In vitro antioxidant and acetylcholinesterase inhibitory properties of the alkaloid fraction of Cissampelos sympodialis Eichler

The objective of this work was to evaluate the antiplasmodial activity and toxicity of the extract and fractions obtained from the bark of Aspidosperma nitidum. The ethanol extract obtained from the powdered bark of plants was acid-base partitioned and phytochemically analyzed. The antiplasmodial activity, in vivo antimalarial activity and in vitro cytotoxicity were acessed. The selectivity index (SI) was calculated. The acute oral toxicity and pathological effects, of the ethanol extract was evaluated in mice. The major constituent of the ethanol extract was suggestive of a β-carboline chromophore. The alkaloid and neutral fractions contained compounds with an aspidospermine core as the major constituent. The ethanol extract (IC50 = 3.60 µg/mL), neutral fraction (IC50 = 3.34 µg/mL) and alkaloid fraction (IC50= 2.32 µg/mL) showed high activity against P. falciparum (W2 strain). The ethanol extract and the alkaloid fraction reduced 80% of the parasitemia of P. berghei (ANKA)-infected mice (dose of 500 mg/kg) in the 5th day, which was not sustainable at the 8th day. A similar result was obtained for chloroquine. The ethanol extract (CC50 = 410.65 µg/mL; SI = 114.07), neutral fraction (CC50 = 452.53 µg/mL; SI = 135.49), and alkaloid fraction (CC50 =346.73 µg/mL; SI 149.45) demonstrated low cytotoxicity and high SI. The ethanol extract (5000 mg/kg; gavage) presented low acute oral toxicity, with no clinical or anatomopathological modifications being observed (in comparison to the control group). In vitro studies with a chloroquine-resistant clone of P. falciparum confirmed the antiplasmodial activity of the A. nitidum ethanol extract, and its fractions had low cytotoxicity for HepG2 cells. In vivo studies with P. berghei–infected mice and acute toxicity studies corroborated these results.

Download Full-text

Flavopereirine—An Alkaloid Derived from Geissospermum vellosii—Presents Leishmanicidal Activity In Vitro

Molecules ◽

10.3390/molecules24040785 ◽

2019 ◽

Vol 24 (4) ◽

pp. 785 ◽

Cited By ~ 3

Author(s):

João Victor da Silva e Silva ◽

Heliton Patrick Cordovil Brigido ◽

Kelly Cristina Oliveira de Albuquerque ◽

Josiwander Miranda Carvalho ◽

Jordano Ferreira Reis ◽

...

Keyword(s):

Physicochemical Characteristics ◽

Inhibitory Effect ◽

Antileishmanial Activity ◽

Lipinski’S Rule ◽

Oligopeptidase B ◽

Mechanism Of Interaction ◽

Low Toxicity ◽

Alkaloid Fraction ◽

Dynamics Simulations

Chemotherapy is limited in the treatment of leishmaniasis due to the toxic effects of drugs, low efficacy of alternative treatments, and resistance of the parasite. This work assesses the in vitro activity of flavopereirine on promastigote cultures of Leishmania amazonensis. In addition, an in silico evaluation of the physicochemical characteristics of this alkaloid is performed. The extract and fractions were characterized by thin-layer chromatography and HPLC-DAD, yielding an alkaloid identified by NMR. The antileishmanial activity and cytotoxicity were assayed by cell viability test (MTT). The theoretical molecular properties were calculated on the Molinspiration website. The fractionation made it possible to isolate a beta-carboline alkaloid (flavopereirine) in the alkaloid fraction. Moreover, it led to obtaining a fraction with greater antileishmanial activity, since flavopereirine is very active. Regarding the exposure time, a greater inhibitory effect of flavopereirine was observed at 24 h and 72 h (IC50 of 0.23 and 0.15 μg/mL, respectively). The extract, fractions, and flavopereirine presented low toxicity, with high selectivity for the alkaloid. Furthermore, flavopereirine showed no violation of Lipinski’s rule of five, showing even better results than the known inhibitor of oligopeptidase B, antipain, with three violations. Flavopereirine also interacted with residue Tyr-499 of oligopeptidase B during the molecular dynamics simulations, giving a few insights of a possible favorable mechanism of interaction and a possible inhibitory pathway. Flavopereirine proved to be a promising molecule for its antileishmanial activity.

Download Full-text

The alkaloid fraction from Buxus sempervirens leaves shows strong in vitro activity against Plasmodium falciparum

Planta Medica ◽

10.1055/s-0033-1351906 ◽

2013 ◽

Vol 79 (13) ◽

Cited By ~ 4

Author(s):

JB Althaus ◽

G Jerz ◽

P Winterhalter ◽

M Kaiser ◽

R Brun ◽

...

Keyword(s):

Plasmodium Falciparum ◽

Vitro Activity ◽

In Vitro Activity ◽

Buxus Sempervirens ◽

Alkaloid Fraction

Download Full-text

Aktivitas Sitotoksik Fraksi Alkaloid Kulit Batang dan Buah Attarasa (Litsea cubeba Lour.) terhadap Sel Kanker Payudara T47D

Talenta Conference Series Tropical Medicine (TM) ◽

10.32734/tm.v1i3.261 ◽

2018 ◽

Vol 1 (3) ◽

pp. 052-055

Author(s):

Aminah Dalimunthe ◽

Poppy Anjelisa Zaitun Hasibuan ◽

Jansen Silalahi ◽

Denny Satria

Keyword(s):

