Inhibition Of Crown Gall Tumors Research Articles

Antitumor characterization of various fractions of Launaea procumbens

The antitumor activity of various six fractions of Launaea procumbens were studied using the potato disk bioassay technique. Three concentrations (10, 100, and 1000 ppm) of all these six fractions were used for characterization of antitumor activity. Among these fractions, methanolic fraction exhibited significant inhibition of crown gall tumors caused by Agrobacterium tumefaciens followed by butanolic fraction. These results revealed that methanolic and butanolic fractions contain bioactive constituents responsible for inhibition of tumor. Further purification and characterization are in progress in our laboratory.

Antioxidative and antitumor properties of in vitro-cultivated broccoli (Brassica oleracea var. italica)

Context: Broccoli [Brassica oleracea L. var. italica Plenck. (Brassicaceae)] contains substantial quantities of bioactive compounds, which are good free radical scavengers and thus might have strong antitumor properties. Enhancing production of plant secondary metabolites could be obtained with phytohormones that have significant effects on the metabolism of secondary metabolites. In that manner, in vitro culture presents good model for manipulation with plant tissues in order to affect secondary metabolite production and thus enhance bioactive properties of plants.Objective: Estimation of the antioxidative and antitumor properties of broccoli cultivated in different in vitro conditions.Materials and methods: In vitro germinated and cultivated broccoli seedlings, as well as spontaneously developed calli, were subjected to Soxhlet extraction. Antioxidative activity of the herbal extracts was determined using 1,1-diphenyl-2-picrylhydrazyl (DPPH•) radical method. Antitumor properties of the extracts were determined using crown-gall tumor inhibition (potato disc) assay.Results: Three, 10, 20, and 30 days old broccoli seedlings, cultivated in vitro on three different Murashige–Skoog media, two types of callus, and seedlings from sterile filter paper were used for extraction. In total, 15 aqueous extracts were tested for antioxidative and antitumor potential. Three day-old seedlings showed the highest antioxidative activity. Eleven out of 15 aqueous extracts demonstrated above 50% of crown-gall tumor inhibition in comparison with the control. Tumor inhibition was in association with types and concentrations of phytohormones presented in growing media.Discussion and conclusions: It is demonstrated that phytohormones in plant-growing media could affect the bioactive properties of broccoli either through increasing or decreasing their antioxidative and antitumor potential.

Structure elucidation and inhibitory effects of self-assembled organotin(IV) esters of p-tolyl acetic acid on bacterial, fungal, brine shrimp, and potato tumor cells

Biologically active new organotin(IV) acetates (1–6) of p-tolyl acetic acid have been synthesized and characterized by multinuclear nuclear magnetic resonance (1H, 13C) and mass spectrometry. The X-ray crystallographic data of compounds (3 and 4) were also collected. These studies show that in diorganotin(IV) compounds (compounds 1, 2, 3, and 6), tin exists in skew trapezoidal geometry with four strong and two weaker bonds, whereas triorganotin(IV) carboxylates (compounds 4 and 5) have four and five coordinated geometries in solution and solid form, respectively. These compounds were screened for a range of biological activities. Antibacterial activities were determined against six pathogenic bacterial strains, three Gram-positive and three Gram-negative; the activities were measured in terms of inhibition zones (mm). Antifungal activities were determined against six pathogenic fungal strains, cytotoxicity by the brine shrimp lethality assay, and antitumor activities by the crown gall tumor inhibition (potato disc) assay.

Evaluation of Antiaris africana methanol extract and compounds for antioxidant and antitumor activities

