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Secondary plant metabolites remain one of the key sources of therapeutic agents despite the development of new approaches for the discovery of medicinal drugs. In the current study, chemical analysis, and biological activities of Kei apple ( Dovyalis caffra ) methanolic extract were evaluated. Chemical analysis was performed using HPLC and GC–MS. Antiviral and anticancer effect were assessed using the crystal violet technique and activity against human liver cells (HepG2), respectively. Antibacterial activity was tested with the disc diffusion method. The obtained results showed that chlorogenic acid (2107.96 ± 0.07 µg/g), catechin (168 ± 0.58 µg/g), and gallic acid (15.66 ± 0.02 µg/g) were the main bioactive compounds identified by HPLC techniques. While, compounds containing furan moieties, as well as levoglucosenone, isochiapin B, dotriacontane, 7-nonynoic acid and tert-hexadecanethiol, with different biological activities were identified by GC–MS. Additionally, inhibition of 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) scavenging was 79.25% at 2000 µg/mL, indicating its antioxidant activity with IC 50 of 728.20 ± 1.04 µg/mL. The tested extract exhibited potential anticancer activity (58.90% toxicity) against HepG2 cells at 1000 µg/mL. Potential bacterial inhibition was observed mainly against Escherichia coli and Proteus vulgaris , followed by Staphylococcus aureus and Bacillus subtilis with a diameter of growth inhibition ranging from 13 to 24 mm. While weak activities were recorded for fungi Candida albicans (10 mm). The extract showed mild antiviral activity against human coronavirus 229E with a selective index (SI) of 10.4, but not against human H3N2 (SI of 0.67). The molecular docking study's energy ratings were in good promise with the experiment documents of antibacterial and antiviral activities. The findings suggest that D. caffra juice extract is a potential candidate for further experiments to assess its use as potential alternative therapeutic agent.

Pyridine, 1,3,4-thiadiazole, and 1,3-thiazole derivatives have various biological activities, such as antimicrobial, analgesic, anticonvulsant, and antitubercular, as well as other anticipated biological properties, including anticancer activity. The starting 1-(3-cyano-4,6-dimethyl-2-oxopyridin-1(2H)-yl)-3-phenylthiourea (2) was prepared and reacted with various hydrazonoyl halides 3a–h, α-haloketones 5a–d, 3-chloropentane-2,4-dione 7a and ethyl 2-chloro-3-oxobutanoate 7b, which afforded the 3-aryl-5-substituted 1,3,4-thiadiazoles 4a–h, 3-phenyl-4-arylthiazoles 6a–d and the 4-methyl-3- phenyl-5-substituted thiazoles 8a,b, respectively. The structures of the synthesized products were confirmed by spectral data. All of the compounds also showed remarkable anticancer activity against the cell line of human colon carcinoma (HTC-116) as well as hepatocellular carcinoma (HepG-2) compared with the Harmine as a reference under in vitro condition. 1,3,4-Thiadiazole 4h was found to be most promising and an excellent performer against both cancer cell lines (IC50 = 2.03 ± 0.72 and 2.17 ± 0.83 µM, respectively), better than the reference drug (IC50 = 2.40 ± 0.12 and 2.54 ± 0.82 µM, respectively). In order to check the binding modes of the above thiadiazole derivatives, molecular docking studies were performed that established a binding site with EGFR TK.

