Given the lack of adequate research on (Dioon spinulosum) Dyer Ex Eichler, this study was conducted focusing on different biological activities and phytochemical investigation of D. spinulosum for the first time. D. spinulosum showed strong protective activity against DNA damage and potent activity against VERO cell line. It also presented antimicrobial and hepatoprotective activity. Phytochemical investigation of the leaves resulted in isolation of two new flavonoids, apigenin 7-O-α-D-glucopyranoside (15) and amentoflavone 7-O-α-Lrhamnopyranoside (16) were isolated from Dioon spinulosum leaves in addition to fifteen known compounds: phytone (1), trans-phytol (2), β-sitosterol (3), stigmasterol (4), oliveriflavone (5), 7,4′,7″,4″′-tetramethylamentoflavone (6), 7,4',7''-trimethylamentoflavone (7), scaidopitysin (8), bilobetin (9), isoginkgetin (10), aromadendrin (11), sotusflavone (12), engeletin (14) and eriocitrin (17) for the first time together with amentoflavone (13). Compounds (11) and (13) displayed very strong cytotoxic activity and showed the highest protective activity against DNA damage.

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Toxoplasmosis and cancer are serious worldwide diseases, and the available drugs cause serious side effects. Investigation for new alternative therapies from natural sources is now an increasing concern. Herein, we carried out, for the first time, an in vitro screening of Cycas rumphii Miq. leaves for toxoplasmocidal effect, using Viruluent RH Toxoplasma gondii, and cytotoxic activity against HEPG-2, HCT-116 and HELA cancer cell lines using MTT assay. Among the tested extracts, the ethyl acetate fraction was the most effective against T. gondii, with an EC50 of 3.51 ± 0.2 µg/mL compared to cotrimoxazole (4.18 ± 0.01 µg/mL) and was the most potent against the tested cell lines, especially HEPG-2, with an IC50 of 6.98 ± 0.5 µg/mL compared to doxorubicin (4.50 ± 0.2 µg/mL). Seven compounds were isolated from the ethyl acetate fraction by extensive chromatographic techniques and fully elucidated using different spectroscopies. Compound (7) is an undescribed 4′, 4′′′ biapigenin di-C-glucoside, which showed a strong cytotoxic activity. Four known biflavonoids (1, 2, 4 and 5) in addition to a phenolic acid ester (3) and a flavonoid glycoside (6) were also isolated. Compounds (1, 3 and 6) were reported for the first time from C. rumphii.

Atropa belladonna L is most important commercial source of pharmaceutical tropane alkaloids. Initiation of callus culture on MS solid media with different concentrations of growth regulators as BA and 2,4 D from different explants shows that 2,4-D only at 1.0mg/L and 2.0mg/l gave the highest callus formation score after 21 days. The highest concentration of atropine (376.62 µg/g DW) and scopolamine (103.16 µg/g DW) were obtained from leaf callus on MS medium supplemented with 2,4 D at 0.5 mg/L after 28 days. The effect of elicitors and precursor feeding on tropane alkaloids production in callus culture were examined. Accumulation of both alkaloids; atropine and scopolamine in callus were enhanced after 8 days with jasmonic acid at concentrations (50 µM), after 15 days with yeast extract at concentrations (0.5 g/L) and after 21days with ornithine at 1mM in comparison with control callus. Salicylic acid inhibits callus growth and accumulation of atropine and scopolamine in treated callus.

Toxoplasmosis and cancer are life-threatening diseases with worldwide distribution. However, currently used chemosynthetic treatments are not devoid of their own intrinsic problems. Natural metabolites are gaining attention due to their lower side effects. In this study, we investigated for the first time Zamia floridana leaves extract and its different fractions for their toxoplasmocidal activity, using Virulent RH Toxoplasma gondii, and cytotoxic activity against MCF-7 and HCT-116 cancer cell lines using MTT assay. The n-butanol fraction was the most potent fraction against T. gondii with an EC50 of 7.16 ± 0.4 µg/mL compared to cotrimoxazole (4.18 ± 0.3 µg/mL). In addition, the n-BuOH fraction showed a significant cytotoxicity against MCF-7 and HCT-116 with IC50 of 12.33 ± 1.1 and 17.88 ± 1.4 µg/mL, respectively, compared to doxorubicin (4.17 ± 0.2 and 5.23 ± 0.3 µg/mL, respectively), with higher safety index against normal cell line (WISH). Therefore, the n-BuOH fraction was investigated for its phytochemicals using extensive chromatographic techniques, which led to the isolation of six compounds that were fully characterized using different spectroscopic techniques. Three biflavonoids (1, 2 and 4) in addition to two phenolic acid derivatives (3 and 5) and a flavonoid glycoside (6) were isolated. Compounds (1, 3, 5 and 6) were reported for the first time from Z. floridana. In silico docking studies for toxoplasmocidal and cytotoxic effects of these compounds revealed that compounds (1, 2, 4 and 6) have promising inhibition potential of either thymidylate synthase-dihydrofolate reductase (TS-DHFR) or cyclin dependent kinase 2 (CDK2) target proteins. This study is considered the first report of chemical and biological investigation of Z. floridana leaves.

