INVITRO CYTO TOXICITY OF TRICHODESMA INDIUM LINN.R.BR., EXTRACTS AGAINST THREE HUMAN CANCER CELL LINES.

         Objective:Trichodesma Indicum Linn.R.Br. of Boraginaceae family was traditionally used as an anticancer plant material. The present study was aimed to evaluate the cytotoxic activity of the plant against three human cancer cell lines-Breast cancer cell line (MCF-7), Cervical cancer cell line (HeLa) and laryngeal epithelial carcinoma cell line(HEp2),since  a few clinical trials are needed to confirm its anticancer activity.Method: The chloroform& ethanol extracts of the plant were used for in-vitro screening. The cytotoxic effect of the plant was analysed by MTT assay.Results: The results obtained are statistically analysed by one way analysis of Variance(ANOVA)and it was found  that the ethanol extract has stronger cytotoxic activity than chloroform extract against all the tested cell lines. However higher degree of cyto toxicity was found to be in ethanol extract against human breast cell line (MCF-7) (IC50 57.41µg/ml).Conclusion: The traditional use of the plant material as anticancer was correlated with its invitro cyto toxicity results. The plant has a remarkable cytotoxic activity against the tested cancer cell lines.Keywords: Boraginaceae, Cytotoxic activity, IC50 value, MTT assay, Trichodesma Indicu

The essential oil constituents of Artabotrys species – A review

Artabotrys species which belongs to Annonaceae family are pleasant smelling and it is attributed to the presence of mono and sesquiterpenoids present in the essential oil of the plant. The objective of the present work is to review the chemical composition of the essential oils reported from twenty different Artabotrys species from various parts of the world. In the various Artabotrys species, the major compounds are monoterpene and sesquiterpene hydrocarbons and oxygenated sesquiterpenes.  The frequently and most commonly identified constituents are β-caryophyllene, caryophyllene oxide, 3-Carene, cyperene, cyperenone and 1,5-epoxy-salvial4(14)-ene.  Other constituents seems to be more specific to the respective Artabotrys species

Priprema, karakterizacija i in vitro procjena toksičnosti micela s kapsantinom na modelu stanične linije karcinoma dojke MDA-MB-231

