Novel saturated 1,2,4-trioxanes and their antimalarial activity against multidrug resistant Plasmodium yoelii nigeriensis in Swiss mice model via oral route.

Novel saturated 6-(4'-aryloxy phenyl) vinyl 1,2,4-trioxanes 12a(1-3)-12d(1-3) and 13a(1-3)-13d(1-3) have been designed and synthesized, in one single step from diimide reduction of 11a(1-3)-11d(1-3). All the newly synthesized trioxanes were evaluated for their antimalarial activity against multi-drug resistant Plasmodium yoelii nigeriensis via oral route. Cyclopentane-based trioxanes 12b1, 12c1 and 12d1, provided 100 % protection to the infected mice at 24 mg/kg × 4 days. The most active compound of the series, trioxane 12b1, provided 100 % protection even at 12 mg/kg × 4 days and 60 % protection at 6 mg/kg × 4 days. The currently used drug, ß-arteether provides only 20 % protection at 24 mg/kg × 4 days.

Novel ether derivatives of 11-azaartemisinins with high order antimalarial activity against multidrug-resistant Plasmodium yoelii in Swiss mice.

This study investigates cutting-edge synthetic chemistry approaches for designing and producing innovative antimalarial drugs with improved efficacy and fewer adverse effects. Novel amino (-NH2) and hydroxy (-OH) functionalized 11-azaartemisinins 9, 12, and 14 were synthesized along with their derivatives 11a, 13a-e, and 15a-b through ART and were tested for their AMA (antimalarial activity) against Plasmodium yoelii via intramuscular (i.m.) and oral routes in Swiss mice. Ether derivative 13c was the most active compound by i.m. route, it has shown 100 % protection at the dose of 12 mg/kg × 4 days and showed 100 % clearance of parasitaemia on day 4 at dose of 6 mg/kg. Amine 11a, ether derivatives 13d, 13e and ether 15a also showed promising antimalarial activity. ß-Arteether gave 100 % protection at the dose of 48 mg/kg × 4 days and 20 % protection at 24 mg/kg × 4 days dose by oral route, while it showed 100 % protection at 6 mg/kg × 4 days and no protection at 3 mg/kg × 4 days by i.m. route.

Exploring apple pectic polysaccharides: Extraction, characterization, and biological activities - A comprehensive review.

Apple (Malus domestica) is a popular and ancient fruit of the Myrtaceae family. Apple fruit is well-known for its great nutritional and phytochemical content consisted of beneficial compounds such as polyphenols, polysaccharides, sterols, and organic acids. Polysaccharides extracted from different parts of the apple fruit, including the peel, pomace, or the whole fruit, have been extensively studied. Researchers have investigated the structural characteristics of these polysaccharides, such as molecular weight, type of monosaccharide unit, type of linkage and its position and arrangement. Besides this, functional properties and physicochemical and of apple polysaccharides have also been studied, along with the effects of extraction procedures, storage, and processing on cell wall polysaccharides. Various extraction techniques, including hot water extraction, enzymatic extraction, and solvent-assisted extraction, have been studied. From the findings, it was evident that apple polysaccharides are mainly composed of (1 â†’ 3), (1 â†’ 6): α-ß-glycosidic linkage. Moreover, the apple polysaccharides were demonstrated to exhibit antioxidant, hepatoprotective, anti-cancer, hypoilipidemic, and enzyme inhibitory properties in vitro and in vivo. The potential applications of apple polysaccharides in the food, cosmetic, pharmaceutical, nutraceutical industries have also been explored in the present review. Overall, the research on apple polysaccharides highlights their significant potential as a source of biologically active compounds with various health benefits and practical applications.

Novel amino- and hydroxy-functionalized 1,2,4-trioxanes and their antimalarial activity against multidrug-resistant Plasmodium yoelii nigeriensis in Swiss mice via intramuscular and oral route.

