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Aims: A new gradient RP-HPLC method was developed for the separation and determination of process related impurities in Palbociclib. Methodology: The chromatographic separation was achieved on a Inert sustain swift (C18) column using a mobile phase comprising of perchloric acid and acetonitrile in a gradient mode at a flow rate of 1 mL/min. over a runtime of 50 minutes. All the eluants were monitored at 230 nm. The optimized method was validated as per ICH guidelines for various parameters. Results: The linearity of the method was proposed in the range of LOQ to 250 % for the drug and its impurities by subjecting the data obtained to statistical analysis using correlation coefficient model (r > 0.99). The method also gave acceptable recovery of all the four impurities at each level and was found to be accurate. The % RSD obtained in the method precision and intermediate precision were less than 2% depicting the precision of the method. The LOD and LOQ values were calculated based on the signal to noise ratio and are indicating the sensitivity of the method. The specificity of the method was checked in the presence of process related impurities and also degradants generated by exposing to a variety of forced degradation conditions. Conclusion: The proposed RP-HPLC method for the determination of process related impurities of Palbociclib could be routinely used in the quality control testing.

Aim: To develop a sensitive headspace GC-MS method for the determination of potential genotoxic impurities in Vigabatrin. Place and Duration of Study: The study was performed in SIONC Pharmaceuticals, Visakhapatnam from June 2020 to March 2021. Methodology: The impurities were determined by selected ion monitoring mode using VF -WAXms (30 mts length, 0.25 mm internal diameter, 1.0 µ film thickness) column. Helium gas was used as carrier gas with a column flow of 1.0 mL/min. and injector temperature maintained at 220 0C. Oven Temperature, loop temperature and transfer line temperature were maintained in the head space at 70oC, 90oC and 100oC respectively. Results: The linearity of the method was proposed in the range of LOQ to 150 % for the genotoxic impurities by subjecting the data obtained to statistical analysis using linear regression model (r2 > 0.99). The method also gave acceptable recovery of all the four impurities at each level and was found to be accurate. The % RSD obtained in the method precision and intermediate precision were less than 11% depicting the precision of the method. The LOD and LOQ values were calculated based on the signal to noise ratio and are indicating the sensitivity of the method. The specificity of the method was checked for blank interference at the retention time of respective impurities. Conclusion: The results proved that the proposed headspace GC-MS method for the study of potential genotoxic impurities of Vigabatrin was sensitive, precise and accurate and could be routinely used in the quality control testing of the active pharmaceutical ingredient.

The aim of the present study was to evaluate pharmacognostical and antimicrobial, antioxidant, anti-inflammatory activity of ethanolic leaf extracts of Alternanthera pungens. The collected plants were washed, dried, cut and ground into coarse powder and macerated with ethanol and extract was dried by rotary vacuum. Phytochemical screening of ethanol extract revealed the presence of steroids, flavonoids, saponins, glycoside, phenols, and proteins. However, alkaloids and glycosides were absence in this species. The ethanolic extract of whole plant of A. pungens was subjected to column chromatography to separate pure compounds. Invitro antioxidant activity was performed by 2, 2 -diphenyl- 1- picrylhydrazyl (DPPH) assay, hydroxy radical scavenging method and superoxide radical scavenging activity. The ethanolic extract of A. pungens was evaluated against antimicrobial activity against two fungal and four bacterial strains. The extracts showed remarkable inhibition of zone of bacterial and results were comparable with that of standard drugs against the organism tested.

Objective: This work aimed to establish and formulate the gossypinproniosomal gel drug delivery system. Methods: Gossypin-loaded proniosomal gels (GPG) was prepared using specific non-ionic surfactants (Spans), followed by particle size (PS), entrapment efficiency (percent EE), in vitro, ex-vivo drug release, and in vitro efficacy of Gossypin against human melanoma cells (A-375). Results: The results showed that the percentage EE for the GPG is appropriate (81.3 %–95.5 %) and they are Nano-sized (189.3–912.0 nm) and the gels diffusion provided the desired sustaining effect for GPG-F7 formulation (75.5 percent). The GPG reported cell viability of 14.9±2.3 percent compared with 16.1±1.1 percent for free Gossypin at the maximum dose of 100 μg/ml for A-375 human melanoma cells after 24 hr incubation time. No major changes were seen in the percentage EE, PS of GPG after storage for 90d, in the physical stability report. Conclusion: The results obtained suggest that the proniosomal drug delivery system can enhance the flux to the skin and achieve the ideal Gossypin sustainability effect. Consequently, the use of proniosomal gel may be advantageous with regard to the topical delivery of Gossypin for melanoma treatment management.

