In vitro Anti-Leishmanial and Anti-Tumour Activities of a Pentacyclic Triterpenoid Compound Isolated from the Fruits of Dregea volubilis Benth Asclepiadaceae

Purpose: Dregea volubilis Benth, commonly known as Jukti in Bengal, is used in the treatment of boils and abscesses from ancient times. The purpose of this study is to elucidate the active compounds and as well as their anti-leishmanial and anti-tumour activities. Methods: Dried and crushed fruits of Dregea volubilis were extracted by petroleum ether (40 - 60°C); the best solvent system had first been verified by analytical Thin Layer Chromatography (TLC). The extract was subjected to TLC and column chromatography (CC) to isolate the pure compounds. Spectradata were obtained by Infra Red pectroscopy, Mass Spectroscopy and Nuclear Magnetic Resonance - Proton Magnetic Resonance (PMR), Carbon Magnetic Resonance (CMR) and Distortionless Enhancement by Polarization Transfer (DEPT) - for structure elucidation of the isolated compound(s). One of the compounds isolated was screened for anti-leishmanial activity against promastigotes of Leishmania donovani and anti-tumour activity on K562 leukemic cell line.Results: A pentacyclic triterpenoid compound was isolated and designated as taraxerone, and then characterized as d-friedoolean-14-en, 3 one together with ß-sitosterol and a long chain lipid fraction.This compound showed in vitro anti-leishmanial activity against promastigotes of Leishmania donovani (strain AG 83) and anti-tumour activity on K562 leukemic cell line. Conclusion: A pentacyclic triterpenoid compound designated as taraxerone and characterized as Dfriedoolean-14-en, 3 one together was successfully isolated. The structure was determined on the basis of spectral analysis (IR, MASS, NMR (PMR, CMR and DEPT) and the compound demonstrated in vitro anti-leishmanial and anti-tumour activities

Epidural Interventions in the Management of Chronic Spinal Pain: American Society of Interventional Pain Physicians (ASIPP) Comprehensive Evidence-Based Guidelines.

BACKGROUND: Chronic spinal pain is the most prevalent chronic disease with employment of multiple modes of interventional techniques including epidural interventions. Multiple randomized controlled trials (RCTs), observational studies, systematic reviews, and guidelines have been published. The recent review of the utilization patterns and expenditures show that there has been a decline in utilization of epidural injections with decrease in inflation adjusted costs from 2009 to 2018. The American Society of Interventional Pain Physicians (ASIPP) published guidelines for interventional techniques in 2013, and guidelines for facet joint interventions in 2020. Consequently, these guidelines have been prepared to update previously existing guidelines. OBJECTIVE: To provide evidence-based guidance in performing therapeutic epidural procedures, including caudal, interlaminar in lumbar, cervical, and thoracic spinal regions, transforaminal in lumbar spine, and percutaneous adhesiolysis in the lumbar spine. METHODS: The methodology utilized included the development of objective and key questions with utilization of trustworthy standards. The literature pertaining to all aspects of epidural interventions was viewed with best evidence synthesis of available literature and recommendations were provided. RESULTS: In preparation of the guidelines, extensive literature review was performed. In addition to review of multiple manuscripts in reference to utilization, expenditures, anatomical and pathophysiological considerations, pharmacological and harmful effects of drugs and procedures, for evidence synthesis we have included 47 systematic reviews and 43 RCTs covering all epidural interventions to meet the objectives.The evidence recommendations are as follows: Disc herniation: Based on relevant, high-quality fluoroscopically guided epidural injections, with or without steroids, and results of previous systematic reviews, the evidence is Level I for caudal epidural injections, lumbar interlaminar epidural injections, lumbar transforaminal epidural injections, and cervical interlaminar epidural injections with strong recommendation for long-term effectiveness.The evidence for percutaneous adhesiolysis in managing disc herniation based on one high-quality, placebo-controlled RCT is Level II with moderate to strong recommendation for long-term improvement in patients nonresponsive to conservative management and fluoroscopically guided epidural injections. For thoracic disc herniation, based on one relevant, high-quality RCT of thoracic epidural with fluoroscopic guidance, with or without steroids, the evidence is Level II with moderate to strong recommendation for long-term effectiveness.Spinal stenosis: The evidence based on one high-quality RCT in each category the evidence is Level III to II for fluoroscopically guided caudal epidural injections with moderate to strong recommendation and Level II for fluoroscopically guided lumbar and cervical interlaminar epidural injections with moderate to strong recommendation for long-term effectiveness.The evidence for lumbar transforaminal epidural injections is Level IV to III with moderate recommendation with fluoroscopically guided lumbar transforaminal epidural injections for long-term improvement. The evidence for percutaneous adhesiolysis in lumbar stenosis based on relevant, moderate to high quality RCTs, observational studies, and systematic reviews is Level II with moderate to strong recommendation for long-term improvement after failure of conservative management and fluoroscopically guided epidural injections. Axial discogenic pain: The evidence for axial discogenic pain without facet joint pain or sacroiliac joint pain in the lumbar and cervical spine with fluoroscopically guided caudal, lumbar and cervical interlaminar epidural injections, based on one relevant high quality RCT in each category is Level II with moderate to strong recommendation for long-term improvement, with or without steroids. Post-surgery syndrome: The evidence for lumbar and cervical post-surgery syndrome based on one relevant, high-quality RCT with fluoroscopic guidance for caudal and cervical interlaminar epidural injections, with or without steroids, is Level II with moderate to strong recommendation for long-term improvement. For percutaneous adhesiolysis, based on multiple moderate to high-quality RCTs and systematic reviews, the evidence is Level I with strong recommendation for long-term improvement after failure of conservative management and fluoroscopically guided epidural injections. LIMITATIONS: The limitations of these guidelines include a continued paucity of high-quality studies for some techniques and various conditions including spinal stenosis, post-surgery syndrome, and discogenic pain. CONCLUSIONS: These epidural intervention guidelines including percutaneous adhesiolysis were prepared with a comprehensive review of the literature with methodologic quality assessment and determination of level of evidence with strength of recommendations

