting almost all the parts of the plant: paper, fabrics, ropes, bio-compounds with excellent insulating capacity, fuel, biodegradable plastic, antibacterial detergents, and food products, such as flour, oils, seeds, herbal teas, and beer, are indeed obtained from hemp. Hemp flowers have also always been used for their curative effects, as well as for recreational purposes due to their psychotropic effects. Cannabis contains almost 500 chemical compounds, such as phytocannabinoids, terpenes, flavonoids, amino acids, fatty acids, vitamins, and macro-, and micro-elements, among others. When utilized as a food source, hemp shows excellent nutritional and health-promoting (nutraceutical) properties, mainly due to the high content in polyunsaturated fatty acids (especially those belonging to the ω-3 series), as well as in phenolic compounds, which seem effective in the prevention of common diseases such as gastrointestinal disorders, neurodegenerative diseases, cancer, and others. Moreover, hemp oil and other oils (i.e., olive oil and medium-chain triglyceride-MCT-oil) enriched in CBD, as well as extracts from hemp dried flowers (Cannabis extracts), are authorized in some countries for therapeutic purposes as a second-choice approach (when conventional therapies have failed) for a certain number of clinical conditions such as pain and inflammation, epilepsy, anxiety disorders, nausea, emesis, and anorexia, among others. The present review will synthetize the beneficial properties of hemp and hemp derivatives in animal nutrition and therapeutics.

Recent Development of Oridonin Derivatives with Diverse Pharmacological Activities.

Oridonin is one of the major components isolated from Isodon rubescens, a traditional Chinese medicine, and it has been confirmed to exhibit many kinds of biological activities including anticancer, anti-inflammation, antibacterial and so on. However, the poor pharmaceutical property limits the clinical applications of oridonin. So many strategies have been explored in the purpose of improving the potencies of oridonin, and structure modification is one thus way. This review outlines the landscape of the recent development of oridonin derivatives with diverse pharmacological activities, mainly focusing on the biological properties, structure-activity relationships, and mechanism of actions.

Protein tyrosine phosphatase 1B(PTP1B) inhibitors from Arnebia euchroma / 中国药学杂志

OBJECTIVE: To study the chemical constituents of the extract of Arnebia euchroma (Royle) Johnst. and screen natural protein tyrosine phosphatase 1B (PTP1B) inhibitors. METHODS: Silica gel, MCI gel, ODS gel, and Sephadex LH-20 chromatographic techniques were used to study the chemical constituents of A. euchroma, the chemical structures were elucidated by analysis of physico-chemical and spectral data, and the inhibitory activity on PTP1B enzyme was tested in vitro. RESULTS: Eight compounds were obtained and their structures were identified as deoxyshikonin (1), shikonin (2), acetylshikonin (3), β, β'-dimethylacrylalkannin (4), quercetin (5), kaempferol (6), kaempferide (7), and β-sitosterol (8). Compounds 1-4 exhibited inhibitory activities on PTP1B with IC50 values of (0.80±0.16), (4.42±0.37), (1.02±0.13), and (0.36±0.08) μmol·L-1, respectively. The study of structure-activity relationship showed that the ring of naphthoquinone might be the key skeleton structure for the inhibition activity on PTP1B, and the 2-substituted long lipo-chain of naphthoquinone significantly affected the activity of these compounds: the increase in the polarity of the lipo-chain led to the reduction of activity, while the increase in the terminal double bond of the lipo-chain led to the enhancement of activity. CONCLUSION: Shikonin derivatives with 1, 4-naphthoquinone skeleton is a new type of leading compounds for the treatment of diabetes.