Breast Cancer ◽

Cytotoxic Activity ◽

In Vitro Study ◽

Ethanol Extract ◽

T47d Cell ◽

Chloroform Fraction ◽

Anticancer Activities ◽

Litsea Cubeba ◽

Alkaloid Fraction

Kanker payudara adalah salah satu jenis dari kanker yang banyak menyerang wanita selain kanker mulut rahim. Tingginya angka kejadian dan resistensi agen kemoterapi menyebabkan perlu dilakukan pencarian bahan alam dengan aktivitas antikanker. Penggunaan bahan alam diharapkan dapat mengatasi resistensi dan efek samping yang terjadi ketika digunakan kemoterapi konvensional. Tujuan penelitian ini untuk mengetahui aktivitas antikanker fraksi kloroform (alkaloid) kulit batang dan buah attarasa pada sel T47D. Ekstrak etanol diekstraksi dengan cara maserasi dan difraksinasi dengan n-heksana dan kloroform pada pH 3, 7, 9. Pengujian sitotoksik secara in vitro menggunakan metode MTT yang kemudian dianalisis menggunakan SPSS 21. Hasil uji sitotoksik (IC50) yang diperoleh setelah pemberian fraksi alkaloid kulit batang dan buah attarasa pH 7 dan 9 adalah sebesar 46,60 ± 0,19; 123,01 ± 14,63 dan 35,89 ± 1,04; dan 98,31 ± 2,51 µg/mL. Fraksi alkaloid kulit batang dan buah attarasa bersifat sitotoksik terhadap sel kanker payudara T47D. Breast cancer is one type of cancer that attacks many women in addition to cervical cancer. The high incidence and resistance of chemotherapy agents causes the need to search for natural products with anticancer activities. The use of natural product is expected to overcome resistance and side effects that occur when used conventional chemotherapy. This research aimed to evaluate the anti-cancer activity of chloroform fraction (alkaloid) from cortex and Fructus of Attarasa on T47D cell. The ethanol extract was prepared by maceration method and then fractionated using n-hexane and chloroform at pH 3, 7, and 9. In vitro study of cytotoxic activity was performed using MTT method, then analyzed using SPSS 21. The IC50 values of cytotoxic activity of alkaloid fraction from cortex and Fructus of Attarasa at pH 7 dan 9 were 46.60 ± 0.19; 123.01 ± 14.63 and 35.89 ± 1.04; dan 98.31 ± 2.51 µg/mL. Alkaloid fraction from cortex skin and Fructus of Attarasa has cytotoxic activity on Breast Cancer T47D Cell

Download Full-text

Ultrastructural Investigations of the Contractile Filaments of Amoebae

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100050950 ◽

1974 ◽

Vol 32 ◽

pp. 188-189

Author(s):

P.L. Moore

Keyword(s):

Cytoplasmic Streaming ◽

Three Dimensional ◽

Freeze Fracture ◽

Amoeboid Movement ◽

Different Types ◽

Chemical Conditions ◽

Complete Interpretation

Previous freeze fracture results on the intact giant, amoeba Chaos carolinensis indicated the presence of a fibrillar arrangement of filaments within the cytoplasm. A complete interpretation of the three dimensional ultrastructure of these structures, and their possible role in amoeboid movement was not possible, since comparable results could not be obtained with conventional fixation of intact amoebae. Progress in interpreting the freeze fracture images of amoebae required a more thorough understanding of the different types of filaments present in amoebae, and of the ways in which they could be organized while remaining functional.The recent development of a calcium sensitive, demembranated, amoeboid model of Chaos carolinensis has made it possible to achieve a better understanding of such functional arrangements of amoeboid filaments. In these models the motility of demembranated cytoplasm can be controlled in vitro, and the chemical conditions necessary for contractility, and cytoplasmic streaming can be investigated. It is clear from these studies that “fibrils” exist in amoeboid models, and that they are capable of contracting along their length under conditions similar to those which cause contraction in vertebrate muscles.

Download Full-text

In Vitro Induction of Crystals of MT Protein by Vinblastine-Colcemid in Mouse Spermatids

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100050676 ◽

1974 ◽

Vol 32 ◽

pp. 132-133

Author(s):

John J. Wolosewick ◽

John H. D. Bryan

Keyword(s):

Endoplasmic Reticulum ◽

Smooth Endoplasmic Reticulum ◽

Nuclear Ring ◽

Rough Er ◽

Distal Direction ◽

In Vitro Induction

Early in spermiogenesis the manchette is rapidly assembled in a distal direction from the nuclear-ring-densities. The association of vesicles of smooth endoplasmic reticulum (SER) and the manchette microtubules (MTS) has been reported. In the mouse, osmophilic densities at the distal ends of the manchette are the organizing centers (MTOCS), and are associated with the SER. Rapid MT assembly and the lack of rough ER suggests that there is an existing pool of MT protein. Colcemid potentiates the reaction of vinblastine with tubulin and was used in this investigation to detect this protein.

Download Full-text

Induction and Differentiation of Dental Epithelium in Vivo and in Vitro

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100053425 ◽

1982 ◽

Vol 40 ◽

pp. 142-145

Author(s):

E. J. Kollar

Keyword(s):

Connective Tissue ◽

Oral Mucosa ◽

Basal Lamina ◽

Functional Derivatives ◽

Specific Source ◽

Dental Epithelium ◽

Connective Tissue Stroma

The differentiation and maintenance of many specialized epithelial structures are dependent on the underlying connective tissue stroma and on an intact basal lamina. These requirements are especially stringent in the development and maintenance of the skin and oral mucosa. The keratinization patterns of thin or thick cornified layers as well as the appearance of specialized functional derivatives such as hair and teeth can be correlated with the specific source of stroma which supports these differentiated expressions.

Download Full-text