Medicinal Compounds Research Articles

Analysis of crude wastewater from two treatment plants in South Wales for 35 new psychoactive substances and cocaine, and cannabis

This study investigates the presence of new psychoactive substances (NPS) and their metabolites in two wastewater treatment plants (WWTPs) situated in South Wales, UK (WWTP-1 and WWTP-2). Analysis was conducted for 35 NPS and metabolites, along with the inclusion of benzoylecgonine (main cocaine metabolite) and cannabis, the most detected illicit substances. Benzoylecgonine was identified as the predominant substance in both WWTPs. Epidemiological calculations revealed the average population consumption of cocaine to be 3.88 mg/d/1000 inhabitants around WWTP-1 and 1.97 mg/d/1000 inhabitants for WWTP-2. The removal efficiency of benzoylecgonine across both WWTPs was observed at an average of 73%. Subsequent qualitative analyses on randomly selected wastewater samples detected medicinal compounds including buprenorphine, methadone, and codeine in both WWTPs. An additional experiment employing enzymatic hydrolysis revealed the presence of morphine, an increased presence of codeine, and 11-Nor-9-Carboxy-THC (THC-COOH) post-hydrolysis. These findings underscore the significant presence of illicit substances and medicinal compounds in wastewater systems with the absence of NPS within the South Wales area, highlighting the necessity for enhanced monitoring and treatment strategies to address public health and environmental concerns.

Telomere-to-Telomere Haplotype-Resolved Genomes of Agrocybe chaxingu Reveals Unique Genetic Features and Developmental Insights.

Agrocybe chaxingu is a widely cultivated edible fungus in China, which is rich in nutrients and medicinal compounds. However, the lack of a high-quality genome hinders further research. In this study, we assembled the telomere-to-telomere genomes of two sexually compatible monokaryons (CchA and CchB) derived from a primarily cultivated strain AS-5. The genomes of CchA and CchB were 50.60 Mb and 51.66 Mb with contig N50 values of 3.95 Mb and 3.97 Mb, respectively. Each contained 13 complete chromosomes with telomeres at both ends. The high mapping rate, uniform genome coverage, high LAI score, all BUSCOs with 98.5%, and all base accuracy exceeding 99.999% indicated the high level of integrity and quality of these two assembled genomes. Comparison of the two genomes revealed that approximately 30% of the nucleotide sequences between homologous chromosomes were non-syntenic, including 19 translocations, 36 inversions, and 15 duplications. An additional gene CchA_000467 was identified at the Mat A locus of CchA, which was observed exclusively in the Cyclocybe cylindracea species complex. A total of 613 (4.26%) and 483 (3.4%) unique genes were identified in CchA and CchB, respectively, with over 80% of these being hypothetical proteins. Transcriptomic analysis revealed that the expression levels of unique genes in CchB were significantly higher than those in CchA, and both CchA and CchB had unique genes specifically expressed at stages of mycelium and fruiting body. It was indicated that the growth and development of the A. chaxingu strain AS-5 required the coordinated action of two different nuclei, with CchB potentially playing a more significant role. These findings contributed to a more profound comprehension of the growth and developmental processes of basidiomycetes.

A novel evaluation mode of Nao An Capsules using multi-wavelength fusion fingerprint combined with quantitative analysis of multi-components by a single marker method and antioxidant activity

