Current Bioactive Compounds - Volume 18, Issue 3, 2022

Background: Phytochemicals are pure chemical compounds found to be present in different plants part such as leaves, fruit, flower, seeds and the whole plant. These pure plant-based chemicals are having power to treat all disorders of the human beings and other higher animal species on earth. Flavonoidal compounds are responsible for the attractive color and important biological properties of plant material. Flavonoids are having a potential role in the treatment of numerous health complications of human beings. Antioxidant properties are one of the best pharmacological properties of all classes of flavonoidal compounds. A significant amount of these flavonoidal compounds are needed in our daily routine diet. Methods: Cirsiliol also called 5,3′,4′-trihydroxy-6,7-dimethoxyflavone is a flavonoidal class chemical found to be present in different plants including Salvia guaranitica. Various literature databases have been searched to know the biological potential of the cirsiliol in medicine. Different scientific research data of cirsiliol have been collected from various literature sources and analyzed in the present work. Detail pharmacological activities of cirsiliol in medicine have been evaluated in the present work through literature data analysis of various scientific research works. However analytical data has also been collected and analyzed in the present work through different literature sources. Results: From the collected data, it was found that cirsiliol is present in the plants such as Artemisia campestris, Artemisia scoparia, Centaurea jacea, Centaurea phyllocephala, Crossostephium chinense, Dracocephalum tanguticum, Eupatorium lindleyanum, Hyptis pectinata, and Iris germanica. Pharmacological data analysis revealed the biological importance of cirsiliol against cancer, inflammatory diseases, obesity-related insulin resistance, and respiratory disorders. However, the biological potential on ileum, benzodiazepine receptor, arachidonate 5-lipoxygenase, and xanthine oxidase has also been well summarized in the present investigation. High-performance liquid chromatography, bioactivity-guided isolation techniques, UPLC-ESI-MS/MS, LCMS and HPLC, and other forms of chromatographic techniques have been applicable for the analysis of cirsiliol in the various plants material. Conclusion: The present investigation revealed the biological importance and therapeutic benefit of cirsiliol in medicine for the development of better remedies against human disorders.

Background: Many species have already been examined regarding their biological activities, but there are nevertheless many more which merit examination, among them Carduncellus pinnatus (Desf), which is one of the less abundant and the less frequent aromatic plants of Asteraceae species, it is one of the species widely distributed in the Mediterranean region. In the present investigation, chemical composition of essential oils of Carduncellus pinnatus and their antioxidant, antimicrobial and antifungal activities were investigated for the first time. Methods: The chemical composition of the essential oils of Carduncellus pinnatus was analyzed by gas chromatography (GC) and gas chromatography, mass spectroscopy (GC/MS) during its vegetative cycle. The antioxidant properties were evaluated by DPPH-radical scavenging and FRAP methods. The essential oil was tested on two-gram positive bacteria, three-gram negative bacteria, two filamentous fungi and one yeast. The toxicity of this essential oil was evaluated from several experiments on five mice tested in the laboratory. Results: The chemical composition of essential oils studied by GC and GC-MS showed a total of twenty-seven compounds constituted mainly by Aplotaxene. Harvest time affected quantitatively but not qualitatively the chemical composition of essential oils. The results showed that Carduncellus pinnatus presented interesting antioxidant properties. In order to assess the biological activities of Carduncellus pinnatus, all essential oil samples were combined together to produce a collective essential oil (Coll EO). The Coll EO showed activity on all tested bacterial strains based on the inhibition diameters obtained. The most interesting antimicrobial activity has been observed against Salmonella typhi, Escherichia coli and Staphylococcus aureus with IC50s 0.4, 1.2 and 1.2 g/L, but which remains weak compared to the Gentamicin control, respectively). Regarding antifungal activity, the largest inhibition was observed against Fusarium solani (IC50= 0.8 g/L). On the other hand, the toxicity test of Coll EO showed no mortality rate to the concentration of 1g/kg injected into the mice Conclusion: The results presented here constitute new findings in the field of the chemical characterization and biological potential of Carduncellus pinnatus.