The liver is a requisite organ in the body, maintaining various physiological functions. Liver damage or toxicity is due to consuming certain chemicals, dietary supplements, drugs, and alcohol at high doses in day-to-day life. Several phytoconstituents acts as hepatoprotective agents. Research advances in analytical techniques and knowledge of active components have allowed research scientists to study the relationship between the phytoconstituents and their activity on the human liver. The review article aims to compile data on promising active constituents that act as lead molecules for future natural products-based drug discovery. The online database, including Web of Science, PubMed, Scopus, and Science Direct, was explored for papers and studied the hepatoprotective activity. Some phytoconstituents act against the chemicals such as CCl4 , paracetamol, alcohol, oxidative stress-induced hepatotoxicity, etc.

Stability indicating RP-HPLC method was developed for the simultaneous quantitation of Sofosbuvir and Velpatasvir in its pharmaceutical dosage form and validated. The drugs were separated on Discovery C18 (150mm x 4.6mm, 5μ) column using 0.01N potassium dihydrogen phosphate buffer and acetonitrile (50:50%v/v) as mobile phase on isocratic mode. The mobile phase is pump into the column at flow rate of 1.0ml/min and column oven temperature is maintained at 30ºC. The drugs were detected at a wavelength 240nm. The retention time for Sofosbuvir and Velpatasvir were found to be 2.32min and 3.34min respectively. The developed method is validated in accordance with ICH guidelines. The method was found to be accurate, precise, specific and robust. The method obeys Beer’s law at a concentration range of 100μg/ml – 600μg/ml of Sofosbuvir and 25μg/ml – 150μg/ml of Velpatasvir, with correlation coefficient of 0.999 for both the drugs. The drugs were found to be stable and less prone to degradation when they are subjected to various stress conditions.

A stability indicating reversed-phase high-performance liquid chromatography method was developed and validated for simultaneous quantification of sofosbuvir and ledipasvir in tablets. The chromatographic separation was done in an isocratic mode using the Discovery C18 (250×4.6 mm, 5 µ particle size) column. The mobile phase 0.1 % ortho phosphoric acid and acetonitrile 45:55 (% v/v) at a flow rate of 1.0 ml/min and at ambient temperature was used. The wavelength used for detection was 270 nm. The retention time for sofosbuvir was found to 2.08 min and that of ledipasvir was 3.06 min. Sofosbuvir and ledipasvir were linear in the concentration ranges of 100 to 600 µg/ml and 22.5 to 135 µg/ml, respectively. The developed method was validated and found to be accurate, specific and robust. Both the drugs were subjected to the stressed conditions like acidic, basic, oxidative, photolytic and thermal conditions. The degradation results were found satisfactory. This method could be applied for the simultaneous estimation of sofosbuvir and ledipasvir in tablets.

Phytochemical evaluation of the chloroform extract of roots of Polygonum viscosum has yielded six compounds, stigmasterol, 7,4-dimethylquercetin, kaempferol, quercetin, myricetin and scutellarein. Among the six compounds isolated and characterized by chemical and spectral (UV, NMR and Mass) analysis in the present phytochemical evaluation, stigmasterol was not reported earlier from P. viscosum. The compounds, 7,4E¹-dimethylquercetin, quercetin and scutellarein were reported from P. hydropiper. Kaempferol from P. amphibium, P. aviculare, P. convolvulus, P. hydropiper, P. lapathifolium and P. persicaria and myricetin from P. aviculare and P. lapathifolium were also reported earlier. This appers to be the first report of the occurrence of all the six compounds from P. viscosum.

