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In the present study, we isolated linalool, geraniol, carvacrol, thymol, menthol and eugenol; synthesised their phenoxyacetic acid derivatives; and assessed their phytotoxic and genotoxic potentials against weeds and agricultural crops. Moreover, the fungicidal activity of both categories of compounds against 12 fungi was examined. Finally, using probabilistic assessment based on Risk Quotient (RQ) by the Monte Carlo simulation (MCS) method, we examined human health risks via oral exposure to these compounds. Toxic potencies to plants demonstrated that all parameters and related indices including germination percentage, mean germination time, germination rate, root length, shoot length, seedling length and vigour index dose-dependently decreased in both weeds and agricultural crops. Based on the comet assay, DNA damage was observed in the root meristems of the plants. Consequently, a significant decrease was observed in head DNA, whereas a significant increase in tail DNA was observed in response to treatments. Besides, the natural components and semisynthetic molecules showed a broad spectrum of fungicidal traits. However, eugenol and eugenoxyacetic acid inhibitory effects on the growth of the tested fungi were similar to that of benomyl. Our probabilistic health risk assessment indicated di minimis risk for natural components and their phenoxyacetic acid derivatives. Sensitivity analysis showed that concentrations of residues of the compounds had the most significant effect on risk. Current findings could offer a platform for developing sustainable approaches to reduce chemical residues and their consequent risks to the environment and human health. [ABSTRACT FROM AUTHOR]

Phytochemical study of the Salvia santolinifolia root extract resulted in the isolation of one new quinone diterpenoid, aegyptinone E (1) as well as two known ones, aegyptinone A (2) and aegyptinone D (3). All the isolated compounds were reported for the first time from S. santolinifolia. Spectroscopic analyses including 1 D and 2 D NMR and HRESIMS were used to determine the chemical structures. Aegyptinone A (2) showed moderate antibacterial activity against Staphylococcus aureus, Staphylococcus epidermis, and Bacillus subtilis with MIC of 25 μg/mL. [ABSTRACT FROM AUTHOR]

Hair loss and hirsutism have been major complaints due to increased concentrations of dihydrotestosterone. The plant Platycladus orientalis, with 5-alpha reductase inhibitor properties, has been used to treat these disorders. Its formulation with lipophilic carriers in SLN possesses high loading capacity and greater permeability to hair follicles. The present study aimed to determine the content of active ingredients in the extract of P. orientalis L. and to prepare and characterize the solid lipid nanoparticles (SLN) of Platycladus orientalis L. extract as a 5-alpha reductase inhibitor. The total methanolic extract was obtained following the maceration technique. This preparation was analyzed by HPLC using Quercetin and Cedrol as standard components. SLNs were prepared by high-shear homogenization and ultrasound. Four Glucire-GMS-Compritol-Precirol lipids and three poloxamer-tween80-Labrasol surfactants were further used in the formulations. Particle size, zeta potential, nanoparticle morphology, encapsulation percentage, crystal structure, physical stability, size, and zeta potential were studied 0, 3, and 6 months after preparation. Within 1-7 days after preparation, formulations containing GMS and compritol lipids became solid and jelly. Meanwhile, the formulations with Precirol as the lipid and Poloxamer as the surfactant with 0.3% extract exhibited desirable properties such as average particle size (192 nm), the encapsulation of the extract inside the nanoparticles was almost 71%, and good zeta potential. This formulation containing precirol as a lipid, poloxamer as a surfactant, and 0.3% plant extract exhibited greater 5-alpha reductase inhibitor activity, and it can be recommended to treat hair loss and hirsutism. [ABSTRACT FROM AUTHOR]