Despite the vital activity of many compounds, they lack that effectiveness due to their low solubility in water. Unfortunately, for this reason, rutin often leads to low tissue permeability and insufficient bioavailability, which has greatly limited its pharmacological utility. Therefore, the present investigation is designed to overcome this problem by formulating the rotin to rotin nanocrystals (RNCs) with studying their some pharmacological applications in vitro and in silico. RNCs were created via the ultrasonication approach and showed a spherical shape via Transmission electron microscopy with a mean particle size of 27 nm. RNCs reflected inhibitory action against Helicobacter pylori with an inhibition zone (IZ) of 22.67 mm compared to rutin (IZ of 18 mm) and standard control (IZ of 19.5 mm). RNCs exhibited less minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) (7.8 µg/mL) than rutin (62.5 µg/mL). The MBC/MIC index of rutin and RNCs indicated their bactericidal properties. RNCs were more acutely ( 92.12%) than rutin (85.43%) for inhibition the H. pylori biofilm formation. A promising half maximal inhibitory concentration (IC 50 ) (6.85 µg/mL) was recorded using RNCs for urease inhibition compared to the IC 50 value of rutin (97.8 µg/mL). The activity of rutin and RNCs was tested against cancer cells of human colon cancer (HT-29) and normal Vero cells. IC 50 values of RNCs were less 168.23 ± 1.15 µg/mL and 297.69 ± 4.23 µg/mL than the IC 50 values of rutin 184.96 ± 4.33 µg/mL and 335.31 ± 2.02 µg/mL against HT-29 cells and normal Vero cells, respectively. Different percentages (72.2, 77.3, and 81.9%) of hemolysis inhibition were recorded using RNCs, but 63.6, 68.9, 73.6, and 80.6% were obtained using rutin at 600, 800, and 1000 µg/mL, respectively. Butyrylcholinesterase (BChE) inhibition % was documented at a lower IC 50 value for RNCs (12.74 µg/mL) than the IC 50 of rutin (18.15 µg/mL). The target molecule underwent molecular docking research against H. pylori [Protein Data Bank (PDB) code: 4HI0], HT-29 cells (PDB code: 2HQ6), and BChE (PDB code: 6EMI) in order to enhance the interactions between rutin and the chosen receptors and to estimate its molecular operating environment (MOE) affinity scoring. Rutin has predicted strong binding interactions and potent activity against the examined proteins 4HI0, 2HQ6, and 6EMI with low binding scores of − 7.47778 kcal/mol, − 7.68511 kcal/mol, and − 9.50333 kcal/mol, respectively.

Multiple biological functions of Mentha pulegium extract were evaluated in the current work. Phytochemical components of the M. pulegium extract were detected by Gas Chromatography-Mass Spectrometry (GC-MS) and High-performance liquid chromatography (HPLC). Moreover, M. pulegium extract was estimated for antioxidant potential by 2,2-Diphenyl-1-picryl-hydrazyl-hydrate (DPPH) free radical scavenging, antimicrobial activity by well diffusion, and anticoagulant activity via prothrombin time (PT) and activated partial thromboplastin time (APTT). GC-MS analysis detected compounds including cholesterol margarate, stigmast-5-en-3-ol, 19-nor-4-androstenediol, androstan-17-one, pulegone-1,2-epoxide, isochiapin B, dotriacontane, hexadecanoic acid and neophytadiene. Chrysoeriol (15.36 µg/mL) was followed by kaempferol (11.14 µg/mL) and 7-OH flavone (10.14 µg/mL), catechin (4.11 µg/mL), hisperdin (3.05 µg/mL), and luteolin (2.36 µg/mL) were detected by HPLC as flavonoids, in addition to ferulic (13.19 µg/mL), cinnamic (12.69 µg/mL), caffeic (11.45 µg/mL), pyrogallol (9.36 µg/mL), p-coumaric (5.06 µg/mL) and salicylic (4.17 µg/mL) as phenolics. Antioxidant activity was detected with IC50 18 µg/mL, hemolysis inhibition was recorded as 79.8% at 1000 μg/mL, and PT and APTT were at 21.5 s and 49.5 s, respectively, at 50 μg/mL of M. pulegium extract. The acute toxicity of M. pulegium extract was recorded against PC3 (IC50 97.99 µg/mL) and MCF7 (IC50 80.21 µg/mL). Antimicrobial activity of M. pulegium extract was documented against Bacillus subtilis, Escherichia coli, Pseudomonasaureus, Candida albicans, Pseudomonas aeruginosa, but not against black fungus Mucor circinelloides. Molecular docking was applied using MOE (Molecular Operating Environment) to explain the biological activity of neophytadiene, luteolin, chrysoeriol and kaempferol. These compounds could be suitable for the development of novel pharmacological agents for treatment of cancer and bacterial infections.

