A new potent antiinfective and antiparasitic 2,3-dihydro-1H-indolizinium chloride, (1), was isolated from Prosopis glandulosa Torr. var. glandulosa. Three additional new (2-4) and one known (5), indolizidines were also isolated, and the dihydrochloride salts of 1-3 (compounds 6, 7 and 8) were prepared. Structures were determined by 1D and 2D NMR and mass spectra. Compound 1 showed potent in vitro antifungal activity against Cryptococcus neoformans and Aspergillus fumigatus (IC 50 values = 0.4 and 3.0 μg/mL, respectively), and antibacterial activity against methicillin-resistant Staphylococcus aureus and Mycobacterium intracellulare (IC 50 values of 0.35 and 0.9 μg/mL, respectively). The remarkable in vitro fungicidal activity of 1-4 against C. neoformans (MFCs = 0.63→1.25 μg/mL) and 2, 3, and 5 against A. fumigatus (MFCs = 0.63→2.5 μg/mL) were similar to amphotericin B, but >2-4-fold more potent than 6-8. Prosopilosidine (1) showed potent in vivo activity at 0.0625 mg/Kg/day/ip for 5 days in a murine model of cryptococcosis by eliminating ~76% of C. neoformans infection from brain tissue compared to ~83% with amphotericin B at 1.5 mg/Kg/day. Compounds 1 and 4 exhibited potent activity and high selectivity index (SI) values against chloroquine sensitive (D6) and chloroquine resistant (W2) strains of Plasmodium falciparum with IC 50 values of 39 and 95 ng/mL, and 42 and 120 ng/mL, respectively; (chloroquine, IC 50 = 17 and 140 ng/mL). Prosopilosine (1) also showed in vivo antimalarial activity with an ED 50 value of ~2 mg/Kg/day/ip against Plasmodium bergheiinfected mice after 3 days of treatment.Plants of the genus Prosopis are trees or shrubs distributed in arid and semiarid tropical and subtropical regions. P. glandulosa Torrey var. glandulosa (Leguminosae), a medium-sized * To whom correspondence should be addressed. Tel. (662) Decoctions of leaves and pods are generally used to make eye washes to treat pink eye. 5 An ethanolic extract of P. glandulosa from Pakistan yielded triterpenes, flavonoids, glycosides and the indolizidine alkaloid juliprosopine. [6][7][8][9][10] Among the indolizidines reported from Prosopis species to date, 6-11 the stereochemistry of juliprosine and juliprosopine were established by chemical synthesis. 12 The piperidinyl indolizidines, such as juliprosopine, and their analogs exhibited in vitro antibmicrobial, antidermatophytic, pesticidal, and amebicidal activities. 11,[13][14][15][16][17][18][19][20] In addition, their toxicity, 20-22 DNA binding activity 23 , inhibitory effects on β-glucosidase enzymes 23 and plant growth inhibitory activities were also reported. 10,24 This paper describes the isolation of the new potent antifungal and antimalarial dihydroindolizinium chloride prosopilosidine (1) from honey mesquite, together with three new analogs prosopilosine (2), isoprosopilosine (3) and isoprosopilosidine (4), and the known juliprosopine (5). 25,26 P. glandulosa Torrey var. glandulosa, has not previously been subjected to chemical or biological investigations. Prosop...
oxidative damage to membranes and may also enhance susceptibility to lipid peroxidation. 5,6 Trace-element deficiencies or problems with its absorption are frequently associated to chronic diseases. Chronic hyperglycemia may cause significant alterations in the status of some micronutrients, and on the other hand, some of these nutrients can directly modulate glucose homeostasis. 7,8 The early imbalances of some specific metals may play a role in upsetting normal glucose and insulin metabolism. 9 Despite the great strides made in the understanding and management of diabetes, the disease and disease related complications remains unabated. Phytochemicals identified from traditional medicinal plants are presenting an exciting opportunity for the development of new types of therapeutics. 10 Epidemiological studies demonstrated that many phytonutrients from fruits might protect the human body against oxidative stress. It is a known fact that nutrition and health care are interrelated. Thus the consumption of natural antioxidant phytochemicals was noted to have potential health benefits. 11 Abelmoschus esculentus, 'AE" (Okra or lady"s finger) is a flowering plant in the mallow family. It is one of the most important vegetables widely cultivated throughout the tropical and temperate regions of the world for its tender fruits. 12 This plant is popular with its mucilaginous properties and has been acclaimed to have various health benefits which include anti-diabetic properties. 13 Okra is also known for being high in antioxidants activity as it is rich in phenolic compounds with important biological properties like quarcetin and flavonol derivatives, catechin oligomers and hydroxycinnamic derivatives. 14 The fruit of this particular plant is rich in nutrients like protein, niacin, riboflavin, thiamine, folate, vitamins A, B6, C and K, Phosphorus, Zinc, Copper, Potassium, Magnesium, Calcium, and Manganese all of which plays vital role in human diet and health.
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