Following the economic and social state of humanity, Malaria is categorized as one of the life-threatening illness epidemics in under developed countries. For the eradication of the same, 1,2,4-trioxanes 17a1-a2, 17b1-b2, 17c1-c2 15a-c, 18 and 19 have been synthesized continuing the creation of a novel series. Additionally, these novel compounds were tested for their effectiveness against the multidrug-resistant Plasmodium yoelii nigeriensis in mice model using both oral and intramuscular (im) administration routes. The two most potent compounds of the series, 17a1 and 17a2, demonstrated 100 % protection at 48 mg/kg x 4 days via oral route, which is twice as potent as artemisinin. In this model artemisinin provided 100 % protection at a dose of 48 mg/kg × 4 days and 80 % protection at 24 mg/kg × 4 days via im route.

Chemical Diversity and Medicinal Potential of Vitex negundo L.: From Traditional Knowledge to Modern Clinical Trials.

BACKGROUND: In Vedic context, Nirgundi (V. negundo) has been utilized for its anti-inflammatory, analgesic, and wound-healing properties. It has been employed to alleviate pain, treat skin conditions, and address various ailments. The plant's leaves, roots, and seeds have all found applications in traditional remedies. The knowledge of Nirgundi's medicinal benefits has been passed down through generations, and it continues to be a part of Ayurvedic and traditional medicine practices in India.

Phytochemicals, therapeutic benefits and applications of chrysanthemum flower: A review.

Chrysanthemum is a flowering plant belonging to a genus of the dicotyledonous herbaceous annual flowering plant of the Asteraceae (Compositae) family. It is a perpetual flowering plant, mostly cultivated for medicinal purposes; generally, used in popular drinks due to its aroma and flavor. It is primarily cultivated in China, Japan, Europe, and United States. These flowers were extensively used in various healthcare systems and for treating various diseases. Chrysanthemum flowers are rich in phenolic compounds and exhibit strong properties including antioxidant, antimicrobial, anti-inflammatory, anticancer, anti-allergic, anti-obesity, immune regulation, hepatoprotective, and nephroprotective activities. The main aim of the present review was to investigate the nutritional profile, phytochemistry, and biological activities of flowers of different Chrysanthemum species. Also, a critical discussion of the diverse metabolites or bioactive constituents of the Chrysanthemum flowers is highlighted in the present review. Moreover, the flower extracts of Chrysanthemum have been assessed to possess a rich phytochemical profile, including compounds such as cyanidin-3-O-(6″-O-malonyl) glucoside, delphinidin 3-O-(6" -O-malonyl) glucoside-3', rutin, quercetin, isorhamnetin, rutinoside, and others. These profiles exhibit potential health benefits, leading to their utilization in the production of supplementary food products and pharmaceutical drugs within the industry. However, more comprehensive research studies/investigations are still needed to further discover the potential benefits for human and animal utilization.

A systematic review on endophytic fungi and its role in the commercial applications.

MAIN CONCLUSION: EF have been explored for its beneficial impact on environment and for its commercial applications. It has proved its worth in these sectors and showed an impact on biological properties of plants by producing various bioactive molecules and enzymes. Endophytes are plant mutualists that live asymptomatically within plant tissues and exist in almost every plant species. Endophytic fungi benefit from the host plant nutrition, and the host plant gains improved competitive abilities and tolerance against pathogens, herbivores, and various abiotic stresses. Endophytic fungi are one of the most inventive classes which produce secondary metabolites and play a crucial role in human health and other biotic aspects. This review is focused on systematic study on the biodiversity of endophytic fungi in plants, and their role in enhancing various properties of plants such as antimicrobial, antimycobacterial, antioxidant, cytotoxic, anticancer, and biological activity of secondary metabolites produced by various fungal endophytes in host plants reported from 1994 to 2021. This review emphasizes the endophytic fungal population shaped by host genotype, environment, and endophytic fungi genotype affecting host plant. The impact of endophytic fungi has been discussed in detail which influences the commercial properties of plants. Endophytes also have an influence on plant productivity by increasing parameters such as nutrient recycling and phytostimulation. Studies focusing on mechanisms that regulate attenuation of secondary metabolite production in EF would provide much needed impetus on ensuring continued production of bioactive molecules from a indubitable source. If this knowledge is further extensively explored regarding fungal endophytes in plants for production of potential phytochemicals, then it will help in exploring a keen area of interest for pharmacognosy.

Acacia catechu (L.f.) Willd.: A Review on Bioactive Compounds and Their Health Promoting Functionalities.

