Current Drug Discovery Technologies - Volume 18, Issue 2, 2021

Background: Vitiligo is a hypopigmentation disorder that affects 1% of the world's population. Vitiligo causes white spots on the skin, mucous membranes, or white hair by destroying skin melanocytes. The pathogenesis of vitiligo is unknown but autoimmune, autocytotoxic, and neural mechanisms are suggested. According to the autoimmune theory, in people with vitiligo, immune cells invade and damage melanocytes. T cells are more commonly present in vitiligo patients' skin and remain in the lesion site, which is composed of CD8 and CD4 T cells. Many studies have been conducted on the presence and role of cytokines such as interleukins and interferongamma (IFN-γ) in the vitiligo process. Aim: This study aimed to introduce herbs effective against vitiligo from the perspective of Persian medicine and to investigate their possible therapeutic mechanisms with the possible effects of herbs on autoimmune mechanisms. Methods: For this purpose, keywords were used to extract data from Persian medicine textbooks, and then relevant scientific databases, including Google Scholar, PubMed, Web of Science, and Scopus were examined. Results: It was found that Persian medicine scholars used 50 different medicinal plants to treat and reduce the complications of vitiligo, and recent scientific studies have proven immune-regulating properties and reducing the effect of many of them on cytokines. Conclusion: According to scientific evidence on immunomodulatory effects, new research into the effects of these plants on vitiligo can lead to the discovery of new drugs and approaches for treating this disease.

Background: Cough is one of the most common medical symptoms for which medical advice is sought. Although cough is a protective reflex responsible for clearing the airways from secretions and foreign bodies, it can be a troublesome symptom that causes discomfort to patients. Due to the increasing interest in herbal remedies in both developed and developing countries, in the current study, we aimed to overview medicinal herbs containing essential oils used as antitussive agents according to Traditional Persian Medicine (TPM) textbooks. We summarized the relevant scientific evidence on their possible pharmacological effects. Methods: To collect the evidence for the treatment of cough or “seaal” (cough in ancient books) from TPM sources, five main medicinal Persian manuscripts were studied. The antitussive herbs were listed and their scientific names were identified and authenticated following botanical reference books. ScienceDirect and PubMed online databases were searched for related mechanisms of action of the reported medicinal plants. Results: Forty-nine herbs containing essential oils have been recommended in TPM for the treatment of cough; 21 of them had at least one known mechanism of action for cough suppression in the scientific literature. According to this review, most of the cited medicinal plants were assessed for either nitric oxide inhibitory or antitussive/expectorant activities. Conclusion: In addition to advantageous effects of antitussive herbs recommended by TPM, the present review highlighted some recent evidence-based data on these promising herbs that could be used as an outline for future research on their medicinal use.

Background: Adiantum capillus-veneris L. (Family: Pteridaceae) is a well-known safe medicinal herb used in traditional and modern medicine due to its beneficial pharmacological properties. The current study aimed to compile a review on phytochemicals, pharmacological properties and toxicological effects of this plant. Methods: An incisive search was conducted through electronic scientific databases including PubMed, Scopus, ScienceDirect, and Cochrane Library using keyword ‘Adiantum capillusveneris’. All related in vivo, in vitro, human (English papers), were selected from the beginning up to 1st January 2019. All letters, conference papers, papers dealing with genetics, agriculture, and pure phytochemistry of the herb were excluded. Results: A. capillus veneris revealed various pharmacological activities including the effects on the remodeling of lung alveolar epithelial cells in a hypoxic environment, anti-toxicity properties in liver and testes, anti-hyperglycemic, and wound healing effects in diabetic or non-diabetic patients, protection against damage to fibroblasts via free radicals, activity against testosteroneinduced alopecia, anticonvulsant, depressant, analgesic and anti-nociceptive activities, as well as effects on urinary output, anti-inflammatory, anti-microbial, antilithiatic, hypothyroidism regulatory, anti-cancer, antidiarrheal and antispasmodic, anti-asthmatic and anti-histaminic, and enzyme inhibition (in Alzheimer’s, diabetes and skin disorders) activities. Conclusion: This plant can be used as a natural potent and safe agent to alleviate numerous medical symptoms and diseases due to its useful pharmacological properties. Thus, further researches are needed in order to compile the clinical effects of this plant via human studies.

