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Ethnomedicinal uses, phytochemistry, pharmacological activities and toxicological profile of Glycosmis pentaphylla (Retz.) DC.: A review

Khandokar L, Bari MS, Seidel V, Haque MA

J Ethnopharmacol, 2021 Oct 05;278:114313.
PMID: 34116186 DOI: 10.1016/j.jep.2021.114313

ETHNOPHARMACOLOGICAL RELEVANCE: Glycosmis pentaphylla (Retz.) DC. is a perennial shrub indigenous to the tropical and subtropical regions of India, China, Sri Lanka, Myanmar, Bangladesh, Indonesia, Malaysia, Thailand, Vietnam, Philippine, Java, Sumatra, Borneo and Australia. The plant is used extensively within these regions as a traditional medicine for the treatment of a variety of ailments including cough, fever, chest pain, anemia, jaundice, liver disorders, inflammation, bronchitis, rheumatism, urinary tract infections, pain, bone fractures, toothache, gonorrhea, diabetes, cancer and other chronic diseases.
AIM OF THE REVIEW: This review aims to present up-to-date information regarding the taxonomy, botany, distribution, ethnomedicinal uses, phytochemistry, pharmacology and toxicological profile of G. pentaphylla. The presented information was analyzed critically to understand current work undertaken on this species and explore possible future prospects for this plant in pharmaceutical research.
MATERIALS & METHODS: Bibliographic databases, including Google Scholar, PubMed, Web of Science, ScienceDirect, SpringerLink, Wiley Online Library, Semantic Scholar, Europe PMC, Scopus, and MEDLINE, were explored thoroughly for the collection of relevant information. The structures of phytoconstituents were confirmed with PubChem and SciFinder databases. Taxonomical information on the plant was presented in accordance with The Plant List (version 1.1).
RESULTS: Extensive phytochemical investigations into different parts of G. pentaphylla have revealed the presence of at least 354 secondary metabolites belonging to structurally diverse classes including alkaloids, amides, phenolic compounds, flavonoids, glycosides, aromatic compounds, steroids, terpenoids, and fatty derivatives. A large number of in vitro and in vivo experiments have demonstrated that G. pentaphylla had anticancer, antimutagenic, antibacterial, antifungal, anthelmintic, mosquitocidal, antidiabetic, antihyperlipidemic, anti-oxidant, anti-inflammatory, analgesic, antipyretic, anti-arsenicosis, and wound healing properties. Toxicological studies have established the absence of any significant adverse reactions and showed that the plant had a moderate safety profile.
CONCLUSIONS: G. pentaphylla can be suggested as a source of inspiration for the development of novel drugs, especially anticancer, antimicrobial, anthelmintic, and mosquitocidal agents. Moreover, bioassay-guided investigations into its diverse classes of secondary metabolites, especially the large pool of nitrogen-containing alkaloids and amides, promises the development of novel drug candidates. Future pharmacological studies into this species are also warranted as many of its traditional uses are yet to be validated scientifically.
Ethnomedicinal uses, phytochemistry, and biological activities of plants of the genus Gynura

Bari MS, Khandokar L, Haque E, Romano B, Capasso R, Seidel V, et al.

J Ethnopharmacol, 2021 May 10;271:113834.
PMID: 33465439 DOI: 10.1016/j.jep.2021.113834

ETHNOPHARMACOLOGICAL RELEVANCE: The genus Gynura (Compositae) includes around 46 species and is native to the tropical regions of Southeast Asia, Africa and Australia. Many species within this genus are used in ethnomedicine to treat various disorders including skin diseases, injuries, ulcers, wounds, burns, sores, scalds, as well as for the management of diabetes, hypertension, hyperlipidemia, constipation, rheumatism, bronchitis and inflammation.
AIM OF THE REVIEW: This review is an attempt to provide scientific information regarding the ethnopharmacology, phytochemistry, pharmacological and toxicological profiles of Gynura species along with the nomenclature, distribution, taxonomy and botanical features of the genus. A critical analysis has been undertaken to understand the current and future pharmaceutical prospects of the genus.
MATERIALS & METHODS: Several electronic databases, including Google scholar, PubMed, Web of Science, Scopus, ScienceDirect, SpringerLink, Semantic Scholar, MEDLINE and CNKI Scholar, were explored as information sources. The Plant List Index was used for taxonomical authentications. SciFinder and PubChem assisted in the verification of chemical structures.
RESULTS: A large number of phytochemical analyses on Gynura have revealed the presence of around 342 phytoconstituents including pyrrolizidine alkaloids, phenolic compounds, chromanones, phenylpropanoid glycosides, flavonoids, flavonoid glycosides, steroids, steroidal glycosides, cerebrosides, carotenoids, triterpenes, mono- and sesquiterpenes, norisoprenoids, oligosaccharides, polysaccharides and proteins. Several in vitro and in vivo studies have demonstrated the pharmacological potential of Gynura species, including antidiabetic, anti-oxidant, anti-inflammatory, antimicrobial, antihypertensive and anticancer activities. Although the presence of pyrrolizidine alkaloids within a few species has been associated with possible hepatotoxicity, most of the common species have a good safety profile.
CONCLUSIONS: The importance of the genus Gynura both as a prominent contributor in ethnomedicinal systems as well as a source of promising bioactive molecules is evident. Only about one fourth of Gynura species have been studied so far. This review aims to provide some scientific basis for future endeavors, including in-depth biological and chemical investigations into already studied species as well as other lesser known species of Gynura.
Fulltext An updated and comprehensive review on the ethnomedicinal uses, phytochemistry, pharmacological activity and toxicological profile of Tinospora crispa (L.) Hook. f. & Thomson

