Evaluation of the Anticancer Activity of Bioactive Fraction G Extracted from \u3cem\u3ePavetta crassipes\u3c/em\u3e in Malignant Brain Tumor Cell Lines

Objective: Natural products have served as sources of lead compounds that are commonly used in the treatment of human diseases including cancer. Pavetta crassipes has been widely demonstrated to have ethnopharmacological potential in the management of malaria, gastrointestinal conditions, central nervous system behavioral disorders, hypertension, and cancer. The goal of our study was to evaluate the biological and molecular effects of Fraction G, obtained from the plant Pavetta crassipes, on glioblastoma invasive growth and survival. Methodology: The antiproliferative effects of Fraction G, obtained from Pavetta crassipes, was evaluated using the trypan blue exclusion, (3-(4, 5-Dimethylthiazol- 2yl)-2, 5-Diphenyltetrazolium Bromide; MTT), and lactate dehydrogenase (LDH) assays. Flow cytometry and Western blotting analyses were carried out to examine the effects of Fraction G on cell cycle check-points and its effects on epidermal growth factor receptor-mediated signaling of AKT and MAPK pathways. Results: In this paper, we report that the Fraction G obtained from the plant Pavetta crassipes induced a reduction in glioma cell viability and proliferation as well as induced an increase in apoptosis as evidenced by cleaved PARP, increased caspase 3/7 activity, and cell cycle arrest in the G0/G1 check point. Furthermore, we report that Fraction G inhibited the phosphorylation of AKT and MAPK following EGF treatment. Conclusion: Taken together, our results demonstrate that Fraction G has potent inhibitory effects on pathways involved in glioblastoma proliferation and survival

Powder Compaction: Compression Properties of Cellulose Ethers

Effective development of matrix tablets requires a comprehensive understanding of different raw material attributes and their impact on process parameters. Cellulose ethers (CE) are the most commonly used pharmaceutical excipients in the fabrication of hydrophilic matrices. The innate good compression and binding properties of CE enable matrices to be prepared using economical direct compression (DC) techniques. However, DC is sensitive to raw material attributes, thus, impacting the compaction process. This article critically reviews prior knowledge on the mechanism of powder compaction and the compression properties of cellulose ethers, giving timely insight into new developments in this field

Synthesis, Physicochemical Characterization, And Functional Properties Of An Esterified Starch From An Underutilized Source In Nigeria

Acha ( Digitaria exilis Stapf), also known as Findi, Hungry rice, Petit mil and White fonio, is a small seeded cereal, indigenous to West Africa, which is generally classified as millet. It grows in various parts of Nigeria, Sierra Leone, Ghana, Guinea Bissau and Benin Republic. That species is the most important of a diverse group of wild and domesticated Digitaria species that are harvested in the savannas of West Africa. It is one of the primary cereals of southern Sudan and Ethiopia in Africa. It has potential to improve human nutrition, boost food security, foster rural development and support sustainable use of lands. In this study, acha starch was subjected to modification by acetylation. The acetylated acha starch with degree of modification 0.78 had reduced foaming capacity and amylose contents. The starches have similar organoleptic properties ranging from white, gritty, non sticky to bland tastes. Physicochemical indices investigated such as true density, bulk and tapped densities, water absorption capacity, moisture content, total and acid insoluble ash, and pH were reduced by the acetylation of acha starch. The modification resulted in a significant (P < 0.05) increase in the solubility as well as water and oil absorption capacities of the starch. Scanning electron microscopy revealed starch granules that were predominantly polygonal in shape. Acetylation did not alter the granule morphology. X-ray pattern of the native starch was A type, with similar pattern in the acetylated derivative. Fourier transform infrared spectroscopy (FTIR) results revealed a new band at 1728 cm-1. Thermogravimetry revealed 3 phase decomposition of both the native and modified starches. The acetylation as revealed by Differential scanning calorimetry studies improved the gelation capacity of the native starch and revealed two endothermic peaks and one exothermic peak each for both starches. There was considerable reduction in the peak temperature of gelatinization (Tp) of native starch and a significant (P<0.05) decrease in the enthalpy of gelatinization (DH) was noticed after acetylation