Research background. Breast cancer is one of the most common cancers and remains a major cause of morbidity and mortality among women worldwide. In developed countries, breast cancer as a multifactorial disease is a major health concern, and its incidence is constantly rising in low and middle-income countries. Numerous studies have demonstrated that phytochemicals such as carotenoids inhibit breast cancer growth and induce apoptosis. We recently enhanced the solubility of capsanthin in water by encapsulating it in diosgenin polyethylene glycol succinate, a novel non-ionic surfactant. Thus, this study aims to evaluate the cytotoxicity of water-soluble capsanthin-loaded micelles in MDA-MB-231 cells in vitro through tetrazolium dye MTT assay. Experimental approach. In the current study, capsanthin, a hydrophobic carotenoid, is extracted from sweet red pepper (Capsicum annuum). Capsanthin-loaded diosgenin polyethylene glycol succinate 1000 (cap-DPGS-1000) micelles were prepared from capsanthin extract (cap) and diosgenin polyethylene glycol succinate 1000 (DPGS-1000) using the solid dispersion method. The capsanthin extract and cap-DPGS-1000 micelles were characterized by UV-visible spectroscopy, high-performance liquid chromatography (HPLC), Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), particle size distribution, polydispersity, and scanning electron microscopy (SEM). The effects of capsanthin extract and cap-DPGS-1000 micelles on a human triple-negative breast cancer cell line (MDA-MB-231) were tested to check the cell viability, proliferation and cytotoxicity of the micelles. Results and conclusions. The solubility of encapsulated cap-DPGS-1000 micelles in water is greatly enhanced and leads to an increased scope for localized drug delivery, a better delivery option for treating residual cancerous tumours. The encapsulated capsanthin showed a sustained release in simulated intestinal fluid (pH=6.8). Our research proposes a sustained drug delivery system that ensures effective and controlled release to the affected site. The characterization data revealed no change in the structure and functional groups in the encapsulated capsanthin. The IC50 value of the cap-DPGS-1000 micelles against MDA-MB-231 breast cancer cells was (3.10±1.09) μg/mL, which is much lower than of capsanthin extract ((81.1±1.5) μg/mL). Capsanthin extract and capsanthin-loaded micelles are promising drug candidates to induce apoptosis and increase reactive oxygen species (ROS) in cancer cells. Novelty and scientific contribution. The result shows the cytotoxic effect of capsanthin and capsanthin-loaded micelles on MDA-MB-231 cell line for the first time. Capsanthin from sweet red pepper (Capsicum annuum) showed remarkable cytotoxic effect on the triple-negative MDA-MB-231 cell line.Pozadina istraživanja. Karcinom dojke jedan je od najčešćih tipova tumora te je još uvijek glavni uzročnik morbiditeta i mortaliteta među ženama diljem svijeta. U razvijenim zemljama ova multifaktorska bolest predstavlja primarni zdravstveni problem, a u stalnom je porastu u srednje i nisko razvijenim zemljama. Mnoga istraživanja pokazuju da fitokemikalije poput karotenoida suzbijaju rast i potiču apoptozu stanica karcinoma dojke. Nedavno smo poboljšali topljivost kapsantina u vodi postupkom inkapsulacije u novom neionskom surfaktantu, diosgenin polietilenglikol sukcinatu. Stoga je svrha ovoga rada bila pomoću MTT testa ispitati in vitro citotoksičnost micela punjenih kapsantinom, topljivih u vodi, na stanice raka MDA-MB-231. Eksperimentalni pristup. U radu je iz ekstrakta slatke crvene paprike (Capsicum annuum) izoliran hidrofobni karotenoid kapsantin. Iz čvrste disperzije ekstrakta i diosgenin polietilenglikol sukcinata 1000 pripremljene su micele. Ekstrakt kapsantina i micele su okarakterizirani pomoću UV-Vis spektroskopije, visokodjelotvorne tekućinske kromatografije, infracrvene spektroskopije s Fourierovom transformacijom, difrakcije X-zraka, raspodjele veličine čestica, polidisperzije i pretražne elektronske mikroskopije. Ispitali smo učinak ekstrakta kapsantina i micela na preživljavanje i rast trostruko negativnih stanica raka dojke (MDA-MB-231) te citotoksičnost micela. Rezultati i zaključci. Bitno se povećala topljivost kapsantina u inkapsuliranim micelama i time proširila mogućnost njegove primjene za ciljanu isporuku, čime se postižu bolji rezultati u liječenju rezidualnih tumora. Inkapsulirani se kapsantin kontrolirano otpuštao pri simulaciji probave u crijevima (pH=6,8). Predloženi sustav za ciljanu isporuku lijeka s produljenim djelovanjem omogućuje učinkovito i kontrolirano otpuštanje aktivne tvari na mjestu djelovanja. Rezultati pokazuju da se pri inkapsulaciji kapsantina nije promijenila njegova struktura, a niti sastav funkcionalnih skupina. Citotoksičnost micela na stanice MDA-MB-231 (IC50=(3,10±1,09) μg/mL) bila je bitno veća od one ekstrakta kapsantina (IC50=(81,1±1,5) μg/mL). Ekstrakt kapsantina i micele s kapsantinom mogu se upotrijebiti za poticanje apoptoze i povećanje količine reaktivnih kisikovih spojeva u stanicama raka. Novina i znanstveni doprinos. Rezultati prvi put prikazuju citotoksični učinak kapsantina i micela s kapsantinom na stanice raka MDA-MB-231. Kapsantin izoliran iz slatke crvene paprike (Capsicum annuum) imao je izniman citotoksični učinak na trostruko negativne stanice raka MDA-MB-231

Antioxidant and acetylcholine esterase inhibition activity of the extract from Centella asiatica obtained by Ultrasound pre-treatment followed by Microwave-assisted extraction method

The extraction of compounds from Centella asiatica a member of the family Apiaceae by adopting Ultrasound assisted Extraction (UAE), Microwave assisted extraction (MAE) and Ultrasound pre-treatment followed by Microwave-assisted extraction were reported. The yield of the extract, phenol content, antioxidant activity and Acetylcholine esterase activity were found to be more in the extract obtained by Ultrasound pre-treatment followed by Microwave-assisted extraction method. The yield of the extract is more by 30.8% to the UAE and MAE methods. The phenol content is 1289 ± 0.57 μg GAE/mL which is 27% higher than the MAE method and 46% higher than the UAE method. HPLC analysis showed that the C. asiatica extract comprised of Madecassoside in major quantity followed by madecassic acid, asiatic acid and asiaticoside. In the antioxidant activity by DPPH assay and AChE inhibitory effect the IC50, value for C. asiatica extract obtained by UAE pre-treated and followed by MAE method is 38.24 μg mL−1 and 26.7±0.49 mg/mL respectively which are substantially higher than the other two methods. So, Ultrasound pre-treatment followed by Microwave-assisted extraction method is found to be a preferable method to get the desired compounds from C. asiatica

SYNTHESIS, ANTICANCER ACTIVITY, MOLECULAR DOCKING, AND ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION TOXICITY STUDIES OF NOVEL BENZOTHIAZINES