With the advent of pandemics and infectious diseases, numerous research activities on natural products have been carried out to combat them. Researchers are investigating natural products for the treatment and/or management of various infectious diseases and/or disorders. Acacia catechu (L.f.) Willd. belongs to the family Fabaceae (subfamily Mimosoideae) known as Khair or Cutch tree, possesses diverse pharmacological actions, and has been widely used in Asia and different parts of the world. The purpose of the present study is to highlight the phytochemical profile of different parts of A. catechu, the different biological activities of A. catechu extract, and the utilization of A. catechu as food and beverage. The present work constitutes a review of A. catechu; we performed searches (books, Google, Google Scholar, and Scopus publications) to compile the work/investigations made on A. catechu to the present. From our survey, it was concluded that the main phytochemicals compounds in A. catechu are protocatechuic acid, taxifolin, epicatechin, epigallocatechin, catechin, epicatechin gallate, procyanidin, phloroglucin, aldobiuronic acid, gallic acid, D-galactose, afzelchin gum, L-arabinose, D-rhamnose, and quercetin. The whole plant of A. catechu possesses a comprehensive variety of medicinal potentials such as antimicrobial, antidiarrheal, antinociceptive, antihyperlipidemic, antiulcer, antioxidant, antidiabetic, antiproliferative, haemolytic, and anti-inflammatory properties due to the presence of bioactive compounds like flavonoids, alkaloids, and tannins. However, even though the plant's metabolites were reported to have many different pharmacological uses, there is limited information about their toxicity or clinical trials. Further research on diverse metabolites of A. catechu should be carried out to ensure the safety or utilization of this plant in the pharma or food industries and in the development of potent plant-based drugs.

Onion and garlic polysaccharides: A review on extraction, characterization, bioactivity, and modifications.

Allium cepa (onion) and Allium sativum (garlic) are important members of the Amaryllidaceae (Alliaceae) family and are being used both as food and medicine for centuries in different parts of the world. Polysaccharides have been extracted from different parts of onion and garlic such as bulb, straw and cell wall. The current literature portrays several studies on the extraction of polysaccharides from onion and garlic, their modification and determination of their structural (molecular weight, monosaccharide unit and their arrangement, type and position of glycosidic bond or linkage, degree of polymerization, chain conformation) and functional properties (emulsifying property, moisture retention, hygroscopicity, thermal stability, foaming ability, fat-binding capacity). In this line, this review, summarizes the various extraction techniques used for polysaccharides from onion and garlic, involving methods like solvent extraction method. Furthermore, the antioxidant, anticancer, immunomodulatory, antimicrobial, anti-inflammatory, and antidiabetic properties of onion and garlic polysaccharides as reported in in vivo and in vitro studies are also critically assessed in this review. Different studies have proved onion and garlic polysaccharides as potential antioxidant and immunomodulatory agent. Studies have implemented to improve the functionality of onion and garlic polysaccharides through various modification approaches. Further studies are warranted for utilizing onion and garlic polysaccharides in the food, nutraceutical, pharmaceutical and cosmetic industries.

A survey on ethnoveterinary medicines used by the tribal migratory shepherds of Northwestern Himalaya.

