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In our current study, a series of reactions with isolated natural flavonoids (2-phenylchromen-4-one) and flavanone (2,3-dihydro-2-phenylchromen-4-one) through Mannich base was carried out by a one-pot three-component reaction. Their structure-activity relationship study (SAR) reveals the anticancer activity of natural compounds and their Mannich bases. The flavones were substituted by imine at position C-8, while in the flavanones, the reaction takes place at positions C-8 and C-3. Spectroscopic techniques characterized all the isolated and newly synthesized derivatives. Anticancer activity was checked on HeLa and MCF-7 (cancer cell lines) and BHK-21 (normal cell line). Using propidium iodide (PI) and DAPI staining as fluorescence microscopic imaging was confirmed the Apoptotic effect of potent compound. Further, it was evaluated by cell cycle analysis through flow-cytometry, reactive oxygen species and lactate dehydrogenase production. The caspase-9 and -3 activity were estimated by mitochondrial membrane potential. Derivative of naringenin, ((2S)-4′,5,7-Trihydroxyflavan-4-one) where reactions occur at position C-3 were active than others.

In our present studies we identify the components of essential oil, crude extracts and fraction of Illicium verum, and evaluation of antibacterial activity. We isolated and identified as 3, 4-dihydroxybenzoic acid (protocatechuic acid) through spectroscopic studies and comparison with the data of the authentic sample [1]. The phase MEA itself was emerged as the active fraction comprising antibacterial, antioxidant and nematocidal constituents, including 3, 4-dihydroxybenzoic acid which also possessed antibacterial, Superb antioxidant and nematocidal activities [1].

The methanolic extract of aerial parts of Tithonia tubaeformis showed significant antioxidant activity in DPPH assay. It was subjected to bioassay guided fractionation affording more active ethyl a...

Hippophae rhamnoides L, commonly called Sea buckthorn, is native to Asia and Europe and and known for its nutritional and medicinal values. The aim of the present study was to investigate the anti-cancer constituents of H. rhamnoides. Among the three isolated compounds namely: 1-(2-hydroxynaphthalen-1-yl) ethan-1-one (1), Oleanolic acid (2), and Hippocorosolate (3), compound 3 was a new corosolic ester derivative. The isolated compounds (2 and 3) displayed anticancer activity against lung (NCI-H460) and breast (MCF-7) cancer cell lines with IC50 values of ~3 µM and ~6 µM, respectively. However, compound 1 was active only against breast cancer cells with IC50 value of ~43 µM. These compounds displayed only weak interactions with minor groove of DNA in DNA-ligand conformational studies and therefore, structural DNA damage was not noted in electrophoretic mobility experiments. It was concluded that new compound 2 possessed more potent anticancer activity than that of known compound 3 against lung cancer cell line.

Alzheimer is a neurodegenerative disease and requires the development of new scaffold to treat it. In this regard, thiazoles derivative are playing their significant role. In the current research paper we have focused our attention for the development of tetrasubstituted thiazole (3a-h) derivatives using domino synthesis by mixing the thiourea as a precursor, with acetophenone in the presence of iodine and tosic acid in DMSO and refluxed for 12–22 h. The structures of the newly synthesized compounds were confirmed by FTIR, 1H NMR, 13C NMR and EIMS analysis. Thiazole derivatives were analyzed for their biological significances against acetyl and butylcholinesterase enzymes and compound 3b and 3d were found more active against these enzyme, respectively. The mode of inhibition was determined for the potent compounds against both the enzymes. Moreover, the molecular docking studies were carried out to explore the interactive behavior of the compounds within the active pocket of enzymes. Furthermore, the derivatives (3a-h) were evaluated for their anticancer potential against HeLa cancer cell lines. Most potent inhibition was observed by compound 3b.

We currently work with fresh, undried and uncrushed flowers, leave and stems which were used to avoid the formation of artifacts through aerial oxidation and enzymatic degradation. These studies have led to the isolation of three new constituents. 2-O-(β-3′-O-acetyl,4′-O-isovaleroyl-rhamnopyranosyl)-1-O-hexyl,3-O-acetyl-β-xylopyranose (Compound 1), 2-O-(β-2′,3′- Di-O-acetyl,4′-O-isovaleroyl-rhamnopyranosyl)-1-O-hexyl,3,4-di-O-acetyl-β-xylopyranose (Compound 2) and 2-O-(β-3′-Oacetyl,4′-O-isovaleroyl-rhamnopyranosyl)-1-O-hexyl,3,4-di-O-acetyl-β-xylopyranos, along with one known 4-hydroxy benzoic acid have been isolated from the leaves and stems of Phlox drummondii. Their structures have been established through chemical and spectral studies including two dimensional NMR (COSY 450 , NOESY, HMQC and HMBC) experiments.

