Organic Chemistry
Mechanistic Overview on the Therapeutic Potential of Alkaloids in Combating Non-small Cell Lung Carcinoma
Non-small Cell Lung Cancer (NSCLC) holds a significant position globally among cancer types. Alkaloids which are natural compounds containing nitrogen atoms are found in various plant sources and play a crucial role in anti-cancer activity offering potential therapeutic applications. They are classified by their chemical structure into categories such as indole alkaloids isoquinoline alkaloids pyrrole and pyrrolizidine alkaloids β-carboline and benzoquinolizidine alkaloids quinazoline alkaloids and diterpene alkaloids. Alkaloid-based treatments offer several advantages in drug design including high bioavailability lower toxicity and effective therapeutic outcomes. Drugs like vinca alkaloids camptothecin and sanguinarine demonstrate high efficacy against lung cancer cells. Combination therapy involving alkaloids can prevent chemoresistance and exhibit high potency against cancer cells. This review highlights the importance of alkaloids in combating chemoresistance in lung cancer. The mechanisms by which alkaloids inhibit the EGFR/AKT/MAPK signaling pathways and induce apoptosis are discussed in detail. In the future alkaloid-based therapeutics for NSCLC and other malignancies may be explored as advanced and effective treatment options.
The Impact of Tea Consumption on Cardiovascular Health
Tea is a popular beverage that comprises various antioxidants. Tea is the second most consumed beverage in the world after water. The three ideal types of tea include black white and green teas. Catechin Epicatechin gallate and Epicatechin are the striped flavonoids coeval in the tea. These flavonoids are freed as a rich source for blood circulation in the heart. Tea possesses anti-inflammatory anti-neoplastic anti-arthritic anti-thrombotic antimicrobial anti-platelet aggregation anti-cholesterol anti-hyperglycemic and immuno-protective properties. Modern empowering research studies contemplate that minimal consumption of tea can also be of advantage to the cardiovascular system (CVS) as it modulates oxidative stress. Consumption of tea is beneficial for cardiovascular diseases such as atherosclerosis coronary artery disease aortic aneurysms peripheral artery disease stroke ischemic heart disease and cardiomyopathy. Consumption of excess tea may also be detrimental to health and we highlight different types of tea. The main aim of the present narrative review is to highlight the natural compounds present in tea and discuss their mechanism of action on the cardiovascular system. Based on evidence gathered from published literature it is thereby concluded that tea is a popular drink with potential cardiovascular health benefits.
Updates on the Anticancer Profile of Lycopene and its Probable Mechanism against Breast and Gynecological Cancer
Natural substances are gaining interest as anticancer agents nowadays due to the adverse effects of synthetic drugs. Among various natural substances lycopene has emerged as a strong antioxidant agent and has been found to be effective against prostate breast colon ovarian liver endometrial cancers etc. This article reviews the therapeutic potential and proposed mechanism of action of lycopene against breast and gynecological cancer from 2005 to now. Experimental studies suggest that lycopene can inhibit tumor growth by regulating various signaling pathways for cell growth arresting the cell cycle and inducing cell apoptosis. Lycopene is reported to combat breast cancer specifically via mechanisms such as regulation of expression of p53 and Bax suppression of cyclin D inhibiting the activation of ERK and Akt signaling pathway and gynecological cancer via various signaling pathways such as STAT3 Nrf2 and NF-κB down-regulation of ITGB1 ITGA5 FAK MMP9 and EMT markers etc.
Topical Herbal Products as Adjuncts to Standard Care for the Management of Diabetic Foot Ulcers
Diabetic foot ulcers (DFUs) constitute one of the most debilitating complications of diabetes mellitus (DM). The use of topical herbal products as adjuvant agents in wound dressing is one of the most widely used practices worldwide. The present review aimed to provide a detailed and comprehensive systematic review focusing on randomized clinical studies and critically analyze not only the clinical outcomes but also the methodological approaches used by these studies.
The present systematic review was conducted according to the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) recommendations. For the extraction of relevant studies three databases were searched: PubMed Web of Science Core Collection and Scopus by two independent researchers.