Sciatica is a common back pain caused by irritation of the sciatic nerve. Current pharmacologic therapies have proven inadequate for many patients with sciatic pain. On the other hand, there is a globally increasing demand for the use and administration of natural medicaments for this disorder. Traditional Persian Medicine (TPM) is a school of medicine and a medicinal plant-based resource for clinical studies put forward by Persian scholars. The aim of the present study is to gather and study the effectiveness of all medicinal plants from five main Persian pharmacopeias. Furthermore, different databases such as PubMed and Scopus have been checked to derive relevant activities for these plants. In all, 99 medicinal plants related to 42 families have been authenticated. Asteraceae and Apiaceae were the most frequent families and roots and seeds were the most reported botanical parts. The employed routes of administration were oral (54%), topical (33%) and rectal (13%). Anti-inflammatory, analgesic activity and antinociceptive properties of medicines are known as some main mechanisms to manage sciatic pain. These functions are possessed by 30%, 15%, and 15% of the studied plants, respectively. Medicaments that can be introduced as lead agents for further investigation are Zingiber officinale Roscoe, Olea europaea L., Strychnos nux-vomica L and Artemisia vulgaris L which showed all of these properties in previous studies. Hence, conducting adducible clinical trials using these lead agents may lead to novel drugs with lesser undesirable and much more therapeutic effects on controlling sciatic pain.

Background: The consumption of natural antioxidants is increasing due to the demand and tendency to natural foods. Punica granatum L. [Punicaceae] is a fruit with various bioactive ingredients. The effectiveness of this plant has been proved against various disorders such as hyperglycemia, hyperlipidemia, blood coagulation, infections, cancer, and dentistry. Among them, there are numerous researches on antimicrobial and antioxidant properties. Subsequently, the present study aimed to compile a review of those properties to outline this herb as a possible natural antioxidant and preservative. Methods: Synchronically, keywords "Punica granatum" with antimicrobial, or antibacterial, antifungal, antiviral, antioxidant and radical scavenging were searched through "Scopus" database up to 31st September 2019. Papers focusing on agriculture, genetics, chemistry, and environmental sciences were excluded, and also related papers were collected. Results: Among 201 papers focusing on related activities, 111 papers have dealt with antioxidant activities focusing based on DPPH assay, 59 with antibacterial, on both gram+ and gram- bacteria, 24 with antifungal effects, mostly on Aspergillus niger and Candida albicans, and 7 papers with antiviral activities. There were about 50 papers focusing on in-vivo antioxidant activities of this plant. Conclusion: Taken together, botanical parts of P. granatum have possessed notable radical scavenging and antimicrobial activities that, with these properties, this plant can be introduced as a natural, safe source of preservative and antioxidant. Accordingly, P. granatum can be applied as excipient with the aforementioned properties in the pharmaceutical and food industries.

Background: Cancer is one of the most prevalent diseases associated with heavy complications in treatment. Mucotoxic cancer therapies such as head and neck radiotherapy and some of the chemotherapy agents may lead to oral mucositis. In addition to its economic consequences, mucositis also affects patients' quality of life. In Traditional Persian Medicine (TPM) manuscripts, several medicaments have been suggested for the treatment of mucositis. Objective: Considering the public welcome for herbal medicine, the current evidence-based review study is conducted to investigate the herbal remedies which have been proposed for oral mucositis in TPM. Methods: At first, a comprehensive survey was done on Qanon fi al-Teb, which is the most important textbook of TPM; then the scientific name of the herbs was authenticated according to the botanical textbooks. At last, data banks including Scopus, Pubmed, Web of science and Science direct were investigated for possible relevant properties of each medicinal plant in the literature. Results: In total, 30 herbs are introduced in this study. According to the registered documents, 18 herbs are reported to have antioxidant, anti-inflammatory, antimicrobial, anti-nociceptive and wound healing properties of which the therapeutic effect of only a few herbs including Glycyrrhiza glabra, Malva sylvestris, Morus nigra, Punica granatum, and Solanum nigrum were directly evaluated against oral mucositis on the literature. Conclusion: Despite the lack of human studies on mucositis for the other discussed herbs, their related pharmacological properties can be considered for new natural drug discovery supported by medieval and traditional experiments.

