Chemical Constituents from Croton Species and Their Biological Activities

Xu, Wen-Hui; Liu, Weiyi; Liang, Qian

doi:10.3390/molecules23092333

Cited by 93 publications

(58 citation statements)

References 125 publications

(149 reference statements)

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“…The Crotons (Euphorbiaceae) represent around 1300 species of trees, shrubs, and herbs widely distributed in the tropics (Salatino et al, 2007;Xu et al, 2018). They have a rich history of ethnomedicinal uses including malaria, inflammation, tuberculosis, and stomach upset (Salatino et al, 2007).…”

Section: Introductionmentioning

confidence: 99%

Leishmanicidal Potential of Hardwickiic Acid Isolated From Croton sylvaticus

et al. 2020

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Leishmania is a parasitic protozoon responsible for the neglected tropical disease Leishmaniasis. Approximately, 350 million people are susceptible and close to 70,000 death cases globally are reported annually. The lack of effective leishmanicides, the emergence of drug resistance and toxicity concerns necessitate the pursuit for effective antileishmanial drugs. Natural compounds serve as reservoirs for discovering new drugs due to their chemical diversity. Hardwickiic acid (HA) isolated from the stembark of Croton sylvaticus was evaluated for its leishmanicidal potential against Leishmania donovani and L. major promastigotes. The susceptibility of the promastigotes to HA was determined using the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide/phenazine methosulfate colorimetric assay with Amphotericin B serving as positive control. HA showed a significant antileishmanial activity on L. donovani promastigotes with an IC 50 value of 31.57± 0.06 µM with respect to the control drug, amphotericin B with IC 50 of 3.35 ± 0.14 µM). The cytotoxic activity was observed to be CC 50 = 247.83 ± 6.32 µM against 29.99 ± 2.82 µM for curcumin, the control, resulting in a selectivity index of SI = 7.85. Molecular modeling, docking and dynamics simulations of selected drug targets corroborated the observed antileishmanial activity of HA. Novel insights into the mechanisms of binding were obtained for trypanothione reductase (TR), pteridine reductase 1 (PTR1), and glutamate cysteine ligase (GCL). The binding affinity of HA to the drug targets LmGCL, LmPTR1, LdTR, LmTR, LdGCL, and LdPTR1 were obtained as-8.0,-7.8,-7.6,-7.5,-7.4 and-7.1 kcal/mol, respectively. The role of Lys16, Ser111, and Arg17 as critical residues required for binding to LdPTR1 was reinforced. HA was predicted as a Caspase-3 stimulant and Caspase-8 stimulant, implying a possible role in apoptosis, which was shown experimentally that HA induced parasite death by loss of

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Section: Introductionmentioning

confidence: 99%

Leishmanicidal Potential of Hardwickiic Acid Isolated From Croton sylvaticus

et al. 2020

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“…The genus Croton comprises over 1300 species that are widely distributed throughout tropical and subtropical regions of the world. Croton species have been used traditionally in Africa, South Asia, and Latin America for the treatment of infections and digestive disorders (Wu and Zhao, 2004;Xu et al, 2018). In Sudan, C. gratissimus, locally known as Um-Geleigla, has been used traditionally for the treatment of hypertension and malaria (Mohamed et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

HPLC-Based Activity Profiling for Antiprotozoal Compounds in Croton gratissimus and Cuscuta hyalina

et al. 2020

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In a screening of Sudanese medicinal plants for antiprotozoal activity, the chloroform fractions obtained by liquid-liquid partitioning from ethanolic extracts of fruits of Croton gratissimus var. gratissimus and stems of Cuscuta hyalina Roth ex Schult. exhibited in vitro activity against axenically grown Leishmania donovani amastigotes. This antileishmanial activity was localized by HPLC-based activity profiling. Targeted preparative isolation afforded flavonoids 1-6, 3methoxy-4-hydroxybenzoic acid (7), and benzyltetrahydroisoquinoline alkaloids laudanine (8) and laudanosine (9) from C. gratissimus, and pinoresinol (10), isorhamnetin (11), (-)-pseudosemiglabrin (12), and kaempferol (13) from C. hyalina. The antiprotozoal activity of 1-13 against L. donovani (axenic and intracellular amastigotes), Trypanosoma brucei rhodesiense (bloodstream forms), and Plasmodium falciparum (erythrocytic stages), and the cytotoxicity in L6 murine myoblast cells were determined in vitro. Quercetin-3,7-dimethylether (6) showed the highest activity against axenic L.

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“…The genus Croton L. (Euphorbiaceae) is well known for producing clerodane diterpenes (Amaral and Barnes, 1998;Salatino et al, 2007;Xu et al, 2018), which are a group of bicyclic diterpenes widespread in the family Euphorbiaceae and known for their wide range of biological activities including anticancer, anti-inflammatory, antifeedant and anti-ulcer among others (Li et al, 2016). Croton oligandrus Pierre ex Hutch is a small aromatic tree growing up to 5 -10 m tall, commonly found in Western and Central African forests (Aubreville, 1983).…”

Section: Introductionmentioning

confidence: 99%