Haque E, Bari MS, Khandokar L, Anjum J, Jantan I, Seidel V, et al.

Phytochem Rev, 2023;22(1):211-273.
PMID: 36345416 DOI: 10.1007/s11101-022-09843-y

Tinospora crispa (L.) Hook. f. & Thomson (Menispermaceae) is a plant indigenous to Africa and South-East Asia. It is widely used in ethnomedicine to alleviate various diseases including hypertension, diabetes, rheumatism, jaundice, inflammation, fever, fractures, scabies, and urinary disorders. A total of 167 phytoconstituents, belonging to 12 different chemical categories, including alkaloids, flavonoids, terpenoids, and phenolic compounds have thus far been isolated from various parts of T. crispa. Numerous in vitro and in vivo investigations have already established the antidiabetic, anticancer, antiparasitic, antimicrobial, immunomodulatory, hepatoprotective, analgesic, antipyretic, antihyperuricemic, and pesticidal activity of this plant, as well as its effects on the cardiac and the central nervous system. Most pharmacological investigations to date have been carried out on plant extracts and fractions. The exact identity of the phytoconstituents responsible for the observed biological effects and their mode of action at the molecular level are yet to be ascertained. Toxicological studies have demonstrated that T. crispa is relatively safe, although dose-dependent hepatotoxicity is a concern at high doses. This review presents a comprehensive update and analysis on studies related to the ethnomedicinal uses, phytochemistry, pharmacological activity and toxicological profile of T. crispa. It provides some critical insights into the current scientific knowledge on this plant and its future potential in pharmaceutical research.
Evaluation of potential bacterial protease inhibitor properties of selected hydroxyquinoline derivatives: an in silico docking and molecular dynamics simulation approach

Riaz F, Hossain MS, Roney M, Ali Y, Qureshi S, Muhammad R, et al.

J Biomol Struct Dyn, 2023 Nov;41(19):9756-9769.
PMID: 36399018 DOI: 10.1080/07391102.2022.2146200

Antimicrobial drug resistance (AMR) is a severe global threat to public health. The increasing emergence of drug-resistant bacteria requires the discovery of novel antibacterial agents. Quinoline derivatives have previously been reported to exhibit antimalarial, antiviral, antitumor, antiulcer, antioxidant and, most interestingly, antibacterial properties. In this study, we evaluated the binding affinity of three newly designed hydroxyquinolines derived from sulfanilamide (1), 4-amino benzoic acid (2) and sulfanilic acid (3) towards five bacterial protein targets (PDB ID: 1JIJ, 3VOB, 1ZI0, 6F86, 4CJN). The three derivatives were designed considering the amino acid residues identified at the active site of each protein involved in the binding of each co-crystallized ligand and drug-likeness properties. The ligands displayed binding energy values with the target proteins ranging from -2.17 to -8.45 kcal/mol. Compounds (1) and (3) showed the best binding scores towards 1ZI0/3VOB and 1JIJ/4CJN, respectively, which may serve as new antibiotic scaffolds. Our in silico results suggest that sulfanilamide (1) or sulfanilic acid (3) hydroxyquinoline derivatives have the potential to be developed as bacterial inhibitors, particularly MRSA inhibitors. But before that, it must go through the proper preclinical and clinical trials for further scientific validation. Further experimental studies are warranted to explore the antibacterial potential of these compounds through preclinical and clinical studies.Communicated by Ramaswamy H. Sarma.