scholarly journals In Vitro Cytotoxicity and Anti-HIV Activity of Crude Extracts of Croton macrostachyus, Croton megalocarpus and Croton dichogamus

2021 ◽  
Vol Volume 13 ◽  
pp. 971-979
Author(s):  
Ermias Mergia Terefe ◽  
Faith Apolot Okalebo ◽  
Solomon Derese ◽  
Joseph Muriuki ◽  
Gaber El-Saber Batiha
2008 ◽  
Vol 63 (1) ◽  
pp. 83-89 ◽  
Author(s):  
Yaseen A. Al-Soud ◽  
Haitham H. Al-Sa’doni ◽  
Houssain A. S. Amajaour ◽  
Kifah S. M. Salih ◽  
Mohammad S. Mubarakb ◽  
...  

A new series of coumarin and benzofuran derivatives were synthesized as potential non-nucleoside reverse transcriptase inhibitors (NNRTIs) by reacting, separately, 4-bromomethylcoumarins, their sulphonyl chlorides, and ethyl 3-(bromomethyl)-6-methoxy-1-benzofuran-2-carboxylate with different imidazoles and their benzo analogs. The antiviral (HIV-1, HIV-2) properties of the newly synthesized compounds were investigated in vitro and all compounds were found to be inactive, except 10 which showed inhibition of HIV-2 with EC50 > 0.51 μgmL−1. The in vitro cytotoxicity of 17 and 19 was assayed against a panel of tumor cell lines consisting of CD4 human T-cells.


2012 ◽  
Vol 12 (S1) ◽  
Author(s):  
Mamidala Estari ◽  
Lunavath Venkanna ◽  
Annem Srinivas Reddy

Author(s):  
Mukhwana Dennis Wafula ◽  
Ayieko Cyrus ◽  
Mweresa Collins ◽  
Ingonga Johnstone ◽  
Matoke-Muhia Damaris

Leishmaniasis is a major public health problem globally. Visceral leishmaniasis is known to be fatal if left untreated, while cutaneous leishmaniasis is the most neglected. The first-line treatment of leishmaniasis is based on pentavalent antimonial drugs which are expensive, requiring inpatient treatment and toxic. The Plants containing active compounds against other protozoan diseases may offer alternatives against leishmania parasites. This study determined the in vitro antileishmanial activity of Olea europaea, Kigelia africana, Terminalia mollis, Croton macrostachyus and Bridella micrantha extracts. The plant samples were dried, pulverized into fine powders and extracted using ethanol at the Center for Traditional Medicine and Drugs Research, KEMRI. The in vitro assays were carried out at the Leishmania laboratory, Centre for Biotechnology Research and Development, KEMRI. In in- vitro assays the inhibitory concentrations (IC50) and Minimum Inhibition Concentration (MIC) on L. major promastigotes, percentage rates of macrophages infected by amastigotes and cytotoxicity on Vero cells were determined. For each parameter analyzed, differences among treatment groups exposed to different drugs were tested by logistic regression. Results showed that promastogote and amastigote growth inhibition was significantly affected by the crude extracts from the plants (P < 0.05) after 24 hours of exposure where the most effective drug was the standard drug (Amphotericin B) while among the crude extracts of the herbal drugs, T. mollis was the most effective against amastigote followed by C. macrostachyus while O. europaea was the least effective. Mammalian cell viability was significantly affected by the various test compounds (P < 0.05) after 24 hours exposure where % cell viability of herbal drugs, B. microstachyus, O. africana resulted to the most toxic effects by reducing the % cell viability to less than 50%. The study recommends the use of T. mollis in management of leishmaniasis in areas they occur. Further analysis of the active compounds that that affect efficacy of the plant extracts is advised.


2018 ◽  
Vol 13 (2) ◽  
pp. 1934578X1801300
Author(s):  
Kassia M. F. Pereira ◽  
Simone S. Grecco ◽  
Carlos R. Figueiredo ◽  
Jorge K. Hosomi ◽  
Mari U. Nakamura ◽  
...  