Type-1 diabetes (T1D) is an autoimmune disorder characterized by impaired insulin release by islet β cells. It has been shown that proinflammatory cytokines released during the disease can exacerbate the condition, while anti-inflammatory cytokines offer protection. This study analyzed the clinical role of interleukin (IL)-6, -8, -10, and vitamin D levels in T1D patients compared to healthy controls. The levels of IL-6, IL-8, IL-10, and vitamin D in the participants’ serum samples were analyzed using ELISA. The findings showed that T1D patients had significantly increased levels ( p  < 0.0001) of fasting blood glucose, HbA1c, systolic blood pressure, low-density lipoprotein, triglycerides, cholesterol, and very low-density lipoprotein and decreased levels of high-density lipoprotein and vitamin D ( p  < 0.0001) compared to healthy controls. Moreover, the levels of IL-6, IL-8, and IL-10 were also significantly greater ( p  < 0.0001) in T1D patients. The study also determined the significance of these cytokines among T1D patients and healthy controls using ROC curves. Furthermore, we found that smokers had significantly higher levels of IL-6 ( p  = 0.01) and IL-8 ( p  = 0.003) than non-smokers. These results showed that elevated levels of IL-6, IL-8, and IL-10, decreased vitamin D levels, and smoking among T1D participants could contribute to the worsening of T1D disease and could serve as predictive indicators.

In the last decade, the urgent need to explore medicinal plants or drug development has increased enormously around the world to overcome numerous health problems. In the present investigation, HPLC indicated the existence of 18 phenolic and flavonoid compounds in the Cupressus sempervirens extract. Hesperetin represents the greatest concentration (25,579.57 µg/mL), while other compounds, such as pyro catechol, rutin, gallic acid, chlorogenic acid, naringenin, and quercetin, were recognized in concentrations of 2922.53 µg/mL, 1313.26 µg/mL, 1107.26 µg/mL, 389.09 µg/mL, 156.53 µg/mL, and 97.56 µg/mL, respectively. The well diffusion method documented the antibacterial/antifungal activity of C. sempervirens extract against E. faecalis, E. coli, C. albicans, S. typhi, S.aureus, and M. circinelloid with 35, 33, 32, 25, 23, and 21 mm inhibition zones, respectively, more than the standard antibiotic/antifungal agent. Low values ranging from 7.80 to 15.62 µg/mL of MIC and MBC were recorded for E. faecalis, E. coli, and C. albicans. From the 1- diphenyl-2-picryl hydrazyl (DPPH) assay, promising antioxidant activity was recorded for C. sempervirens extract with IC50 of an 8.97 µg/mL. Moreover, ferric reducing antioxidant power (FRAP) and total antioxidant capacity assays (TAC) confirmed the antioxidant activity of the extract, which was expressed as the ascorbic acid equivalent (AAE) of 366.9 ± 0.2 µg/mg and 102 ± 0.2 µg/mg of extracts, respectively. α-amylase and α-glucosidase inhibition % were determined to express the antidiabetic activity of the extract in vitro, with promising IC50 value (27.01 µg/mL) for α-amylase compared to that of acarbose (50.93 µg/mL), while IC50 value of the extract for α-glucosidase was 19.21µg/mL compared to that of acarbose 4.13 µg/mL. Prothrombin time (PT) and activated partial thromboplastin time (APTT) revealed the role of C. sempervirens extract as an anticoagulant agent if compared with the activity of heparin. Binding interactions of hesperetin and gallic acid were examined via the Molecular Operating Environment (MOE) Dock software against E. faecalis (PDB ID: 3CLQ), C. albicans (PDB ID: 7RJC), α-amylase (PDB ID: 4W93), and α-glucosidase (PDB ID: 3TOP). The obtained results shed light on how molecular modeling methods might inhibit the tested compounds, which have the potential to be useful in the treatment of target proteins.