Nutritional deficiency is a major concern in developing countries, resulting in serious health consequences like mental and physical growth retardation. Moringa oleifera (Moringa), a nutritious plant growing in tropical regions of developing countries, is a candidate for overcoming nutritional deficiency. Moringa leaves are rich in protein including sulphur containing amino acids. It contains high amounts of vitamin C than oranges, a higher concentration of vitamin A than carrots, higher calcium content than milk and more potassium than bananas. Moreover, there is 9 times more iron in moringa than spinach and 4 times more fiber than oats. This review enlightens and explores the nutritional diversification of Moringa oleifera and other benefits which make it a better choice to use in our daily diet to combat malnutrition.

Osteoarthritis (OA) is known to be the leading cause of pain and disability in the elderly. The prevalence of this disease in adults over 60 years was 9.6% in men and 18% in women. The therapeutic goals of this disease generally include pain relief with the least side effects, improvement of articular function and improvement of life, in which pharmacological and nonpharmacological treatments are performed in different protocols. Due to the common side effects of pain relievers and complaints after invasive joint surgeries, there is a growing interest in the use of Traditional and Complementary protocols in OA treatment. In this paper, different sources of Traditional Persian Medicine (TPM) were searched to obtain any evidence evaluating any medicinal plants in the management of OA. Over 250 effective medicinal plants for the treatment of OA have been introduced in these sources, and by searching electronic databases including PubMed and Scopus, we have found that of these plants, 39 have direct or indirect evidence in the treatment of this complication by different mechanism of actions such as effect on Body mass index (BMI), obesity and dyslipidemia, anti-inflammatory, anti-nociceptive and antioxidant activity. The most important medicinal plants with direct evidence in the management of OA are Allium sativum, Commiphora mukul, Linum usitatissimum, Matricaria chamomilla, Nigella sativa, Zingiber officinale, and Piper nigrum. Medicinal plants seem to be a valuable source for discovering and identifying new drugs for treatment of OA; however, since most of the studies are preclinical, further clinical trials are required to achieve more conclusive results.

Introduction: According to Rome IV, functional dyspepsia is diagnosed with the presence of dyspepsia in the absence of organic or metabolic causes. FD caused by several factors, such as impaired gastric accommodation and hypersensitivity to gastric distention. Several studies have reported the effectiveness of herbal medicine on FD. This article, thus, reviews Persian herbal medicine in FD. Methods: Electronic databases, including Pubmed, Scopus, Cochrane, Embase, Web of science and Ovid, were searched so as to find clinical articles related to dyspepsia and herbal medicine by July 2019. Our search strategies were traditional medicine, complementary and alternative medicine, herb, plant, and dyspepsia. We excluded all articles except Persian clinical trials. Results: We found 34 clinical trials with 15 herbs and 4 compound herbal remedies like Asparagus racemosus, Brassica oleracea, Cynara scolymus, Ocimum basilicum, Mentha longifolia, Mentha pulegium, Mentha piperata, Pimpinella anisum, Nigella sativa, Mastic gum, Curcuma longa, Pistatio Atlantica, Glycyrrhiza glabra, Solanum tuberosum and Zingiber officinale and compound remedies of Rosa damascene & Crocus sativus, Trachyspermum copticom & Apium graveolence, Carum carvi & Mentha pipperata, Gingiber officinalis & Cynara scolymus are effective in functional dyspepsia. Conclusion: Many people use herbal and traditional remedies for the treatment of disorders such as gastrointestinal disorders, especially in Asian countries. Several studies reported the efficacy of herbal medicine in functional dyspepsia. Although their mechanisms are not fully understood, it seems they can modulate GI motility and improve symptoms of FD.

Background: Seaweeds, including marine brown algae, are traditional food sources in Asia. Phlorotannins, as the product of the polyketide pathway, are mainly found in brown algae. Different properties have been attributed to this group of marine products ranging from antiallergic to anticancer activity. Mechanism of action is not obvious for all these properties, but there are some explanations for such effects. Objective: The current study aimed to review the phlorotannins and to assess the beneficial uses in medicine. Methods: Different databases were explored with the exact terms “Phlorotannin”, “Seaweed” and “Brown Algae”. Data assembly was finalized by June 2019. The papers showing the effects of phlorotannins in medicine were gathered and evaluated for further assessment. Results: General physiological aspects of phlorotannins were firstly evaluated. Different arrays of pharmacological properties ranging from anti-diabetic activity to cancer treatment were found. The mechanism of action for some of these beneficiary properties has been confirmed through rigorous examinations, but there are some features with unknown mechanisms. Conclusion: Phlorotannins are characterized as a multifunctional group of natural products. Potential antioxidant characteristics could be attributed to preventive and/or their curative role in various diseases.