Kalanchoe pinnata (Crassulaceae) is a medicinal plant distributed in several areas of the World. Their leaves have been used, in folk medicine, for anxiety and sleep disorders among other proposes. Chemically, this plant is composed by organic acids, flavonoids, bufadienolides, triterpenoids and some ubiquitous compounds. In this study, the fresh leaves of K. pinnata were extracted in an accelerated solvent extraction (ASE) system using H2O (cold and hot) as well as with EtOH:H2O 1:1. The obtained crude extracts were analyzed by HPLC-UV-MS. As a result, were identified organic acids and flavonoids, these being quercetin-3- O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside, kaempferol-3- O-α-L-arabinopiranosyl-(1→2)-α-L-rhamnopyranoside, quercitrin, and trans- p-coumaryl glutaric acid the main compounds in the studied extracts. Obtained results revealed the predominance of flavonoids in extracts prepared using hot H2O (70 26 α 2.19%) or EtOH:H2O 1:1 (74.65 α 5.39%) while a reduction in the amount of these compounds was observed in the extracts prepared using cold H2O (54.41 α 2.93%). Additionally, crude extracts from leaves of K. pinnata extracted with hot H2O and EtOH:H2O 1:1 showed in vitro cytotoxicity on five tested cancer cell lines: murine melanoma (B16F10), human melanoma (A2058), human cervical carcinoma (HeLa), human leukemia (HL-60), and human glioblastoma (U87-MG), with IC50 values in the range of 10.6 α 2.5-91.3 α 7.2 μg/mL. On the other hand, the extract prepared using cold H2O displayed reduced potential. These crude extracts were also tested against human foreskin fibroblasts (non-tumorigenic cells) showing IC50 values ranging from 79.5 to 90.2 μg/mL. In conclusion, our results showed the impact that different extraction methods have on the chemical composition and pharmacological activity, which are notable for the anticancer activity associated to flavonoids.


2021 ◽  
Vol 46 (1) ◽  
Author(s):  
A. Usman ◽  
R.H. Mohammad ◽  
A.O. Abdullahi ◽  
A.H. Zakari ◽  
N.L. Usman

The root bark of Calotropis procera (Family: Asclepiadaceae) was extracted with methanol. The methanolic extract was separated into hexane, chloroform, ethyl acetate, and water soluble fractions. The ethyl acetate fraction was subjected to bioassay-guided fractionation and final purification was achieved by column chromatography. The structure of the compound was elucidated by spectroscopic methods (ESI-MS, 1H and C NMR, COSY, HSQC, and HMBC) and the comparison of the data obtained with that reported in the literature. It was concluded that the compounds isolated was taxifolin 4’-O-β-D-glucopyranoside, a dihydroquercetin glycoside. The crude extracts of hexane, chloroform, ethylacetate, and water soluble fractions of methanol extract and the isolated compound were subjected to antioxidant activity using 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay and brine shrimp lethality bioassay. The result shows that the maximum inhibitions in the DPPH assays were isolated compound (51.7 %), methanol (80.7 %), and water (29.2 %) fractions while ascorbic acid standard was (84.4 %). However, the results for hexane, chloroform and ethyl acetate fractions in the DPPH assays were poor and hence discarded. The results for the in vitro cytotoxicity activity shows that ethyl acetate and hexane fractions showed significant cytotoxicity with LC50 value of 1.0±0.2 and 2.4 ±0.1 respectively. 


Author(s):  
M. R. Kamala Priya ◽  
Manickam Ashokkumar ◽  
Lucia K. Precilla ◽  
Luke Elizabeth Hanna ◽  
Priya R. Iyer

Abstract Background Globally, HIV/AIDS is a major public health issue. Currently, available antiretroviral therapy (ART) has a number of impediments. The need for long-term usage of antiretroviral drugs is associated with the problem of drug resistance, high cost, and other side effects. Hence, there is a constant urge for the development of novel drugs to combat the disease. The synthesis of nanoparticles is of great interest because of their reported application in diverse fields. In contrast to chemical synthesis, green synthesis is inexpensive and enviro-safe. Results Calophyllum inophyllum (CI) is a plant that is known to possess anti-HIV activity. Hence, this plant was exploited for the synthesis of gold nanoparticles (AuNPs) in the present study. Two parts of the plant, namely, the fruit and leaves (CIF and CIL) were used for the synthesis of nanocompounds. The two nanocompounds were tested on HIV-1 isolates at different concentrations and the EC50 values were determined. While CIF-AuNP demonstrated very good anti-HIV activity with an EC50 value of 0.09097 ng/ml, CIL-AuNPs did not show significant anti-HIV activity. Conclusions The present study is a novel attempt to produce nanocompounds that incorporate the medicinal properties of certain plants that are known to have anti-HIV activity within nanoparticles, such that the compound possesses the attributes of a nanomaterial alongside the phytoactivity. Our results provide evidence to suggest that the CIF-AuNP can be further explored for in vivo activity. In vitro cytotoxicity of the AuNPs was checked in VERO cell lines using the MTT assay. Cytotoxicity was observed to be minimal at all the tested concentrations.


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