Nao An Capsules (NAC) are utilized in the acute phase of cerebral thrombosis and are appropriate for patients in the recovery stage exhibiting symptoms of qi deficiency and blood stasis. Nevertheless, there has been a lack of recent research on the overall quality control of NAC. The objective of this study is to establish a comprehensive quality control strategy for NAC. This article presents a methodology based on the average linear quantitative fingerprinting method (ALQFM) in conjunction with multi-wavelength high performance liquid chromatography (HPLC) fusion fingerprinting, quantized Fourier transform infrared (FT-IR) spectroscopy and ultraviolet (UV) spectral techniques to comprehensively evaluate NAC from both qualitative and quantitative perspectives. Subsequently, quantitative analysis of multi-components by a single marker (QAMS) method and the Standard Curve Method (SCM) were used to quantitatively determine 10 quality markers (Q-markers) in 22 batches of samples, with the results indicating that QAMS is a reliable method for quantifying active ingredients. Chemometrics methods such as principal component analysis (PCA) and principal component analysis (HCA) were also used to analyze the quality of samples. To achieve a thorough and methodical evaluation, a combined assessment of the three fingerprints was executed. Subsequently, an in vitro antioxidant activity experiment was performed utilizing the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging technique. By employing a partial least squares (PLS) model, the correlation between HPLC fingerprint chromatography and antioxidant activity was investigated. The study found that out of the 59 common peaks in the five-wavelength fusion fingerprint spectra of NAC, 33 peaks exhibit antioxidant activity. In this study, multi-wavelength fusion HPLC, quantized FT-IR and UV were jointly used to effectively identify functional groups and fingerprint information in compounds. It can fully and quickly obtain the fingerprint information of the compounds in the sample. NAC multi-components quantification and overall quality evaluation were performed using ALQFM and QAMS and chemometrics methods. We have developed a new approach for comprehensive, rapid, and cost-effective quality control of traditional Chinese medicine (TCM) compound preparations.

The Role of Medicinal Plants in the Treatment of Oral Cancers in vitro: A Systematic Review

Introduction: The use of medicinal plant compounds for cancer treatment has been considered since ancient times. This systematic study aimed to conduct a review on the effects of medicinal plant extracts on oral cancer cell lines in vitro. Methods: In this systematic study, articles were searched in databases, including PubMed, Google Scholar, ScienceDirect, Web of Science, and Scopus, using keywords as "herbal drugs", "medicinal plants", "extract", "essence", "oral cancer", "in vitro", and "clinical trials". Results: After searching the articles according to inclusion and exclusion criteria, removing duplicates, and reviewing full-text articles, the researchers entered the data of all the collected articles into Endnote X9. Initially, 14,650 studies were identified, but after applying the inclusion/ exclusion criteria, 21 studies were selected. Conclusion: According to the inclusion and exclusion criteria, 21 studies have been selected. The study's findings have revealed that medicinal plants have the potential to inhibit the growth of oral cancer cells, making them a promising candidate for further research on cancer treatment.

Investigation of the Effects of Energy-Efficient Drying Techniques and Extraction Methods on the Bioactive and Functional Activity of Banana Inflorescence

Plant-derived foods with therapeutic potential have strong connection with both the pharmaceutical and nutraceutical industries. The effectiveness of these therapeutic properties is heavily influenced by the thermal treatment during drying and extraction methods. Traditional convective drying is a very energy incentive and lengthy process. Although some advanced and hybrid drying methods have been developed, these have not been applied in drying of banana inflorescence. In this study, we investigated the effects of freeze-drying (FD) and intermittent microwave convective drying (IMCD), as well as traditional convective oven drying (CD), on the polyphenol profile of banana inflorescence when extracted using the energy-efficient Accelerated Solvent Extraction method (ASE). Our findings revealed that the freeze-dried banana inflorescence powder exhibited the highest extraction of bioactive compounds when using 75% methanol at 100 °C as a solvent. It recovered 2906.3 ± 20.83 mg/100 g of the phenolic compounds and 63.12 ± 0.25% antioxidant activity under the optimal extraction conditions. While IMCD was found to be the second-best drying method in terms of preserving bioactive compounds, its operational time and cost were significantly lower compared to freeze-drying. Furthermore, our study confirmed the presence of medicinal compounds such as gallic acid, protocatechuic acid, caffeic acid, coumaric acid, catechin, ferulic acid, kaempferol, and quercetin in banana inflorescence. The development of innovative functional foods and pharmaceutical ingredients through green extraction methods and optimal drying conditions holds significant potential to save energy in the process, enhance human health, and promote environmental sustainability and circular economy processes. These efforts align with supporting Sustainable Development Goals (SDGs) 3 and 12.

Advances in the treatment of diabetic peripheral neuropathy by modulating gut microbiota with traditional Chinese medicine.