Objective: The Center of Drug Evaluation and Research (CDER) in the food and drug administration (FDA) approves new drugs every year. This review discusses the novel drugs of the FDA in 2018, with emphasis on the breakthrough drugs, the milestones in the approved list, and drugs with the highest expected sales in 2024. Methods: The following scientific search engines were surveyed for the clinical trials of the drugs approved by the FDA in 2018: Pubmed, Springer link, ScienceDirect, Scopus, Wiley online library, Taylor and Francis, and Google Scholar. The total forecast sales were compared based on information from the Cortellis database, EvaluatePharma, and Nature Biobusiness Briefs. Results: The 2018 year was full of good news for the drug market in the USA, with 59 new drug approvals by the FDA, which is the highest number of approvals in the last twenty years. The oncology and the antimicrobial drugs represent almost 50% of the new list, which gives hope to cancer patients and subjects with infectious diseases. In the 2018 FDA list, a number of drugs are expected to exceed 1$ billion dollars of sales by 2024. Conclusion: The new drugs approved by the FDA in 2018 have been reviewed. This year showed the highest number of new drug approvals in the last two decades. Among the 59 drugs approved in 2018, 14 drugs are considered breakthroughs, which revive hope for many poorly managed diseases. The list also contains 19 drugs that are first in class and 43 that were given priority reviews.

Background: Mycobacterium tuberculosis, being a resistive species is an incessant threat to the world population for the treatment of Tuberculosis (TB). An advanced genetic or a molecular level approach is mandatory for both diagnosis and therapy as the prevalence of multi drug-resistant (MDR) and extensively drug- resistant (XDR) TB. Methods: A literature review was conducted, focusing essentially on the development of biomarkers and targets to extrapolate the Tuberculosis Drug Discovery process. Results and Discussion: In this article, we have discussed several substantial targets and genetic mutations occurring in a diseased or treatment condition of TB patients. It includes expressions in Bhlhe40, natural resistance associated macrophage protein 1 (NRAMP1) and vitamin D receptor (VDR) with its mechanistic actions that have made a significant impact on TB. Moreover, recently identified compounds; imidazopyridine amine derivative (Q203), biphenyl amide derivative (DG70), azetidine, thioquinazole, tetrahydroindazole and 2- mercapto- quinazoline scaffolds for several targets such as adenosine triphosphate (ATP), amino acid and fatty acid have been briefed for their confirmed hits and therapeutic activity.

Aims and Objective: In this study, a novel quantitative structure activity relationship (QSAR) model has been developed for inhibitors of human 5-alpha reductase type II, which are used to treat benign prostate hypertrophy (BPH). Methods: The dataset consisted of 113 compounds-mainly nonsteroidal-with known inhibitory concentration. Then 3D structures of compounds were optimized and molecular structure descriptors were calculated. The stepwise multiple linear regression was used to select descriptors encoding the inhibitory activity of the compounds. Multiple linear regression (MLR) was used to build up the linear QSAR model. Results: The results obtained revealed that the descriptors which best describe the activity were atom type electropological state, carbon type, radial distribution function (RDF), barysz matrix and molecular linear free energy relation. The suggested model could achieve satisfied square correlation coefficient of R² = 0.72, higher than of many previous studies, indicating its superiority. Rigid validation criteria were met using external data with Q² > 0.5 and R² = 0.75, reflecting the predictive power of the model. Conclusion: The QSAR model was applied for screening botanical components of herbal preparations used to treat BPH, and could predict the activity of some, among others, making reasonable attribution to the proposed effect of these preparations. Gamma tocopherol was found to be an active inhibitor, in consistence with many previous studies, anticipating the power of this model in the prediction of new candidate molecules and suggesting further investigations.