A search of the three databases resulted in the identification of 5528 records which were reduced to 3224 after removal of duplicates. The application of inclusion and exclusion criteria left 35 full-text articles assessed for eligibility. Finally 13 articles were excluded and only 22 articles were advanced to the final analysis. Most studies reported details of local ulcer management only while others reported the additional systemic/surgical measures used for management. The present review identified 18 botanical agents/preparations used alone or in combination with other agents as adjuvant agents in treatment of DFUs. In most situations these agents proved to be effective.
The present review reported the methodological approaches and clinical outcomes of botanical extracts used topically for the treatment of diabetic foot ulcers in randomized controlled studies. These agents proved to be generally effective. However many gaps existed in the study designs which may limit the evidence-based value of these studies.
Biological Evaluation of Cucumis trigonus (Roxb.) for Memory Enhancing Activity in Scopolamine-induced Amnesia in Mice
Plants have been employed for centuries to enhance human health due to their cost-effectiveness and minimal adverse effects. Numerous plants exhibit a wide spectrum of pharmacological activities and various herbal medicines are currently being investigated for their memory-enhancing properties.
Cucumis trigonus (Roxb.) commonly known as Kachari or Bitter gourd is one such plant with diverse pharmacological attributes. Historically the fruits of C. trigonus have been utilized for addressing various conditions like leprosy pyrexia icterus hyperglycemia chronic cough bronchitis abdominal fluid accumulation anemia obstipation diverse gastrointestinal disease and cognitive impairment. The current investigation aims to explore the memory enhancement properties of C. trigonus rooted in its traditional applications particularly against scopolamine-induced amnesia in mice. Morris water maze and elevated plus maze paradigms were employed to evaluate cognitive performance. Furthermore the research examined acetylcholine neurotransmission oxidative stress markers and cerebral histopathology.
The results showed that C. trigonus ethanol extract (dose- 150 or 300 mg/kg. p.o.) markedly (p < 0.05) improved memory in scopolamine-induced amnesia in mice and significantly (p < 0.05) elevated hippocampus acetylcholine concentration. These findings revealed that the ethanol extract of C. trigonus fruits mitigates memory deficits and demonstrates neuroprotective efficacy analogous to the reference drug Piracetam. Additionally the extract showed notable in vivo antioxidant activity. The occurrence of flavonoids and phenols is likely to be responsible for its memory-enhancing effects due to their antioxidant properties which help to prevent the loss of neurons.
These results support the efficacy and potential of C. trigonus ethanol extract as an affordable alternative form of herbal medicine for the treatment of Amnesia.
An In-depth Analysis of Luteolin Regarding its Preclinical, Clinical and Nanoformulations Perspectives
A natural product is a natural compound or substance produced by a living organism that is found in nature. The term natural product has also been prolonged for commercial purposes to refers to dietary supplements cosmetics and food produced from natural sources without added artificial ingredients. Luteolin a bioflavonoid found abundantly in various fruits vegetables and medicinal plants has gained significant attention in recent years due to its potential pharmacological properties. This comprehensive review explores the multifaceted aspects of luteolin encompassing clinical studies experimental research kinetic analyses nanotechnology-based formulations and synergistic interactions with conventional drugs. The introduction section describes the various sources and biological functions of luteolin and emphasizes its importance in the realm of medicine. The clinical studies section provides insights into the therapeutic potential of luteolin in various human diseases highlighting its efficacy safety profile and potential mechanisms of action. Experimental studies exploring luteolin's mechanisms of action cellular interactions and therapeutic effects in various disease models. It elucidates underlying the biological mechanism of luteolin shedding light on its antioxidant anti-inflammatory anti-cancer and neuroprotective effects. Furthermore a detailed pharmacokinetic study examines the absorption distribution metabolism and excretion (ADME) of luteolin offering valuable information for optimizing its dosing regimens and enhancing therapeutic outcomes. The integration of nanotechnology in luteolin formulations is discussed focusing on innovative nanoformulations that improve its solubility stability and targeted delivery thus enhancing its bioavailability and efficacy. Additionally this review delves into the synergistic interactions between luteolin and conventional drugs emphasizing the potential for combination therapies to enhance treatment outcomes and reduce adverse effects. The synergistic mechanisms preclinical and clinical evidence and future prospects of these combinations are explored in detail. Future applications of luteolin appear to be very promising in a variety of fields including personalized medicine disease-specific medicines and preventative healthcare.