Objective: To study the anthelmintic activity of phytochemically charaterized chloroform extracts of Millettia auriculata leaves and stems. Methods: Chloroform extracts of leaves and stems were prepared. Phytochemical characterisation involved preliminary screening, optimisation of solvent system in thin layer chromatography (TLC) and UV absorption measurement of each bright yellow (in view of a common physical property of flavonoids) TLC fraction for each extract. Anthelmintic activity of each extract was carried out for different concentrations (10, 20 and 40 mg/mL) using Pheretima posthuma. Results: Phytochemical characterisation of the extracts revealed the presence of steroids/ triterpenes, phenolics/flavonoids and carbohydrates with optimum TLC-separation in chloroformhexane, 19:1. All the investigated extracts possessed significant anthelmintic activity (P

Four compounds viz α-amyrin, β- amyrin, bauerenol and ellagic acid were isolated from the methanolic extract of Rotula aquatica roots. The structures of these compounds were elucidated on the basis of spectroscopic data analysis and chemical evidence. The extract was evaluated for hepatoprotective activity against carbon tetrachloride induced hepatotoxic model at a dose levels of 200,400 and 800 mg/ kg body weight and compared with that of the standard silymarin (25mg/kg body weight). It showed good hepatoprotective activity in a dose dependent manner. The extract was also screened for antimicrobial activity against various types of organisms like bacteria and fungi.

Aims The present study was aimed to study the in vitro antioxidant property by DPPH, superoxide, and hydroxyl radical scavenging assays, in vivo hepatoprotective activity by CCl4 induced hepatotoxicity in albino rats, formulation of polyherbal hepatoprotective tablets containing equal quantities of methanolic extract of roots of Begonia laciniata Roxb., whole plant of Cuscuta epithymum (L.) L and whole plant of Dendrobium ovatum (L.) Kraenzl., which were used traditionally in Chittoor and Khammam districts of Andhra Pradesh, India. Methods Formulation was developed by direct compression method using super tab-11SD, primojel, talc and magnesium stearate as excipients and then subjected to evaluation of precompression and post compression parameters. Results and conclusion All the selected plants showed dose dependant antioxidant property, highest at 360 μg dose and significant dose dependant hepatoprotective activity, highest at a dose of 400 mg/kg b.w compared to standard drug silymarin, the histopathological studies also confirmed protective effects of extracts against CCl4-induced liver injuries. The observations from formulation support the ideal properties of compressed tablets and its feasibility for large-scale commercial production.

Mulberry belongs to the genus Morus of the family Moraceae. It is an economically important plant being used for sericulture. Studies have been reported on the chemical composition and nutritional potentials of some mulberry sp ecies worldwide. In the present study the chemical examination of Morus indica leaves on conventional extraction and various chromatographic methods , led to the isolation of five compounds - β - sitosterol - 3 - O - β - D - glucoside , β - sitosterol , salvigenin, cirisima ritin and quercitin . All the compounds were characterized by 2D NMR, MS spectral data and comparison with the published data for the known compounds. All the compounds were reported for the first time from the leaves of this species. The work was further e xtended to test the crude extracts for antibacterial and antifungal activities. The results from the present study have shown that the species have considerable activity against selected bacterial and fungal strains which can be attributed to the presence of steroidal and phenolic compounds in the crude extracts of Morus indica.

Objectives: The objective of this study is to evaluate the neuroprotective effect of gossypin (isolated from Hibiscus vitifolius) against global cerebral ischemia/reperfusion (I/R) injury-induced oxidative stress in rats. Materials and Methods: Sprague Dawlet rats of wither gender were used in the study. Evaluation of cerbroprotective activity of bioflavonoid gossypin (in 5, 10 and 20 mg/kg oral doses) isolated from H. vitifolius was carried out by using the global cerebral I/R model by bilateral carotid artery occlusion for 30 min, followed by 24 h reperfusion. The antioxidant enzymatic and non-enzymatic levels were estimated along with histopathological studies. Result: Gossypin showed dose-dependent neuroprotective activity by significant decrease in lipid peroxidation (P < 0.001) and increase in the superoxide dismutase, catalase, glutathione and total thiol levels in gossypin treated groups when compared to control group. Cerebral infarction area was markedly reduced in gossypin treated groups when compared to control group. Conclusion: Gossypin showed potent neuroprotective activity against global cerebral I/R injury-induced oxidative stress in rats.