Diabetic peripheral neuropathy (DPN) is one of the strongest risk factors for diabetic foot ulcers (neuropathic ulcerations) and the existing ulcers may further deteriorate due to the damage to sensory neurons. Moreover, the resulting numbness in the limbs causes difficulty in discovering these ulcerations in a short time. DPN is associated with gut microbiota dysbiosis. Traditional Chinese medicine (TCM) compounds such as Shenqi Dihuang Decoction, Huangkui Capsules and Qidi Tangshen Granules can reduce the clinical symptoms of diabetic nephropathy by modulating gut microbiota. The current review discusses whether TCM compounds can reduce the risk of DPN by improving gut mic-robiota.

Immunomodulatory effect of tibetan medicine compound extracts against ORFV in vitro by metabolomics

Ovine contagious pustular dermatitis (ORF) is one of the main diseases of sheep and is a zoonotic disease caused by Ovine contagious pustular dermatitis virus (ORFV) infection, posing a significant constraint on sheep breeding industry and human health. The Tibetan medical formulation composed of Polygonum leucoides, Polygonum xanthoxylum and Acanthophora rotunda significantly regulated lymphocyte immune function following ORFV stimulation, although the mechanism remains unclear. In order to study the immunomodulatory effects and mechanism of three Tibetan medicinal extracts (Polygonum leucoides, Polygonum xanthoxylum, and Acanthophora rotunda) against ORFV in vitro, sheep peripheral blood lymphocytes were isolated in vitro and treated with different concentrations of Tibetan medicine compound extract solution after ORFV infection. The cytokine expression levels in lymphocytes were measured at 4 h, 8 h and 12 h. Additionally endogenous metabolites in lymphocytes at 0 h, 4 h, 8 h and 12 h were quantified by untargeted metabolomics method. The results showed that, the extracts could regulate the lymphocyte immune factors altered by ORFV, and regulate the lymphocyte immune function through cysteine and methionine metabolic pathways as well as the pyrimidine metabolic pathways, potentially alleviating the immune evasion induced by ORFV.

Fufang Zhenzhu Tiaozhi (FTZ) capsule ameliorates diabetic kidney disease in mice via inhibiting the SGLT2/glycolysis pathway

Ethnopharmacological relevanceFufang Zhenzhu Tiaozhi (FTZ) capsule is a hospital preparation of a patented traditional Chinese medicine compound. FTZ has been clinically used for nearly 13 years in the treatment of diabetes and glycolipid metabolic diseases. With the significant benefits of SGLT2 inhibitor in patients with diabetic kidney disease (DKD), it provides a research avenue to explore the mechanism of FTZ in treating this disease based on glycolysis pathway. Aim of the studyTo explore the pharmacological characteristics of FTZ in DKD mice and its impact on the glycolysis pathway. Materials and methodsWe induced a DKD model in C57BL/6 mice by injection of streptozotocin (STZ) combined with long-term high-fat diet. We administered three doses of FTZ for 12 weeks of treatment. Kidney function, blood lipid levels, glucose tolerance, and key glycolytic enzymes were evaluated. Renal pathological changes were observed using HE, MASSON, and PAS staining. The potential targets of the active ingredients of FTZ in the glycolysis pathway were predicted using network pharmacology and molecular docking. Validation was performed using immunohistochemistry and Western blotting. ResultsFTZ effectively reduces blood glucose, total cholesterol, triglyceride, low density lipoprotein cholesterol, 24 h proteinuria, serum creatinine, blood urea nitrogen, and increases urinary glucose levels. Glucose tolerance and renal pathological changes were significantly improved by FTZ treatment. Pinusolidic acid, a component of FTZ, shows good binding affinity with three active pockets of SGLT2. WB and immunohistochemistry revealed that FTZ significantly inhibits the expression of SGLT2 and its glycolytic related proteins (GLUT2/PKM2/HK2). Hexokinase, pyruvate kinase, and lactate dehydrogenase in the kidney were also significantly inhibited by FTZ in a dose-dependent manner. ConclusionFTZ may alleviate the progression of DKD by inhibiting the activation of the SGLT2/glycolytic pathway. Our study provides new insights into the clinical application of FTZ in DKD.

