Light and electron microscopic studies on the Y organ of the freshwater crab Travancoriana schirnerae

AbstractThe fine structure of the premoult Y organ in the freshwater crab Travancoriana schirnerae revealed elliptical epithelial gland cells with large, eccentric, multinucleolated nuclei and ample cytoplasm. The cytoplasm showed numerous polymorphic mitochondria with tubular cristae, highly anastomosed tubules and vesicles of smooth endoplasmic reticulum (SER), rich free ribosomes, small amounts of cisternae of rough endoplasmic reticulum (RER), microtubules and was devoid of Golgi complexes. Mitochondria were of two types the more abundant micromitochondria with electron dense matrix and the less abundant macromitochondria with moderately dense matrix. The tubular SER was particularly concentrated towards the basal region of the cell, intermingled with mitochondria and dense patches of free ribosomes while the vesicular SER lie close to the lateral plasma membrane. Large vesicles with flocculent substances, a few electron dense granules and multivesicular bodies could also be noticed in the gland cell cytoplasm. Aggregations of microvesicles which appeared close to the lateral plasma membrane, in association with dilated SER cisternae and microtubules, possibly suggest the intercellular exchange of substances. The plasma membrane beneath the basal lamina was composed of invaginations and the apical surface possessed numerous microvilli which serve to increase the surface area for metabolic exchange. Towards the apical region, the lateral plasma membrane of adjacent cells was linked by tight junctions. The presence of extraordinarily abundant tubular SER, high proportion of mitochondria with tubular cristae and rich free ribosomes could well be elucidated in favour of steroid production by the gland cells

Virtual screening and in vitro assay of potential drug like inhibitors from spices against Glutathione-S-Transferase of Meloidogyne incognita

Glutathione S-transferases (GSTs) enzymes are critical antioxidant and detoxification system responsible for long-term existence of nematodes in host species. Hence, 16 phytochemicals predicted and reported to have potential nematicidal activity have been docked to GST enzyme of Meloidogyne incognita to assess their binding affinity and inhibitory activity. In vitro effects of these phytochemicals from in silico results have been done for validation of docking studies and efficacy in GST inhibition of following compounds such as alpha- pinene, alpha- terpineol, beta- caryophyllene, capsaicin, cinnamic acid, citronellol, curcumin, eugenol, geraniol, isoeugenol, linalool, myristicin, neral, NVA (N-vanillylnonanamide), piperine, vanillin have been revealed. Nematode inhibition in vitro bioassay for selected compounds could conclude that maximum mortality was observed with highest concentrations of beta- caryophyllene (78%) followed by eugenol (61.6%), cinnamic acid (55%) and N-vanillylnonanamide (49%). These findings thus suggest that the above phytochemicals could be potentially developed as nematicidal molecules against M. incognita infections

Anti-Arthritic Potential of the Plant Justicia Gendarussa Burm F

OBJECTIVE: To evaluate the anti-arthritic potential of the plant Justicia gendarussa using two different rat models. MATERIALS AND METHOD: The anti-arthritic potential of the alcoholic extract of the plant Justicia gendarussa was evaluated using the Freund's adjuvant-induced and collagen-induced arthritic rat models. The rats were treated with the ethanolic extract of Justicia gendarussa and with standard aspirin. RESULTS: The ethanolic extract of Justicia gendarussa showed significant anti-arthritic activity that was statistically similar to that of aspirin. Our results suggest that the alcoholic extract of Justicia gendarussa exhibits significant anti-arthritic potential

Selected novel 5'-amino-2'-hydroxy-1,3-diaryl-2-propen-1-ones arrest cell cycle of HCT-116 in G0/G1 phase

