Phytochemical Screening and in vitro Anticancer Activity of Some Medicinal Plants Grown in the Kingdom of Saudi Arabia

SUMMARY: This study evaluated the phytochemical screening, antioxidant capacity, and in vitro anticancer activities of four plants namely, Gypsophila capillaris, Anabasis lachnantha, Haloxylon salicornicum, and Horwoodia dicksoniae which belong to four different families: Caryophyllaceae, Amaranthaceae, Chenopodiaceae, Brassicaceae, respectively. The total phenolics, anthocyanins, saponins, total antioxidant capacity (TAC), and DPPH assays were determined by spectrophotometer. In vitro anticancer activity was assessed using two human cancer cell lines; hepatocellular carcinoma (HepG-2) and breast adenocarcinoma (MCF-7) to estimate the inhibition concentration 50 % (IC50). The results showed that H. dicksoniae has the highest concentrations of phenolics and saponins, while H. salicornicum has the highest DPPH. The highest concentration of TAC was found in G. capillaries. Among the tested extracts, G. capillaries and H. salicornicum have the potential activity against MCF-7 and HepG-2 cell lines in vitro. The content of polyphenols in G. capillaries was profiled by high-performance liquid chromatography (HPLC). The highest concentration among the phenolic compounds was chlorogenic (60.8 µg/ml) while the highest concentration among the flavonoid compounds was hesperidin (1444.92 µg/ml). In summary, G. capillaries and H. salicornicum extracts have potent anticancer activity against HepG-2 and MCF-7 cell lines.

Este estudio evaluó la detección fitoquímica, la capacidad antioxidante y las actividades anticancerígenas in vitro de cuatro plantas, Gypsophila capillaris, Anabasis lachnantha, Haloxylon salicornicum y Horwoodia dicksoniae, que pertenecen a cuatro familias diferentes: Caryophyllaceae, Amaranthaceae, Chenopodiaceae y Brassicaceae, respectivamente. Los ensayos de fenólicos totales, antocianinas, saponinas, capacidad antioxidante total (TAC) y DPPH se determinaron mediante espectrofotómetro. La actividad anticancerígena in vitro se evaluó utilizando dos líneas celulares de cáncer humano; carcinoma hepatocelular (HepG-2) y adenocarcinoma de mama (MCF- 7) para estimar la concentración de inhibición del 50 % (IC50). Los resultados indicaron que H. dicksoniae tiene las concentraciones más altas de fenólicos y saponinas, mientras que H. salicornicum tiene el DPPH más alto. La mayor concentración de TAC se encontró en G. capillaries. Entre los extractos probados, G. capillaries y H. salicornicum tienen actividad potencial contra líneas celulares MCF-7 y HepG-2 in vitro. El contenido de polifenoles en G. capillaries se perfiló mediante cromatografía líquida de alta resolución (HPLC). La concentración más alta entre los compuestos fenólicos fue clorogénica (60,8 µg/ml), mientras que la concentración más alta entre los compuestos flavonoides fue la hesperidina (1444,92 µg/ml). En resumen, los extractos de Gypsophila capillaris y H. salicornicum tienen una potente actividad anticancerígena contra las líneas celulares HepG-2 y MCF-7.

Fingerprinting of strong spermatogenesis steroidal saponins in male flowers of Phoenix dactylifera (Date Palm) by LC-ESI-MS.

A fingerprint of steroid saponins, the major constituent in 80% methanolic fraction from the male flowers of Phoenix dactylifera has been established. Under ESI-MS/MS conditions, the fragmentation patterns of [M - H]- ions exclusively displayed signals corresponding to the cleavage of the glycosidic bonds, thus allowing a rapid identification of 21 steroidal saponins. Moreover, two unique among them conjugated with histidine were detected by LC-ESI (-)-MS and DFT and were given tentative names of 3-o-histidine-26-o-hexosyl-dioscin and 3-o-histidine-26-o-dihexosyl-hydroxydioscin. Their steroidal saponins exhibited a significant improvement of the sperm cells count, motility and viability in male rats. These effects could be attributed to enhancing the levels of sex hormones.

Phenolic Compounds from the Fruits of Medemia argun, a Food and Medicinal Plant of Ancient Egypt.

Medemia argun is a mysterious and little known monotypic fan palm from the Nubian Desert Oases of southern Egypt and northern Sudan. Its fruits have been found in the tombs from the 5th Dynasty (ca. 2500 BC) to Roman times (6-7th century AD), including the celebrated tomb of Tutankhamun. In ancient Egypt, the fruits of this palm were widely distributed and were highly valued, as confirmed by their frequent occurrence in offerings in the tombs. In order to elucidate the chemical composition of the phenolic fraction, phytochemical investigation of the BuOH extract of fruits was carried out to afford eight compounds (1-8), among which was the new 2,4-dihydroxy-6-methylacetophenone 2-0-ß-D-glucopyranoside (1). With the aim to investigate if the high shelf life of M argun fruits could be related to the occurrence of antioxidant principles that were able to prevent oxidative reactions, the evaluation was carried out of the in vitro antioxidant activity by Trolox equivalent antioxidant capacity (TEAC) assay of the extract and isolated compounds.

Microbial biotransformation as a tool for drug development based on natural products from mevalonic acid pathway: A review.

Natural products are structurally and biologically interesting metabolites, but they have been isolated in minute amounts. The syntheses of such natural products help in obtaining them in bulk amounts. The recognition of microbial biotransformation as important manufacturing tool has increased in chemical and pharmaceutical industries. In recent years, microbial transformation is increasing significantly from limited interest into highly active area in green chemistry including preparation of pharmaceutical products. This is the first review published on the usage of microbial biocatalysts for some natural product classes and natural product drugs.