ETHNOPHARMACOLOGICAL RELEVANCE: Tribal migratory shepherds (Gaddi) living in the Northwestern Himalayan region are well known for their nomadic lifestyle in which tribal migratory shepherds along with their livestock which mainly include sheep and goat migrate seasonally in the Northwestern Himalayan region from high hills to low hills for the survival of their livestock from cold winters and hot summer. Due to harsh environmental conditions, heavy snowfall, heavy rainfall, wild animal attacks, no medical facilities, no transportation, and no electricity facilities tribal migratory shepherds mostly rely on plant species mentioned for ethnoveterinary use to treat livestock disease. AIM OF STUDY: The aim of our study is to conduct ethnoveterinary survey for the first time to document the contemporary oral ethnoveterinary knowledge of Gaddi shepherds living in Northwestern Himalayan region. METHODOLOGY: The documentation of plant species mentioned for ethnoveterinary use was executed through extensive field surveys from 2017 to 2019. Data were collected through direct interviews by administrating questionnaire among tribal migratory shepherds. RESULTS: A total of 181 plant species mentioned for ethnoveterinary use belonging to the same or different families were documented during the seasonal migration of shepherds from Northwestern Himalayan region. Most frequently occurring family of plant species mentioned for ethnoveterinary was Poaceae, leaves and roots were reported to be the most frequently used plant parts. Most frequently documented plant species for ethnoveterinary use were Cynodon dactylon, Chenopodium album, Zanthoxylum armatum, Aloe vera, Azadirachta indica and Cannabis sativa. Chrysopogon serrulatus, Cynodon dactylon, and Vitex negundo were reported with high use reports. Some of the endemic species of Northwestern Himalayan region such as Elymus himalayanus and Euphorbia pilosa and one endangered species Picrorhiza kurrooa were reported in current study. CONCLUSION: It is observed that there is a need to raise awareness among the tribal migratory shepherds about the sustainable use and conservation of some of the plant species mentioned for ethnoveterinary use. This study provided an inventory of plant species mentioned for ethnoveterinary use having significant ethnoveterinary potential, however there is need of scientific evaluations by in vitro, in vivo and clinical studies.

Ethnomedicinal plants used for the treatment of neurodegenerative diseases in Himachal Pradesh, India in Western Himalaya.

ETHNOPHARMACOLOGICAL RELEVANCE: Medicinal plants are considered as a healthcare resource and widely used by rural people in their traditional medicine system for curing neurodegenerative diseases. Neurodegenerative diseases refer to incurable and debilitating conditions that result in progressive degeneration/death of nerve cells or neurons in the human brain. This review is mainly focused on the usage of different ethnomedicinal plants in the treatment of different neurodegenerative diseases in Himachal Pradesh. Study reveals total of 73 ethnomedicinal plants, which are used for treating different neurological disorders in different areas of Himachal Pradesh. The data is compiled from the different sources that described the detailed information of plants in tabular form and highlights the significance of different phytochemicals on neuroprotective function. The present study also provides the scientific data and clinical (in-vivo and in-vitro) studies in support of ethnomedicinal use. AIM OF THE STUDY: This review aims to provide information of ethnomedicinal plants which are used for the treatment of neurodegenerative diseases in Himachal Pradesh. MATERIALS AND METHODS: Information on the use of ethnomedicinal plants to treat various neurological disorders has been gathered from a variety of sources, including various types of literature, books, and relevant publications in Google Scholar, Research Gate, Science Direct, Scopus, and Pub Med, among others. The collected data is tabulated, including the botanical names of plants, mode of use and the disease for which it is used for curing, etc. RESULTS: There are 73 ethnomedicinal plants that are used to cure various neurological disorders, with the most plants being used to treat epilepsy problem in Himachal Pradesh. CONCLUSION: Numerous phytochemicals and extracts from diverse plants were found to have a protective effect against neurodegenerative diseases. Antioxidant activity is known to exist in a variety of herbal plants. The most common bioactive antioxidant chemicals having their significant impacts include flavonoids, flavones, coumarins, lignans, isoflavones, catechins, anthocyanins, and isocatechins.

Novel hydrazone derivatives of N-amino-11-azaartemisinin with high order of antimalarial activity against multidrug-resistant Plasmodium yoelii nigeriensis in Swiss mice via intramuscular route.

Novel hydrazone derivatives 10a-m were prepared from N-Amino-11-azaartemisinin (9) and screened for their antimalarial activity by oral and intramuscular (i.m.) routes against multidrug-resistant Plasmodium yoelii in Swiss mice model. Several of the hydrazone derivatives showed higher order of antimalarial activity. Compounds 10b, 10g, 10m provided 100% protection to the infected mice at the dose of 24 mg/kg × 4 days via oral route. Fluorenone based hydrazone 10m the most active compound of the series, provided 100% protection at the dose of 6 mg/kg × 4 days via intramuscular route and also provided 100% protection at the dose of 12 mg/kg × 4 days via oral route. While artemisinin gave 100% protection at 48 mg/kg × 4 days and only 60% protection at 24 mg/kg × 4 days via intramuscular (i.m.) route. Compound 10m found to be four-fold more active than artemisinin via intramuscular route.

