Quantitative standardization of pharmacologically active components from antiplasmodial plant Solanum nudum Dunal (wild and in vitro)

Solanum nudum Dunal (Solanaceae) is most commonly known and used by the population of the colombian Pacific coast as an antimalarial treatment. This article study into optimization and quantitative analysis of compounds steroidal over time of development of this species when grown in vitro and wild. A new steroidal compound named SN6 was elucidated by NMR and a new method of quantification of seven steroidal compounds (Diosgenone DONA and six steroids SNs) using HPLC-DAD-MS in extracts of cultures in vitro and wild was investigated. Biology activity of extracts was found to a range of antiplasmodial activity in FCB2 and NF-54 with inhibitory concentration (IC50) between (17.04 -100 μg/mL) and cytotoxicity in U-937 of CC50 (7.18 -104.7 μg/mL). This method creates the basis for the detection of seven sterols antiplasmodial present in extracts from S. nudum plant as a quality parameter in the control and expression of phytochemicals.

A review on the pharmaceutical activity of Solanum surattense

The traditional medicinal plants are believed to be an impotent source of phytochemicals with potential therapeutic effects, and caring for different diseases. The plant Solanum surattense has active phytochemicals like saponins, alkaloid, phenols, solamargine, solasurine, solasonine, gum, ascorbic acid, sterols, torvoside K, torvoside L, khasianine, glycosides, flavonoids, aculeatiside A, solamargine, glycoalkaloid, steroidal compound, steroidal alkaloids, polyphenol (caffeic acid), coumarins (esculentin and aesculin), steroids (carpesterol, campesterol, daucosterol, stigmasterol, cycloortanol, and cholesterol), triterpinins, and sapogenin. This medicinal plant is widespread in pharmaceutics and still presents a large source of active phytochemicals with different activity such as antimicrobial, anti-larvicidal, anthelmintic, antimalarial, antioxidant, antidiabetic, anti-asthmatic, and anti-cancerous. This review of the literature revealed new researches on the phytochemicals of S. surattense that how the active phytochemicals are performed different activities on the molecular level in vital aspects.

Design and In Vivo Pharmacokinetic Evaluation of Triamcinolone Acetonide Microcrystals-Loaded PLGA Microsphere for Increased Drug Retention in Knees after Intra-Articular Injection

A novel polymeric microsphere (MS) containing micronized triamcinolone acetonide (TA) in a crystalline state was structured to provide extended drug retention in joints after intra-articular (IA) injection. Microcrystals with a median diameter of 1.7 μm were prepared by ultra-sonication method, and incorporated into poly(lactic-co-glycolic acid)/poly(lactic acid) (PLGA/PLA) MSs using spray-drying technique. Cross-sectional observation and X-ray diffraction analysis showed that drug microcrystals were evenly embedded in the MSs, with a distinctive crystalline nature of TA. In vitro drug release from the novel MSs was markedly decelerated compared to those from the marketed crystalline suspension (Triam inj.®), or even 7.2 μm-sized TA crystals-loaded MSs. The novel system offered prolonged drug retention in rat joints, providing quantifiable TA remains over 28 days. Whereas, over 95% of IA TA was removed from joints within seven days, after injection of the marketed product. Systemic exposure of the steroidal compound was drastically decreased with the MSs, with <50% systemic exposure compared to that with the marketed product. The novel MS was physicochemically stable, with no changes in drug crystallinity and release profile over 12 months. Therefore, the TA microcrystals-loaded MS is expected to be beneficial in patients especially with osteoarthritis, with reduced IA dosing frequency.

INHIBITION OF TUMOUR NECROSIS FACTOR (TNF) ACTIVITY BY A NEW ERGOSTANE STEROID FROM CLEOME DROSERIFOLIA

Objective: To isolate steroidal compound from Cleome droserifolia and explore its activity against tumour necrosis factor (TNF) using molecular docking studies.Methods: Extraction of the plant material was carried using two successive solvents and three compounds were isolated using column chromatography. The isolated compounds were identified using different spectroscopic data such as 1D, 2D nuclear magnetic resonance (NMR), ultraviolet-visible spectroscopy (UV-Visible), fourier transform infrared spectroscopy (FT-IR) and electrospray ionization mass spectroscopy (ESI-MS). Molecular docking was carried in order to investigate the activity of the ergostane derivative as tumour necrosis factor inhibitor.Results: Two steroidal compounds were isolated and identified as ergost-5,7,9,24 (28)-tetraen-3-one (1) and β-sitosterol glucoside (3) by means of spectroscopic measurement. 1-dodecanol (2) was also isolated. The ergostane derivative showed several binding sites with TNF-αConclusion: The new ergostane derivative isolated from the aerial parts of Cleome droserifolia is introduced to serve as a potential tumour necrosis factor inhibitor and may be used as a lead compound for the treatment of rheumatoid arthritis.

(10R,13R)-17-(6-Hydroxy-5-methylheptan-2-yl)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-ol hemihydrate: a bioactive steroid isolated from the Indian herbArtemisia reticulata

The title tetracyclic steroidal compound, C27H46O2·0.5H2O, crystallized as a monohydrate with two independent molecules (1and2) in the asymmetric unit. In both molecules, the conformations of the three cyclohexane rings (A,BandC) are chair, half-chair and chair, respectively. The fourth ring,D, has a twisted conformation on the bond linking theDandCrings. The crystal structure is stabilized by hydrogen bonding with the two independent molecules being linked through the solvent water moleculeviavarious O—H...O hydrogen bonds, forming layers parallel to (-101).