Bioactive Building Blocks and Potential Pharmacological Perspectives of Green Coffee: A Review

Coffee is known to be one of the popular beverages today on the globe. Due to its easy availability and preparation, it is consumed by the population of almost all countries. This wonder crop was discovered in the 6th century in Ethiopia. Since then, people have also used various brewing methods to extract hundreds of the bioactive compounds present in these aromatic seeds. No doubt, excessive consumption of the same can be harmful too. As a functional food, coffee is known to have multiple health benefits. Coffee beans contain vitamins, minerals, caffeine, chlorogenic acid, and various other biologically active ingredients. This review briefly describes the major biologically active compounds present in these seeds – caffeine, trigonelline, diterpenes, and chlorogenic acid (CGA). It also aims to describe various bioactive activities such as antioxidant, antiproliferative, antibacterial, antiviral, etc., against variable hallmarks. Thus, explaining different pharmacological effects for the welfare of the human population.

Effect of Two Drying Methods on the Bioactive Cashew Apple Varieties Consumed in the City of Garoua (Northern Cameroon)

Aims: The cashew tree (family Anacardiaceae) grows widely in many parts of African countries, including Cameroon. Its fruit and nut are used for food and several studies have shown their beneficial effects on health. This work aimed to evaluate the impact of two drying methods on the content of bioactive compounds and antioxidant activity. Methodology: Four varieties (VAR 1, VAR 2, VAR 3, VAR 4) of cashew apple samples were collected and drying using sun-dried and oven-dried to a constant weight, and then ground in a blender to a powder, the fresh one was cut up and crushed in a blender. All sample were reconstituted with distilled water and polyphenols, flavonoids, alkaloids contents, and antioxidant activity through different mechanisms (DPPH radical, FRAP and TAC assays) were assessed. Results: Alkaloids ranged from 1.50 mg EQui/g MF to 5.69 mg EQui/g DM for fresh and oven-dried VAR 1 respectively, polyphenols ranged from 786.15 mg EAG/g MF to 2836.92 mg EAG/g DM for fresh and oven-dried VAR 1 respectively, flavonoids ranged from 8.18 mg EAG/g MF to 295.45 mg EAG/g DM for fresh and oven-dried VAR 2 respectively. TAC values ranged from 13.09 mg EAA/g MF to 67.06 mg EAA/g for fresh and oven-dried VAR3 and VAR2 respectively. The highest DPPH radical scavenging value (86.25%) was obtained with fresh VAR 4 and the lowest (25.67%) with fresh VAR 1. The highest ferric reducing antioxidant power (FRAP) was obtained with fresh VAR 1 and VAR 3 (0.27 mg AAE/g MF) and the lowest with VAR 3 and VAR 4 oven-dried (0.23 mg AAE/g MF). Conclusion: In conclusion, the different cashew varieties studied in this work are a good source of antioxidants. The drying method significantly affects bioactive compounds and antioxidant activities. A weak but not significant correlation was obtained between the number of bioactive compounds and antioxidant activities.

Mechanistic Validation of an Ergogenic T. arjuna Standardized Extract (Oxyjun®) Using a Molecular Docking Approach

The bark of the tree Terminalia arjuna commonly referred as Arjuna is widely used in Ayurveda as a therapeutic agent for heart disease. More recently, a proprietary botanical extract of T. arjuna with tradename, Oxyjun®, demonstrated cardiotonic and ergogenic benefits for the first time in a younger and healthier population. However, the mechanism of action and biological actives of this novel sports ingredient were not clear. A molecular docking approach was adopted to understand the protein-ligand interactions and establish the most probable mechanism(s) of cardio vascular actions of the phytoconstituents of the T. arjuna standardized extract (TASE). Twenty-one phytochemicals (ligands) were chosen from Arjuna and their binding affinities against eight proteins serving cardiovascular functions (target proteins) were investigated. Autodock Vina was used to carry out the molecular docking studies. Potential efficacy in humans was assessed on the basis of ADMET properties and Lipinski’s Rule of 5. We found that arjunic acid, arjungenin, arjunetin, arjunglucoside1, chrysin, kaempferol, luteolin, rhamnetin and taxifolin demonstrated good docking scores and bioactivity.