A methanol extract from the stem bark of Antiaris africana Engler (Moraceae), as well as compounds isolated and identified as betulinic acid (1), 3β-acetoxy-1β,11α-dihydroxy-olean-12-ene (2), ursolic acid (3), oleanolic acid (4), strophanthidol (5), periplogenin (6), convallatoxin (7), strophanthidinic acid (8), methyl strophanthinate (9), and 3,3′-dimethoxy-4′-O-β-d-xylopyronosylellagic acid (10), were tested for their antioxidant and anticancer activities. The DPPH radical scavenging assay was used for the antioxidant test while the potato disk tumor induction and XTT assays were used to detect antitumor activities. The antioxidant test showed that the methanol extract and compounds 1, 9, and 10, as well as vitamin C, used as reference antioxidant drug, were able to interact with more than 50% DPPH. The results of the potato disk tumor induction assay also indicated a pronounced tumor reducing activity of the methanol extract (83.12%) and compound 10 (96.64%). Samples showing more than 20% inhibition of Crown gall tumors were then tested against human DU-145 and hepatocarcinoma Hep G2 cells. The results showed inhibitory activities of 64.12% and 73.62%, respectively, on DU-145 and Hep G2 cells for the methanol extract. Compound 10 showed the highest inhibition potency on both cell lines with more than 70% inhibition at 50 μg/mL. The methanol extract showed an IC50 value lower than this at 30 μg/mL, a threshold value for potential antineoplastic extracts. The results of the present study provide supportive data for the traditional anticancer use of A. africana and indicate that the methanol extract as well as compound 10 represent a potential source of medicine for the treatment of cancer, having also interesting antioxidant properties.

Inhibition of crown-gall tumorigenesis with plant extracts

Measurement of the inhibition of crown-gall tumors on potato discs is an antitumor bioassay method for detection of anti-tumor compounds from higher plants. In this study, after surface sterilization, tuber discs were co-cultivated with Agrobacterium tumefaciens B6S3 for two days. The discs were then inoculated on MS media with the crude extracts obtained from different parts of various plants – Allium sativum L. (Liliaceae), Salvia verbenaca L., Rosmarinus officinalis L., Ocimum basiculum L., Lavandula stoechas L. (Lamiaceae), Althaea cannabina L. (Malvaceae), Petroselinum sativum Mill. (Apiaceae), Pelargonium radicula L. (Geraniaceaea), Juglans regia L. (Juglandaceae), Platanus orientalis L. (Platanaceae), Laurus nobilis L. (Lauraceae), Ranunculus ficaria L. (Ranunculaceae), and Abies equi-trojani Aschers. et Sint. Ex Boiss (Pinaceae). Tumors appeared after 10-15 days, and tumor inhibition was detected only in six plant extracts of 13 (A. sativum, R. officinalis, P. orientalis, L. nobilis, R. ficaria, and A. equi-trojani) when compared to control material. Constitutive tumor inhibition activities were higher in these plant extracts (63.5%, 56.1%, 61.7%, 54.6%, 69.7%, and 57.9% at 0 min; 58.8%, 54.6%, 58.8%, 48.4%, 62.6%, and 51.6% for 15 min after bacterial inoculation).

Synthesis and biological evaluations of some Schiff-base esters of ferrocenyl aniline and simple aniline

Abstract The synthesis and biological studies of some long chain esters containing Schiff bases and their ferrocenyl analogues were carried out. The 4-amino ferrocene was prepared by the reported method. Long chain esters were synthesized by the condensation of different aliphatic acids with the corresponding aldehyde. The esters were then reacted with aniline as well as with 4-aminophenyl ferrocene to give corresponding Schiff bases. All the synthesized compounds were analyzed by elemental, FTIR and proton NMR studies, were also investigated for a range of biological activities. Determined by crown gall tumor inhibition assay. Antioxidant and DNA protective activities were determined by DPPH free radical scavenging assay and OH radical induced oxidative DNA damage assay, respectively. Among all test compounds, o-hydroxy-p-n-octadecanoyloxy-benzylidine-p-ferrocenyl aniline (FA2.1: a ferrocene containing Schiff base) showed highest antitumor, DPPH free radical scavenging and DNA protective activities.

