Total Vaginectomy in a True Hermaphrodite: A Case Report.

A case is reported herein of a true hermaphrodite (TH) with an ovotestis, a uterus, a vagina, and an underdeveloped phallus. The patient was raised by his parents as a male, based on the presence of a phallus with ambiguous genitalia. He started experiencing breast enlargement at the age of 14 and menarche by the age of 17. He was reviewed using ultrasound, magnetic resonance imaging of the abdomen, and karyotyping, and the reports showed evidence of Mullerian structures and 46 XX karyotyping. Based on the preferences of the patient and his parents and their psychological outlook toward the male gender, a total mastectomy, hysterectomy, bilateral gonadectomy, and total vaginectomy were performed. This was followed by reconstruction of the male genitalia and supplemented with male hormone replacement therapy. Accordingly, a TH was assigned a male gender.

Design, synthesis and evaluation of 1-(1,5-bis(4-substituted phenyl)-2-methyl-1H-pyrrol-3-yl)-N-methylmethanamines as SERT inhibitors with potential antidepressant action.

BM212 is a potent anti-TB agent with pharmacophoric features similar to the antidepressant drug sertraline. The shape-based virtual screening of the DrugBank database on BM212 resulted in the identification of several CNS drugs with appreciable Tanimoto scores. The docking simulations also ascertained the selectivity of BM212 towards the serotonin reuptake transporter protein (SERT) with a docking score of -6.51 kcal mol-1. Based on the SAR data available for sertraline and other antidepressant drugs, we designed, synthesized and screened twelve 1-(1,5-bis(4-substituted phenyl)-2-methyl-1H-pyrrol-3-yl)-N-methylmethanamines (SA-1 to SA-12) for in vitro SERT inhibition and in vivo antidepressant activity. The compounds were screened for in vitro 5HT reuptake inhibition using the platelet model. Among the screened compounds, (1-(1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)-N-methylmethanamine) showed the same serotonin uptake inhibition (absorbance 0.22) as that of the standard drug sertraline (absorbance 0.22). BM212 had an effect on 5-HT uptake, albeit a weaker one compared to the standard (absorbance 0.671). Further, SA-5 was screened for in vivo antidepressant activity using the unpredictable chronic mild stress (UCMS) protocol to induce depression in mice. The effect of BM212 and SA-5 on the behaviour of the animals was assessed and compared against the standard drug sertraline. SA-5 at 20 mg per kg body weight was found to have a statistically significant impact on the behaviour of depressed animals.

Preliminary Study on the Effect of Nitrogen Fertilisation on Phytochemical Content Quality of Gynura procumbens.

The study was carried out to examine the effects of nitrogen (N) fertilisation on phytochemical content quality, to determine types of phytochemicals compositions, and to establish phytochemicals marker compounds in Gynura procumbens. In this two factors study, three stages of harvesting (H) time and three rates of N were laid out according to Randomised Complete Block Design (RCBD). Physiological and biochemical attributes were recorded to exhibit the trend for plant quality. The results showed that, N has affected phytochemical content significantly (p < 0.05) with stronger effect on physiological and biochemical attributes (p < 0.01). The results suggested that 0 and 90 kg/ha N, respectively are highly and least effecting the Photo, Cond, TChlC, TCC, TPrc, TLiC, TPC and TFC.

Kajian ini dijalankan untuk mengkaji kesan baja nitrogen (N) terhadap kualiti kandungan fitokimia, menentukan jenis komposisi fitokimia dan menentukan sebatian penanda fitokimia dalam Gynura procumbens. Kajian ini melibatkan dua faktor; masa penuaian dan kadar N, dan mengikut RCBD. Kesan-kesan terhadap faktor fisiologi dan biokimia tumbuhan telah direkodkan dalam tiga peringkat penuaian untuk memperlihatkan corak dan kualiti pertumbuhan dan kandungan fitokimia. Nitrogen memberi kesan yang jelas terhadap kandungan fitokimia (p < 0.05), dengan kesan yang signifikan terhadap faktor fisiologi dan biokimia (p < 0.01) tumbuhan. Keputusan menunjukkan bahawa 0 dan 90 kg/ha N masing-masing memberi kesan yang sangat tinggi dan paling sedikit terhadap Photo, Cond, TChlC, TCC, TPrC, TliC, TPC dan TFC.

