Cancer is a complex group of diseases initiated by abnormal cell division with the potential of spreading to other parts of the body. The advancement in the discoveries of omics and bio- and cheminformatics has led to the identification of drugs inhibiting putative targets including vascular endothelial growth factor (VEGF) family receptors, fibroblast growth factors (FGF), platelet derived growth factors (PDGF), epidermal growth factor (EGF), thymidine phosphorylase (TP), and neuropeptide Y4 (NY4), amongst others. Drug resistance, systemic toxicity, and drug ineffectiveness for various cancer chemo-treatments are widespread. Due to this, efficient therapeutic agents targeting two or more of the putative targets in different cancer cells are proposed as cutting edge treatments. Heterocyclic compounds, both synthetic and natural products, have, however, contributed immensely to chemotherapeutics for treatments of various diseases, but little is known about such compounds and their multimodal anticancer properties. A compendium of heterocyclic synthetic and natural product multitarget anticancer compounds, their IC50, and biological targets of inhibition are therefore presented in this review.
The leaf oils of samples of Lippia multiflora Moldenke collected from different geographic areas of Togo and from cultivated plants were analyzed by GC and GC/MS. Three types of essential oils were characterized, one which is rich in neral and geranial, (23–89%) and two other types, poor in neral and geranial, containing either 1,8-cineole (16–63%) or thymol (15–40%) and p-cymene (15–20%) as the major components. The oils obtained exhibited insecticidal activity against the bruchid Callosobruchus maculatus Fab. in a dose-dependent manner.
Cryptolepis sanguinolenta (Lindl.) Schlt., the main source of cryptolepine alkaloid, is intensively exploited in the wild to treat malaria and Lyme disease. In this study, the influence of four inorganic fertilizers (supplying N, P, K, or NPK) and four growth periods (3, 6, 9, and 12 months after transplanting) on the herb’s root biomass, cryptolepine content and yield, and biological activities were investigated in a pot and field trial. The results showed the application of N (in the form of Urea or NPK) increased root biomass yield, cryptolepine content, and cryptolepine yield compared to unfertilized plants. The 9-month-old plants recorded the maximum cryptolepine content (2.26 mg/100 mg dry root) and cryptolepine yield (304.08 mg/plant), indicating the perfect time to harvest the herb. Plant age at harvest had a more significant influence (50.6–55.7%) on cryptolepine production than fertilizer application (29.2–33.3%). Cryptolepine extracts from 9- to 12-month-old plants had the highest antiplasmodial activity (IC50 = 2.56–4.65 µg/mL) and drug selectivity index (2.15–3.91) against Plasmodium falciparum Dd2. These extracts were also cytotoxic to Jurkat leukaemia cell lines (CC50 < 62.56 µg/mL), indicating the possible use of cryptolepine for cancer management. Growing the herb in the field increased cryptolepine yield 2.5 times compared to growth in a pot, but this did not influence the antiplasmodial activity of the extract. Commercial cultivation of C. sanguinolenta for 9 months combined with N application could be a promising solution to the sustainable use of this threatened medicinal species.
This review discusses the structural diversity of the dichapetalins and related compounds from the genera Dichapetalum and Phyllanthus, their manifestation in the diversity of their biological activities, and areas of potential future research.
Cryptolepis sanguinolenta (Lindl.) Schlt. is an important multipurpose medicinal plant used for the treatment of ailments such as malaria. Despite the ongoing efforts in domesticating the herb, the ideal planting density and its benefits are unknown. A study was conducted to determine the influence of six C. sanguinolenta accessions and three planting densities (15, 30 and 45 plants/1.8 m2) on root biomass, cryptolepine concentration and cryptolepine yield. Also, benefit-cost ratios were determined for each plant density across the four cultivation periods (9, 12, 15 and 18 months). The cultivation of C. sanguinolenta at the highest planting density (45 plants/1.8 m2) increased root biomass (value), cryptolepine content (2.08 mg/100 mg dry root) and cryptolepine yield (23.31 mg mg/1.8 m2) compared to those cultivated at lower planting densities (15 and 30 plants/1.8 m2). The duration for growing C. sanguinolenta had a more significant influence on cryptolepine yield but not the cryptolepine content. Plants cultivated for 15 months gave the maximum cryptolepine yield (10.33 g/bed), indicating 15 months as the optimum time to harvest the roots. The benefit-cost analysis revealed that growing the plant at a density of 45 plants/1.8 m2 (25,920 plants/acre) for 18 months was a more profitable venture with a benefit-cost ratio of 3.45. Commercial cultivation of C. sanguinolenta at 45 plants per bed area of 1.8 m2 (25,920 plants/acre) for 15-18 months is recommended as the most profitable and promising cropping practice to ensure the sustainable supply of planting material.