The search for anticancer drugs is of continuous interest. Arecoline is an alkaloid with anticancer activity. Herein, the metabolism of arecoline through fungal transformation was investigated for the discovery of potential anticancer drugs with higher activity and selectivity. Compounds 1–5 were isolated, and their structures were fully elucidated using various spectroscopic analyses, including 1D and 2D NMR, ESIMS, and HRESIMS. This is the first report for the isolation of compounds 1 and 2. An MTT assay was performed to determine the cytotoxic activity of arecoline and its metabolites in vitro using non-small-cell lung cancer A549 and leukemia K562 cell lines compared to staurosporine and doxorubicin as positive controls. For the non-small-cell lung A549 cell line, arecoline hydrobromide, staurosporine, and doxorubicin resulted in IC50 values of 11.73 ± 0.71 µM, 10.47 ± 0.64 µM, and 5.05 ± 0.13 µM, respectively, while compounds 1, 3, and 5 exhibited IC50 values of 3.08 ± 0.19 µM, 7.33 ± 0.45 µM, and 3.29 ± 0.20 µM, respectively. For the leukemia K562 cell line, the IC50 values of arecoline hydrobromide, staurosporine, and doxorubicin were 15.3 ± 1.08 µM, 5.07 ± 0.36 µM, and 6.94 ± 0.21 µM, respectively, while the IC50 values of compounds 1, 3 and 5 were 1.56 ± 0.11 µM, 3.33 ± 0.24 µM, and 2.15 ± 0.15 µM, respectively. The selectivity index value of these compounds was higher than 3. These results indicated that compounds 1, 3, and 5 are very strong cytotoxic agents with higher activity than the positive controls and good selectivity toward the tested cancer cell lines. Cell cycle arrest was then studied by flow cytometry to investigate the apoptotic mechanism. Docking simulation revealed that most compounds possessed good binding poses and favorable protein-ligand interactions with muscarinic acetylcholine receptor M3-mAChR protein. In silico study of pharmacokinetics using SwissADME predicted compounds 1–5 to be drug-like with a high probability of good oral bioavailability.

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Background: Gymnosperms are naked seed-producing plants and still a dark area in scientific researches although they considered as a rare gift of the nature. Cycads are one of the largest groups of living Gymnosperms. The three extant families of Cycadales are Cycadaceae, Stangeriaceae, and Zamiaceae. According to review of literature, availability of the plants in Egypt, preliminary phytochemical screening of leaves of some plants of gymnosperms belong to Cycadals order, and the results of biological screening, six plants were chosen to be our target of this study. These plants were Cycas pectinata and Cycas thoursaii (Family Cycadacea), Dioon spinulosum, Dioon mejiae, Dioon merolae and Encephalartous laurantianous (Family Zamiaceae). Aim: The study has been classified into two parts: 1) Preliminary biological and phytochemical screening of leaves of the six plants. 2) Biological activities and phytochemical investigation of the leaves of Dioon spinulosum, the most active plant. Biological investigation of six plants belonging to Cycadals order cultivated in Egypt. Materials and Methods: Antioxidant activity was investigated using different methods: a) Bleomycin-dependent DNA damage, b) ABTS method, c) Assay for erythrocyte hemolysis. For antimicrobial activity, all the plants extracts were individually evaluated for in vitro antibacterial activity against Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis) and Gram-negative bacteria (Escherichia coli and Pseudomonas aeuroginosa). The anti-fungal activity was tested against two fungi (Candida albicans and Aspergillus flavus). For biological investigation of D. spinulosum leaves extract. Activity of D. spinulosum total methanol extract, pet-ether, methylene chloride, ethyl acetate and n-butanol fractions were investigated. For biological investigation of pure isolated compounds from D. spinulosum, nine compounds were subjected to further investigation for antioxidant and cytotoxic activities. Results: Dioon spinulosum showed significant activity among investigated compounds. Phytochemical investigation of D. spinulosum leaves resulted in isolation of two new flavonoids, apigenin 7-O-a-D-glucopyranoside and amentoflavone 7-O-α-L-rhamnopyranoside, in addition to fifteen known compounds: phytone, trans-phytol β-sitosterol, stigmasterol, oliveriflavone, 7,7 '',4',4''' tetra-O-methyl amentoflavone, 7,7'',4' tri-O-methyl amentoflavone, scaidopitysin, bilobetin, isoginkgetin, aromadendrin, sotusflavone, engeletin, and eriocitrin for the first time together with amentoflavone. Secondary metabolites isolated from D. spinulosum displayed the highest protective activity against DNA damage, higher than the positive control. A promising future may await D. spinulosum in drug discovery. Conclusion: Results from this study clearly demonstrated that D. spinulosum total methanol extract offered an evident for its improvement in the hepatocyte structural changes.