Reduction of the Double Bond of 6-Arylvinyl-1,2,4-trioxanes Leads to a Remarkable Increase in Their Antimalarial Activity against Multidrug-Resistant Plasmodium yoelii nigeriensis in a Swiss Mice Model.

Novel 6-arylethyl-1,2,4-trioxanes6a-i and 7a-i are easily accessible in one step from the diimide reduction of 6-arylvinyl-1,2,4-trioxanes 5a-i. All of these new trioxanes were assessed for their oral antimalarial activity against multidrug-resistant Plasmodium yoelii nigeriensis in a Swiss mice model. Most of the saturated trioxanes 6c, 6f, 6g, 6h, and 6i, the active compounds of the series, provided 100% protection to the malaria-infected mice at a dose of 24 mg/kg × 4 days. Further, trioxane 6i, the most active compound of the series, also showed 100% protection even at a dose of 12 mg/kg × 4 days and 20% protection at a dose of 6 mg/kg × 4 days. In this model, ß-arteether provided 100% protection at a dose of 48 mg/kg × 4 days and only 20% protection at a dose of 24 mg/kg × 4 days via the oral route, which was found to exhibit 4-fold antimalarial activity compared with the currently used drug ß-arteether.

Rare Case of Spontaneous Pneumorrhachis in a Young Male with COVID-19.

Here we present a rare case of spontaneous pneumomediastinum complicated with pneumorrhachis (PR) in a young man who is a known case of carcinoma rectosigmoid region. Our young male was diagnosed with novel coronavirus disease 2019 (COVID-19) and remained asymptomatic for any respiratory complaints. Though an association of pneumomediastinum has been reported in COVID 19 patients, to the best of our knowledge, this is the first report of PR in a COVID-19 oncological case. The role of a radiologist is to identify this condition as cases reported earlier may have serious neurological consequences. Pursuing the cause can be a diagnostic challenge but it reaps the clinical benefit in the appropriate management.

Plant-Based Antioxidant Extracts and Compounds in the Management of Oral Cancer.

Oral cancer continues to be a leading cause of death worldwide, and its prevalence is particularly high in developing countries, where people chew tobacco and betel nut on a regular basis. Radiation-, chemo-, targeted-, immuno-, and hormone-based therapies along with surgery are commonly used as part of a treatment plan. However, these treatments frequently result in various unwanted short- to long-term side effects. As a result, there is an urgent need to develop treatment options for oral cancer that have little or no adverse effects. Numerous bioactive compounds derived from various plants have recently attracted attention as therapeutic options for cancer treatment. Antioxidants found in medicinal plants, such as vitamins E, C, and A, reduce damage to the mucosa by neutralizing free radicals found in various oral mucosal lesions. Phytochemicals found in medicinal plants have the potential to modulate cellular signalling pathways that alter the cellular defence mechanisms to protect normal cells from reactive oxygen species (ROS) and induce apoptosis in cancer cells. This review aims to provide a comprehensive overview of various medicinal plants and phytoconstituents that have shown the potential to be used as oral cancer therapeutics.

Ethnomedicinal Plants Used in the Health Care System: Survey of the Mid Hills of Solan District, Himachal Pradesh, India.

The study was performed in the mid hills of the Dharampur region in Solan district of Himachal Pradesh, India. At the study site, a total of 115 medicinal plants were documented (38 trees, 37 herbs, 34 shrubs, 5 climbers, 1 fern, and 1 grass). In the study region, extensive field surveys were performed between March 2020 and August 2021. Indigenous knowledge of wild medicinal plants was collected through questionnaires, discussions, and personal interviews during field trips. Plants with their correct nomenclature were arranged by botanical name, family, common name, habitat, parts used, routes used, and diseases treated. In the present study, the predominant family was Rosaceae, which represented the maximum number of plant species, 10, followed by Asteraceae and Lamiaceae, which represented 8 plant species. The rural inhabitants of the Dharampur region in the Solan district have been using local plants for primary health care and the treatment of various diseases for a longer time. However, information related to the traditional knowledge of medicinal plants was not documented. The rural inhabitants of the Dharampur region reported that the new generation is not so interested in traditional knowledge of medicinal plants due to modernization in society, so there is an urgent need to document ethnomedicinal plants before such knowledge becomes inaccessible and extinct.