Antifungal Activity of the Essential Oils of Osteophloeum platyspermum (Myristicaceae) against Malassezia spp. and Candida albicans Influenced by Seasonality and Climatic Factors

Aims: Malassezia spp. are involved in a wide range of mammalian skin diseases. The introduction of new drugs is a need. Natural products are known to be effective in the treatment of microbial pathogens. The present study analyzed the O. platyspermum leaf essential oils (EOs) antifungal activity. Study Design: 18 terpenes from 13 O. platyspermum leaf EOs are related to seasonal and climatic variations occurring during the dry (DS) and rainy (RS) seasons in the Amazon Rain-Forest, verified by means of multivariate analyses. Place and Duration of the Study: the study was conducted at the Center for Research in Biodiversity (Microbiology Laboratory and Cell Culture Laboratory), Paulista University, biological activity evaluations occurred between January/2019 and December 2019). Methodology: microdilution broth assay was used in the minimal bactericidal concentration (MBC). Multivariate analyses were used to access the relationship among MBC, seasonality and terpene composition of the EOs. Results: Malassezia pachydermatis showed higher sensitivity to the EOs than M. furfur or C. albicans. The DS EOs were linked to the presence of limonene, myrcene, α-terpineol, linalool, terpinen-4-ol, cubenol-1-epi, influenced by insolation, temperature and evaporation, while β-elemene, γ-elemene, neo-intermedeol, elemol, α-cadinol, spathulenol, isospathulenol, viridiflorol, δ-amorphene and ledol were linked to the RS EOs, and were influenced by precipitation, relative humidity and wind velocity. DS EOs showed better antifungal activity against both Malassezia species, and the presence of the six discriminative terpenes was essential for the antifungal activity. Conclusions: The DS EOs are a potential source of new leads to defeat animal dermatological microbes.

Microwave Assisted Extraction of Berberine and Preparation of Berberine Hydrochloride from Berberis Aristata Variety of Nepal, and Quantification using RP-HPLC and HPTLC Methods

Berberis aristata a Himalayan woody spiny shrub with yellow flowers and red berries commonly called as Daruharidra in Sanskrit and locally in Nepal is called as Chutro or Chitra. The root and stem are the two parts widely used in traditional medicines of India and China. Berberine is the key active ingredient present in stem and root parts. Berberine hydrochloride is the derivative of berberine. The present study aimed to study the microwave assisted extraction of berberine and its conversion into berberine hydrochloride and quantifying by RP-HPLC and HPTLC methods.In the present paper we have mentioned microwave assisted extraction of berberine and preparation of berberine hydrochloride in detail. Berberine extracted from roots of Berberis aristata using microwave assisted extraction in 80% ethanol to obtain 20% pure berberine crude by HPTLC densitometry at 350 nm absorption. The crude berberine was further purified to berberine hydrochloride by adding 10% Hcl in aqueous solution of berberine and allowed to crystallize at 5 0C over 24 hours. The crystals were further purified and recrystallized in ethanol and subjected to RP-HPLC. Reverse phase HPLC was carried out on Shimadzu UV detector at wave length of 265 nm using Acetonitrile-0.1% phosphoric acid solution (50:50) (add 0.1g sodium dodecyl sulfonate per 100ml) as the mobile phase; Phenomenex RP-column (250 mm × 4.6 mm, 5 μm), With flow rate 1.0 mL/minute, 5 µL injection volume, column temperature 25 0C for run time of 35 minutes, and retention time of berberine hydrochloride was 12.008 minutes with purity of 82% and recovery of 90% yield obtained.

A Narrative Review of Libidibia ferrea: Botanical Aspects, Ethnopharmacological Properties, Phytochemical Characteristics, Toxicity, and Experimental Tests