Molecular Docking and Dynamic Simulation Studies of Bioactive Compounds from Traditional Medicinal Compounds Against Exfoliative Toxin B from Staphylococcus aureus

Background Staphylococcal scalded skin syndrome (SSSS) is a dermatological condition caused by Staphylococcus aureus, characterized by exfoliative toxin B, and its increasing resistance to conventional antibiotics necessitates the search for new therapeutic options. Aim The study aimed to investigate the potential of traditional medicinal compounds (TMCs) as potential pharmaceuticals against SSSS using molecular-level research. Introduction Staphylococcus aureus, commonly known as S. aureus, is the main cause of SSSS. These infections are a major concern for public health because they are becoming resistant to antibiotics. There is an urgent need for new medications to effectively fight against this infection. The main objective of this study was to assess the interaction between TMC compounds and S. aureus exfoliative toxins ETA and ETB utilizing computational approaches. Materials and Methods The investigation selected TMC compounds based on their potential to combat S. aureus infections. To predict binding affinities with the ETB toxin, molecular docking simulations were performed using AutoDock and AutoDock Vina. In order to evaluate the stability and interaction dynamics with the toxins, the most promising compound was subjected to a 100 ns molecular dynamics simulation. Stability was evaluated through various methods. Results Liquiritin showed the highest binding affinity, with a docking score of −7.6 kcal/mol. MD simulation confirmed the complex’s stability, and the binding free energy of −17.76 kcal/mol indicated potent inhibitory activity against S. aureus ETB. Conclusion Liquiritin, a TMC, effectively inhibits S. aureus toxins ETB, with promising potential for treating SSSS and antibiotic-resistant infections, requiring further research.

η6-Arene Ru(II) Complexes as Modulators of Amyloid Aggregation.

Inorganic medicinal compounds represent a unique and versatile source of potential therapeutics in many diseases and, more recently, in neurodegeneration. Herein we investigated the effects of two η6-arene Ru(II) complexes on the self-aggregation processes of several amyloidogenic peptides endowed with different kinetics and primary sequences. The Ru(II) complexes exhibit, around the metal ion, two chlorides, one NHC = N-heterocyclic carbene, with a glucosyl and a methyl substituent and separately a hexamethylbenzene, which is named Ru1, and one benzene, named Ru2. Both complexes were demonstrated to bind monomeric amyloids suppressing aggregation as evidenced in thioflavin T (ThT) binding assays and autofluorescence experiments. Electrospray ionization mass spectrometry (ESI-MS) indicated the formation of direct adducts between amyloid and metal complexes, which determined the marked conformational variation of peptides and a rescue of cellular viability in SH-SY5Y cells. The complex Ru2 was demonstrated to be a more potent inhibitor of amyloid aggregation compared to Ru1 likely because of the less hindrance of the arene moiety. The presented data strongly support the in vitro ability of η6-arene Ru(II) complexes to suppress amyloid aggregation, providing insights into their potential application as novel therapeutics in neurodegenerative diseases.

Active Targets and Potential Mechanisms of Erhuang Quzhi Formula in Treating NAFLD: Network Analysis and Experimental Assessment.

The purpose of this research was to investigate the main active components, potential targets of action, and pharmacological mechanisms of Erhuang Quzhi Formula (EHQZF) against NAFLD using network pharmacology, molecular docking, and experimental validation. The main active chemical components of EHQZF and the potential targets for treating NAFLD were extracted and analyzed. The PPI network diagram of "Traditional Chinese Medicine-Active Ingredients-Core Targets" was constructed and the GO, KEGG, and molecular docking analysis were carried out. Identification of components in traditional Chinese medicine compounds was conducted by LC-MS. NAFLD models were established and relevant pathologic indicators and Western blot were analyzed in vivo and ex vivo. Totally 8 herbs attributed to the liver meridian and 20 corresponding targets of NAFLD were obtained from EHQZF. Flavonoids and phenolic acids as the main components of EHQZF treated NAFLD through the MAPK/AKT signaling pathway. Pathway enrichment analysis focused on the MAPK/AKT signaling pathway and apoptosis signaling pathway. Molecular docking showed that Quercetin and Luteolin had stable binding structures with AKT1, STAT3, and other targets. Experiments showed that EHQZF reduced lipid accumulation, regulated changes in adipose tissue, inhibited the MAPK/AKT signaling pathway and exert multiple components, several targets, and multiple pathway interactions to treat NAFLD.