Di‐ and Triorganotin(IV) Esters of 3,4‐Methylenedioxyphenylpropenoic Acid: Synthesis, Spectroscopic Characterization and Biological Screening for Antimicrobial, Cytotoxic and Antitumor Activities

Nine biologically significant organotin(IV) esters of 3,4-Methylenedioxyphenylpropenoic acid (L) were synthesized with the general formulae [R2SnL2], where R includes Me(1), Et(3), But(4), Oct(5), Ph(8), and [R3SnL], in which R is Me(2), Cy(6), Ph(7), and But(9). The acid and its compounds were characterized by basic analytical techniques comprising elemental analysis, FTIR and mass spectrometry in solid state and by Multinuclear (1H, 13C and 119Sn) NMR in solution form, which provides some important information about the different coordination behaviors of metal in both solid and solution. Methylenedioxy moiety in these compounds enhances the biological activity of these compounds. These compounds were screened for a range of biological activities. Antibacterial activities were determined against six pathogenic bacterial strains, three gram-positive and three gram-negative, the activities were measured in terms of inhibition zones (mm). Results demonstrate that diorganotin derivatives are more active than triorganotin derivatives and ligand acid. Antifungal activity was determined against six pathogenic fungal strains, cytotoxicity by the brine shrimp lethality assay, and antitumor activity by crown gall tumor inhibition (potato disc) assay. Results for antifungal activity, cytotoxicity, and antitumor activity of these compounds demonstrate that triorganotin derivatives are more active than diorganotin derivatives and ligand. Finally, the results were compared with similar reports in the literature.

Synthesis, Chemical Characterization and Biological Screening for Cytotoxicity and Antitumor Activity of Organotin (IV) Derivatives of 3,4-Methylenedioxy 6-nitrophenylpropenoic Acid

A series of mono-, di- and triorganotin compounds with general formulae [RSnL(2)Cl], R = Bu (compound 3), [R(2)SnL(2)], where R = Me, Et, Bu, Oct (compounds 1, 2, 4 and 6) and [R(3)SnL], where R = Bu, Cy and Ph (compounds 5, 7 and 8) and where L = 3,4-methylenedioxy-6-nitrophenylpropenoic acid have been prepared and characterized by elemental analysis, multinuclear ((1)H-, (13)C- and (119)Sn-) NMR and mass spectrometry. The ligand and its respective organotin complexes were screened for cytotoxicity using the brine shrimp lethality assay and for antitumor activity using the crown gall tumor inhibition (potato disc) assay. The bioassay results support the conclusion that the biological activities of these synthetic compounds are in the following order: [RSnL(2)Cl] < [R(2)SnL(2)] < [R(3)SnL].

The colleflaccinosides, two chiral bianthraquinone glycosides with antitumor activity from the lichen Collema flaccidum collected in Israel and Russia

Colleflaccinosides A and B, two chiral bianthraquinone glycosides from the two geographical varieties of lichen Collema flaccidum collected in Russia and Israel have been isolated as new natural products. Their structures were elucidated using UV, CD, IR, MS, 1D and 2D NMR spectral data, and chemical degradation. The colleflaccinosides B had significant antitumor activity in the crown gall tumor inhibition test.

Lytophilippines A–C: novel macrolactones from the Red Sea hydroid Lytocarpus philippinus

Lytophilippines A–C, new chloro-containing macrolactones, were isolated from the Red Sea hydroid Lytocarpus philippinus and their structures were elucidated by IR, UV, MS, 1H and 13C NMR, and by chemical degradation. The compounds gave positive results in the crown gall tumor inhibition test and brine shrimp toxicity assay.

Cytotoxicity screening of some South American Solanaceae

Alcoholic extracts of seven plants belonging to the Solanaceae family were phytochemically screened and evaluated for their cytotoxic activity by Brine Shrimp Test (BST) with Artemia salina larvae, Inhibition of Cell Division Test (ICDT) on sea urchin Loxechinus albus fertilized eggs and inhibition of crown gall tumors on Potato Disk Bioassay (PDB). From Salpichroa diffusa, bioassay-guided chromatographic separation afforded some active fractions from which epi-katonic acid was identified.

Evaluation of antitumor activity of some medicinal plants of Bangladesh by potato disk bioassay

The antitumor activity of the ethanolic extracts of 12 medicinal plants of Bangladesh, including the vincristine–vinblastine producing Catharanthus roseus was studied using the potato disk bioassay technique. Among these, 10 plant extracts at 25.0-μg/disc exhibited significant inhibition of crown gall tumors caused by Agrobacterium tumefaciens.