Introduction: Jucá or pau-ferro (Libidibia ferrea) is an arboreal plant from the Fabaceae family. It is commonly used in traditional medicine in the treatment of various diseases, including inflammatory process. Aims: The objective of this narrative review is to present botanical aspects, ethnopharmacological properties, phytochemical characteristics, toxicity highlighting, and experimental models with L. ferrea. Results: Botanical Aspects: Jucá has several uses such as in landscaping (stem and canopy), in arborization of urban areas. Ethnopharmacological Properties: It is used in the treatment of various diseases such as diabetes, flu, asthma and, inflammatory processes of which different parts are used (root, stem bark, leaves, fruits, seeds). Phytochemical Characteristics: Phenolic compounds, fatty acids, and terpenoids are among the compounds monthly used. Toxicity: In vivo models have been used to verify toxicity and in most studies the plant presented no toxicity in its use. Experimental studies: Animals, such as mice, dogs, rats, etc. and different models of studies to analyze the action of the plant were used. Conclusions: Such low toxicity, associated with its widespread use in folk medicine and its various effects demonstrated in the studies included in this Review have corroborated for the continuity of the research with L. ferrea. New studies, however, ought to follow methodological guidelines, such as the Animal Research: reporting in vivo Experiments (ARRIVE) so that, a methodological design secures more homogeneous studies capable of quantifying the actual size of the effect in the plant may have in clinical studies.

Aqueous Extract of Alstonia boonei Bark Reduces Chronic Hyperglycemia and Prevents its Complications through Increase of Hepatic Global Dna Methylation in Diabetic Wistar Rats

Aim: DNA methylation profile is involved in several physiological processes. Its alterations in the liver of diabetic patients characterized by global hypomethylation are associated with the pathophysiology of type 2 diabetes and its complications. The present study has evaluated the effect of the aqueous extract of Alstonia boonei barks on the global methylation of hepatic DNA in association with hyperglycemia and diabetes complications induced by high-fat diet (HFD) feeding and administering of streptozotocin (STZ) which mimics the metabolic abnormalities very similar to those seen in human Type 2 diabetes. Methods: A. boonei barks were harvested, processed, dried, ground and an aqueous extraction was prepared (ratio 1/10 w/v). An in vivo study was conducted in an animal model of high-fat-streptozotocin (HF-STZ) induced diabetes. Rats were divided into five groups of five rats each: a normoglycemic group, an untreated hyperglycemic group, three hyperglycemic groups including two test groups receiving aqueous extract of A. boonei barks (AEAB) by esophageal gavage at the doses of 200 and 400 mg/kg body weight once daily and a reference group receiving metformin at 10 mg/kg body weight. After 28 days of experimentation during which fasting blood glucose levels were taken every 14 days under fasting conditions, the animals were sacrificed. Plasma and liver homogenate samples from the sacrificed rats were used for biochemical assays (markers of oxidative stress such as malondialdehyde level, superoxide dismutase (SOD) and catalase activity, and markers of lipid profile such as total cholesterol, and triglycerides, HDL-c, LDL-c and VLDL-c). The analysis of the global DNA methylation profile was performed by the immunoprecipitation. Pearson's correlation was used to evaluate the relationship between the values. Results: The aqueous extract increased the hepatic DNA methylation by 0.41% and 0.63% at 200 and 400 mg/kg body weight, respectively, compared to metformin (0.47%±0, 05). This effect was significantly associated with the hypoglycemic effect obtained at 400 mg/kg body weight with a decrease in initial blood glucose level of -29.87%. Conclusion: AEAB reduces chronic hyperglycemia and prevents its complications by increasing global hepatic DNA methylation.

Plant Therapeutic Proteases: Chemical Aspects, Applications and Pharmaceutical Formulations

Background: Plants are important sources of therapeutic proteases with expressive activity, stability, specificity, and efficiency. These proteases are employed at low concentrations and produce lesser side effects. They have complex tridimensional structures whose maintenance is a challenge, requiring specific conditions to guarantee the biological and pharmacological activities of these compounds. Aims: To conduct a literature review about plant therapeutic proteases, their principal biochemical aspects, potentials and clinical applications, and main pharmaceutical formulations. Materials and Methods: The present study consisted of a bibliographic survey of the major plant therapeutic proteases. An investigation was performed in the PUBMED, SciELO, ScienceDirect and Academic Google databases using the keywords plant enzymes, therapeutic protease, immobilization, formulation. Results: Some plant therapeutic proteases, such as papain and bromelain, are employed to treat many diseases and conditions, but the complexity of their structures is an important limitation of their uses. Thus, the structure and activities of their formulations need to be stabilized and protected against degradation, with improved pharmacokinetics, a prolonged time of action, reduced toxic effects, and proper direction towards their therapeutic target. Nanotechnology has made it possible to manufacture drug carriers such as polymeric nano- and microparticles, hydrogels, dendrimers and liposomes which are able to increase their efficacy and clinical applicability, as well as patient compliance. Sustainability initiatives that use Green Chemistry together with nanobiotechnology have managed to reduce the risks of toxicity to organisms and the environment. Green synthesis uses lower concentrations of metal ions, water-soluble, biocompatible and non-toxic compounds, as well as seeking energy efficiency and using renewable sources of raw materials. Conclusions: Investigations about new formulations of plant therapeutic proteases using biodegradable and biocompatible polymers is of great biomedical interest because they generate less toxic new biopharmaceuticals, in addition to protecting and stabilizing the enzymatic structure.