Objective: The objective of the present study was to develop and validate a new stability-indicating method for the quantification of lenvatinib mesylate in bulk drug and pharmaceutical dosage form using ultra performance liquid chromatography (UPLC).Methods: The optimized chromatographic conditions for elution of drug included UPLC HSS C18 (100 mm × 2.1 mm, 1.8 m) column, mixture of 0.1% orthophosphoric acid and acetonitrile (50:50 v/v%) mobile phase run on an isocratic mode at a flow rate of 0.3 mL/min, 240 nm detection wavelength, and column oven temperature maintained at 30°C.Results: The retention time for lenvatinib was found to be 1.24 min. The developed method was validated for various validation parameters in accordance with the International Conference on Harmonization guidelines. The method obeyed Beer’s law in the concentration range of 2.5– 15 μg/mL with a correlation coefficient of 0.9996. The percentage relative standard deviation and percentage recovery were determined to be 0.4 and 99.66–100.30%, respectively. The developed method was found to be accurate, precise, specific, linear, rugged, and robust. Forced degradation studies were conducted by exposing the drug to diverse stress conditions such as acidic, basic, peroxide, neutral, photolytic, and thermal conditions. The net degradation was obtained within the limits.Conclusion: The developed method for the estimation of lenvatinib can be employed to routine analysis of pharmaceutical dosage form.

Ethnopharmacological relevance Traditionally, the whole plant is used for various diseases, including neuronal disorders. Aim of the study To evaluate the neuroprotective effect of Matricaria recutita L. against global cerebral ischemia/reperfusion (I/R) injury-induced oxidative stress in rats. Materials and methods Neuroprotective activity was carried out by global cerebral ischemia on Sprague–Dawley rats by bilateral carotid artery (BCA) occlusion for 30 min followed by 60 min reperfusion. The antioxidant enzymatic and non-enzymatic levels were estimated along with cerebral infarction area and histopathological studies. Results The Matricaria recutita L. methanolic extract showed dose-dependent neuroprotective activity by significant decrease in lipid peroxidation (LPO) and increase in the superoxide dismutase (SOD), catalase (CAT), glutathione (GSH) and total thiol levels in extract treated groups as compared to ischemia/reperfusion group. Cerebral infarction area was significantly reduced in extract treated groups as compared to ischemia/reperfusion group. Conclusion The methanolic extract of Matricaria recutita L. showed potent neuroprotective activity against global cerebral ischemia/reperfusion injury-induced oxidative stress in rats.

In the present study we analyzed the cytotoxicity on RAW and HT-29 cell lines by MTT assay and antiprotozoal activity on Trypanosoma, Leishmania and Plasmodium parasites of different flavonoids isolated from three species of Tephrosia, T. calophylla, T. pulcherrima and T. pumila. Pulcherrimin exhibited toxicity towards RAW and HT-29 cell lines at low concentrations. Candidone, millettone and pongachin showed toxicity towards HT-29 cell lines at low concentrations. The isolated compounds were characterized by spectral data, including 2D NMR, 1H-1H COSY and 13C-1H COSY experiments.

A novel isoflavan-4-ol (pumilanol), ( re l)-3β-(2′-hydroxy-4′,5′-methylenedioxyphenyl)-6-methoxy-4α,7-dihydroxybenzo-3,4-dihydropyran ( 1 ) and two known flavonoids, tephrinone ( 2 ) and rotenone ( 3 ) together with lupeol and stigmasterol were isolated from the roots of Tephrosia pumila (Fabaceae) from a collection made in Andhra Pradesh, India. The structures of the compounds were determined by MS, 1D and 2D-NMR spectral analysis. Pumilanol ( 1 ) exhibited significant antiprotozoal activity against T. b. rhodensiense , T. cruzi and L. donovani with IC 50 of 3.7, 3.35 and 17.2 μg/mL, respectively, but displayed high toxicity towards L-6 (IC 50 of 17.12 μg/mL) rat skeletal myoblasts.

