Chem. Pharm. Bull.(オピニオン)

In recent years, tools for the development of new drugs have been dramatically improved. These include genomic and proteomic research, numerous biophysical methods, combinatorial chemistry and screening technologies. In addition, early ADMET studies are employed in order to significantly reduce the failure rate in the development of drug candidates. As a consequence, the lead finding, lead optimization and development process has gained marked enhancement in speed and efficiency. In parallel to this development, major pharma companies are increasingly outsourcing many components of drug discovery research to biotech companies. All these measures are designed to address the need for a faster time to market. New screening methodologies have contributed significantly to the efficiency of the drug discovery process. The conventional screening of single compounds or compound libraries has been dramatically accelerated by high throughput screening methods. In addition, in silico screening methods allow the evaluation of virtual compounds. A wide range of new lead finding and lead optimization opportunities result from novel screening methods by NMR, which are the topic of this review article.

Drug Discovery Today

Diabetes mellitus is one of the major health problems in the world, the incidence and associated mortality are increasing. Inadequate regulation of the blood sugar imposes serious consequences for health. Conventional antidiabetic drugs are effective, however, also with unavoidable side effects. On the other hand, medicinal plants may act as an alternative source of antidiabetic agents. Examples of medicinal plants with antidiabetic potential are described, with focuses on preclinical and clinical studies. The beneficial potential of each plant matrix is given by the combined and concerted action of their profile of biologically active compounds.

https://www.mdpi.com/2218-273X/9/10/551/pdf

Antidiabetic Potential of Medicinal Plants and Their Active Components.

Apigenin: A dietary flavonoid with diverse anticancer properties.

Heavy metals in contaminated environment: Destiny of secondary metabolite biosynthesis, oxidative status and phytoextraction in medicinal plants.

Sudanese folk medicine represents a unique blend of indigenous cultures with Islamic, Arabic and African traditions. In addition, Sudan encompasses different terrains and climatic zones, ranging from desert and semi-desert in the north to equatorial with a short rainy season (semi-aridand semi-humid) in the centre to equatorial with a long rainy season (arid-humid and equatorialhumid) in the south. This variation contributes to the immense diversity of vegetation in the region. The flora of Sudan consists of 3137 species of flowering plants belonging to 170 families and 1280 genera. It is estimated that 15% of these plants are endemic to Sudan. The intersection of diverse cultures and the unique geography holds great potential for Sudanese herbal medicine. Medicinal and aromatic plants and their derivatives represent an integral part of life in Sudan. Indigenous remedies are the only form of therapy available to the majority of poor people. It has been estimated that only 11% of the population has access to formal health care. Therefore, research on the desired pharmacological effects and possible unwanted side effects or toxicity is required to improve efficacy and safety of Sudanese herbal medicine. In the future, it would be preferable to promote the use of traditional herbal remedies by conversion of raw plant material into more sophisticated products instead of completely replacing the traditional remedies with synthetic products from industrialized countries. The present review gives an overview of traditional Sudanese medicinal and aromatic herbs and their habitats, traditional uses, and phytochemical constituents.

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Gems from traditional north-African medicine: medicinal and aromatic plants from Sudan

Ten plants indigenous to Sudan and of common use in Sudanese folk-medicine, were examined in vitro for antimalarial activity against schizonts maturation of Plasmodium falciparum, the major human malaria parasite. All plant samples displayed various antiplasmodial activity. Three plant extracts caused 100% inhibition of the parasite growth at concentrations of plant material ≤ 500 ug/ml. The two most active extracts that produced 100% inhibition of the parasite growth at concentration of plant material ≤ 50 µg/ml were obtained from the seeds of Nigella sativa and the whole plant of Aristolochia bracteolata. The ten plants were phytochemically screened for their active constituents. The two most active plants showed the presence of sterols, alkaloids and tannins.