Recent Advances in Alkaloids from Papaveraceae in China: Structural Characteristics and Pharmacological Effects.

The Papaveraceae plant family serves as a botanical reservoir for a variety of medicinal compounds that have been traditionally utilized in Chinese medicine for numerous generations. Growing attention towards the pharmaceutical potential of Papaveraceae has resulted in the identification of many alkaloids, which have attracted significant attention from the scientific community because of their structural complexity and wide range of biological activities, such as analgesic, antihypertensive, antiarrhythmic, anti-inflammatory, antibacterial, anti-tumor, anti-cancer, and other activities, making them potential candidates for medical use. The primary objective of this review is to analyze the existing literature on the historical use of Papaveraceae plants, focusing on their alkaloid structures and relationship with pharmacological effects, as well as provide a theoretical basis for their clinical application, with the goal of unveiling the future potential of Papaveraceae plants.

Regio- and Enantioselective N-Heterocyclic Carbene-Catalyzed Annulation of Aminoindoles Initiated by Friedel-Crafts Alkylation.

Chiral indoles annulated on the benzene ring are unique and significant in natural and medicinal compounds. However, accessing these enantioenriched molecules has often been overlooked. The present study introduces an organocatalytic protocol to access these compounds efficiently, demonstrated by substrate scope, functional group tolerance, and using only 1 mol % of a chiral conjugated acid catalyst. Additionally, the study explores regioselectivity, gram-scale reactions, and follow-up transformations, underscoring the method's potential.

Quality evaluation of Qiangli Tianma Duzhong (QLTMDZ) employing UHPLC-MS: A multivariate statistical analysis across multiple dosage forms and manufacturers

Traditional Chinese medicine (TCM) and its preparations have become increasingly popular in recent years. Nonetheless, due to the high complexity of the compounds in Traditional Chinese Patent Medicine (TCPM), the quality differences between different dosage forms and products from various manufacturers pose numerous challenges and difficulties in quality evaluation. The Qiangli Tianma Duzhong (QLTMDZ) prescription, comprising twelve TCM, is widely used in China. Despite its prevalence, current research on QLTMDZ is limited and lacks in-depth and systematic analysis of the chemical composition of the prescription. In this study, a comprehensive strategy was proposed for characterizing the chemical profile of QLTMDZ based on UHPLC-Q-TOF-MS. A total of 122 compounds were identified in QLTMDZ under both positive and negative ion modes. Subsequently, multivariate statistical methods such as principal component analysis (PCA) and orthogonal partial least squares-discriminant analysis (OPLS-DA) were conducted in the MS-DIAL software to further elucidate quality differences among 55 batches of QLTMDZ samples from seven manufacturers. Lastly, multiple reaction monitoring (MRM) mode was utilized in conjunction with UHPLC-QQQ-MS, for the precise quantification of the identified 24 compounds within the QLTMDZ preparation and providing supplementary information in quality evaluation. The established analytical method in this study is sensitive and efficient, enabling qualitative and quantitative analysis of the chemical constituents within QLTMDZ. The application of multivariate statistical analyses effectively discriminates samples based on different dosage forms and manufacturers, thereby providing new research directions and scientific support for further studies on the quality control of the prescription.

Functionalized Polymeric Micelles for Targeted Cancer Therapy: Steps from Conceptualization to Clinical Trials.