Altered kinetics of circulating progenitor cells in cardiopulmonary bypass (CPB) associated vasoplegic patients: A pilot study.

Vasoplegia observed post cardiopulmonary bypass (CPB) is associated with substantial morbidity, multiple organ failure and mortality. Circulating counts of hematopoietic stem cells (HSCs) and endothelial progenitor cells (EPC) are potential markers of neo-vascularization and vascular repair. However, the significance of changes in the circulating levels of these progenitors in perioperative CPB, and their association with post-CPB vasoplegia, are currently unexplored. We enumerated HSC and EPC counts, via flow cytometry, at different time-points during CPB in 19 individuals who underwent elective cardiac surgery. These 19 individuals were categorized into two groups based on severity of post-operative vasoplegia, a clinically insignificant vasoplegic Group 1 (G1) and a clinically significant vasoplegic Group 2 (G2). Differential changes in progenitor cell counts during different stages of surgery were compared across these two groups. Machine-learning classifiers (logistic regression and gradient boosting) were employed to determine if differential changes in progenitor counts could aid the classification of individuals into these groups. Enumerating progenitor cells revealed an early and significant increase in the circulating counts of CD34+ and CD34+CD133+ hematopoietic stem cells (HSC) in G1 individuals, while these counts were attenuated in G2 individuals. Additionally, EPCs (CD34+VEGFR2+) were lower in G2 individuals compared to G1. Gradient boosting outperformed logistic regression in assessing the vasoplegia grouping based on the fold change in circulating CD 34+ levels. Our findings indicate that a lack of early response of CD34+ cells and CD34+CD133+ HSCs might serve as an early marker for development of clinically significant vasoplegia after CPB.

Effects of some gelling agents and their concentrations on conversion of oil palm polyembryoids into plantlets.

Oil palm, a tropical plant with an economic life of 20-25 years, is on high demand since its oil (palm oil) is now considered to be the world's most consumed oil. Despite the high potential for the use of clonal materials, the tissue culture technique for oil palm is difficult and laborious. One of the key steps of the process is the conversion of polyembroids into plantlets. Gelling agent has been implicated to play a role in ensuring the conversion of oil palm polyembryoids into complete plantlets. In the present study, for the first time, we report the effects of two types of common gelling agents, Agar Type 900 and Gelrite®, for enhanced conversion of oil palm polyembryoids into plantlets. Polyembryoids, developed from embryonic calli, were cultured and incubated on Murashige and Skoog semisolid media supplemented with Agar (Type 900) at 8-12 g/l or gellan gum (Gelrite®) 1.5-3.5 g/l. The effects of gelling agents on polyembryoid conversion was assessed based on the percentages of viability, survival, and polyembryoids that swelled, enlarged, and turned green, as well as on the basis of morphological characteristics, viz, number of shoots, leaves, roots, secondary somatic embryos, and callus formation. Based on the results of this study, in comparison to Agar Type 900, the Gelrite® with 3.5 g/l concentration was chosen as an effective gelling agent for conversion of polyembryoids into plantlets, since it resulted in 100% survival with 53.3% completely developed plantlets (multiple shoots with roots). The successful conversion of polyembryoids into plantlets achieved in this study, using the optimized gelling agent could be useful for pre-storage or post-storage conversion in many other plant species as well.

Cryopreservation of oil palm (Elaeis guineensis Jacq.) polyembryoids via encapsulation-desiccation.

The current report assesses the efficiency of encapsulation-desiccation protocol to cryopreserve oil palm (Elaeis guineensis Jacq.) polyembryoids. Specifically identified polyembryoids, comprising of haustorium and torpedo-shaped structures, were encapsulated [comprising 3% (w/v) sodium alginate and 100 mM CaCl2]. Calcium alginate-encapsulated and sucrose-precultured polyembryoids were subjected to different spans of desiccation in a laminar air-flow cabinet, followed by freezing in liquid nitrogen. The effect of sucrose preculture (with gradual exposure to 0.3, 0.5, 0.75 and 1 M for 7 days) and dehydration periods (0-10 h) under sterile air-flow on post-freezing survival and regrowth of encapsulated polyembryoids were studied. Cryopreserved and thawed polyembryoids (initially precultured in sucrose, followed by 9 h air-desiccated to 23.3% moisture content) displayed the highest survival percentage (73.3%) and regeneration (of shoot, root and secondary somatic embryo) on Murashige and Skoog regrowth medium containing sucrose (0.3-1 M) and 0.2 mg/l 2,4-dichlorophenoxy acetic acid. In addition, ultrastructural study using scanning electron microscopy exhibited successful revival of cryopreserved polyembryoids, owing to retention of cellular membrane stability through optimized and protected (encapsulated) desiccation. The present study thus substantiates the potential of this encapsulation-desiccation procedure in cryopreservation of oil palm polyembryoids for long-term conservation programs.