Background: Ozonation is a non-thermal process that can remodel the chemistry and bioactivity of plant extracts. We evaluated whether ozonating green tea extract enhances its phenolic composition and in vitro bioactivity in relation to nutrition and food applications, with potential clinical applications. Methods: Ethanolic green tea extract (GTE) was exposed to ozone (0–7 L/min, 5 h) to yield an ozonated extract (GTOE). Phenolics were quantified by the HPLC. Bioactivities included antimicrobial testing (agar diffusion; MIC/MBC/MFC), antibiofilm formation, time-kill kinetics (0–180 min), bacteria-induced hemolysis in human RBCs, DPPH radical scavenging, pancreatic lipase inhibition, and scratch-wound closure in human fibroblasts. Data from n = 3 independent experiments were analyzed by one-way ANOVA with Tukey’s post hoc test (α = 0.05). Results: Ozonation increased gallic acid (3150.92 to 3229.69 µg/g) and ellagic acid (2470.66 to 2789.40 µg/g), while catechin decreased slightly (2634.09 to 2535.09 µg/g). Compared with GTE, GTOE produced larger inhibition zones and lower MIC/MBC/MFC against Candida albicans, Bacillus subtilis, Staphylococcus aureus, Klebsiella pneumoniae, and Salmonella typhi; Aspergillus niger remained unsusceptible. For example, inhibition zones for S. aureus and K. pneumoniae increased by 2–4 mm and MIC/MBC values were 2-8-fold lower. Candida albicans showed marked sensitivity (MFC 500 to 125 µg/mL). GTOE exhibited superior, dose-dependent antibiofilm activity across all tested strains, reaching up to 97.82% inhibition, (highest for S. aureus and S. typhi, at 75% MBC). GTOE reduced bacterial counts more rapidly than GTE across all tested strains, achieving full eradication within 150 min. Bacteria-induced hemolysis was inhibited by 97% at 75% MIC with GTOE, versus 93–96% with GTE. Antioxidant capacity improved (DPPH IC50 3.31 vs. 5.54 μg/mL), as did lipase inhibition IC50 6.06 vs. 17.69 μg/mL). Wound closure at 48 h increased (GTOE 61.1%; GTE 56.8%; control 50.8%). Conclusions: Controlled ozonation of green tea extract remodeled phenolics and consistently enhanced antimicrobial, antibiofilm, antioxidant, potential anti-obesity, and wound-healing activities in vitro. These results support food-grade optimization and safety/by-product profiling, followed by in vivo validation at diet-relevant doses, to enable nutrition, food, and potential clinical applications.

Background/Objectives: Medicinal plants are an abundant source of bioactive molecules, particularly in arid environments, such as Saudi Arabia, where Ocimum basilicum L. (Saudi basil) has long been used for its therapeutic properties. This study aimed to examine the phytochemical profile and bioactivities of non-ozonated (untreated) and ozonated methanolic extracts of O. basilicum and to determine whether ozonation enhances their biological effects, with a focus on antidiabetic, anti-Alzheimer, anti-inflammatory, antimicrobial, and cytotoxic properties. Methods: Fresh leaves of O. basilicum were extracted with methanol, subjected to ozonation, and analyzed by HPLC. In vitro assays were conducted to evaluate α-amylase, α-glucosidase, and BChE inhibition, RBC membrane stabilization, antibacterial activity against Helicobacter pylori and cytotoxicity using normal lung fibroblasts (WI-38) and human colorectal adenocarcinoma cell line (Caco-2). Results: Ozonation modified the phytochemical profile, enriching chlorogenic and rosmarinic acids. Ozonated extracts exhibited stronger inhibition of α-amylase with an IC50 of 5.09 µg/mL compared to 13.6 µg/mL of untreated Saudi basil and α-glucosidase (IC50 6.15 µg/mL vs. 9.42 µg/mL). They also showed enhanced BChE inhibition with an IC50 of 13.4 µg/mL compared to 31.8 µg/mL of non-ozonated extract. In addition, ozonated extracts produced significant anti-inflammatory effects by stabilizing RBCs, with an IC50 of 8.04 µg/mL compared to 8.44 µg/mL for untreated extracts and 4.41 µg/mL for indomethacin. Ozonated extracts produced larger H. pylori inhibition zones (26.7 mm) and an MBC/MIC ratio of 1. Cytotoxicity testing revealed that ozonated extracts were less toxic to WI-38 cells, with IC50 values of 437.89 µg/mL versus 191.06 µg/mL, and 149.14 µg/mL compared to 103.7 µg/mL of untreated Saudi basil in Caco-2 cells. Conclusions: Ozonation enriches the phytochemical composition of O. basilicum, enhancing antidiabetic, neuroprotective, anti-inflammatory, and antibacterial activities while reducing cytotoxicity on normal cells. These findings support the potential of ozonated O. basilicum as a safe and promising natural therapeutic candidate for metabolic, neurodegenerative, and infectious diseases.

