Current Bioactive Compounds - Volume 18, Issue 6, 2022

As we enter into the era of modern medicine, breast cancer remains a significant public health concern that has a noteworthy global impact in developed and developing countries. The modern era has seen an increase in the knowledge of the molecular mechanisms underlying cancer progression, leading to many anticancer drugs. The practice of curing certain diseases with the help of plant-derived compounds was one of the traditional methods. Phytochemicals and derivatives present in plants have shown a promising effect for improving efficiency in the treatment of cancer patients and reducing adverse reactions such as integration therapy with chemotherapeutic agents. The primary objective of this review is to compile ongoing research, preclinical studies, and clinical trials of some of the important phytochemicals. In recent years, increasing evidence from preclinical and clinical studies suggests that phytochemicals can favorably modulate several signaling pathways involved in cancer development and progression. Furthermore, phytoconstituents or plant- derived compounds show synergistic action against breast cancer when integrated with chemotherapy. Thus, the therapeutic potential of naturally occurring phytochemicals is of great interest as a part of integration therapy in cancer care. This review focuses on phytochemicals from quinones, terpenoids, alkaloids, polyphenols, steroidal lactones, and glycosides classes that help treat breast cancer. In addition, the phytochemicals act by various pharmacological mechanisms like carcinogen inactivation, inhibiting proliferation, cell cycle arrest, and apoptosis. Collectively, detailed information about specific classes of phytoconstituents along with their mechanism of action is mentioned in this review.

Phytosteroids are biologically active compounds found naturally in herb plasma membranes, with a chemical composition similar to animal plasma membrane cholesterol. It can be found in almost all fats abundant plant’s diets. One of the vital phytosterols is β-sitosterol which has several biological activities. It has been proved in various in-vivo and in-vitro research in which β-sitosterol stabilized several physiological activities like as antioxidant, CNS activity (like anti-alzheimer, anxiolytic and sedative effects, CNS depressant activity), lipid-lowering effects (like nonalcoholic fatty liver disease), antidiabetic, anti-inflammatory and analgesic effects, anticancer and immunomodulatory, protective effects in pulmonary fibrosis, wound healing effects and anti-viral and COVID-19 activity. The experimental research on β-sitosterol shows that it can be used as a nutritional supplement to combat variousexisting diseases. In this review, we are highlighting the most significant pharmacological action of β-sitosterol on the basis of available literature.

Background: Peach gum is a natural gum exudate secreted from a peach tree (Prunus persica) by a process known as physiological gummosis. Peach gum is a natural biopolymer that is composed of acidic polysaccharides with a high percentage of arabinose and galactose subunit, which classifies it as an arabinogalactan. Objective: This review summarizes the composition, chemical structures, physical properties and biological properties of peach gum, and its potential biotechnological applications. Methods: A literature search was performed using Google Scholar with keywords as Peach Gum and Prunus persica. Only articles written in English and articles with downloadable full-texts were included in this review. Results: Peach gum polysaccharides possess antibacterial, antioxidant and anti-diabetic, and hypolipidemic properties. Excellent emulsification properties of PGP show that it has the potential to be employed as a food-grade emulsifier. Conclusion: PGP exhibits excellent emulsification, antioxidant, antibacterial, anti-diabetic and hypolipidemic properties. As plastic pollution has become an alarming global issue, PGP could be a promising edible raw material in the field of bioplastic research and development.

Background: Cancer is undoubtedly a major challenge of modern era and is the second leading cause of death in the world. Lung cancer is the second most common cancer and the leading cause of cancer death among men and women. Non-Small Cell Lung Cancer (NSCLC) accounts for 84% of all lung cancer diagnosed. Benzimidazoles are important heterocyclic compounds possessing a variety of biological activities such as anticancer, antioxidant, anti-inflammatory, and analgesic, anti-viral, anti-bacterial, anti-fungal and hypoglycemic activities. Pyrazolines reported antitumor, immunosuppressive, antibacterial and anti tubercular agents. Biological activities of the benzimidazole derivatives depend on the functional group attached to the benzimidazole moiety. Objective: The present research focused on incorporating pyrazoline nucleus into benzimidazole nucleus to form a potent anticancer agent targeting lung cancer therapy. Methods: The in silico novel pyrazoline substituted benzimidazole derivatives were designed. Docking was performed to know the binding interactions of the newer agents with the enzymes. The compounds were found to be active in docking studies synthesized and tested for anticancer activity. In vitro screening of the selected derivatives for anticancer activity by MTT assay method showed very good results. Cytotoxicity of compounds BZ1, BZ2, BZ10 and BZ16 studied against fibrosarcoma and lung cancer cell line. Results: The compound BZ1 showed highest activity against fibrosarcoma and lung cancer cell line. Conclusion: Further studies on these compounds to prove it as a lead compound in cancer therapy should be conducted.

