Current Bioactive Compounds - Volume 19, Issue 3, 2023

The aim of this work was to conduct an in vitro assessment of the possible cytotoxic effects of homeopathic drugs and consider possible mechanisms. Background: Homeopathy is still widely used as a complementary (alternative) medicine in different countries throughout the world. However, the method raises a lot of scientific debate about its effectiveness and mechanisms of action. This is especially true concerning the use of homeopathy in cancer treatment. Objective: This work aimed to comparatively assess the cytotoxic effect of homeopathic remedies on tumor cell cultures. Materials and Methods: We studied different dilutions of homeopathic medicines: Hydrastis, Conium and Carcinosinum. Cell lines of prostate cancer PC-3, breast cancer MDA-MB-231, and lymphoblastic leukemia Jurkat were used as model tumor objects. Standard colorimetric MTT test and cytometric analysis of cells were used here to assess the viability and parameters of apoptosis of cells. Results: Comparative assessment of the cytotoxic and apoptosis-inducing effects did not reveal significant differences in the viability of tumor cells in the groups exposed to homeopathic preparations among themselves and in comparison with the control group. The effects of the action of homeopathic remedies are shown only in the form of trends. Some possible mechanisms of the obtained results are considered. Conclusion: The results obtained in vitro indicated the absence of a direct cytotoxic effect in the studied homeopathic preparations. Despite the objective data, this does not allow us to make a final conclusion about the absence of antitumor activity of these drugs in vivo, since the possible or potential effects depend on the parameters of a living organism that are difficult to control and are often based only on hypothetical mechanisms. Some aspects of the action of homeopathy probably cannot be reproduced in vitro.

Background: Astragalus gossypinus Fisch. is one of the Astragalus (Leguminosae) species that has been used in traditional medicine due to its phenomenal pharmacological and biological activities. Objective: In this research, the mutagenicity, anti-mutagenicity, and antioxidant potential of two different extracts of root (chloroform and ethyl acetate) and chloroform extract of aerial parts of Astragalus gossypinus were investigated. Methods: Antioxidant property was expressed as the ability of each extract to scavenge the free radicals like DPPH (2, 2-diphenyl-1-picrylhydrazyl) and mutagenicity and anti-mutagenicity were evaluated with the Ames test using Salmonella typhimurium strain TA100. Results: All extracts exhibited antioxidant capacity. Among them, the ethyl acetate extract of the root (IC50 = 289.29 μg/mL) was reported to be the best one, followed by the chloroform extract of the root (IC50 = 327.2 μg/mL), probably due to a higher percentage of phenolic and flavonoid compounds in these extracts. Chloroform extract of the root had the strongest anti-mutagenicity on S. typhimurium strain TA100, with a potential anti-mutagenic index ranging from 90.4867±5.84227 % to 50.2950±1.37308 %. Moreover, all tested extracts have neither direct nor indirect exerted mutagenic activity against this special strain of S. typhimurium. In the present research, saponins, flavonoids, and phenolic compounds are proposed to be antioxidant and antimutagenic agents in all extracts. Conclusion: The results of this study showed that the potent antioxidant and anti-mutagenic activity of A. gossypinus make it possible to use it as a natural antioxidant or bio-preservative in various medicinal formulations and cancer prevention.

Background: Diabetes is a problem of public health; in consequence, the increasing prevalence of both diseases needs more functional food products with efficiency and low cost to support treatment. Methods: Flavonoids from the herbal formulation of Portulaca oleracea, Zingiber officinale, and Tamarindus indica were extracted by ultrasound-assisted extraction technology, where several experiments were conducted to determine the implication of three independent variables on the higher production of flavonoids. Extraction time, ethanol concentration, and the liquid-solid ratio were determined as optimal conditions. Furthermore, flavonoids of interest in the extract were determined by using HPLC with UV/vis and mass spectrum and direct comparison reference compounds. Then was determined and compared the effect of extracts from P. oleracea (P), Z. officinale (Z), T. indica (T), and its combination (PTZ) on high-fat-diet-induced diabetic C57BL6/J mice. Results: The optimum conditions provided by the model include an extraction time of 30 min, an ethanol concentration of 50%, and a liquid/solid ratio of 40:1 mL/g, The anti-diabetic effect of an extract rich in polyphenolic compounds was evaluated using streptozotocin (STZ) and a high-fat diet-induced diabetic mouse. Effect of extracts on high-fat-diet-induced diabetic mice include decreased FER, improved insulin sensitivity, fasting blood glucose, and serum lipid, and showed reducing bodyweight gain associated with a reduction of food intake. Extracts have protective effects on kidneys, and liver improve lipolysis and successively decrease adipose tissue. Treatment with the polyherbal mixture has shown no toxic effects, possessed potent antihyperlipidemic, antihyperglycemic effects, and decreased glycated hemoglobin. The serum insulin level significantly increased (p < 0.05) on the polyherbal extract treatment, supporting the evidence of β-cell reestablishment in the pancreas. By reducing body weight and food intake, plasma adiponectin level increased while serum leptin level significantly decreased compared with the HFD group. In addition, the activities of key enzymes of carbohydrate metabolism, antioxidant enzymes, lipid peroxidation markers, and glycogen content were also improved in diabetic mice. Conclusion: The combined form of P. oleracea, Z. officinale, and T. indica had better antidiabetic properties compared with a single therapy, especially related to their high content of phytochemicals in comparison with the bioactive content of a single plant. The results presented here indicated that the use of PTZ due to their synergistic effects can be helpful against diabetes, improving the factors associated with this disease.