Antitumor alkaloid from Glycosmis pentaphylla

Arborinine, an acridone alkaloid obtained from Glycosmis pentaphylla, exhibited significant inhibition of crown gall tumors produced by Agrobacterium tumefaciens in a potato disc bioassay.

The Use of Biological Assays to Evaluate Botanicals

The Department of Medicinal Chemistry and Molecular Pharmacology’s laboratory has adopted four “bench top” bioassays which do not require higher animals to screen and direct the fractionation of botanical extracts in drug discovery efforts. These are: 1. The brine shrimp lethality test (BST) (a general bioassay), 2. The inhibition of crown gall tumors on discs of potato tubers (an antitumor bioassay), 3. The inhibition of frond proliferation in duckweed (a bioassay for herbicides and plant growth stimulants), and 4. The yellow fever mosquito larvae lethality test (a bioassay for pesticides). The materials and procedures for those bioassays will be briefly described. The authors’ results in applying these simple methods in the discovery of Annonaceous acetogenins will be presented to illustrate their successful use. The BST is especially suggested as an inexpensive, simple, and rapid means of standardization of bioactivity in heterogeneous botanical products.

Five novel mono-tetrahydrofuran ring acetogenins from the seeds of Annona muricata.

Bioactivity-directed fractionation of the seeds of Annona muricata L. (Annonaceae) resulted in the isolation of five new compounds: cis-annonacin (1), cis-annonacin-10-one (2), cis-goniothalamicin (3), arianacin (4), and javoricin (5). Three of these (1-3) are among the first cis mono-tetrahydrofuran ring acetogenins to be reported. NMR analyses of published model synthetic compounds, prepared cyclized formal acetals, and prepared Mosher ester derivatives permitted the determinations of absolute stereochemistries. Bioassays of the pure compounds, in the brine shrimp test, for the inhibition of crown gall tumors, and in a panel of human solid tumor cell lines for cytotoxicity, evaluated relative potencies. Compound 1 was selectively cytotoxic to colon adenocarcinoma cells (HT-29) in which it was 10,000 times the potency of adriamycin.

Screening of Panamanian Medicinal Plants for Brine Shrimp Toxicity, Crown Gall Tumor Inhibition, Cytotoxicity and DNA Intercalation

ude extracts from 20 Panamanian plants used in traditional medicine have been screened for brine shrimp toxicity, tumor inhibition, DNA-intercalation and cytotoxicity tests in a clonogenic assay in V79 suspension culture gassed with air or nitrogen. Of the 20 plant extracts, 8 (40%) proved active in DNA intercalation. The most active were the methanol extracts of Bidens pilosa (root), Jatropha curcas (leaf), Pereskia bleo (whole plant), Isertia hypoleuca (leaf), Cyperus luzulae (root), Vernonia patens (leaf and stem), Alibertia edulis (stem) and Justicia graciliflora (aerial parts). Sixteen (80%) of the 20 methanol plant extracts were active in potato disc tumor inhibition assay; Cyperus luzulae (root), Justicia graciliflora (aerial parts), Pereskia bleo (whole plant) and Vernonia patens (leaf and stem) being the most active. Cytotoxicity in the clonogenic assay was observed only in three plant extracts: Cyperus luzulae, Piper auritum and Psychotria correae, whereas high brine shrimp toxicity (LC 50 &lt;100 p.p.m.) was observed in 13(65%) of the 20 plant extracts tested. These results appear to show a good correlation between the three bioassays: brine shrimp toxicity, tumor inhibition and DNA intercalation. The latter bioassay is rapid, economical, and can be used in activity guided fractionation of plant extracts.

Phytochemical and Biological Studies on Saudi Medicinal Plants Part 9. Antitumor Testing

Ethanol and/or the chloroform from chloroform: water partitioned ethanol extracts of 106 higher plant species growing in Saudi Arabia were examined in a series of in vitro and in vivo antitumor bioassays. Bioactivity in the form of 9KB or 9PS cytotoxicity, brine shrimp toxicity, toxicity to mice during 3PS testing, inhibition of crown gall tumors on potatoes, and for in vivo 3 PS antileukemic effects was detected in over 25 species which now are candidates for future bioactivity-directed fractionations. The results are presented in tabular form alphabetically by plant families.