Cancer is still ranked among the top three causes of death in the 30- to 69-year-old age group in most countries and carries considerable societal and macroeconomic costs that differ depending on the cancer type, geography, and patient gender. Despite advances in several pharmacological approaches, the lack of stability and specificity, dose-related toxicity, and limited bioavailability of chemotherapy (standard therapy) pose major obstacles in cancer treatment, with multidrug resistance being a driving factor in chemotherapy failure. The past three decades have been the stage for intense research activity on the topic of nanomedicine, which has resulted in many nanotherapeutics with reduced toxicity, increased bioavailability, and improved pharmacokinetics and therapeutic efficacy employing smart drug delivery systems (SDDSs). Polymeric micelles (PMs) have become an auspicious DDS for medicinal compounds, being used to encapsulate hydrophobic drugs that also exhibit substantial toxicity. Through preclinical animal testing, PMs improved pharmacokinetic profiles and increased efficacy, resulting in a higher safety profile for therapeutic drugs. This review focuses on PMs that are already in clinical trials, traveling the pathways from preclinical to clinical studies until introduction to the market.

Anti-angiogenic Activities of Methanol Extracts of Imbao (Anodontia edentula) Using Chorioallantoic Membrane Assay

Angiogenesis is a physiological process with a role in vessel proliferation that is significant in tumor development. Inhibition of this process is called anti-angiogenesis, employing the use of various natural medical agents. These include mollusks, which are deemed as a source of different medicinal compounds that can act as anti-angiogenesis treatments utilized in cancer therapy. This study aims to investigate different concentrations of methanol extracts of a molluscan marine bivalve, Anodontia edentula, and determine the anti-angiogenic activity of the extract using chorioallantoicmembrane (CAM) assay. By utilizing vessel count analysis, results show A. edentula extracts exhibit anti-angiogenic activity, with negative values in percent growth and positive values in percent inhibition. Two out of four concentrations of extracts (1000 and 500 ppm) exhibit no significant difference with positive control (ibuprofen) regarding its anti-angiogenic ability. It is highly recommended to investigate the compounds responsible for the angiogenic inhibition observed in A. edentula.

Screening and analysis of the targeted compounds in Choerospondias axillaris extract by receptor chromatographic column with immobilized angiotensin II type 1 receptor.

As a result of the lack of modern techniques, the study of Tibetan medicine has been hindered in identifying bioactive compounds. Herein, we established a chromatographic approach using an immobilized angiotensin II type 1 receptor (AT1R) via a one-step method triggered by haloalkane dehalogenase. The bioactive compounds from Choerospondias axillaris (Guangzao) were screened and identified using the immobilized AT1R followed by MS. Frontal analysis (FA) and adsorption energy distribution (AED) were used to evaluate the association constants. Molecular docking was used to investigate the binding configurations, and the surface efficiency index, binding efficiency index, and ligand-lipophilicity efficiency (LLE) were calculated to assess the drug-like properties. The results identified naringenin, pinocembrin, and chrysin as the compounds that specifically bind to AT1R in Guangzao. FA and AED confirmed that there is only one type of binding site between these compounds and AT1R. The association constants were (2.40 ± 0.02) × 104 M-1 for naringenin (5.22 ± 0.26) × 104 M-1 for pinocembrin, and (4.27 ± 0.14) × 104 M-1 for chrysin, respectively. These compounds can bind with AT1R through the orthosteric binding pocket. Naringenin exhibited better LLE than pinocembrin and chrysin. These results confirmed the feasibility of using the immobilized AT1R column for screening and analyzing bioactive compounds in Tibetan medicines.

Navigating the Landscape of Coronary Microvascular Research: Trends, Triumphs, and Challenges Ahead.