Background: The Adiantum lunulatum is a medicinally important pteridophyte used to treat inflammatory related diseases. The phytochemical profile of this plant is poorly investigated. Objective: Here, we screened the nonpolar phytochemicals and their interactions with cyclooxygenase 2 (COX-2) enzyme (inflammation), transient receptor potential cation channel V member 1 (TRPV1), and transient receptor potential channel 3 (TRPC3) receptors (pain). Methods: The identification and molecular docking analysis used gas chromatography-mass spectrometry (GC-MS), AutoDock Vina, and BIOVIA discovery studio visualizer 2020. The online computer tools Swiss ADME and admetSAR predicted these compounds bioavailability and toxicity. Results: GC-MS analysis detected the 12 different compounds. Five compounds with high similarity to mass spectrum were selected for molecular docking. This includes 2, 4 di-tert-butylphenol; n-hexadecanoic acid (palmitic acid); 2 pentadecanone, 6, 10, 14-trimethyl-; Quinoline 1, 2 dihydro 2, 2, 4 trimethyl and 3, 7, 11, 15-tetramethyl hexadec 2-en-1-yl acetate. These compounds showed interaction with the binding pocket of COX-2, TRPV1, and TRPC3 proteins. This interaction with enzyme and receptor activity causes a reduction in inflammatory pathogenesis. Conclusion: This study enhances our fundamental knowledge of biologically important volatile phytochemicals in Adiantum lunulatum dichloromethane extract and its possible effects in reducing inflammatory responses.

Background: Prunus armeniaca L. is widely cultivated around the world. High consumption of its fruit produces a large number of apricot kernel shells. The valorization of this byproduct in terms of polyphenol compounds seems to be important. Objective: This study aimed to optimize the extraction of phenolic compounds from apricot kernel shells by different extraction techniques by studying the effects of different parameters on the extraction efficiency, and the comparison between the Box-Behnken Design and the Central Composite Design of the response surface methodology is done in order to have good extraction estimation. Methods: In this study, response surface methodology; Box-Behnken and Central Composite Designs, was used to contrast the efficacy and investigate the principal interactions of three operating parameters (ethanol concentration, microwave power, and extraction time), in the optimization of phenolic compounds extraction from apricot kernel shells by microwave-assisted extraction, ultrasonic-assisted extraction, and maceration techniques. Results: The results indicated that the optimal total phenolic compounds obtained with microwave assisted extraction techniques by Box-Behnken Design was 9.30 ± 0.22 mg/g, where the ethanol concentration, microwave power, and extraction time, were 45.85%, 370.5 W, and 11 min, respectively. However, the optimal total phenolic compounds revealed by Central Composite Design were 8.86 ± 0.05mg/g under ethanol concentration, microwave power, and extraction time of 51.99%, 394.37W, and 9.68min, respectively. Conclusion: This work proposes the best mathematical model to optimize the extraction of polyphenols from this by-product which seems to be a possible source of phenolic compounds that can be used in the food, cosmetic, and pharmaceutical industries.

Peptides are small biomolecules that act as bioactive or host defense molecules. These peptides have a significant role in medicine because of their broad spectrum antimicrobial properties. Marine sources are the largest supply of peptides and natural small molecules since they represent half of the total global biodiversity. Among the different crab species, the horseshoe crab is widely used for extracting the peptides. The horseshoe crab is a marine and brackish water arthropod; it plays a crucial role in the reel and whelk fishing industry and the production of important pharmaceutical bioactive components. This review highlights the details of the extraction and purification of antimicrobial peptides from the horseshoe crab. These peptides represent trends and opportunities for the future, with a focus on the pharmaceutical industries.