Background: The olive tree (Olea europaea L.), the most widespread plant species in the Mediterranean basin, includes two forms: cultivated (var Europaea) and wild (var Sylvestris). Wild olive trees or oleasters cover large areas in Algeria. It has been shown that oil from oleaster has a higher content of phenolic compounds, which could have antimicrobial properties. Objective: The objective of this study was to assess the antibacterial activity of phenolic extracts from four Algerian oleaster oils and an extra virgin olive oil (EVOO) from Chemlal variety. Methods: Phenolic compounds were determined by UHPLC-MS. Antibacterial activity was tested against six referenced human enteropathogenic bacteria by the agar disc diffusion method by measuring the diameters of the zone of inhibition. Results: The results revealed a similarity between the phenolic composition of oleasters 1 and 3 and between oleaster 4 and EVOO; however, the phenolic composition of oleaster 2 that the poorer was markedly different with a higher content of free phenolic alcohols and lower in secoiridoids. Almost all bacteria showed to be sensitive against the antibiotics, with the value of ZOI ranging from 5-32 mm; otherwise, most of the oleaster extracts exhibited higher antibacterial activity than the EVOO with ZOI values of 7-12mm. A significant correlation was noted between phenolic content and antibacterial activity. Conclusion: These results show that oleaster oil can be considered a high potential food.

Background: Coniferous cones are a by-product of forestry and wood logging, used for many possible purposes, e.g., the extraction of polyphenols. Objective: The aim of the present article was the comparison of the antioxidant polyphenol content of the differently matured cones of 17 selected conifers, either common in Hungary or yet uninvestigated. Methods: Total polyphenol content, ferric reducing antioxidant power and 2,2-diphenyl-1-picrylhydrazyl assays were used to determine the antioxidant contents. A scoring system was implemented using the three assay results to evaluate and compare the overall antioxidant power of the samples. Result and Conclusion: Highest antioxidant contents were found in green cones, followed by mature and opened cones. Taxa with the highest scores were Tsuga canadensis, Cryptomeria japonica, Chamaecyparis lawsoniana, Thuja orientalis, Metasequoia glyptostroboides and Picea abies. For the samples with the highest overall antioxidant power the high-performance liquid chromatographic/ tandem mass spectrometric polyphenol profiling was carried out (green cones of T. canadensis and P. abies) and 83 compounds have been tentatively identified and described. Results contribute to the future bioactivity testing and evaluation of the cone extracts of T. canadensis and P. abies.

Background: Citrus fruits, especially clementines, are among the most consumed fruits in the world. Clementine consists of pulp (endocarp) and peel (epicarp) which are rich in carotenoids. After using fruit pulp, peels are usually discarded as waste; the valorization of the latter in the recovery of its beneficial components, mainly carotenoids, may seem to be important. Objective: The main objective of this study is to determine the optimal conditions allowing the extraction of a high carotenoids yield from clementine peels. Methods: The microwave-assisted extraction method (MAE) was applied for extraction of total carotenoids from Citrus clementina peels, and the response surface methodology (RSM) was used to investigate the influence of extraction parameters, including hexane concentration, microwave power, irradiation time, and solvent to solid ratio, on the extraction yield, then the results were modeled using a second order regression. Total carotenoids yield of clementine peel extract obtained under optimal microwave-assisted extraction conditions was compared to extracts performed using two conventional extraction methods (maceration and Soxhlet). Results: The optimal conditions for microwave-assisted extraction were 68 % of hexane concentration using 561 W of microwave power during 7.64 min of irradiation time, 43 ml/g of solvent-tosolid ratio using two successive extractions. Under optimized conditions of microwave-assisted extraction, the recovery of carotenoid content was 186.55 μg/g dry matter (DM), which was higher than that obtained by the two conventional methods, maceration extraction (ME; 160.53 μg/g DM) and Soxhlet extraction (SE; 162.68 μg/g DM). Conclusion: From this study, it can be concluded that microwave-assisted extraction is an efficient method for carotenoid recovery and considering its high yield in reduced time, it could be recommended for extraction of these bioactive compounds from clementine peels.

Background: Citrus polymethoxylated flavones (PMFs) reduce the synthesis of liver lipoproteins in animal and in vitro cell assays, but few studies have evaluated the direct effects of their metabolites on this highly regulated process. Objective: The aim of the study was to investigate the effects of representative metabolites of PMF on the secretion of liver lipoproteins using the mammalian cell Huh7.5. Methods: In this study, the influences of three PMFs and five previously isolated PMF metabolites on hepatic apoB-100 secretion and microsomal transfer protein (MTP) activity were evaluated. Tangeretin (TAN), nobiletin (NOB) and 3,5,6,7,8,3′,4′-heptamethoxyflavone (HMF), their glucuronides (TAN-Gluc, NOB-Gluc and HMF-Gluc) and oxidatively demethylated metabolites (TAN-OH, NOB-OH, HMF-OH), were incubated with Huh7.5 cells to measure their inhibitory effects on lipid synthesis. Results: The results showed that TAN, HMF and TAN-OH reduced the secretion of apoB-100 in a dose-dependent manner, while NOB and the other tested metabolites showed no inhibition. MTP activity in the Huh7.5 cells was significantly reduced in the presence of low concentrations of TAN and high concentrations of NOB-OH. This study also showed that PMFs and PMF metabolites produced a wide range of effects on apoB-100 secretion and MTP activity. Conclusion: The results suggest that while PMFs and their metabolites control dyslipidemia in vivo, the inhibition of MTP activity cannot be the only pathway influenced by these compounds.