Since the discovery and subsequent widespread use of antibiotics, a variety of bacterial species of human and animal origin have developed numerous mechanisms that render bacteria resistant to some, and in certain cases to nearly all antibiotics, thereby limiting the treatment options and compromising effective therapy. In the present study, the green synthesis of nanoparticles is carried out by the reduction of silver acetate in the presence of crude methanolic root extracts of Diospyros paniculata, a member of family Ebenaceae. The UV-Vis absorption spectrum of the biologically reduced reaction mixture showed the surface plasmon peak at 428 nm, a characteristic peak of silver nanoparticles. X-ray diffraction (XRD) analysis confirmed the face-centered cubic crystalline structure of metallic silver. The average diameter of Ag NPs is about 17 nm from Transmission Electron Microscopy (TEM) which is in good agreement with the average crystallite size (19 nm) calculated from XRD analysis. Further the study has been extended to the antimicrobial activity against test pathogenic Gram (+), Gram (-) bacterial and fungal strains. The biologically synthesized silver nanoparticles showed promising activity against all the tested pathogenic strains and the activity has been enhanced with the increased dose levels. (C) 2016 Elsevier B.V. All rights reserved.

Chemical investigation of the roots of Diospyros assimilis had led to the isolation and characterization of six naphthalene derivatives, two 2-naphthaldehyes, namely 4-hydroxy-3,5-dimethoxy-2-naphthaldehyde 1, 4-hydroxy-5-methoxy-2-naphthaldehye 2, its related isomer 5-hydroxy-4-methoxy-2-naphthaldehyde 3 and three commonly occurring naphthoquinones, diospyrin 4, 8'-hydroxyisodiospyrin 5 and the simple monomer, plumbagin 6. Their chemical structures were established by detailed NMR investigations including 1H and 13C NMR, HSQC, HMBC and NOESY experiments. In addition, the naphthalene derivatives 1-5 were evaluated for their in vitro antiprotozoal activity against protozoan parasites belonging to the genera Trypanosoma, Leishmania and Plasmodium. Among the tested compounds, naphthaldehyde 1 showed moderate inhibition of the growth of the parasites, T. brucei, T. cruzi, L. donovani with IC50 values of 19.82, 12.28 and 38.78 microM and displayed cytotoxicity towards rat skeletal myoblasts (L-6 cells) with IC50 of 174.94 microM, while 2 and 3 were found to be comparatively less active to 1. The dimeric quinones 4 and 5 exhibited good activity against T. brucei and L. donovani with IC50 of 1.12 and 8.82 microM and 12.94 and 16.66 microM respectively.

Three 2-naphthaldehydes, including the novel 4-hydroxy-3,5-dimethoxy-2-naphthaldehyde, the simple naphthoquinone plumbagin and the dimeric naphthoquinones diospyrin and 8′-hydroxyisodiospyrin have been isolated from the roots of Diospyros assimilis and their structures established by spectroscopic analysis.

From the leaves of Zizyphus glabrata, a new dammarane-type triterpene, pseudojujubogenin -3-O- β -D-glucopyranoside, along with the known ceanothane triterpenes, granulosic acid, ceanothic acid and daucosterol were isolated. The structures of the compounds were fully characterized by detailed NMR investigations including 1H and 13C NMR, HSQC, COSY, HMBC and NOESY experiments. In addition, the dammarane glycoside was tested for its potential to inhibit various bacteria and was found to possess significant bactericidal activity. The 1H, 13C and full 2D-NMR data on granulosic acid has also been presented. This is the first report on the chemical constituents of the leaves of Z. glabrata.

A review of phytoconstituents and biological activities of Digitalis species has been presented. Despite the fact that there are about 24 species of this genus spread around the world, the present survey revealed that only 17 species have been studied phytochemically. Hence an attempt is made to present a review on the phytochemical studies of Digitalis species which would possibly serve as a source for much potent cardioactive molecules.

The aqueous extract of the Cocculus hirsutus aerial parts (100 and 200 mg/kg, p.o.) showed significant diuretic activity and laxative effect in rats. The acute toxicity, orally evaluated in mice, was found to be higher than 3000 mg/kg.

Objective: To study the antihyperglycaemic and wound healing activity of the leaf extracts of Lantana camara Linn. on rats. Materials and methods: Antihyperglycaemic activity of the aqueous extract of the leaves was evaluated by using both normoglycaemic and alloxan induced hyperglycaemic rats. The wound healing activity was assessed for both leaf juice and hydroalcoholic (ethanol 50% v/v) extract of the leaves on excised rats. Results: The aqueous extract was found to produce significant reduction of blood glucose concentration between 2-4 h of administration in alloxan induced hyperglycaemic rats at tested dose levels. However, in normoglycaemic animals, the extract at 400mg/kg produced significant reduction of blood glucose between 2-4 h of administration. In the wound healing studies, the leaf juice was found to be more active than the extract. Conclusion: In the light of the alarming toxicity of the plant, the use of this plant in whole or any part there of need to be carefully regulated until the toxic principles of the plant are identified and removed, to ensure a safe and effective treatment for diabetes.