The biological properties of plant oils are improved by their conversion to nanoemulsions (NEs). This study evaluated the antimicrobial, antioxidant, and anti-hemolytic efficacy of coconut and salad rocket oils and their NEs. The result of the gas chromatography-mass spectroscopy analysis of the oils showed varied constituents such as palmitic acid, trimethylsilyl ester; 2,3-bis(acetyloxy)propyl laurate in salad rocket oil, 2-lauro-1,3-didecoin, n-butyl laurate; laurin, tri-; laurin in coconut oil. NEs diameter of salad rocket and coconut oils was 24.6 and 29.2 nm, respectively. More inhibitory activity of NEs compared with non-NEs form against Bacillus cereus, Staphylococcus aureus, Escherichia coli, Salmonella typhi, Candida albicans, and Aspergillus flavus was detected. Coconut oil and its NEs caused 14.3% (anti-hemolysis 85.7%) and 22% hemolysis (anti-hemolysis 78%), respectively. Salad rocket oil and its NEs caused hemolysis 3.4% and 20.9%, respectively at 1000 µg/mL. Antioxidant activity of salad rocket and coconut oil reflected more IC50 (39.3 and 109.4 µg/mL) than its NEs (35.8 and 80.5 µg/mL), respectively. Molecular docking of trimethylsilyl ester and 2-lauro-1,3-didecoin against S. aureus (PDB=7BGE) and C. albicans protein (PDB=3DRA) revealed optimal binding mode that had the most energy interaction with the binding sites.

It is worth noting that laurel (Laurus nobilis L.) contains several pharmacologically and nutritionally active compounds that may differ according to the pretreatment process. The current study is designed to clarify the effect of moist heat on the phenolic and flavonoid constituents and anti-Helicobacter pylori, antioxidant, antidiabetic, and anti-Alzheimer’s activities of laurel leaf extract (LLE). Unmoist-heated (UMH) and moist-heated (MH) LLEs showed the presence of numerous flavonoid and phenolic constituents, although at different levels of concentration. MH significantly induced (p < 0.05) the occurrence of most compounds at high concentrations of 5655.89 µg/mL, 3967.65 µg/mL, 224.80 µg/mL, 887.83 µg/mL, 2979.14 µg/mL, 203.02 µg/mL, 284.65 µg/mL, 1893.66 µg/mL, and 187.88 µg/mL, unlike the detection at low concentrations of 3461.19 µg/mL, 196.96 µg/mL, 664.12 µg/mL, 2835.09 µg/mL, 153.26 µg/mL, 254.43 µg/mL, 1605.00 µg/mL, 4486.02 µg/mL, and 195.60 µg/mL using UMH, for naringenin, methyl gallate, caffeic acid, rutin, ellagic acid, coumaric acid, vanillin, ferulic acid, and hesperetin, respectively. Chlorogenic acid, syringic acid, and daidzein were detected in the UMH LLE but not in the MH LLE, unlike pyrocatechol. The anti-H. pylori activity of the UMH LLE was lower (23.67 ± 0.58 mm of inhibition zone) than that of the MH LLE (26.00 ± 0.0 mm of inhibition zone). Moreover, the values of MIC and MBC associated with the MH LLE were very low compared to those of the UMH LLE. Via MBC/MIC index calculation, the UMH and MH LLEs showed cidal activity. The MH LLE exhibited higher anti-biofilm activity (93.73%) compared to the anti-biofilm activity (87.75%) of the MH LLE against H. pylori. The urease inhibition percentage was more affected in the UMH LLE compared to the MH LLE, with significant (p < 0.05) IC50 values of 34.17 µg/mL and 91.11 µg/mL, respectively. Promising antioxidant activity was documented with a very low value of IC50 (3.45 µg/mL) for the MH LLE compared to the IC50 value of 4.69 µg/mL for the UMH LLE and the IC50 value of 4.43 µg/mL for ascorbic acid. The MH LLE showed significantly higher (p < 0.05) inhibition of α-glucosidase and butyrylcholinesterase activities, with IC50 values of 9.9 µg/mL and 17.3 µg/mL, respectively, compared to those of the UMH LLE at 18.36 µg/mL and 28.92 µg/mL. The molecular docking of naringenin showed good docking scores against acetylcholinesterase 1E66 and butyrylcholinesterase 6EMI, indicating that naringenin is an intriguing candidate for additional research as a possible medication for Alzheimer’s disease.