The methanolic extract of aerial parts of

The study was aimed at evaluating various biological actions of widely consumed Areca catechu nut. The nut's ethanolic extract exhibited cytotoxicity (lung cancer cell line), embryotoxicity (chick embryo), phytotoxicity (Lemna minor), insecticidal (Rhyzopertha dominica), anti-bacterial (Pseudomonas aeruginosa), anti-fungal (Microsporum canis) and mitogenic (human blood lymphocytes) actions. The standardization results revealed presence of 1.7 μ g arecoline per mg of extract. In conclusion, the Areca nut is endowed with both harmful and beneficial biological actions. Keeping in view its wide consumption and ease of availability, the aforesaid information should be channelized for health and agricultural benefits.

We describe the oxidation of flavanones by employing phenyliodonium diacetate to form the flavone (15), isoflavone (8) and 2,3-dihydrobenzofurane (18) in this study. The oxidative method was found to be regioselective and dependent on the substitution pattern present on the two aromatic rings of the starting flavanone. The structures of products obtained were fully characterized by using IR, 1 H and 13 C NMR spectroscopy and Mass spectrometry. X-ray crystallography further confirms the structures of flavones and isoflavone. The density field theory calculations have also been performed to get more insight about the structures, electronic and spectroscopic properties of synthetic flavonoid derivatives. The geometrical parameters such as bond lengths and angels showed a good correlation with the values obtained through X-ray crystallography. Moreover, the theoretically simulated vibrational and UV-vis spectral values are in agreement with the experimental results.

Illicium verum Hook F Star anise belongs to the family Illiciacea In traditional medicine it is used for variety of ailments The current study was aimed at investigating the antioxidant potential of I verum IV constituents Various extract fractions and pure compounds of I verum were explored for their antioxidant activity using DPPH diphenyl picrylhydrazyl and deoxyribose sugar assays The structure of pure compound was elucidated through spectral studies UV IR EIMS and H NMR data In DPPH assay the methanolic extract of I verum displayed antioxidant activity with an IC of mg ml Among its various fractions the ethyl acetate IV EA appeared to be potent antioxidant with IC value of mg ml and its sub fractions theethyl acetate soluble sub fraction of ethyl acetate fraction IV EA EA S was most potent with IC of mg ml Further fractionation led to potent sub fraction i e Petroleum ether ethyl acetate insoluble sub fraction IV EA PE EA I with an IC of mg ml The purified fraction subsequently appeared to be most potent mg ml which led to the isolation of dihydroxy benzoic acid protocatechuic acid as active principle In deoxyribose degradation assay the IV E IV EA and protocatechuic acid also demonstrated antioxidant activity with IC of approximately and mg ml respectively In conclusion the protocatechuic acid residing in I verum most probably underlies its antioxidant action

Owing to the biological importance of cyclic sulfonamides (sultams), herein we report a new, facile and cost-effective method for the synthesis of sultams that makes use of a reaction between dansyl amide and easily accessible benzaldehydes under mildly acidic conditions. All compounds were obtained in good yields (69-96%). Consequently a series of cyclic sulfonamides (7a-7n) was synthesized and characterized using FTIR, MS and NMR spectroscopy, crystal structure of compound 7b has also been determined. All compounds were evaluated for their potential to inhibit alkaline phosphatase (bTNAP and bIAP). All compounds were found to be excellent inhibitors of bTNAP with IC50 values in lower micro-molar range (0.11-6.63μM). Most of the compounds were selective inhibitors of bTNAP over bIAP. Only six compounds were found to be active against bIAP (IC50 values in the range 0.38-3.48μM). Molecular docking studies were carried out to identify and rationalize the structural elements necessary for efficient AP inhibition.

Three new flavonoids, lawsochrysin ( 1 ), lawsochrysinin ( 2 ), and lawsonaringenin ( 3 ) were isolated from the leaves of Lawsonia alba Lam. along with four flavonoids 3′,4′-dimethoxy flavone ( 4 ), 7-hydroxy flavone ( 5 ), 3,3′,4′,7-tetrahydroxy flavanone ( 6 ) and rhoifolin ( 7 ) hitherto unreported from this genus. Their structures were elucidated on the basis of spectroscopic evidences. Compounds ( 3 ) and ( 6 ) showed a good urease inhibition activity IC 50 = 139.1 ± 0.77 and 184.53 ± 0.61 μM respectively, ( 6 ) also showed a DPPH radical scavenging activity with IC 50 = 33.83 μM.