A Comprehensive Pharmacological Review of Natural Products Active Ingredients in Ulcerative Colitis
Ulcerative colitis (UC) is a nonspecific prolonged and recurrent autoimmune disease characterized by diarrhea mucopurulent stools and abdominal pain. Modern medicine believes that the disease is related to infectious genetic psychiatric allergic and especially autoimmune factors but the exact cause is unknown. Given that the disease is recurrent aggravating and persistent and has a certain cancer rate it is increasingly urgent to find effective treatments. It has been proved that UC is related to the abnormal regulation of signaling pathways in the body dysregulation of intestinal ecology and intestinal immune disorders and natural products active ingredients for the treatment of UC have the advantage of long-term efficacy and less toxic side effects compared to existing drugs. This paper reviews the pharmacological mechanisms associated with UC to gain insight into the therapeutic mechanisms of natural products active ingredients for UC and to better understand the advantages and potential of natural products active ingredients in the treatment of UC. This will provide guidance for the development of new therapeutic strategies and drugs and offer new hope for improving the quality of life of patients with UC.
Pathway Targeting and Mechanistic Elucidation of Phyto-compounds Relevant in Triple-negative Breast Cancer (TNBC)
Of the several forms of breast cancer triple-negative breast cancer (TNBC) is the most aggressive it is not responsive to traditional human/hormonal epithelial growth factor receptor 2 (HER2)-targeted therapies because the corresponding receptor targets are absent TNBC tends to be more invasive in form metastasis have an early recurrence rate and develop medication resistance. For TNBC some of the most popular types of treatments are resection chemotherapy and radiation therapy. Several studies are being carried out for the development of novel treatment approaches for improved TNBC diagnosis. As our knowledge of the molecular mechanisms behind the development of cancer has grown a vast array of anticancer drugs has been developed. The use of chemically produced pharmaceuticals has not significantly raised the overall survival rate over the previous few decades. As such novel approaches and cutting-edge chemopreventive medications are needed to improve the efficacy of existing TNBC therapies. Naturally occurring compounds derived from plants called phytochemicals are valuable resources for the development of novel medications for TNBC treatment. These phytochemicals often function by modulating molecular pathways associated with the onset and propagation of TNBC. Some of the specific methods include boosting antioxidant status deactivating carcinogens stopping proliferation inducing cell cycle arrest promoting apoptosis and immune system modulation. This review's main goal is to give a summary of the active components of natural products together with details on their molecular targets pharmacological action and current level of understanding. Several natural compounds that particularly target the pathways linked to TNBC in our study have been thoroughly described by us. We have done extensive research on many natural substances that could lead to the discovery of new targets for TNBC treatment.
Is there Any Role for Bach Flowers, Lavender Oil and Hypericum in Psychiatry?
Alternative medicine is a term encompassing several approaches proposed for their healing effects instead of conventional medicine. The present narrative review aimed at exploring the possible use of some popular alternative treatments to manage anxiety and depression with a specific focus on Bach flowers lavender oil and Hypericum which are among the most popular alternative remedies in Italy.
A thorough search was conducted across electronic databases such as PubMed Google Scholar and PsycINFO for English-written papers published in peer-reviewed journals available in full-text or abstract. The primary keywords included “Alternative medicine” “Anxiety” “Depression” “Bach Flowers” “Lavender Oil” and “Hypericum”. Studies were included if they met the following criteria: focus on the Bach flowers lavender oil or hypericum in the treatment or management of anxiety and depression.