Purpose : To investigate the anti-inflammatory and analgesic activities of the Amorphophallus Bulbifer in Wistar rats and mice. Methods : The anti-inflammatory activity of the hydroalcohol extract of A. bulbifer whole plant at dose levels of 100 and 200 mg/kg p.o. in rats was determined with a plethysmograph paw volume difference of the animals pre- and post-treatment. Ibuprofen (10 mg/kg) was employed as reference standard. Analgesic activity was evaluated using tail flick and tail immersion techniques, by measuring the reaction time of the animals treated with either standard or extract. Pentazocin (30 mg/kg) was used as reference standard. Results : The extract showed significant anti-inflammatory and analgesic activities at the two test dose levels at the 4th hour (p < 0.001). The extract exhibited anti inflammatory activity of 56.5 (p < 0.001) and 57.1 % (p < 0.001) inhibition compared to the control group in the carrageenan and histamine-induced inflammation model at a dose of 200 mg/kg. For analgesic activity, the extract showed reaction times of 7.33 (p < 0.001) and 7.83 (p < 0.001) min in the tail flick and tail immersion models, respectively, at a dose of 200 mg/kg while the normal and reference groups exhibited reaction times of 2.16, 2.66 and 8.16 (p < 0.001) and 8.5 (p < 0.001) in the tail flick and tail immersion methods, respectively. Conclusion : Based on the findings, it can be concluded that Amorphophallus bulbifer possesses antiinflammatory and analgesic properties and this lends some support for its use in traditional medical practice. Keywords : Amorphophallus bulbifer, Anti-inflammatory activity, Analgesic activity

Objective : The genus Tephrosia is a rich source for unusual flavonoids. The present work is aimed to isolate new molecules of biological interest. Materials and methods : The root powder of T. procumbens was extracted with chloroform and concentrated. The residue was subjected to column chromatography and fractional crystallization by organic solvents and their mixtures of increasing polarity which afforded crystalline compounds and were identified by spectroscopic methods. Results and conclusions : Among the isolates, two candidates calopogonium isoflavone B and 2', 7' 8-trimethoxy-4' , 5' -methylenedioxy isoflavone are reported for the first time from this species.

The mast cell-mediated allergic reactions are involved in many allergic diseases, such as asthma, allergic rhinitis and sinusitis. Stimulation of mast cells initiates the process of degranulation, resulting in the release of mediators such as histamine and an array of inflammatory cytokines. In this report, we investigated the effect of gossypin (a biflavonoid) and suramin (a synthetic polysulphonated naphtylurea) on the mast cell-mediated allergy model, and studied the possible mechanism of their action. Both gossypin and suramin inhibited (P0.001) compound 48/80-induced systemic anaphylaxis reactions, antiprurities (P0.001) and reduced the histamine release in rats. Further, both showed significant (P0.001) protection against rat peritoneal mast cells activated by compound 48/80. Thus, our findings provide evidence that gossypin and suramin inhibit mast cell-derived allergic reactions.

A new compound, (2 S)- p-hydroxyphenethyl 2-bromo-2-methyldodeconate (1) and 7,3′-dimethoxy-5,4′-dihydroxy flavone, together with lupeol and stigmasterol were isolated from the stem bark of Citharexylum fruticosum (Verbenaceae). The structures of the compounds were established on the basis of the interpretation of NMR (1H, 13C, COSY and HMBC) spectra, as well as low and high-resolution mass spectrometric data. In this paper, we report on the structure elucidation of 1.