Esophagotomy in a domestic fowl: a rare case report.

BACKGROUND: Foreign body in esophagus in birds is rarely reported in literature. Most common site of foreign body in birds is proventriculus and ventriculus. The purpose of this study is to discuss the diagnosis of a large sharp foreign body in the distal third of the neck by plain radiography and its retrieval through esophagotomy and subsequent survival of the fowl. CASE DESCRIPTION: An Aseel breed of domestic fowl (Gallus domesticus) was referred to the surgery department with a history of swelling in the neck and subsequent anorexia since 24 h, but normal water intake. Radiological examination revealed a large fish bone in esophagus. Because of the sharp edges of the foreign body esophagotomy was performed rather than per os (po) retrieval or milking of the foreign body into the crop and performing an ingluviotomy. FINDINGS/TREATMENT AND OUTCOME: Esophagotomy was performed under local infiltration using a diluted solution of lignocaine. Fish bone pieces were retrieved from the esophagus of the fowl. The esophagotomy incision was closed in two layers using polyglactin 910 no: 3-0. Postoperatively, the owner was advised to administer Enrofloxacin po at 10 mg/kg body weight (BW)/day for seven days and Tramadol (10 mg/kg BW, BID) for three days in water. This case was followed up for 8 months. There were no complications noticed by the owner. CONCLUSION: It could be concluded that prompt intervention and surgical management may be necessary for retrieval of sharp esophageal foreign bodies lodged in the distal cervical esophagus of domestic fowl.

Encapsulation of in vitro Plectranthus amboinicus (Lour.) Spreng. shoot apices for propagation and conservation.

This investigation demonstrates an efficient method of propagation, short-term conservation, and germplasm exchange for Plectranthus amboinicus (Lour.) Spreng. encapsulated propagules. In vitro-derived shoot apices (shoot tips and nodal segments) which showed 100% survival on MS medium supplemented with 0.4 mg/L 6-benzylaminopurine were selected for encapsulation studies. Shoot apices measuring about 3-5 mm in size showed the ability to break the beads and exhibited 100% survival and regrowth. The combination of 3% (w/v) sodium alginate and 100 mM CaCl2 was found to be ideal for forming uniformally spherical beads, and successive preservation of encapsulated shoot apices into plantlets. The encapsulated shoot tips were relatively more effective than the nodal segments in terms of shoot growth and multiplication. Encapsulated shoot tips retained the ability to regrow (63.3%) for up to 40 days when maintained at 4 °C. Encapsulated shoot tips effectively converted into plantlets on agar medium (78%) and peat moss (58%) under in vitro conditions. Encapsulated shoot tips on agar medium showed a higher shoot regeneration (9.91 ± 0.15 shoots per explant) ability than the peat moss (5.71 ± 0.34 shoots per explant), while the highest rooting (12.16 ± 0.23 roots per explant) was observed on peat moss. Thus, calcium alginate encapsulation holds latent qualities that could be explored to develop a future alternative method of propagation, short-term storage and germplasm distribution for elite genotypes of Plectranthus sp.

Amarogentin, a secoiridoid glycoside, activates AMP- activated protein kinase (AMPK) to exert beneficial vasculo-metabolic effects.