Smooth Muscle Contraction Induced by \u3cem\u3eIndigofera dendroides\u3c/em\u3e Leaf Extracts May Involve Calcium Mobilization via Potential Sensitive Channels

The contractile effects of the aqueous extract of the leaves of Indigofera dendroides (ID) were studied on the gastrointestinal motility in mice and isolated smooth muscle preparations obtained from rats and guinea pigs. The contractile effects of 10−6 M acetylcholine, 80 mM KCl and 1.6 mg/ml ID were measured on the rat ileal smooth muscle exposed to calcium-free buffer or physiological solution, to determine the calcium pools mobilized by extract for activation of contraction. Acute toxicity test (LD50) was also carried out in mice. The result showed that ID (0.05–3.2 mg/ml) produced a concentration-dependent contraction of the guinea pig and rat ileum. These responses were not blocked by mepyramine (2.49 × 10−9 M), verapamil (8.14 × 10−9 M), or pirenzepine (4.7 × 10−7 M), but were blocked completely by atropine (2.92 × 10−9 M). A signi.cant increase in propulsion of gastrointestinal motility was observed. Acetylcholine, KCl and ID produced contractions in Ca2+ free media. The phasic components of the contractile responses to Ach as well as the tonic component of K+ and ID-induced contractions were relatively resistant to short periods of calcium-free exposure. Ach, K+ and ID still caused contractions in the presence of verapamil. The data revealed that ID-induced contractions were not mediated by histaminergic receptors, calcium channels, M1 muscarinic receptors. It also suggests that Ach mobilize Ca from some tightly bound or intracellular pool, whereas high K+ and ID may mobilize Ca from some superficial or loosely-bound pool

Effect of the aqueous extract of African Mistletoe, <i>Tapinanthus sessilifolius</i> <span style="font-size:14.0pt;line-height:115%;font-family:"Times New Roman"; mso-fareast-font-family:"Times New Roman";color:black;mso-ansi-language:EN-IN; mso-fareast-language:EN-IN;mso-bidi-language:HI" lang="EN-IN">(P. Beauv) van Tiegh leaf on gastrointestinal muscle activity</span>

571-574<span style="font-size:14.0pt;line-height: 115%;font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" color:black;mso-ansi-language:en-in;mso-fareast-language:en-in;mso-bidi-language:="" hi"="" lang="EN-IN">Effects of the aqueous extract of T. sessilifolius on the gastrointestinal muscle were investigated on smooth muscle preparations isolated from rabbit jejunum, guinea pig ileum and on gastrointestinal transit in mice. Elemental analysis of the extract was also carried out. The aqueous extract of T. sessilifolius evoked a concentration dependent contraction of the rabbit jejunum and guinea pig ileum. The contractions evoked by the extract were not attenuated either by atropine or mepyramine, but they were completely blocked by verapamil. The elemental analysis revealed the presence of Mg, Zn, Fe,Cu, and very high concentration of Ca. The intraperitoneal LD50 in mice was found to be 1500 mg/kg. The aqueous extract of T. sessilifolius possesses active components that may be mediating the observed biological activity through calcium mobilization.</span

Poly-Electrophilic Sesquiterpene Lactones from Vernonia amygdalina: New Members and Differences in Their Mechanism of Thiol Trapping and in Bioactivity

In addition to known compounds, the leaves of Vernonia amygdalina afforded the new sesquiterpene lactones 14-O-methylvernolide (2), 3'-deoxyvernodalol (6), and vernomygdalin (8). These and related compounds were evaluated for modulation of a series of thiol trapping-sensitive transcription factors (NF-κB, STAT3, and Nrf2), involved in the maintenance of the chronic inflammatory condition typical of human degenerative diseases. Vernolide (1) emerged as a potent inhibitor of STAT3 and NF-κB and showed cytostatic activity toward the prostate cancer cell line DU45, arresting the cell cycle at the S phase. The exomethylene lactones are characterized by multiple Michael acceptor sites, as exemplified by vernolide (1) and vernodalol (5). By using the nuclear magnetic resonance-based cysteamine assay, the most reactive thiophilic site could be identified in both compounds, and competitive experiments qualified vernolide (1) as being more thiophilic than vernodalol (5), in agreement with the results of the pharmacological assays