Background: Sargassum cristaefolium, as one of the brown seaweeds locally found in Indonesia, is extracted using the serial technique employing different solvents. Methods: S. cristaefolium powder (50 mesh) was extracted with three different solvents, including hexane, ethyl acetate, and methanol. S. cristaefolium powder residue was dried prior to serial re-extraction using different solvents. Three serial extracts were obtained and named as 1-stage extract, 2-stage extract, and 3-stage extract. Besides, a single-step extract (i.e., extraction using only methanol) was produced to be compared with three serial extracts in antibacterial activity tests (against E. coli and S. aureus). The three serial extracts were detected for their antibacterial compounds using GC-MS, LC-HRMS, and FT-IR. Results: The 3-stage extract exhibited the highest extraction yield. On S. aureus, the inhibition zone in all extracts was not significantly different. On E.coli, the highest inhibition zone (5.42±0.14 mm) was of the 3-stage extract; indeed, it was higher than both antibiotic and a single- step extract. Antibacterial compounds, such as phenol, 9-Tricosene(Z)-, palmitic acid, and oleamide, were present in all extracts. Other antibacterial compound types, both the 1-stage and 2-stage extracts, contained 7 types, whilst the 3-stage extract contained the most types (11 types). Particularly, hexyl cinnamic aldehyde, betaine and several cinnamic aldehyde groups were detected only in the 3-stage extract comprising the dominant area. The carboxylic acid groups were detected in all extracts to confirm the fatty acid structure. Conclusion: The serial extraction technique could produce the 3-stage extract which exhibited the strongest antibacterial activity and contained the richest antibacterial compounds.

Background: The prevailing multiple drug resistance among the bacterial species is alarmingly rising day to day, becoming a global threat. Many infectious diseases have become untreated due to the development of resistance in bacterial species, which have a considerable impact on mortality. Methods: In this present study, we aimed to synthesize a series of 12 compounds [S1-S12], which are azetidinone derivatives of nicotinic acid. The in vitro antibacterial studies were performed against certain species of gram-negative and gram-positive bacteria. Molecular docking studies were performed to identify the affinity towards the target protein. The antioxidant study was also performed for the synthesized compounds. Results: All the synthesized compounds exhibited moderate to potent antibacterial activity with a MIC range of 9.8-21.6 μgmL^-1, compounds were active against all tested micro-organisms. The compounds substituted with electron-donating groups like hydroxyl showed higher antioxidant activity compared to others. Docking studies were performed on the active site of DNA gyrase [PDBID: 5L3J,2XCT, 1W7Q]. Conclusion: The present study reveals that the compounds synthesized exhibit very good antimicrobial activity and antioxidant activity. Therefore, these compounds may be used as a lead for the anticancer, anti-tubercular and other chemotherapeutic agents in future studies.

Background: Aromatic and medicinal plants have been used to substitute synthetic drugs with natural bioactive products. Objective: The current investigation was conducted to evaluate phenol and flavonoid contents, antibacterial, antioxidant, and anti-hypertensive potentials of three extracts of Margotia gummifera aerial parts. Methods: The antibacterial effect was assessed using the wells agar diffusion method against 11 strains. The antioxidant effect was evaluated using different methods, 2, 2-diphenyl-1-picrylhydrazyl, total antioxidant capacity, ferric reducing ability power, cupric reducing antioxidant capacity, and β-carotene/linoleic acid bleaching assay. The anti-hypertensive activity was performed using hippuryl-histidyl-leucine substrates. Results: The highest yield, i.e., 19.801%, was obtained by the hydro-methanolic extract. However, ethyl acetate extract seemed to be rich in phenolic and flavonoid compounds compared to other extracts, i.e., 822.14±69.10 mg GAE g^-1 ext. and 117.28±1.80 mg RE g^-1 ext., respectively. The high free radical scavenging activity was mentioned in ethyl acetate extract with IC50 of 48.820±1.25 μg/ml. The same extract showed better antioxidant activity in all tested procedures. In antibacterial activity, the hydro-methanolic extract exhibited moderate effect against all tested bacteria except Salmonella enterica and Enterococcus faecalis which gave 18±2.0 and 16±1.0 mm of inhibition, whereas it seemed to be inactive towards two Gram-negative bacteria. Concerning anti-hypertensive activity, all extracts can inhibit the Angiotensin-I Converting Enzyme, but the potential effect was given by hydro-methanolic and aqueous extracts, 97.75% and 96.65%, respectively. Conclusion: It can be stated that the bioactive compounds of Margotia gummifera extracts had different biological activities, which confirm their therapeutic uses in traditional medicine.

Background: Globularia alypum L. is a Mediterranean plant of the Globulariaceae family which has been used in folk medicine to cure several diseases. Different studies have been done in vitro and in vivo using diverse G. alypum extracts to understand this traditional use. Methods: In this study, Tunisian G. alypum leaf methanol extract (GAME) was chemically identified using LC-ESI-MS, then examined in vitro for its antioxidant, antibacterial, and antifungal activities. Besides, a molecular docking study was also conducted. Results: Nineteen phenolic compounds were detected, with trans-cinnamic acid (45.14%) and luteolin 7-O-glucoside (19.82%) being the dominant ones. The GAME demonstrated important antioxidant activities, especially against 2, 2-diphenyl-l-1-picrylhydrazil (DPPH) radical (IC50 = 16.1±1.1 μg.ml^-1) and exhibited an anti-proliferative effect against Vero cells with (IC50 2091 ± 177 μg.ml^-1). Data also reveals that the GAME inhibited the growth of oral bacteria, in particular Streptococcus oralis (MICs value ranged from 2560 to 20480 μg.ml^-1). In addition, GAME has a significant antifungal action, especially against Candida albicans ATCC 90028 (MIC=2560 μg.ml^-1). Docking study identified one of the major molecules (luteolin 7-O-glucoside) present in the GAME extract, displaying a good interaction with tyrosinase (docking score -9.6 kcal.mol^-1) and other antibacterial (tyrosyl-tRNA synthetase, gyrase, deformylase) and antifungal (n-myristoyltransferase, chitinase) target proteins. Conclusion: This study illustrates that GAME has potent sources of antioxidants and antimicrobials useful in combating oral bacteria. Hence GAME can be of reasonable use in food technology, processing, as well as the medical field.