INTRODUCTION: AMP-activated protein kinase (AMPK) is a drug target for treatment of metabolic and cardiovascular complications. Extracts of Gentianaceace plants exhibit anti-diabetic and anti-atherosclerotic effects, however, whether their phyto-constitutents activate AMPK remains to be determined. METHODS: Molecular docking of Gentiana lutea constituents was performed with crystal structure of human α2ß1γ1 trimeric AMPK (PDB ID: 4CFE). Binding of Amarogentin (AG) to α2 subunit was confirmed through isothermal titration calorimetry (ITC) and in vitro kinase assays were performed. L6 myotube, HUH7 and endothelial cell cultures were employed to validate in silico and in vitro observations. Lipid lowering and anti-atherosclerotic effects were confirmed in streptozotocin induced diabetic mice via biochemical measurements and through heamatoxylin and eosin, Masson's trichrome and Oil Red O staining. RESULTS: AG interacts with the α2 subunit of AMPK and activates the trimeric kinase with an EC50 value of 277 pM. In cell culture experiments, AG induced phosphorylation of AMPK as well as its downstream targets, acetyl-coA-carboxylase (ACC) and endothelial nitric oxide synthase (eNOS). Additionally, it enhanced glucose uptake in myotubes and blocked TNF-α induced endothelial inflammation. Oral supplementation of AG significantly attenuated diabetes-mediated neointimal thickening, and collagen and lipid deposition in the aorta. It also improved circulating levels of lipids and liver function in diabetic mice. CONCLUSION: In conclusion, AG exerts beneficial vasculo-metabolic effects by activating AMPK. GENERAL SIGNIFICANCE: Amarogentin, a naturally occurring secoiridoid glycoside, is a promising lead for design and synthesis of novel drugs for treatment and management of dyslipidemia and cardiovascular diseases.

Biosynthesis, Characterization and Biological Activities of Silver Nanoparticles from Pogostemon cablin Benth. Methanolic Leaf Extract.

This study reports the biosynthesis of silver nanoparticles (AgNPs) using methanolic leaf extract of Pogostemon cablin Benth. (Patchouli) as a reducing agent, and their potent biological (antibacterial, antioxidant and anticancer) activities. The P. cablin extract when exposed to silver nitrate reduced silver ions to form crystalline AgNPs within 1 h of incubation at room-temperature. UV-visible spectra showed a sharp surface plasmon resonance (SPR) at around 430 nm for the biosynthesized AgNPs and the XRD pattern indicated the crystalline planes of the face centered cubic silver. The FE-SEM analysis revealed the occurrence of predominant spherical shaped AgNPs with a huge disparity in their particle size distribution with an average size of 25 nm, while, the FTIR data confirmed the bio-reduction and capping of AgNPs by several phytocompounds present in the methanolic leaf extract. AgNPs effectively inhibited the growth of all the tested human pathogenic bacterial strains (Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli), while, the methanolic leaf extract failed to inhibit the growth of S. aureus and P. aeruginosa. AgNPs showed the highest free radical scavenging activity (79.0 ± 0.76%) compared to methanolic leaf extract (68.3 ± 0.68%) at 100 µg/ml. Further, the cytotoxicity study using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) confirmed that AgNPs successfully inhibited the human colon adenocarcinoma cell line (HT-29) in a dose dependent manner. At higher concentrations (500 µg/ml), only 4% of cells survived after 72 hrs of exposure with IC50 value of 120 µg/ml. Thus, these findings offer a new source of biomolecules with diverse biological activities.

Dispersion aided tenside disintegration of seagrass Syringodium isoetifolium: Towards biomethanation, kinetics, energy exploration and evaluation.

In this study, an attempt was made to enhance the biomethanation potential of seagrass (Syringodium isoetifolium) by the aid of disperser-tenside (polysorbate 80) disintegration for the first time in literature. A disperser rpm of 10,000 for 20 min and PS 80 dose of 0.000864 g/g TS were selected as ideal parameters for effectual seagrass biomass disintegration. Dispersion aided tenside disintegration (DTD) with a disperser energy consumption of 349 kJ/kg TS, was observed to be efficacious with a biomass lysis rate of 25.6%. The impact of DTD on bioacidification and biomethanation assay with respect to volatile fatty acids concentration (1100 mg/L) and methane generation (0.256 g/g COD), was greater than dispersion disintegration (DD) (800 mg/L; 0.198 g/g COD). Thus, S. isoetifolium is considered as a promising substrate to attain the third generation biofuel goals in the near future.

Production of bioactive cyclotides in somatic embryos of Viola odorata.