A series of 5’-amino-2’-hydroxy-1,3-diaryl-2-propen-1-ones (AC1-AC15) were synthesized by Claisen-Schmidt condensation of 5'-acetamido-2’-hydroxy acetophenone with various substituted aromatic aldehydes. The synthesized compounds were characterized by FTIR, 1H NMR and mass spectrometry and evaluated for their selective cytotoxicity using MTT assay on two cancer cell lines namely breast cancer cell line (MCF-7), colon cancer cell line (HCT-116) and one normal kidney epithelial cell line (Vero). Among the tested compounds, AC-10 showed maximum cytotoxic effect on MCF-7 cell line with IC50 value 74.7 ± 3.5 μM. On HCT-116 cells, AC-13 exhibited maximum cytotoxicity with IC50 value 42.1 ± 4.0 μM followed by AC-14 and AC-10 with IC50 values 62 ± 2.3 μM and 95.4 ± 1.7 μM respectively. All tested compounds were found to be safe on Vero cell line with IC50 value more than 200 μM. Based on their highest efficacy on HCT-116, AC-10, AC-13 and AC-14 were selected for mechanistic study on this cell line by evaluating changes nucleomorphological characteristics using acridine orange-ethidium bromide (AOEB) dual stain and by analyzing cell cycle with flow cytometry using propidium iodide stain. In AOEB staining, all three tested compounds showed significant (p < 0.05) increase in percentage apoptotic nuclei compared to control cells, with highest increase in apoptotic nuclei by AC-13 treatment (31 %). Flow cytometric studies showed cell cycle arrest by AC-10 and AC-14 treatment in G0/G1 phase and by AC-13 in G0/G1 and G2/M phase. The study reflected the potential of AC-10, AC-13 and AC-14 to be the lead molecules for further optimization

Poly-lactic acid nanoparticles (PLA-NP) promote physiological modifications in lung epithelial cells and are internalized by clathrin-coated pits and lipid rafts

BackgroundPoly-lactic acid nanoparticles (PLA-NP) are a type of polymeric NP, frequently used as nanomedicines, which have advantages over metallic NP such as the ability to maintain therapeutic drug levels for sustained periods of time. Despite PLA-NP being considered biocompatible, data concerning alterations in cellular physiology are scarce.MethodsWe conducted an extensive evaluation of PLA-NP biocompatibility in human lung epithelial A549 cells using high throughput screening and more complex methodologies. These included measurements of cytotoxicity, cell viability, immunomodulatory potential, and effects upon the cells’ proteome. We used non- and green-fluorescent PLA-NP with 63 and 66 nm diameters, respectively. Cells were exposed with concentrations of 2, 20, 100 and 200 µg/mL, for 24, 48 and 72 h, in most experiments. Moreover, possible endocytic mechanisms of internalization of PLA-NP were investigated, such as those involving caveolae, lipid rafts, macropinocytosis and clathrin-coated pits.ResultsCell viability and proliferation were not altered in response to PLA-NP. Multiplex analysis of secreted mediators revealed a low-level reduction of IL-12p70 and vascular epidermal growth factor (VEGF) in response to PLA-NP, while all other mediators assessed were unaffected. However, changes to the cells’ proteome were observed in response to PLA-NP, and, additionally, the cellular stress marker miR155 was found to reduce. In dual exposures of staurosporine (STS) with PLA-NP, PLA-NP enhanced susceptibility to STS-induced cell death. Finally, PLA-NP were rapidly internalized in association with clathrin-coated pits, and, to a lesser extent, with lipid rafts.ConclusionsThese data demonstrate that PLA-NP are internalized and, in general, tolerated by A549 cells, with no cytotoxicity and no secretion of pro-inflammatory mediators. However, PLA-NP exposure may induce modification of biological functions of A549 cells, which should be considered when designing drug delivery systems. Moreover, the pathways of PLA-NP internalization we detected could contribute to the improvement of selective uptake strategies

Caesalpinia sappan – A medicinal and dye yielding plant

75-82Natural products have provided a variety of lead structures, which serve as templates for the development of new drugs. The water kept in Caesalpinia sappan Linn. (Sappan lignum) heartwood is being used in Kerala as herbal drinking water for its antithirst, blood purifying, antidiabetic, improvement of complexion and several other properties. The plant is also being used worldwide for a large number of traditional medicinal purposes. Modern day research confirms its cytotoxic, antitumor, antimicrobial, antiviral, immunostimulant and several other activities. Several triterpenoids, flavonoids, oxygen heterocycles, etc. were isolated. Brazilin is found to be the main constituent of the plant responsible for several of its biological activities. The use of heartwood as a colouring agent for wine, meat, fabric, etc. is well established. It has the potential to hit the market as a safe natural colouring agent with good medicinal value for food products, beverages and pharmaceuticals. There is also a scope for further research to establish its medicinal properties and to identify lead compounds for drug development