Nanometrology has been considered a key to the future of nanotechnology recently. It is particularly important for nanoparticle market development that is commonly applied in different areas of science. The adoption of nanotechnologies in food and agrochemical industries represents a new frontier, with particular regard to plant defence against pathogen agents. Nanometrology deals with a broad range of measurements, as well as chemical and structural characterization, electronic, thermal, and mechanical properties, fabrication and monitoring of nanodevices, and theoretical modelling of nanomaterials properties. Besides the scientific and technological values of a global standard offered by nanometrology, there are also several industry-related values. In this paper, the most common areas of science emphasized the most frequently applied methods by the example of techniques/tools that have been described from a metrological standpoint at a nanosize scale. Therefore, at the microscopic scale may be widely applied: optical techniques, for example, X-ray Photoelectron Spectroscopy (XPS), or optical transmission. Moreover, Scanning Electron Microscopy (SEM) and Energy Dispersive X-ray Spectroscopy (EDX) can be used for microscopic characterization, while Scanning Probe Microscopy (SPM), consisting of Scanning- Tunnelling Microscopy (STM) and Atomic Force Microscopy (AFM), as well as Transmission- Electron Microscopy (TEM), can be employed at the nanoscopic scale. The review has also mentioned Secondary Ion Mass Spectroscopy (SIMS) to analyze secondary ions using a mass spectrometer. In addition, Electron Energy Loss Spectroscopy (EELS) using high-energy electrons from sample penetration or Fourier Transform Infrared Spectroscopy (FTIR) to obtain the infrared spectrum of a sample were also presented. Particle size analysis can be analyzed by performing Small-/Wide-Angle X-ray Scattering (SAXS/WAXS) and Dynamic Light Scattering (DLS) techniques. A specific metrology approach is required for most nanoparticle-based products; that is, the way nanometrology is significant for production quality control and for toxicology studies. This review gives an update on the metrological approaches and applications, with particular attention to nanometrology for different areas of scientific research, i.e., food, agricultural, nutraceutical, biological and medical ones. The novelty character of this paper is to discuss the application of nanotechnologies under metrological principles and approaches at the interface of different integrated, multipurpose and multidisciplinary application fields. The following topics are explored here: i) metrology: definitions, principles, and main features; ii) calibration methods and techniques; iii) measurement methods and systems; iv) proficiency testing; v) nanometrology. Particularly, nanometrology was highlighted in the following directions: significance of the nanodimension, nanometrology in chemical research, nanometrology for the characterization of nanoparticles, nanometrology in biological and medical sciences, mechanical nanometrology, electrical nanometrology and applications of nanometrology in agriculture and food industry.

To combat the escalating antimicrobial resistance, we must constantly develop new medications. Recently, scientists more focused on endophytes to search for novel antimicrobial natural products. Endophytes are explored as 'bio-factories' of natural bioactive therapeutic compounds. These are microbes exhibited in plant living tissues without causing any harmful effect. Many therapeutic compounds isolated from endophytes are produced from biosynthetic pathways and belong to various structural groups like terpenoids, steroids, quinines, and phenols. Therapeutic compounds produced by endophytes exhibit different pharmacological properties. Fungal genera more commonly reside to plant tissue as compared to bacterial genera. The current review emphasizes comprehensive data on the antibacterial and antifungal activity and bio-therapeutic compounds produced by fungal and bacterial endophytes of some medicinal plants.

Neem (Azadirachta indica), a Meliaceae family member, is a rapidly growing tropical evergreen tree with a thick, branching trunk. It has been used for hundreds of years in traditional Indian medicine as a home cure against numerous human illnesses in the Indian and African continents. Different components of the plant, including the flowers, leaves, seeds, and bark, have been used to treat both acute and chronic human illnesses, as well as an insecticide, antibiotic, larvicidal, antimalarial, antibacterial, antiviral, and spermicidal. The plant's anticancer qualities have been extensively researched in terms of its preventative, protective, tumor-suppressive, immunomodulatory, and apoptotic actions against different cancers and their molecular processes. Triple-negative breast cancer (TNBC), which lacks the expression of progesterone and estrogen receptors, has a dismal prognosis and no viable therapeutic options. Gedunin compound isolated from Azadirachta indica's seed oil shows potential anticancer effect against triple-negative breast cancer (TNBC) cancer cells, which acts as heat shock protein 90 (Hsp90) inhibitor.

Background: Diabetes is a chronic disease affecting more than 8.5 % adult population in the world. Among various issues caused by diabetes, wound healing is a major cause of concern. Objective: Injuries are most common, and can be caused normally by abrasion, laceration (cuts), injury, etc. But in diabetes, they do not heal so easily and cause problems. It can be due to a compromised immune system, neuropathy, poor circulation, infections etc., which could lead to amputation or even death. Current therapies for the treatment of wound healing in diabetic patients, have side effects of their own, as there is no particular drug for the healing of wounds. Methods: Numerous surveys in literature were carried out to reveal the obstacles in diabetic wound healing and current approaches to its management with emphasis on alternative therapies. Relevant peer-reviewed research publications were searched through various online bibliographic databases such as ScienceDirect, PubMed, Scopus, Google Scholar, and ResearchGate (all English-language articles). Results: Repurposed drugs include a class of statin, phenytoin, estrogen, and DPP4 inhibitors. Plants with wound healing activity include Rosmarinus officinalis, Radix Rehmannia, Carica papaya, Aloe vera, Catharanthus roseus, Punica granatum, etc. have been explored in pre-clinical studies. Besides these studies, a lot of other studies, including clinical trials, have been performed for wound healing in diabetes by using different procedures like Honey-dressing, Royal Jelly, Extracorporeal Shock wave therapy, Manuka honey-impregnated dressing, LeucoPatch system, etc. Conclusion: In this review, an approach was made to study wound healing in diabetes and various options that could be best suited for the treatment of wounds in diabetes.