Viola odorata L. (Violaceae), an Indian medicinal plant, contains a plethora of cyclotides, which are a class of cyclic peptides derived from plants, possessing several applications. Somatic embryo culture of V. odorata was developed, via indirect somatic embryogenesis, to serve as an alternative to natural plant biomass for sustainable and continuous production of its bioactive ingredients, such as cyclotides. Among the various combinations of phytohormones tested, Murashige and Skoog medium supplemented with 1 mg/l thidiazuron gave rise to the maximum frequency of induction (86.7%) and a high number of somatic embryos (3) from an embryogenic callus. Identification and characterization of cyclotides in the somatic embryos were carried out using a Fourier transform mass spectrometer coupled with liquid chromatography (LC-FTMS). Among the cyclotides identified in the study, few were found to be exclusively present in the somatic embryo culture. Furthermore, the relative abundance of the cyclotides was higher in somatic embryo extract than in the natural plant extract. The biological activities (cytotoxic, haemolytic and antimicrobial) of the somatic embryos and the parent plant were compared. Unlike the natural plants, the somatic embryo extracts demonstrated specificity i.e. they were found to be potent against cancerous cells but not against non-cancerous cell line or red blood cells. In contrast to the plant extract, the somatic embryos extracts were found to be potent against Escherichia coli and Staphylococcus aureus. These results suggest that somatic embryos of V. odorata (rich in cyclotides) can be used as an alternative to plant biomass for its therapeutic applications and germplasm conservation.

Anticancer potential of rosmarinic acid and its improved production through biotechnological interventions and functional genomics.

Rosmarinic acid (RA) is a highly valued natural phenolic compound that is very commonly found in plants of the families Lamiaceae and Boraginaceae, including Coleus blumei, Heliotropium foertherianum, Rosmarinus officinalis, Perilla frutescens, and Salvia officinalis. RA is also found in other members of higher plant families and in some fern and horned liverwort species. The biosynthesis of RA is catalyzed by the enzymes phenylalanine ammonia lyase and cytochrome P450-dependent hydroxylase using the amino acids tyrosine and phenylalanine. Chemically, RA can be produced via methods involving the esterification of 3,4-dihydroxyphenyllactic acid and caffeic acid. Some of the derivatives of RA include melitric acid, salvianolic acid, lithospermic acid, and yunnaneic acid. In plants, RA is known to have growth-promoting and defensive roles. Studies have elucidated the varied pharmacological potential of RA and its derived molecules, including anticancer, antiangiogenic, anti-inflammatory, antioxidant, and antimicrobial activities. The demand for RA is therefore, very high in the pharmaceutical industry, but this demand cannot be met by plants alone because RA content in plant organs is very low. Further, many plants that synthesize RA are under threat and near extinction owing to biodiversity loss caused by unscientific harvesting, over-collection, environmental changes, and other inherent features. Moreover, the chemical synthesis of RA is complicated and expensive. Alternative approaches using biotechnological methodologies could overcome these problems. This review provides the state of the art information on the chemistry, sources, and biosynthetic pathways of RA, as well as its anticancer properties against different cancer types. Biotechnological methods are also discussed for producing RA using plant cell, tissue, and organ cultures and hairy-root cultures using flasks and bioreactors. The recent developments and applications of the functional genomics approach and heterologous production of RA in microbes are also highlighted. This chapter will be of benefit to readers aiming to design studies on RA and its applicability as an anticancer agent.

Enhancing biomethanation from dairy waste activated biomass using a novel EGTA mediated microwave disintegration.

A novel approach to explore the impact of calcium specific chelant - Ethylene glycol tetra acetic acid (EGTA) on deflocculation followed by biomass disintegration using microwave (MW) was investigated. In the first phase of the study, the EGTA dosage of 0.012 g/g suspended solids (SS) was found to be optimal for disassociating the biomass. Subsequent disintegration of biomass in microwave (EGTA-MW) yielded a biomass lysis and solids reduction of about 39.7% and 30.5%. EGTA-MW disintegration reduces the amount of specific energy required to disintegrate the biomass from 18,900 kJ/kg TS to 13,500 kJ/kg TS, when compared to control. The impact of EGTA-MW disintegration on anaerobic digestion was also evident from its methane yield (235.3 mL/g VS) which was 36.2% higher than control. An economic assessment of this study provides a net profit of 8.48 €/ton in EGTA-MW and highly endorsed for biomass disintegration.

Biogenic Synthesis, Characterization and Evaluation of Silver Nanoparticles from Aspergillus niger JX556221 Against Human Colon Cancer Cell Line HT-29.