ABSTRACTObjective: A series of benzothiazine compounds were studied for absorption, distribution, metabolism, and excretion (ADME) properties to assestheir drug-like properties. Compounds 1-10 with favorable ADME properties were selected for molecular docking studies as PIM1 kinase inhibitors.Methods: Synthesis of compound 1 and 7 by conventional heating and characterized by various methods. Molecular docking carried out using Glidesoftware; ADME toxicity predicted using QuickPro.Results: Compound 1 showed a Glide score of −7.622 kcal/mol with good hydrophobic and hydrophilic interactions with PIM1 kinase proteins andappears to be more potent. Structure-activity relationship study was made among the 10 compounds, and a basic template was arrived at. An analysisof the structure - Affinity relationships suggested that the substituent at position three is important in influencing affinity.Conclusion: Compounds with an alkyl spacer between the carboxyl group and the core benzothiazine ring are required for binding of the compoundswith the PIM1 kinase. It was further confirmed by its in vitro anticancer activity of compound 1 against K562 cell lines by 3-(4, 5dimethythiazol-2yl)-2,5-diphenyltetrazoliumbromideassaybyexhibitingan IC50 value of 36.82 μg/ml.Keywords: Benzothiazine, Molecular docking, Absorption; distribution; metabolism; and excretion properties, In vitro anticancer activity

SYNTHESIS OF NOVEL CYCLOHEXANONE DERIVATIVES AS BCR-ABL T1351 INHIBITORS

Objective: Several 3(rd) generation inhibitors are being developed for the treatment of patients with Chronic myelogenous leukemia (CML). The present work mainly aims to discover novel small molecular inhibitors against important molecular target T3151 ABL mutant involved in leukemia.Methods: Docking study was carried out and the binding affinity of the proteins with the phenothiazine compounds 3a-h and 7a-c was measured. The docking scores of the N-acylated compounds 7a-c are higher than 3a-h. The drug likeliness of these compounds was tested by the Lipinski's rule of five. The phenothiazine compounds with good docking scores and 7a-c were synthesized and screened by in-vitro methods for inducing antiproliferative effect by trypan blue and MTT assay and induction of apoptosis in K562 cells.Results: All the N-acylated compounds and, in particular, 7c with a chloro substituent in the para position of the phenyl ring appeared to be most potent molecule with an IC50 value of 32.44 and 24.01(µg/ml) by trypan blue and MTT assay respectively. Further, a dose-dependent increase in LDH release was observed, confirming the antiproliferative potential of the compounds.Conclusion: The compounds 7a-c was tested for antiproliferative effect against K562 cell lines by MTT assay LDH assay and Trypan blue assay. All the compounds 7a-h behaves as 3(rd) generation inhibitors for the treatment of patients with Chronic myelogenous leukemia (CML). These can act as a template for the further development and optimization studies.Â

Effect of Graphite Filler on the Physiochemical Properties of Graphite Reinforced Thermoset Rooflite – Unsaturated Polyester Resin Composites

Received: 24.01.24. Revised: 09.02.24. Accepted: 09.02.24. Available online: 29.02.24.The authors would like the thank the Principal, and Head of the department of Chemistry, Government Arts college, Udumalpet 642 126, for allowing us to conduct the experi-ments. We extend our thanks to Dr. R. Venckatesh, Depart-ment of Chemistry, Government Arts college, Udumalpet 642 126 for helping us in the IR spectral studies of the sam-ples. The Authors wish to thank DST FIST DST-FIST-2018 (SR/FST/COLLEGE-417/2018) (TPN-2011) laboratory of the department for providing assistance to this research.The crystallinity index of the studied composite materials increased due to the enhanced interaction between the resin matrix and graphite filler.Agglomeration due to higher concentration of graphite filler lowers the interfacial contact and affects the mechanical characteristics of the composites.The glass transition temperature increases with the addition of graphite.When the percentage of graphite in composites is raised, the limiting oxygen index revealed that the composites are self-extinguishing.The synthetic composites exhibit a consistent swelling behavior in response to different chemical environments.It is well known that many polymers are insulators with poor mechanical properties, which limit their use in fuel cell applications. Physicochemical properties of the polymers can be improved by adding conductive fillers. Carbon-based materials like graphite, which provides excellent mechanical strength and thermal conductivity to the polymer matrices, is of special interest because of its abundance, low cost and light weight when compared to other carbon allotropes. In the present work we describe the physicochemical properties of rooflite unsaturated polyester resin/graphite composites. Rooflite resin and three of its composites containing 1%, 3% and 5% of graphite by weight (C-2, C-3, and C-4, respectively) were synthesized and characterized by FTIR spectral data. XRD showed two peaks at 2 = 27.37°and 55.40° with d spacing value of 3.2559 nm and 1.6571 nm, respectively, indicating the change in degree of crystallinity of the composite. The calculated crystallinity for the resin is 7.3%, and for C-2, C-3 and C-4 its values are 12.1%, 14.3%, 17.1%, respectively, evidencing the interactions between the graphite and polymer matrix. The composites showed fractured surfaces and porous rough structure with randomly distributed vascularized cavities. Agglomeration occurs, when the concentration of graphite increases. The glass transition temperature for the pure resin is 65.9 °C and increases when the resin is filled with graphite. Thermogravimetric analysis (TGA) of the composites showed no marked difference between Tmax and Tfinal, and LOI values of C-3 and C-4 are above 21%, making them self-extinguishable materials that could be used for making bipolar plates. The chemical resistance investigation against water, NaCl, NaOH, acetic acid, and toluene showed more resistance to acid than alkali solutions. These rooflite resin/graphite composites could be further studied to explore the possibility of making bipolar plates, which are an essential component of fuel cells

