The Amaryllidaceae as a source of antiplasmodial crinane alkaloid constituents.

Malaria is prevalent in tropical and subtropical regions of the globe. With over 200 million cases reported annually, particularly in sub-Saharan Africa, it is an unnecessary burden to already overworked and ailing healthcare structures. Traditional medicine (TM) remains vibrant in most of these regions wherein plants often serve as the first line of defense against malaria. Given this fact as well as the successes elsewhere of therapies such as Artemisia annua emanating from evidence-based TM, interest in plants as a source of new antimalarial drugs has been rejuvenated. The bulbous plant family Amaryllidaceae is recognized for its structurally-diverse alkaloid constituents which exhibit interesting biological properties. This review focuses on the in vitro activities demonstrated by its crinane alkaloids against various strains of the malaria-causing parasite Plasmodium falciparum. The survey embraces the twelve genera of the Amaryllidaceae whose nineteen representative species have been examined for antiplasmodial crinane alkaloid principles. A total of seventy-two compounds were screened against nine strains of P. falciparum, with the α-crinanes reflecting better overall activities than their corresponding ß-crinane subgroup congeners. In terms of potency, an ED50 of 0.14 µg/mL (for augustine in the D-6 strain) and IC50 of 0.35 µg/mL (for haemanthidine in the K1 strain) were the lowest activity indices observed. Structure-activity relationship studies afforded useful insight on the antiplasmodial pharmacophore and the features supporting its efficacy. Overall, crinane alkaloids have provided a useful platform for the study of antiplasmodial effects, not only in terms of potency but also in terms of structural diversity.

Cytotoxic and Genotoxic Activities of Alkaloids from the Bulbs of Griffinia gardneriana and Habranthus itaobinus (Amaryllidaceae).

BACKGROUND: Amaryllidaceae plants are known to be a great source of alkaloids, which are considered an extensive group of compounds encompassing a wide range of biological activities. The remarkable cytotoxic activities observed in most of the Amaryllidaceae alkaloids derivatives have prompt the chemical and biological investigations in unexplored species from Brazil. OBJECTIVE: To evaluate the cytotoxic and genotoxic properties of alkaloids of Griffinia gardneriana and Habranthus itaobinus bulbs and study the role of caspase-3 as a molecular apoptosis mediator. METHODS: Methanolic crude extracts of Griffinia gardneriana and Habranthus itaobinus bulbs were submitted to acid-base extraction to obtain alkaloid-enriched fractions. The obtained fractions were fractionated using chromatographic techniques leading to isolation and identification of some alkaloids accomplished via HPLC and 1H-NMR, respectively. Molecular docking studies assessed the amount of free binding energy between the isolated alkaloids with the caspase-3 protein and also calculated the theoretical value of Ki. Studies have also been developed to evaluate in vitro cytotoxicity and genotoxicity in such alkaloids and apoptosis activation via the caspase pathway using both tumor and normal cell lines. RESULTS: Seven alkaloids were isolated and identified. Among these, 11-hydroxyvittatine and 2-α-7- dimethoxyhomolycorine were not cytotoxic, whereas tazettine, trisphaeridine, and sanguinine only showed activity against the fibroblast lineage. Lycorine and pretazettine were 10 to 30 folds more cytotoxic than the other alkaloids, including cancerous lines, and were genotoxic and capable of promoting apoptosis via the caspase-3 pathway. This result supports data obtained in docking studies wherein these two compounds exhibited the highest free energy values. CONCLUSION: The cytotoxicity assay revealed that, among the seven alkaloids isolated, only lycorine and pretazettine were active against different cell lines, exhibiting concentration- and time-dependent cytotoxic actions alongside genotoxic action and the ability to induce apoptosis by caspase-3, a result consistent with those obtained in docking studies.

Palyno-anatomical studies of monocot taxa and its taxonomic implications using light and scanning electron microscopy.

Palyno-anatomical study of monocots taxa using Light and Scanning Electron Microscopy (SEM) was first time conducted with a view to evaluating their taxonomic significance. Studied plants were collected from different eco-climatic zones of Pakistan ranges from tropical, sub-tropical, and moist habitats. The aim of this study is to use palyno-anatomical features for the correct identification, systematic comparison, and investigation to elucidate the taxonomic significance of these features, which are useful to taxonomists for identifying monocot taxa. A signification variation was observed in quantitative and qualitative characters by using the standard protocol of light microscopy (LM) and SEM. Epidermal cell length varied from maximum in Allium griffthianum (480 ± 35.9) µm at the adaxial surface to minimum in Canna indica (33.6 ± 8.53) µm on abaxial surface. Maximum exine thickness was observed in Canna indica (4.46) µm and minimum in Allium grifthianum (0.8) µm. Variation was observed in shape and exine ornamentation of the pollen, shape of the epidermal cell, number, size, and type of stomata, guard cell shape, and anticlinal wall pattern. Based on these palyno-anatomical features a taxonomic key was developed, which help in the discrimination of studied taxa. In conclusion, LM and SEM pollen and epidermal morphology is explanatory, significant, and can be of special interest for the plant taxonomist in the correct identification of monocots taxa.

Antifungal activity of some Sternbergia taxa: effects on germ tube and biofilm formation

Natural products are rapidly becoming the primary sources of novel antimicrobial agents, as resistance to existing antimicrobial agents is increasing. Apart from determining the antimicrobial activity of natural products, it is also important to understand their effects on the virulence factors of microorganisms. This study aimed to determine the antimicrobial activity of Sternbergia species prevalent in Turkey and investigate their role in the inhibition of germination tube and biofilm formation, both of which are known to be important virulence factors of Candida albicans. The antimicrobial activities of the plant extracts were evaluated using bore-plate and broth microdilution method. The extracts' capacity to inhibit the formation of the germ-tube was also evaluated. The findings of our study revealed that Sternbergia lutea, Sternbergia vernalis possessed antimicrobial activities, with MIC values ranging between 0.048 mg/mL and 0.39 mg/mL. The highest antimicrobial activity was observed against Candida dubliniensis (0.048 mg/mL). While evaluating the inhibition of fungal germination activities, S. vernalis extract (at a concentration of 0.09 mg/mL) was found to be the most effective against C. albicans ATCC 90028 strain. The results also indicated that S. vernalis extracts at sub-MIC levels inhibited germ tube formation and modulated the tail-length of germinated cells, both of which are important virulence factors of C. albicans. Furthermore, the inhibition of biofilm-formation was also investigated, and it was found that two Sternbergia spp. extracts at or below MIC levels inhibited biofilm formation.