Phenolic Compounds from the Natural Sources and Their Cytotoxicity

Natural phenolic compounds are considered as one of the important secondary metabolites for their chemopreventive and chemotherapeutic effects in cancer. These compounds show potent activities for cancer prevention and its treatment. There are many phenolic compounds present in medicinal and edible plants such as, flavonoids, bioflavonoids, stilbenes, chalconoids, chromones, phenylpropanoids, curcuminoids, coumarins, tannins, lignans, neolignans, anthraquinones, quinones, xanthones, phenolic acids and their glycosides and many more. The antioxidant potential of phenolic compounds is almost bolded in the treatment and prevention of cancer. Mono phenolic, polyphenolic and phenolic acids compounds from a large variety of plants, foods, spices, insects, fungus, beverages, lichens, algae and mammals have been shown to inhibit or attenuate the initiation, progression and spread of cancers in cells in vitro and in animals in vivo. In this chapter, we try to cover general view and the recent literature to summarize structural information and cytotoxic effects of phenolic compounds on different cancer cell lines from medicinal herbs and plants

Green Chemistry and Synthesis of Anticancer Molecule

Green chemistry is a modern area of chemistry merged with chemical engineering methods. It highlighted the synthesis of molecules in a manner of using environment-friendly chemical reagents with low waste material for enhancing environmental performance which reduce the formation of hazard substances. Modern researches are trying to reduce the risk of human kind health and the environment of our world by doing magnificent work in the field of green chemistry. In the pharmaceutical field, green chemistry works very well with the formation of many drugs and it utilizes non-hazards, reproducible and environment-friendly solvents with low time and money costs by using catalyst, microwave, ultrasonic, solid phase and solvent-free synthesis. Until now, scientist has synthesized many anticancer molecules by using these modern green chemistry techniques. These compounds showed significant anticancer activities against many human cancer cell lines. In this chapter, we will cover different views and the recently published literature to summarize the role of green chemistry in the synthesis of anticancer compounds

Evaluation of Antiulcer and Cytotoxic Potential of the Leaf, Flower, and Fruit Extracts of Calotropis procera

Calotropis procera is traditionally used for treating many diseases including ulcers and tumors. It was thus deemed of interest to investigate and compare the antiulcer and cytotoxic activities of C. procera leaf, flower, and fruit extracts in an attempt to verify its traditional uses. Phytochemical studies on the fruits, flowers, and leaves of C. procera, collected from the desert of Saudi Arabia, led to the isolation of one new lignan 7′-methoxy-3′-O-demethyl-tanegool-9-O-β-D-glucopyranoside and five known compounds from the flowers, four compounds from leaves, and a flavonoid glycoside and a lignan glycoside from the fruits. The structures of compounds were determined by spectroscopic techniques. Ethanol extracts of the three parts of C. procera were evaluated for their antiulcer activity and we found that the leaf extract possessed a powerful antiulcer activity which could be considered as a promising drug candidate. All the extracts and the isolated compounds were evaluated for their cytotoxic activity against MCF-7, HCT-116, HepG-2, and A-549 human cancer cell lines. Compound 2 was highly active on all the cell lines, whereas compounds 5 and 11 were more selective on colon and liver cell lines. Compound 10 demonstrated a significant activity on liver and lung cancer cell lines

Pharmacological Evaluation of Secondary Metabolites and Their Simultaneous Determination in the Arabian Medicinal Plant Plicosepalus curviflorus Using HPTLC Validated Method