Herbal Mixtures: Aspects Related to the Quality of Chinese Medicine Formulas and Perspectives for Products Registration in Brazil

Traditional medicine products are easily found in different regions of the world. Given this scenario, the World Health Organization (WHO) is very interested in the rational insertion of these resources, especially in primary pharmaceutical care in emerging countries. One of the main concerns of the WHO is with the population's access to traditional medicine products without quality guaranteed by regulatory and health control agencies in the country of origin. In ancient Chinese Pharmacology and Medicine, products based on associated drugs, used by boiling in water (decoction), successfully contribute to maintaining the health of Chinese people. In Brazil, the sanitary legislation of herbal mixtures for medicinal teas allows the sanitary notification of these products as traditional herbal medicines. On the other hand, the lack of clinical services to monitor consumption and the scarcity of evidence to ensure safety and efficacy, add to the inadequacy of the products to sanitary standards, the lack of inspection, and the definition of quality parameters for the evaluation of mixtures. Due to the chemical complexity of herbal mixtures, the correct identification of drugs through conventional techniques is usually possible for individual species, making it necessary to develop more comprehensive approaches. These testes allow to investigate the presence and/or absence of multiple pre-established markers, through the concept of fingerprint similarity and evaluation by chemometric tools. Liquid chromatography integrated with mass spectrometry and multivariate data analysis proved to be the most used method. Among the objectives of this critical and prospective review are: to describe the probable origin of medicinal teas, the theoretical foundation of the compositions in pharmacology and traditional Chinese medicine, the modern techniques developed in the quality control of herbal mixtures, and the perspectives for rational and safe insertion of traditional herbal medicines in Brazilian pharmaceutical care.

Viability and Vigor of Cerrado Cashew Seeds (Anacardium humile) on Different Substrates

The little cashew from the Cerrado (Anacardium humile) is a kind of family anacardiáceaceas, a shrubby plant of great incidence in the Brazilian Cerrado. It is a small pseudofruit, of acidic and juicy flavor, which is known to have colors ranging from yellow to red. It can be consumed naturally or in juices, drinks, sweets. However, its true fruit is the chestnut. Seed germination is influenced by factors such as the substrate, which can be improved in order to improve germination, resulting in the acquisition of more vigorous seedlings. The experiment was conducted in a greenhouse at the Federal Institute of Education, Science and Technology of Tocantins, city of Gurupi/TO, from 26 October 2017 to 15 February 2018. Seeds were collected directly from the pseudofruits. The highest root length value was obtained for seedlings of the following substrates: bs + ws + pb (7.1 cm and 12.5 cm) and ws (6.7 cm and 10.7 cm), intermediate values: or + rs + vl (6.3 cm and 10.0 cm) and hw + vl + sawdust + cp + ws (5.5 cm and 9.5 cm), and lower values on substrates: bs (5.7 cm and 8.0 cm) and bs + rs + sawdust (6,6 cm e 9,0 cm). It was also observed that the highest value referring to the first emergency count and seedling emergence once again stood out the substrates bs + ws + pb (61.0 % and 87.5 %) and ws (56.2% and 86.2 %). Intermediate results were obtained from hw substrates + vl + sawdust + cp + ws(44.0 % and 81.0 %) and or + rs + vl (48.4 % and 81.2 %) and lower for bs substrates (37.5% and 72.0 %) and bs + rs + sawdust (45.3% and 77.0 %). The substrates: bs + ws + pb and washed sand provided the highest values of viability and vigor in cashew seeds.