Ethnopharmacological relevance Traditionally Berberis aristata is employed for its supposed properties in treatment of joint pain and also used in alleviating symptoms of menopause. Aim of the study The aim of the present study is to evaluate the antiosteoporotic effect of Berberis aristata in ovariectomized (OVX) rats. Materials and methods Sprague–Dawley rats were divided into sham and OVX groups. The OVX rats were further divided into four groups, which received standard estrogen (0.0563 mg/kg) and 100, 300, and 500 mg/kg aqueous-methanol extract of Berberis aristata, daily for 42 days. The uterine weight, bone loss, ash content, biomechanical, biochemical and histopathological observation were carried out for antiosteoporotic activity. Results The experimental animals treated with Berberis aristata aqueous-methanol extract showed dose dependent activity. The significant increase in uterine weight, femur BMD, ash content and lumbar hardness were observed. In addition, increased levels of calcium and phosphorus in serum and significant decreased in urine were observed as compared to control OVX group. The histopathological results also confirm the protective effect of extract. Conclusion The present findings strongly suggest that Berberis aristata possess the potent antiosteoporosis activity in ovariectomized rats and substantiates the ethnic use in treatment of postmenopausal osteoporosis.

A new phenolic glucoside, ( rel)-2-(4′,6′-dibenzoyl-β-glucopyranosyloxy)-7-(1α-hydroxy-2α-ethoxy-6α-acetyloxy-3-oxocyclohex-4-enoyl)-benzyl alcohol (Flacourticin) (1) and the known, 2-(4′,6′-dibenzoyl-β-glucopyranosyl)-5-hydroxy benzyl alcohol (4′-benzoylpoliothrysoside) (2) together with the new, (2E)-heptyl-3-(3,4-dihydroxyphenyl) acrylate (3), (+)-catechin (4) and sitosterol-β-D-glucoside were isolated from Flacourtia indica. Their structures were assigned on the basis of 1D, 2D-NMR and as well by analysis of the LC-ESIMS data. The isolated compounds (1-4) were evaluated for α,α-diphenyl-β-picrylhydrazyl (DPPH) radical scavenging activity, and 3 was found to be two-fold less potent, with an IC50 =12.01 μg/mL, compared to the positive control, Rutin, (IC50 = 5.83 μg/mL).

1-((Substituted)methyl)quinoxaline-2,3(1H,4H)-dione (2a–e) and 1-((substituted)acryloyl)quinoxaline-2,3(1H,4H)-dione (4a–c) were synthesized from quinoxaline-2,3(1H,4H)-dione 1 and evaluated for their antimicrobial activities. Results of the antitubercular screening against Mycobacterium tuberculosis H37Rv showed that the compounds 2b, 3, and 4a were the most effective, with minimum inhibitory concentrations of 8.012, 8.561, and 8.928 μg/ml, respectively. All the compounds exhibited significant antibacterial and considerable antifungal activities.

A benzil, calophione A, 1-(6′-Hydroxy-1′,3′-benzodioxol-5′-yl)-2-(6″-hydroxy-2″-isopropenyl-2″,3″-dihydro-benzofuran-5″-yl)-ethane-1,2-dione and three coumestan derivatives, tephcalostan B, C and D were isolated from the roots of Tephrosia calophylla. Their structures were deduced from spectroscopic data, including 2D NMR 1 H– 1 H COSY and 13 C– 1 H COSY experiments. Compounds were evaluated for cytotoxicity against RAW (mouse macrophage cells) and HT-29 (colon cancer cells) cancer cell lines and antiprotozoal activity against various parasitic protozoa. Calophione A exhibited significant cytotoxicity with IC 50 of 5.00 (RAW) and 2.90 μM (HT-29), respectively.

Six quinones were isolated from the chloroform extract of the roots of Diospyros sylvatica and identified as 2-methyl-anthraquinone, plumbagin, diosindigo, diospyrin, isodiospyrin and microphyllone. The effect of the root extract on the orientation and survival of the subterranean termite, Odontotermes obesus was tested. In addition, four of these quinones were tested on the survival of the subterranean termite. In a direct-choice experiment, exposure to an extract-treated filter disc had a significantly repellent effect over the solvent-treated filter disc. The no-choice experiment revealed the toxic property of the extract as well as the tested quinones and showed high mortality of the O. obesus workers after 48 h on forced exposure. The major termiticidal components identified were plumbagin, isodiospyrin and microphyllone while diospyrin was not toxic to termites at the concentration tested. All the quinones are reported for the first time from D. sylvatica.

Chemical examination of the chloroform extract of the roots of Milletia auriculata has yielded three new prenylated isoflavones in addition to the previously reported isoflavones isoauriculatin, auriculin, millettin, auriculatin, scandenone and the rotenoid sumatrol.