Nanobiotechnology has emerged as a promising technology to develop new therapeutically active nanomaterials. The present study was aimed to biosynthesize AgNPs extracellularly using Aspergillus niger JX556221 fungal extract and to evaluate their anticancer potential against colon cancer cell line, HT-29. UV-visible spectral characterization of the synthesized AgNPs showed higher absorption peak at 440 nm wavelength. Transmission Electron Microscopy (TEM) analysis revealed the monodispersed nature of synthesized AgNPs occurring in spherical shape with a size in the range of 20-25 nm. Further, characterization using Energy Dispersive Spectroscopy (EDX) confirmed the face-centred cubic crystalline structure of metallic AgNPs. FTIR data revealed the occurrence of various phytochemicals in the cell free fungal extract which substantiated the fungal extract mediated AgNPs synthesis. The cytotoxic effect of AgNPs was studied by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The results evidenced the cytotoxic effect of AgNPs on HT-29 cell lines in a dose dependent manner. The highest activity was found at 100 µg/ml concentration after 24 h of incubation. Use of propidium iodide staining examination method confirmed the cytotoxic effect of AgNPs through inducing cell apoptosis. AgNPs cytotoxicity was found to be through elevating reactive oxygen species (ROS), and caspase-3 activation resulting in induced apoptosis. Therefore, this research finding provides an insight towards the development of novel anticancer agents using biological sources.

Potential applications of lactic acid bacteria and bacteriocins in anti-mycobacterial therapy

Tuberculosis (TB) is a communicable disease caused by Mycobacterium tuberculosis (M. tuberculosis). WHO estimated that 10.4 million new (incident) TB cases worldwide in year 2016. The increased prevalence of drug resistant strains and side effects associated with the current anti-tubercular drugs make the treatment options more complicated. Hence, there are necessities to identify new drug candidates to fight against various sub-populations of M. tuberculosis with less or no toxicity/side effects and shorter treatment duration. Bacteriocins produced by lactic acid bacteria (LAB) attract attention of researchers because of its 'Generally recognized as safe' status. LAB and its bacteriocins possess an effective antimicrobial activity against various bacteria and fungi. Interestingly bacteriocins such as nisin and lacticin 3147 have shown antimycobacterial activity in vitro. As probiotics, LAB plays a vital role in promoting various health benefits including ability to modulate immune response against various infectious diseases. LAB and its metabolic products activate immune system and thereby limiting the M. tuberculosis pathogenesis. The protein and peptide engineering techniques paved the ways to obtain hybrid bacteriocin derivatives from the known peptide sequence of existing bacteriocin. In this review, we focus on the antimycobacterial property and immunomodulatory role of LAB and its metabolic products. Techniques for large scale synthesis of potential bacteriocin with multifunctional activity and enhanced stability are also discussed.

An insight into the genotoxicity assessment studies in dipterans.

The dipterans have been widely utilized in genotoxicity assessment studies. Short life span, easy maintenance, production of large number of offspring in a single generation and the tissues with appropriate cell populations make these flies ideal for studies associated to developmental biology, diseases, genetics, genetic toxicology and stress biology in the group. Moreover, their cosmopolitan presence makes them suitable candidate for ecological bio-monitoring. An attempt has been made in the present review to reveal the significance of dipteran flies for assessing alterations in genetic content through various genotoxicity biomarkers and to summarize the gradual advancement in these studies. Recent studies on genotoxicity assays in dipterans have opened up a broader perspective for DNA repair related mechanistic studies, pre-screening of chemicals and environmental bio-monitoring. Studies in dipterans, other than Drosophila may be helpful in using them as an alternative model system for assessment of genotoxicity, especially at the gene level and further extension of these studies give a future insight to develop new strategies for maintaining environment friendly limits of the toxicants.

Synthesis of different heterocycles-linked chalcone conjugates as cytotoxic agents and tubulin polymerization inhibitors.