Unusual fernane and gammacerane glycosides from the aerial parts of Spergula fallax.

The aerial parts of Spergula fallax afforded four glycosides (1-4) based on two new triterpene aglycones (1a and 2a), along with the known hopane glycoside succulentoside A. Compound 1 was identified as belonging to the fernane class, unusual migrated hopane triterpenoids, mainly isolated from ferns and only rarely from higher plants. Compounds 2-4 were assigned as gammacerane glycosides, having as aglycone a hydroxylated derivative of tetrahymanol. The structures of the isolated compounds 1-4 and their aglycones 1a and 2a obtained by acid hydrolysis were elucidated by spectroscopic data interpretation. The growth inhibitory activity of the isolated compounds and their aglycones was evaluated against the HeLa and DLD-1 cancer cell lines.

Profiles of steroidal saponins from the aerial parts of Tribulus pentandrus, T. megistopterus subsp. pterocarpus and T. parvispinus by LC-ESI-MS/MS.

INTRODUCTION: Tribulus is a well-known pharmaceutical herb that has been used for a long time in the traditional Chinese and Indian systems of medicine for the treatment of various diseases. It has been found that the genus Tribulus is rich in biologically active furostane-, cholestane- and spirostane-type steroidal saponins. OBJECTIVE: To develop a rapid, sensitive and accurate method based on liquid-phase extraction followed by high-performance liquid chromatography and electrospray ionisation mass spectrometry (HPLC-ESI-MS) to identify different saponins in three species of the genus Tribulus, and to quantify the compounds that are already known. METHODOLOGY: After extraction from the species studied, the extracts were subjected to HPLC analyses with an XTerra® MS C(18) -column and a binary mobile phase consisting of 0.05% formic acid in water and acetonitrile, and with an ESI-MS detection in the negative ion mode. Data were acquired and processed using the Xcalibur 1.3 software. RESULTS: The results exhibited that the profiles of native steroidal glycosides of both T. pentandrus and T. megistopterus subsp. pterocarpus were very similar to each other, but that of T. parvispinus was remarkably different. The fragmentation patterns provided evidence that the saponins possess spirostane-, cholestane- and furostane-type aglycones. Quantitative analyses suggested that these species are a rich source of steroidal saponins. CONCLUSION: HPLC-ESI-MS/MS allowed identification of the key compounds without preparative isolation of the components from the crude extract of Tribulus species.

Antifungal effects of Ficus sycomorus and Pergularia tomentosa aqueous extracts on some organs in Bufo regularis treated with Aspergillus niger.

The antifungal efficacy of Ficus sycomorus and Pergularia tomentosa plant extracts on Bufo regularis experimentally infected with Aspergillus niger was studied. After an oral administration of the pathogen for 15 days, the blood, kidney and liver were examined. Treatment with A. niger produced a reduction in red blood count cells and hemoglobin content. Also, both livers and kidneys revealed marked destruction and degenerative changes. These changes included congestion of blood vessels, leukocytic infiltration, and cytoplasmic vacuolization of the hepatocytes. As well as complete destruction of the cellular boundaries of the tubular epithelia, inflammatory leukocytes between the intertubular spaces, destruction and necrosis in renal tubule cells and the swollen glomeruli with wide glomerular spaces were seen. Pretreatment with F. sycomorus and P. tomentosa plant extracts 1h prior the administration of A. niger for two weeks improved blood parameters and protected against hepatic and renal damage as observed from histological examination and reduced spore numbers in culture media on these organs.

Strong antioxidant phenolics from Acacia nilotica: profiling by ESI-MS and qualitative-quantitative determination by LC-ESI-MS.

Acacia nilotica (L.) Del. syn is a species rich in polyphenolic constituents, in which catechins are hypothesized to possess antioxidant properties and to play a role in the anti-inflammatory activity of several plants. Due to the complexity of catechin derivatives, the investigation of this class of natural compounds has been limited by difficulties in their separation. In this paper, rationalization of the phenolics occurring in the 80% EtOH extract of Acacia nilotica pods, on the basis of ESI-MS and ESI-MS/MS profiles, has been proposed. Additionally, an LC-ESI-MS qualitative study has been performed by using a C18 polar endcapped stationary phase. The fragmentation pattern obtained evidenced the presence in A. nilotica pods of galloylated catechin- and gallocatechin derivatives along with galloylated glucose derivatives. The structures were confirmed by NMR, after isolation of the pure compounds. In addition, the radical scavenging activities of extracts and pure compounds were investigated, by using the TEAC assay. Furthermore quantitative analyses were performed by LC-ESI-MS/MS, confirming the interest of this species as a rich source of very strong antioxidant principles.

Cardenolide glycosides from Pergularia tomentosa and their proapoptotic activity in Kaposi's sarcoma cells.

Continuing our investigations on plants belonging to the Asclepiadaceae family, three new cardenolide glycosides, 3'-O-beta-D-glucopyranosylcalactin (1), 12-dehydroxyghalakinoside (2), and 6'-dehydroxyghalakinoside (3), along with the known ghalakinoside (4) and calactin (5), were isolated from the roots of Pergularia tomentosa. The structures of these compounds were elucidated by extensive spectroscopic methods including 1D- and 2D-NMR experiments as well as ESIMS analysis. The isolated cardenolides caused apoptotic cell death of Kaposi's sarcoma cells.