Role of nano-capacitor on dielectric constant enhancement in PEO:NH4SCN:xCeO2 polymer nano-composites: Electrical and electrochemical properties

Solution casting technique has been successfully employed to prepare nano-composite films. Various weight ratios of cerium oxide (CeO2) nanoparticle were added to a PEO:NH4SCN:xCeO2 polymer matrix to enhance the ionic conductivity at ambient temperature. The electrical and electrochemical properties of the composite electrolyte systems have been investigated using impedance, dielectric properties (ɛ*, tanδ, and M*), transfer number measurement (TNM), linear sweep voltammetry (LSV), and cyclic voltammetry (CV) techniques. The highest ionic conductivity of ∼8.57 × 10−4 S/cm is obtained for the system incorporated with 3 wt.% of CeO2 filler. This study presented a new approach and the complex permittivity confirmed that the real part value of dielectric constant (ɛ′) for all samples has found to be much higher than the imaginary part (ɛ″) value. The appearance of the peaks at a characteristic frequency in the loss tangent indicates the existence of relaxation. Low dielectric modulus is observed for 3 wt.% of CeO2 incorporated. The TNM measurements confirmed the ionic conductivity of NCSPEs and ion transport tion of films have been found to be 0.84, 0.96 and 0.92 for 1 wt.%, 3 wt.%, and 5 wt.% of CeO2, respectively. The system incorporated with 3 wt.% of CeO2 has discovered to be electrochemically stable up to 1.4 V. From the CV analysis it is noticeable that the energy storage mechanism of the EDLC is a combination of double-layer capacitance and pseudo capacitance. A value of 88.9 F/g is achieved at 20 mV/s

SEASONAL VARIATION IN THE ESSENTIAL OIL COMPOSITION OF MAJORANA HORTENSIS MOENCH FROM WESTERN GHATS REGION OF SOUTH INDIA.

Objective: To evaluate the seasonal variation in the composition of essential oil of Majorana hortensis Moench from Western Ghats region of South India during summer and winter seasons and to find out the chemo type of oil. Method: The essential oil from the plant is extracted by hydro distillation method using Clevenger type apparatus. The compounds are analysed by GC-MS method and identified by NIST library verification.  Results: Winter season oil contains trans-sabinene hydrate along with other constituents in considerable quantity whereas in summer season oil, terpinen-4-ol is the predominant constituent. Conclusion: Winter season is suitable for oil production in Western Ghats region of South India. The winter seasonal oil belongs to sabinene hydrate/terpinen-4-ol chemo type which is more fragrant than summer seasonal oil. On comparison with the literature datas, it has been found that the chemo type of the oil is similar to that of Egyptian oil in both summer and winter seasons. Keywords: : Majorana hortensis Moench, GC-MS, Trans-Sabinene hydrate, Terpene-4-ol

Isolation of phytoconstituents from the flowers of <em>Couroupita guianensis</em>

709-713Couroupita guianensis is used extensively as an ingredient in many Ayurveda preparations which cure gastritis, scabies, bleeding piles, dysentery, and scorpion poison. The flower has been subjected to sequential extraction using petroleum ether, chloroform, ethyl acetate and methanol solvents. A new compound I Cycloart-24-en-3-ol-4'-exomethylene heptadeconate along with stigmasterol II, p-coumaric acid III, o-coumaric acid IV, caffeic acid V and quercetin VI have been isolated by column chromatography and characterised using IR, 1H and 13C&nbsp;NMR and MS spectral data. Compound I, III, IV and V are reported for the first time from C. guianensis