Objective(s): Rosa damascena Herrm. belonging to the Rosaceae family has demonstrated antiinflammatory and anti-oxidant effects previously. Excessive production of free radicals and activation of tyrosinase enzyme caused by UV induces excessive concentration of melanin pigment and skin spots in the long term. Therefore, finding natural sources with anti-oxidant and antityrosinase effects helps to regulate the melanogenesis process. In the current research, we investigated the antimelanogenic, anti-oxidant, and anti-tyrosinase effects of its essential oil, methanol extract (MeOH), and different fractions including n-hexane, dichloromethane (CH2Cl2), n-butanol (BuOH), ethyl acetate (EtOAc), and H2O of R. damascena in B16F10 cell line. Materials and Methods: For this purpose, impacts of extracts and essential oil of R. damascena were investigated on cell viability, cellular tyrosinase, melanin content, mushroom tyrosinase, reactive oxygen species (ROS) production, as well as the amount of tyrosinase protein in the B16F10 murine melanoma cell line. Results: Essential oil, MeOH, and different fractions of R. damascena were not cytotoxic on B16F10 cells. However, they had significant reducing effects on mushroom tyrosinase activity, melanin content, and ROS production. Also, there is a significant decrease in tyrosinase protein levels at 200 µg/ml but not at other concentrations. Conclusion: Therefore, the essential oil, MeOH, and different fractions of R. damascena had promising antimelanogenic activity via repression of mushroom tyrosinase activity and ROS production. [ABSTRACT FROM AUTHOR]

Objective(s): Salvia abrotanoides is considered as a new source of tanshinone-producing plants in Iran. Symbiosis of endophytic fungi with their host plants is an effective tool to promote the growth and secondary metabolism of medicinal herbs. Therefore, using endophytic fungi as a biotic elicitor is a proper solution to increase the yield of plant products. Materials and Methods: In this study, some endophytic fungi were first isolated from the root of S. abrotanoides, then two of them (Penicillium canescens and Talaromyces sp.) were co-cultivated with the sterile seedling of S. abrotanoides in pot culture. After proving the colonization of these fungi in the root tissues by microscopic studies, their effects on the production of critical medicinal compounds such as tanshinones and phenolic acids were investigated in the vegetation stage (120 days). Results: Our results showed that the content of cryptotanshinone (Cry) and tanshinone IIA (T-IIA) in plants inoculated with P. canescens increased by 77.00% and 19.64%, respectively, compared with non-inoculated plants (control). The contents of mentioned compounds in plants inoculated with Talaromyces sp. increased by 50.00% and 23.00%, respectively. In this case, in plants inoculated with P. canescens, it was found that the level of caffeic acid, rosmarinic acid, and its PAL enzyme activity increased by 64.00%, 69.00%, and 50.00%, respectively, compared with the control. Conclusion: Endophytic fungi have specific modes of action and the ability to provide multiple benefits. Each of the two strains is a highly considerable microbial resource for the growth and accumulation of active compounds of S. abrotanoides. [ABSTRACT FROM AUTHOR]

On the basis of biological activities of the ethyl acetate extracts of four Xenorhabdus sp. including Xenorhabdus nematophila FUM 220, Xenorhabdus nematophila FUM 221, Xenorhabdus bovienii FUM 222, and Xenorhabdus bovienii FUM 223, X. nematophila FUM 220 was preferentially selected to track the isolation of responsible compounds. Chemical study on the ethyl acetate extract of X. nematophila isolate FUM220 which is derived from the native nematode Steinernema carpocapsae (Rhabditida: Steinernematidae), was evaluated, and eleven compounds, including xenocoumacin II (1), xenortide-396 (2), xenortide A (3), xenortide-410 (4), xenortide-449 (5), xenematide A 663 (6), rhabdopeptide-574 (7), rhabdopeptide-588 (8), rhabdopeptide-687 (9), rhabdopeptide-701 (10), and nematophin-273 (11) were characterized. In this experimental study, we surveyed the antitumoral potential of bacterial extract and bacterial metabolites to treat human breast cancer (MCF-7), human lung cancer (A549), and murine Tumor (B16) cell lines. We observed that all samples were cytotoxic, but bacterial extracts of X. nematophila FUM 220 and X. bovienii FUM 223 showed higher toxicity on mentioned cell lines. Potent cytotoxic activity was found for compounds 6 and 11 with IC50 of 6.2 μg/ml against human lung cancer A549 cell lines, too. These compounds showed moderated antibacterial activity against Xanthomonas oryzae pv. oryzae strain Xoo-IR42 (Xanthomonadales: Xanthomonadaceae) (MIC of 62.5 μg/ml) and Staphylococcus aureus strain 1112 (Bacillales: Staphylococcaceae) (MIC of 100 μg/ml). The bacterial extracts from X. bovienii FUM 222 showed strong inhibition of the growth of S. aureus strain 1112, by a minimal inhibitory concentration assay (MIC of 53.5 μg/ml). Xenorhabdus genera produce metabolites with potent cytotoxic and antibacterial activity. Single compounds can be isolated, identified, and commercialized, but various species or strains may change their anticancer or antimicrobial potential. The present study brings new clues regarding the qualified of Xenorhabdus as future peptide sources for supplying natural bioactive compounds and challenge multidrug-resistant bacteria, treat cancer, and plant diseases. [ABSTRACT FROM AUTHOR]