Role of aldose reductase (ALR2) in diabetic complications such as retinopathy, nephropathy, neuropathy, and cataract etc. is well-evident. ALR2 in the first step of polyol pathway reduces glucose to sorbitol whose elevated level leads to diabetic cataract, characterize by clouding of the lens in the eye that affects vision. Inhibition of ALR2 enzyme with small molecules as inhibitor is a rapid approach for diabetic management. In the present study the synthetic route to synthesize desired benzopyrazines and a library of sixteen (16) methyl benzopyrazines were screened against aldose reductase. From the bioactivity results, the 3'-hydroxyphenyl benzopyrazine 6l was found most active (IC50 = 1.34 ± 0.07 µM) while 3'-bromophenyl analogue 6i showed comparable activity for ALR2 (IC50 = 3.48 ± 0.66 µM) as compared to standard sorbinil (IC50 = 3.14 ± 0.02 µM). Both compounds (6l and 6i) showed excellent selectivity for ALR2 over aldehyde reductase (ALR1) which has important role in detoxification of toxic aldehydes. The structure of two regio-isomers were fully characterize by 1H and 13C NMR two dimensional NMR techniques including COSY, NOESY, HSQC, and HMBC. Regio-isomers separation was proved to be difficult in different solvent systems. Only an isomer of 3'-bromo benzopyrazine 6i' was isolated that help to assign the structure of regioisomers from NMR data. All the benzopyrazines were fully characterized by using different spectral techniques including 1H, 13C NMR, IR spectroscopy, and mass spectrometry.

The aim of the study was to explore the traditional use of Cinnamomum cassia against depression. The standardised methanolic extract of the bark of C. cassia was evaluated for antidepressant activity using various behavioural tests, i.e. tail suspension test (TST), forced swim test (FST) and locomotor activity test. The serotonergic and noradrenergic modulation was assessed using 5-hydroxytryptophan (5-HTP)-induced head twitches and yohimbine potentiation tests, respectively. The fluoxetine and phenelzine were used as positive controls in the study. The C. cassia extract significantly decreased the immobility time in TST (maximum effective dose tested was 50 mg/kg) while no effect was observed in FST and locomotor activity test. The extract significantly increased the 5-HTP-induced head twitches while yohimbine-induced lethality remained unaltered. The aforementioned results are similar to that caused by fluoxetine. The standardised methanolic extract of C. cassia demonstrated antidepressant activity that can be attributed to rise in serotonin levels.

Ethnopharmacological relevance: Ocimum basilicum belongs to the genus Ocimum (Lamiaceae). Many species of this genus including O. basilicum have been traditionally used for the treatment of a variety of diseases including respiratory diseases and symptoms of tuberculosis. Aim of study The aim of the study was to evaluate the activity of pure constituents of O. basilicum , a plant used in traditional medicine to treat respiratory diseases including symptoms of tuberculosis, against Mycobacterium tuberculosis H37Rv. Materials and methods The crude methanolic extract from the aerial parts (leaves, fruits and flowers) of the plant was separated into EtOAc and water subextracts and the EtOAc subextract was further divided into acidic and neutral fractions. Each of these was subjected to fractionation through column chromatography followed by prep. TLC. Several pure compounds were thus isolated and their activity was determined against M. tuberculosis H37Rv using MABA assay. Results Nine compounds were assayed for antituberculosis activity which exhibited upto 49% inhibition of M. tuberculosis H37Rv at 6.25 μg/mL. These include one new compound bacilicin, the structure of which was elucidated based on 2D-NMR (HSQC, HMBC, COSY and NOESY) and Ms spectral analysis. The known compounds were identified on the basis of comparison of their spectral data with those reported earlier. Conclusions Inhibition of M. tuberculosis by pure compounds from O. basilicum supports the use of this plant in ethnomedicine as a remedy for symptoms of tuberculosis. The results also suggest that the activity of the plant may be due to a synergistic effect of active compounds including those investigated in the present studies, and hence this plant is a potential candidate for obtaining further new antituberculosis natural products.

A pentacyclic triterpene, oleanderocioic acid, two flavonoidal glycosides, quercetin-5-O-[α-L-rhamnopyranosyl-(1→6)]-β-D-glucopyranoside and kaempferol-5-O-[α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside, and a cardenolide, oleandigoside, together with 11 known compounds, were isolated from the leaves of Nerium oleander. Their structures were elucidated on the basis of spectroscopic analysis. The growth inhibitory and cytotoxic activities of eight compounds were evaluated against the MCF-7 human breast cancer cell line using a sulforhodamine B assay. Three compounds, oleandrin, odoroside A and B were further assayed using a panel of 57 human cancer cell lines.

A new lignan, rayalinol (1) and a new sesquiterpene kairatene (2) were isolated from Eurotia ceratoides (L.) along with four hitherto unreported syringaresinol, dehydrodiconiferyl aldehyde, dihydrodehydrodiconiferyl alcohol, and dehydrodiconiferyl alcohol and two previously reported constituents ferulic acid and β-sitosterol. The structures of the new constituents were elucidated by extensive spectroscopic means and chemical evidences. Rayalinol is a biogenetically interesting compound with a hitherto unreported 9a homolignane skeleton. Its biosynthetic origin is suggested.

Structural revision of lawsonicin, a natural product of Lawsonia alba, is reported based upon comparison of its spectral data with that of the naturally occurring dihydrobenzo[b]furan neolignan (rac)-trans-dihydrodehydrodiconiferyl alcohol, which is found to be identical. A concise synthesis of dihydrodehydrodiconiferyl alcohol, via Rh(2)[S-DOSP](4)-catalysed intramolecular C-H insertion, is described.