Novel naphthyl based 1,2,4-trioxanes: Synthesis and in vivo efficacy in the Plasmodium yoelii nigeriensis in Swiss mice.

A new series of 1,2,4-trioxanes 9a1-a4, 9b1-b4, 10-13 and 9c1-c4 were synthesized and evaluated against multidrug-resistant Plasmodium yoelii nigeriensis in Swiss mice via oral and intramuscular (i.m.) routes. Adamantane-based trioxane 9b4, the most active compound of the series, provided 100% protection to the infected mice at the dose 48 mg/kg × 4 days and 100% clearance of parasitemia at the dose 24 mg/kg × 4 days via oral route. Adamantane-based trioxane 9b4, is twice active than artemisinin. We have also studied the photooxygenation behaviour of allylic alcohols 6a-b (3-(4-alkoxynaphthyl)-but-2-ene-1-ols) and 6c (3-[4-(tert-butyl-dimethyl-silanyloxy)-naphthalen-1-yl]-but-2-en-1-ol). Being behaving as dienes, they furnished corresponding endoperoxides, while behaving as allylic alcohols, they yielded ß-hydroxyhydroperoxides. All the endoperoxides (7a-c) and ß-hydroxyhydroperoxides (8a-c) have been separately elaborated to the corresponding 1,2,4-trioxanes, except from endoperoxide 7c. It is worthy to note that TBDMS protected naphthoyl endoperoxide 7c unable to deliver 1,2,4-trioxane, which demonstrated the strength of the O-Si bond is not easy to cleave under acidic condition.

Synthesis of novel 1,2,4-trioxanes and antimalarial evaluation against multidrug-resistant Plasmodium yoelii nigeriensis.

Malaria epidemics represent one of the life-threatening diseases to low-income lying countries which subsequently affect the economic and social condition of mankind. In continuation in the development of a novel series of 1,2,4-trioxanes 13a1-c1, 13a2-c2, and 13a3-c3 have been prepared and further converted into their hemisuccinate derivatives 14a1-c1, 14a2-c2, and 14a3-c3 respectively. All these new compounds were evaluated for their antimalarial activity against multidrug-resistant Plasmodium yoelii nigeriensis in mice by both oral and intramuscular (im) routes. Hydroxy-functionalized trioxane 13a1 showed 80% protection and its hemisuccinate derivative 14a1 showed 100% protection at a dose of 48 mg/kg × 4 days by both routes, which is twice active than artemisinin by oral route.

Evaluation of Nutritional, Phytochemical, and Mineral Composition of Selected Medicinal Plants for Therapeutic Uses from Cold Desert of Western Himalaya.

The aim of this study was to determine the elemental and nutritive values of leaf parts of 10 selected wild medicinal plants, Acer pictum, Acer caecium, Betula utilis, Oxalis corniculata, Euphorbia pilosa, Heracleum lanatum, Urtica dioica, Berberis lycium, Berberis asiaticaand, and Quercus ilex, collected from the high hills of the Chitkul range in district Kinnaur, Western Himalaya. The nutritional characteristics of medicinal plant species were analyzed by using muffle furnace and micro-Kjeldahl methods, and the mineral content in plants was analyzed through atomic absorption spectrometry. The highest percentage of used value was reported in Betula utilis (0.42) and the lowest in Quercus ilex (0.17). In this study, it was found that new generations are not much interested in traditional knowledge of ethnomedicinal plants due to modernization in society. Therefore, there is an urgent need to document ethnomedicinal plants along with their phytochemical and minerals analysis in study sites. It was found that rural people in western Himalaya are dependent on wild medicinal plants, and certain steps must be taken to conserve these plants from extinction in the cold desert of Himalayan region. They are an alternative source of medicine because they contain saponin, alkaloid, and flavonoid etc. as well as minerals. The leaves used for analysis possesses good mineral content, such as Na, N, K, P, Zn, Fe, Cu, Mn, Ca, Mg, and S. Hence, in the current study it was observed that medicinal plants are not only used for therapeutic purposes, but they can also be used as nutritional supplements.