A Minor Acylated Triterpenoid Saponin from the Seeds of Pithecellobium dulce

A novel acylated triterpenoid saponin, designated pithecelloside, is isolated from the seeds of Pithecellobium dulce and characterised as 3-O-[a-L-arabinopyranosyl-(1 ! 2)-a-L-arabinopyranosyl-(1 ! 6�-b-D-glucopyranosyl]- 21b-O-[(20E)-60-hydroxy-20,60-dimethylocta-20,70-dienoyl]acacic acid 1

A Triterpenoid Saponin Possessing Antileishmanial Activity from the Leaves of Careya Arborea

Bioguided-fractionation of the methanol extract of the leaves of Careya arborea led to isolation of a triterpenoid saponin, designated arborenin, and characterized as 3-O-b-D-glucopyranosyl(1!2)-b-D-glucopyranosyl-2a,3b-dihydroxy-taraxast-20-en-28-oic acid (1), together with desacylescin III (2). The structures were determined on the basis of extensive 2D NMR spectroscopic analysis. The saponin showed in vitro antileishmanial activity against Leishmania donovani (strain AG 83)

Polyoxypregnane glycosides from the flowers of Dregea volubilis

Three novel polyoxypregnane glycosides, volubiloside A, B and C (1–3), were isolated from the flowers of Dregea volubilis Linn., and their structures were elucidated as drevogenin d-3-O-b-d-glucopyranosyl (1!4)-6-deoxy-3-O-methyl-b-d-allopyranosyl (1!4)- b-d-cymaropyranosyl (1!4)-b-d-cymaropyranoside, drevogenin d-3-O-b-d-glucopyranosyl (1!4)-6-deoxy-3-O-methyl-b-d-allopyranosyl (1!4)-b-d-cymaropyranosyl (1!4)-b-d-digitoxopyranoside and drevogenin P-3-O-b-d-glucopyranosyl (1!4)-6-deoxy- 3-O-methyl-b-d-allopyranosyl (1!4)-b-d-cymaropyranosyl (1!4)-b-d-cymaropyranoside, respectively, on the basis of extensive NMR experiments, MALDI-TOF MS, and some chemical strategies

Woodfordia Fruticosa: Traditional Uses and Recent Findings

Woodfordia fruticosa Kurz of the family Lythraceae is a plant of tropical and subtropical region with a long history of medicinal use. A wide range of chemical compounds including tannins (especially those of macrocyclic hydrolysable class), flavonoids, anthraquinone glycosides, and polyphenols have been isolated from this species in recent times. Extracts and metabolites of this plant, particularly those from flowers and leaves, possess useful pharmacological activities. A comprehensive account of the chemical constituents and the biological activities is presented and a critical appraisal of the ethnopharmacological issues is included in view of the many recent findings of importance on this plant

Efficient Synthesis of Novel Tetrahydropyrrolo[30,40:3,4]Pyrrolo[2,1-a] Isoquinoline Derivatives via a Simple and Convenient MCR in Aqueous Micellar System

A simple and efficient one-pot three component synthesis of tetrahydropyrrolo[30,40:3,4]pyrrolo[2,1- a]isoquinoline-9,11-dione derivatives has been achieved from variously substituted isoquinolines, 2- bromo acetophenone and N-aryl maleimide derivatives in an aqueous micellar medium. The synthesis represents an environmentally benign alternative to classical method

Facile Synthesis of Seven to Nine-Membered-Fused Tricyclic Quinolones and Quinolinium Salts under Phase Transfer Catalyzed Conditions

Phase transfer catalyzed one-pot syntheses of fused oxazepino, oxazocino, and oxazonino quinolinium cations and quinolones were achieved from 8-hydroxy quinoline derivatives with 1,u-dihaloalkanes. Structures of all the products were elucidated by spectroscopic analysis. Single crystal X-ray crystallographic analysis of three compounds and graphical superposition of the structures indicate that products having sevenmembered ring are less planar compared to the product having eight-membered ring

Synthesis of a Novel Quinoline Derivative, 2-(2-Methylquinolin-4- ylamino)-N-phenylacetamide—A Potential Antileishmanial Agent

Some novel quinoline derivatives were prepared and tested for antileishmanial activity. 2-(2-Methylquinolin-4-ylamino)- N-phenylacetamide (2) was found to be significantly more active than the standard antileishmanial drug sodium antimony gluconate (SAG) in reducing the parasite load both in the spleen and liver at a much lower concentration in hamster models. The results suggest that the compound could be exploited as an antileishmanial drug. # 2002 Elsevier Science Ltd. All rights reserved

Synthesis of Novel Benzoxazocino Quinoliniums and Quinolones Under PTC Conditions and Their Application in Suzuki Cross Coupling Reaction For the Construction of Polynuclear Heteroaromatics

A general and highly efficient synthetic protocol under phase transfer catalytic condition has been established for the synthesis of fused tetracyclic oxazocinoquinolone analogues which served as the precursors for novel biaryl quinolones using microwave assisted Suzuki cross coupling reaction