© The Author(s) 2019. The present study aimed to identify biologically active secondary metabolites from the rare plant species, Pulsatilla patens subsp. patens and the cultivated P. vulgaris subsp. vulgaris. Chromatographic fractionation of the ethanolic extract of the roots of P. patens subsp. patens resulted in the isolation of two oleanane-type glycosides identified as hederagenin 3-O-β-d-glucopyranoside (2.7 mg) and hederagenin 3-O-β-d-galactopyranosyl-(1→2)-β-d-glucopyranoside (3.3 mg, patensin). HPLC analysis of the methanolic extract of the crude root of P. patens subsp. patens and P. vulgaris subsp. vulgaris revealed the presence of Pulsatilla saponin D (hederagenin 3-O-α-l-rhamnopyranosyl(1→2)-[β-d-glucopyranosyl(1→4)]-α-l-arabinopyranoside). Chromatographic analysis using GC-MS of the silylated methanolic extracts from the leaves and roots of these species identified the presence of carboxylic acids, such as benzoic, caffeic, malic, and succinic acids. The extracts from Pulsatilla species were tested for their antifungal, antimicrobial, and antimalarial activities, and cytotoxicity to mammalian cell lines. Both P. patens subsp. patens and P. vulgaris subsp. vulgaris were active against the fungus Candida glabrata with the half-maximal inhibitory concentration (IC 50 ) values of 9.37 µg/mL and 11 µg/mL, respectively. The IC 50 values for cytotoxicity evaluation were in the range of 32–38 μg/mL for P. patens subsp. patens and 35–57 μg/mL for P. vulgaris subsp. vulgaris for each cell line, indicating general cytotoxic activity throughout the panel of evaluated cancer and noncancer cells

Bioactivity and chemical characterization of Acalypha fruticosa Forssk. growing in Saudi Arabia

Acalypha is an important genus of the Euphorbiaceae family. The genus is represented by five species in Saudi Arabia. Acalypha fruticosa Forssk. Fl. Aeg is traditionally used as a cure for stomachache, dyspepsia, rheumatism, dermatitis, and swellings of the body. The present study endeavors to provide a phytochemical and biological evaluation of the plant, with the aim of relating activity to constituting secondary metabolites in the plant. Column chromatographic separation of the methanol extract led to the isolation of four compounds namely 2-methyl-5,7-dihydroxychromone 5-O-β-d-glucopyranoside 1, acalyphin 2, apigenin 3 and kaempferol 3-O-rutinoside 4. The plant extracts and the isolated compounds were subjected to biological assays to screen peroxisome proliferator-activated receptor alpha (PPARα) and PPARγ agonistic, anti-inflammatory and cytotoxic activities. Results proved for the first time, the PPARγ activator effect of acalyphin, as well as its promising anti-inflammatory activity, in addition to the dual PPAR activator effect of the chromone glucoside. The plant extracts and isolated compounds were non-cytotoxic to the tested cell lines. Thus A. fruticosa could be a valuable source of important therapeutics that may hold clinical prospect

Antimicrobial guaianolide sesquiterpenoids from leaves of the Saudi Arabian plant Anvillea garcinii

Anvillea garcinii is a medicinal plant used in the Arab region for intestinal diseases, lungs and liver diseases, digestive problems, and as an anti-diabetic. Repeated chromatographic purifications of A. garcinii leaves led to the isolation of two undescribed guaiane sesquiterpene lactones (1–2), along with four known germacranolides (3–6). The structures of the new compounds were established using spectroscopic (1D, 2D NMR) and spectrometric methods (ESIMS). Compounds 1 and 2 were shown to possess hydroxyl substituents at position 9, a structural feature rarely reported in guaianolide-type sesquiterpenes. The antimicrobial activity of 1–6 was screened against five different gram-positive/negative bacteria and the fungi Candida albicans and C. parapsilosis. Compounds 1 and 2 displayed remarkable antifungal effect against C. albicans and C. parapsilosis and potent antibacterial activities against Staphylococcus aureus

Antiulcer Activity of Different Extracts of Anvillea garcinii and Isolation of Two New Secondary Metabolites

Anvillea garcini

Bioactive Phenolic Amides from Celtis africana

Nine compounds have been isolated for the first time from Celtis africana, namely trans-N-coumaroyltyramine (1), trans-N-feruloyltyramine (2), trans-N-caffeoyltyramine (3), lauric acid (4), oleic acid (5), palmitic acid (6), lupeol (7), β-sitosterol (8) and oleanolic acid (9), respectively. Their structures have been elucidated by different spectroscopic techniques. The isolated compounds were screened for their antioxidant, anti-inflammatory and acetylcholinestrease enzyme inhibitory activities. Compounds 1–3 showed significant antioxidant and anti-inflammatory activities and weak to moderate acetylcholinestrease enzyme inhibition activity