Objective(s): Neobaicalein is one of the rich plant flavonoids isolated from the roots of Scutellaria spp. In this study, we evaluated and compared cytotoxic activity and the related apoptosis mechanisms of neobaicalein from Scutellaria litwinowii Bornm. & Sint. ex Bornm on apoptosis-proficient HL-60 cells and apoptosis-resistant K562 cells. Materials and Methods: Cell viability, cell apoptosis, caspase activity, and apoptosis-related protein expression were measured using MTS assay, propidium iodide (PI) staining and flow cytometry, caspase activity assay, and western blot analysis, respectively. Results: Neobaicalein significantly reduced cell viability in a dose-dependent manner using the MTS assay (P<0.05). The IC50 values (μM) against HL-60 and K562 cells after 48 hr treatment were 40.5 and 84.8, respectively. Incubation of HL-60 and K562 cells with 25, 50, and 100 μM neobaicalein for 48 hr, significantly increased the number of apoptotic cells and showed cytotoxic effects compared with the control group. Treatment with neobaicalein significantly increased Fas (P<0.05) and the cleaved form of PARP (P<0.05), and decreased the Bcl-2 levels (P<0.05) in HL-60 cells, whereas neobaicalein significantly increased Bax (P<0.05) and the cleaved form of PARP (P<0.05), and the caspases of the extrinsic and intrinsic pathways including caspases-8 (P<0.0001), -9 (P<0.01), and effector caspase-3 (P<0.0001) levels in K562 cells compared with the control group. Conclusion: It seems neobaicalein might cause cytotoxicity and cell apoptosis through interaction with the different apoptosis-related proteins of apoptotic pathways in HL-60 and K562 cells. Neobaicalein may exert a beneficial protective effect in slowing the progression of hematological malignancies. [ABSTRACT FROM AUTHOR]

Endophytic fungi are often producing host plant metabolites. Tanshinones are secondary metabolites of the Salvia genus which are also produced by some endophytic fungi. Efficient secondary metabolite production in endophytic fungi drops significantly after sequential subcultures. 5-azacytidine (5-AC) is an analog of the naturally occurring pyrimidine nucleoside cytidine and a DNA methyltransferase inhibitor. In this relation, 5-AC is an effective tool to induce the expression of silenced secondary metabolite genes in fungi. We isolated 4 endophytic fungi from the roots of Salvia abrotanoides which produced tanshinone. Cryptotanshinone and tanshinone IIA were produced by Penicillium canescens, Penicillium nodositatum, and Penicillium pinophilum, while Paraphoma radicina only produced tanshinone IIA. The maximum amount of tanshinones was extracted from P. pinophilum culture with 130.826 mg cryptotanshinone/g of dry weight and 50.155 mg Tanshinone IIA/g of dry weight. These amounts were significantly more than tanshinones produced in plant roots (0.55 mg cryptotanshinone/g of dry weight, 1.3 mg Tanshinone IIA/g of dry weight). In the third subculture, tanshinone production decreased significantly. 5-azacytidine as an epigenetic modifier retrieved tanshinone production in the third subculture of P. pinophilum. Also, 5-azacytidine treatment made a big jump in Tanshinone IIA production in P. radicina (63.176 mg TIIA/g of dry weight) besides increasing Tanshinone IIA production in P. nodositatum cultures. This is the first report using 5-azacytidine to improve tanshinone production in endophytic fungi. Our results confirm that 5-azacytidine is an efficient, easy, and quick chemical to felicitate secondary metabolite production in endophytic fungi. [ABSTRACT FROM AUTHOR]