https://journals.sagepub.com/doi/pdf/10.4137/EHI.S4108

Antiplasmodial Activity of Some Medicinal Plants Used in Sudanese Folk-medicine

Apigenin is a common dietary flavonoid with considerable cytotoxic activity in vitro and in vivo. Despite many mechanistic studies, less is known about resistance factors hampering apigenin's activity. We investigated the ATP-binding cassette (ABC) transporters BCRP/ABCG2, P-glycoprotein/ABCB1 and its close relative ABCB5. Multidrug-resistant cells overexpressing these ABC transporters were not cross-resistant toward apigenin. Moreover, apigenin inhibited not only P-glycoprotein but also BCRP by increasing cellular uptake of doxorubicin and synergistic inhibition of cell viability in combination with doxorubicin or docetaxel in multidrug-resistant cells. To perform in silico molecular docking studies, we first generated homology models for human P-glycoprotein and ABCB5 based on the crystal structure of murine P-glycoprotein. Their nucleotide binding domains (NDBs) revealed the highest degrees of sequence homologies (89%-100%), indicating that ATP binding and cleavage is of crucial importance for ABC transporters. Molecular docking of apigenin bound to the NDBs of P-glycoprotein and ABCB5 in molecular docking studies. Hence, apigenin may compete with ATP for NDB-binding leading to energy depletion to fuel the transport of ABC transporter substrates. Furthermore, we performed COMPARE and hierarchical cluster analyses of transcriptome-wide mRNA expression profiles of the National Cancer Institute tumor cell line panel. Microarray-based mRNA expressions of genes of diverse biological functions (signal transduction, transcriptional regulation, ubiquitination, autophagy, metabolic activity, xenobiotic detoxification and microtubule formation) significantly predicted responsiveness of tumor cells to apigenin. In conclusion, apigenin's activity is not hampered by classical mechanisms of multidrug resistance and the inhibition of ABC transporters by apigenin indicates that apigenin may overcome multidrug resistance in otherwise refractory tumors.

Activity of the dietary flavonoid, apigenin, against multidrug-resistant tumor cells as determined by pharmacogenomics and molecular docking.

Evaluating ancient Egyptian prescriptions today: Anti-inflammatory activity of Ziziphus spina-christi.

Diabetes mellitus is a chronic metabolic disease with life-threatening complications. Despite the enormous progress in conventional medicine and pharmaceutical industry, herbal-based medicines are still a common practice for the treatment of diabetes. This study evaluated ethanolic and aqueous extracts of selected Sudanese plants that are traditionally used to treat diabetes. Extraction was carried out according to method described by Sukhdev et. al. and the extracts were tested for their glycogen phosphorylase inhibition, Brine shrimp lethality and antioxidant activity using (DPPH) radical scavenging activity and iron chelating activity. Extracts prepared from the leaves of Ambrosia maritima, fruits of Foeniculum vulgare and Ammi visnaga, exudates of Acacia Senegal, and seeds of Sesamum indicum and Nigella sativa. 
Nigella sativa ethanolic extract showed no toxicity on Brine shrimp Lethality Test, while its aqueous extract was toxic. All other extracts were highly toxic and ethanolic extracts of Foeniculum vulgare exhibited the highest toxicity. All plant extracts with exception of Acacia senegal revealed significant antioxidant activity in DPPH free radical scavenging assay.
 These results highly agree with the ethnobotanical uses of these plants as antidiabetic. This study endorses further studies on plants investigated, to determine their potential for type 2 diabetes management. Moreover isolation and identification of active compounds are highly recommended.

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Hassan S. Khalid

Papers

Gems from traditional north-African medicine: medicinal and aromatic plants from Sudan

Antiplasmodial Activity of Some Medicinal Plants Used in Sudanese Folk-medicine

Activity of the dietary flavonoid, apigenin, against multidrug-resistant tumor cells as determined by pharmacogenomics and molecular docking.

Evaluating ancient Egyptian prescriptions today: Anti-inflammatory activity of Ziziphus spina-christi.

A study of antioxidant activity, enzymatic inhibition and in vitro toxicity of selected traditional sudanese plants with anti-diabetic potential