A series of new heterocycles-linked chalcone conjugates has been designed and synthesized by varying different alkane spacers. These conjugates were tested for their in vitro cytotoxic potential against a panel of selected human cancer cell lines namely, lung (A549 and NCI-H460), prostate (DU-145 and PC-3), colon (HCT-15 and HCT-116), and brain (U-87 glioblastoma) by MTT assay. Notably, among all the tested compounds, 4a exhibited potent cytotoxicity on NCI-H460 (lung cancer) cells with IC50 of 1.48±0.19µM. The compound 4a showed significant inhibition of tubulin polymerization and disruption of the formation of microtubules (IC50 of 9.66±0.06µM). Moreover, phase contrast microscopy and DAPI staining studies indicated that compound 4a can induce apoptosis in NCI-H460 cells. Further, the flow-cytometry analysis revealed that compound 4a arrests NCI-H460 cells in the G2/M phase of the cell cycle. In addition, molecular docking studies of the most active compounds 4a and 4b into the colchicine site of the tubulin, revealed the possible mode of interaction by these new conjugates.

Leptadenia reticulata (Retz.) Wight & Arn. (Jivanti): Botanical, Agronomical, Phytochemical, Pharmacological, and Biotechnological Aspects.

Leptadenia reticulata (Retz.) Wight & Arn. (Apocynaceae), is a traditional medicinal plant species widely used to treat various ailments such as tuberculosis, hematopoiesis, emaciation, cough, dyspnea, fever, burning sensation, night blindness, cancer, and dysentery. In Ayurveda, it is known for its revitalizing, rejuvenating, and lactogenic properties. This plant is one of the major ingredients in many commercial herbal formulations, including Speman, Envirocare, Calshakti, Antisept, and Chyawanprash. The therapeutic potential of this herb is because of the presence of diverse bioactive compounds such as α-amyrin, ß-amyrin, ferulic acid, luteolin, diosmetin, rutin, ß-sitosterol, stigmasterol, hentricontanol, a triterpene alcohol simiarenol, apigenin, reticulin, deniculatin, and leptaculatin. However, most biological studies on L. reticulata are restricted to crude extracts, and many biologically active compounds are yet to be identified in order to base the traditional uses of L. reticulata on evidence-based data. At present, L. reticulata is a threatened endangered plant because of overexploitation, unscientific harvesting, and habitat loss. The increased demand from pharmaceutical, nutraceutical, and veterinary industries has prompted its large-scale propagation. However, its commercial cultivation is hampered because of the non-availability of genuine planting material and the lack of knowledge about its agronomical practices. In this regard, micropropagation techniques will be useful to obtain true-to-type L. reticulata planting materials from an elite germplasm to meet the current demand. Adopting other biotechnological approaches such as synthetic seed technology, cryopreservation, cell culture, and genetic transformation can help conservation as well as increased metabolite production from L. reticulata. The present review summarizes scientific information on the botanical, agronomical, phytochemical, pharmacological, and biotechnological aspects of L. reticulata. This comprehensive information will certainly allow better utilization of this industrially important herb towards the discovery of lead drug molecules.

GC-MS Based Metabolite Profiling, Antioxidant and Antimicrobial Properties of Different Solvent Extracts of Malaysian Plectranthus amboinicus Leaves.

This study evaluates the phytochemistry, antioxidant, and antimicrobial effects of Plectranthus amboinicus leaves extracted in different solvents. The methanol extract contained the highest total phenolic (94.37 ± 1.24 mg GAE/g) and flavonoid contents (26.90 ± 1.35 mg RE/g) and exhibited the highest DPPH scavenging activity (90.13 ± 3.32%) followed by the acetone extract (80.23 ± 3.26%) at 500 µg/mL concentration. Similarly, the highest ferric ion reduction potential (849.63 ± 30.95 µM of Fe (II)/g dry weight) was exhibited by the methanol extract followed by the acetone extract (695.92 ± 25.44 µM of Fe (II)/g dry weight). The methanol extract showed greater antimicrobial activity against all the tested pathogens (Bacillus subtilis, Methicillin-resistant Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, and Candida albicans). However, both hexane and acetone extracts failed to inhibit E. coli. S. aureus and C. albicans were more susceptible to all the extracts. Further, GC-MS analysis confirmed the occurrence of a total 46 phytocompounds in different solvent extracts. Some of the major compounds included carvacrol (37.7%), tetracontane (16.6%), squalene (15.6%), tetrapentacontane (13.7%), and Phytol (12.9%). In conclusion, extraction solvents influenced the recovery of phytocompounds and the highest pharmacological activities of the methanol extract could be correlated to the presence of additional bioactive compounds.