Background: Lignans are biologically important phenolic compounds that exist in different levels of various plants; yet, flaxseed is one of the richest sources of such compounds. Lipoxygenase enzymes are associated with many inflammatory-related diseases such as arthritis, allergic asthma, psoriasis, cardiovascular disease, kidney disease, skin diseases, and neuropsychiatric disorders, as in Alzheimer's disease. Not only are these enzymes involved in many types of cancers, but they are also very crucial to find new LOX inhibitors to treat human diseases such as cancer or cardiovascular disease. Screening for lipoxygenase inhibitory activities of flaxseeds lignans extracts in various methods is reported in this work. Methods: Extracts of samples of flaxseeds (Linum usitatissmum) were prepared using the following methods: a- extraction with continuous stirring with 80% ethanol, b- extraction with a mixture of equal volumes of diethyl ether and ethyl acetate after direct acid hydrolysis, c- Extraction with 50% ethanol followed by alkaline hydrolysis. Total flavonoids, total phenolic of these extracts were compared. The scavenging potential of free radicals was determined using the DPPH method. The inhibitory potential against the lipoxygenase enzyme was determined by using the soybean lipoxygenase enzyme. Results: The highest phenolic content was in the extract prepared with ethanol 80% with continuous stirring, with phenolic content of (126.848 mg GAE /g). While the highest flavonoid was content in the extract prepared with a mixture of equal volumes of diethyl ether and ethyl acetate after direct acid hydrolysis, with flavonoid content reached (7.8 mg QE / g). Moreover, the scavenging potential of free radicals expressed in terms of IC50 (μg/ml) showed extraction with a mixture of equal volumes of diethyl ether and ethyl acetate after direct acid hydrolysis exhibited higher antioxidant capacity (IC50=22.257±0.095 μg/ml) followed by 80% ethanol extract. The median inhibitory concentration (IC50) was calculated according to the LOX enzyme inhibitory method. The IC50 value of a mixture of equal volumes of diethyl ether and ethyl acetate after direct acid hydrolysis extract of flaxseeds is 73.689±0.585 μg/ml. Conclusion: The mixture of equal volumes of diethyl ether and ethyl acetate extract after direct acid hydrolysis gives stronger scavenging potential of free radicals and lipoxygenase inhibitory effects than the other extracts in this study. Therefore, according to the results we got in our study, flaxseed extracts can be a potential source of novel therapeutics to treat many diseases related to the LOX enzyme.

Objectives: Ruta tuberculata forssk. (Rutaceae) is an aromatic plant widely used in traditional Algerian medicine due to its pharmaceutical virtues against various disorders. This study aims to determine the phenolic profile of aqueous (RAE) and methanol (RME) extracts of R. tuberculata aerial parts and to investigate their acute oral toxicity, as well as their possible antiproliferative and hepatoprotective effects. Methods: Polyphenols were identified by quantitative LC-MS/MS analysis. Oral acute toxicity was performed according to OCDE guidelines. The hepatoprotective activity was evaluated by paracetamol-induced hepatotoxicity and supported by biochemical and histological analysis of liver and kidneys. The antiproliferative activity against human colorectal HT-29 and ovarian OV2008 cancer cell lines was determined using SRB assay. Results: LC-MS/MS analysis revealed that RME has higher phenols and flavonoids content than RAE; however, its major identified flavonoids are Kaempferol, rutin, and naringenin. R. tuberculata seems mildly toxic at several doses, with oral LD50 greater than 5000 mg/kg. The significant increase in hepatic markers enzymes activities as well as cholesterol, triglycerides, and glycemic levels, caused by PCM-administration, was potentially reduced following the co-treatments with vitamin C and RME, respectively, compared to RAE. Moreover, RME-treatment markedly prevented all histological changes. Compared to RAE, RME (100 μg/mL) exhibited excellent antiproliferative activity against both tested cancer lines (% inhibition ≥ 80%). Conclusion: Both R. tuberculata extracts (200 mg/kg/daily) were non-toxic and exerted a potential hepatoprotective effect against PCM-induced hepatotoxicity. Accordingly, RME may be considered a good candidate for the development of new therapies against colorectal and ovarian cancers.