Coronary microvascular dysfunction (CMD) refers to structural and functional abnormalities of the microcirculation that impair myocardial perfusion. CMD plays a pivotal role in numerous cardiovascular diseases, including myocardial ischemia with non-obstructive coronary arteries, heart failure, and acute coronary syndromes. This review summarizes recent advances in CMD pathophysiology, assessment, and treatment strategies, as well as ongoing challenges and future research directions. Signaling pathways implicated in CMD pathogenesis include adenosine monophosphate-activated protein kinase/Krüppel-like factor 2/endothelial nitric oxide synthase (AMPK/KLF2/eNOS), nuclear factor erythroid 2-related factor 2/antioxidant response element (Nrf2/ARE), Angiotensin II (Ang II), endothelin-1 (ET-1), RhoA/Rho kinase, and insulin signaling. Dysregulation of these pathways leads to endothelial dysfunction, the hallmark of CMD. Treatment strategies aim to reduce myocardial oxygen demand, improve microcirculatory function, and restore endothelial homeostasis through mechanisms including vasodilation, anti-inflammation, and antioxidant effects. Traditional Chinese medicine (TCM) compounds exhibit therapeutic potential through multi-targeted actions. Small molecules and regenerative approaches offer precision therapies. However, challenges remain in translating findings to clinical practice and developing effective pharmacotherapies. Integration of engineering with medicine through microfabrication, tissue engineering and AI presents opportunities to advance the diagnosis, prediction, and treatment of CMD.

Georgian Medicinal Plants as Rich Natural Sources of Antioxidant Derivatives: A Review on the Current Knowledge and Future Perspectives.

The study of antioxidants is of pivotal importance in biomedicine as these molecules could be involved in biological pathways associated with disease. The identification of new antioxidants together with the acquisition of a deeper knowledge on their biology, could lead to the use of these compounds as drugs for innovative treatments. Plants are an important reservoir of phytodrugs that in many cases can be isolated with good extraction yields directly from the vegetal source and are often endowed with a low toxicity profile. Georgia, a country situated on the Black Sea coast in the Caucasus region at the intersection of Western Asia and Eastern Europe, is renowned for its unique woodland habitats and immense biological diversity due to the great variety of climate zones and landscapes. Many wild plants in the area are used as remedies for a number of illnesses in the local traditional medicine. However, the scientific knowledge of these sources of natural drugs and of their molecular components is still far from exhaustive. Therefore, with the present work we reviewed the scientific literature on some of the main Georgian medicinal plants and found that several species are a valuable source of hydrophilic and hydrophobic antioxidants, endowed in some cases with a high ROS-scavenging ability. The analysis of the literature also demonstrated that most of the medicinal extracts and compounds isolated from these plants are beneficial in suppressing multiple diseases in vitro. This review will provide information for scientists looking to develop secure plant-based pharmaceuticals as well as a rationale for using Georgian medicinal plants for the treatment of a range of diseases.

Application of a kosmotrope (Na2CO3) and chaotrope (NaCl) in chemometric optimization of aqueous two-phase extraction of bioactive compounds in Hypoxis iridifolia.

Enterolactone, coumaric acid and vitexin are polyphenolic compounds present in a variety of fruits, vegetables, cereals and plants. These bioactive compounds are in high demand due to their antioxidant property in various tissues and organs. The purpose of this study was to develop a simultaneous extraction method, an aqueous two-phase extraction (ATPE) method, that would enable the extraction of these compounds from Hypoxis iridifolia. This environmentally friendly extraction method only applied water and ethanol as extraction solvents for these analytes from the plant matrix. After phase separation, the analytes were salted-out from the aqueous phase into the organic phase with the aid of a chaotrope (NaCl) or kosmotrope (Na2CO3). Thereafter, the analytes were withdrawn by a micro-pipette for analysis on the high-performance liquid chromatography-photodiode array detector. Optimization was conducted using a central composite design, where three parameters were examined which involved percentage ethanol, centrifugation time and salt type. Generally, the optimized conditions for extraction were an ethanol percentage of 100% and a centrifugation time of 10min, which yielded concentrations of 2942, 23,823 and 8881mg kg-1 for enterolactone, vitexin and coumaric acid, respectively, in the presence of a kosmotrope. The optimized conditions of extraction in the presence of chaotrope were an ethanol percentage of 66% and a centrifugation time of 10min with concentrations of 6727, 20,833 and 8618mg kg-1 for enterolactone, vitexin and coumaric acid, respectively. The ATPE method involving Na2CO3 was a better extractant of all the compounds studied relative to that of NaCl. The superior extraction capability of Na2CO3 in ATPE could serve as a prototype for the development of efficient extraction methods to meet the high demand for medicinal compounds derived from natural products.