The scientific evidence supporting the benefits of Bach flowers for anxiety and depression is still inconclusive with some studies suggesting potential benefits in reducing anxiety symptoms and other showing no significant effects. Lavender oil has been explored for its potential therapeutic effects on anxiety and depression but even in this case the overall findings remain controversial due to methodological limitations. St. John’s Wort (or Hypericum) showed some effect in mild to moderate depression with efficacy comparable to standard antidepressants and fewer side effects although its use requires careful cautions when prescribed with other drugs.
The overall findings of the present review would indicate that the scientific evidence about the possible usefulness of Bach flowers lavender oil and Hypericum is limited. If the effectiveness of Bach flowers is controversial some potential benefits of lavender oil and Hypericum have been reported however they need to be replicated and deepened in controlled clinical studies.
Synthetic Approaches and Reactivity of 3-Aminothieno[2,3-b]pyridine Derivatives A Review
The synthesis and chemical reactivity of 3-aminothieno[23-b]pyridine derivatives have been extensively studied due to their importance in medicinal chemistry and material sciences. This review focuses on the various synthetic strategies employed for their preparation including reactions involving 12-dihydro-2-thioxopyridine-3-carbonitrile derivatives phase-transfer catalysis and Thorpe-Ziegler cyclization. Additionally the chemical reactivity of these compounds is explored highlighting transformations such as cyclizations functional group modifications and coupling reactions. These advancements underline the versatility of 3-aminothieno[23-b]pyridines as valuable intermediates in organic synthesis and their potential for further functionalization in diverse chemical frameworks.
Triazine Derivatives: Their Synthesis and Biological Properties - A Review
Triazine compounds have become crucial entities in the pharmaceutical field due to their remarkable structural diversity and wide range of biological activities. This review explores their prominent role in drug discovery and development focusing on their efficacy as potent anticancer antiviral antimicrobial and antioxidant agents. Recent advances in synthetic methodologies using various starting materials such as nitrile biguanide bromoester arylamine and cyanide chloride are reviewed along with their implications for improved pharmacological properties including anticancer antibacterial antioxidant anti-inflammatory and antimicrobial effects. In addition the structure-activity relationship of triazine derivatives is explored offering insight into the key structural features that contribute to their therapeutic potential. This relationship plays an essential role in optimizing their efficacy as therapeutic agents helping to guide the development of more effective drugs with improved pharmacological profiles.
Recent Advances in Fluorometric Detection of Carcinogenic Heavy Metal Ions Using Fluorogenic Chemosensors: An Overview
In recent years a significant focus has been directed toward fluorogenic chemosensors for the optical detection of heavy metal ions due to their detrimental effects on both the environment and human health. Methods combining fluorometry and colorimetry have been widely utilized for sensing heavy metal ions because they are straightforward lucrative easy to use and enable rapid on-site analysis. As a result numerous research groups have dedicated extensive efforts to developing versatile fluorometric and colorimetric sensors for heavy metals. The development of innovative highly selective and sensitive chromogenic fluorosensors along with their detection capabilities remains a captivating area within supramolecular chemistry. This review outlines key aspects of the detection process including spectroscopic changes selectivity sensitivity visible colour shifts and potential in vivo recognition of heavy metal ions. It also emphasizes recent progress over the past decade in the fluorometric and colorimetric detection of heavy metal cations such as Hg2+ Cd2+ As3+/As5+ and Pb2+ using chromogenic and fluorogenic chemical receptors.
Indane-1,3-dione as a Versatile Intermediate for the Synthesis of 4-azafluorenones
Indane-13-dione is a reactive cyclic β-diketone that could be employed for preparing various molecular systems of potential biological applications. Among these 4-azafluorenones (also known as indeno[12-b]pyridines) represent one of the most promising classes of carbocyclic systems. Indeno-fused pyridines possess a wide range of medicinal properties including anti-proliferative activity and DNA topoisomerase Iα/Iiα inhibitory activity. In this review we presented all reports from 2000 to 2024 that cover the synthesis of indeno[12-b]pyridines and diindeno[12-b:2'1'-e]pyridines starting from indane-13-dione. The review is classified according to the type of reaction conditions that were applied. Additionally the reports that are related to the new trends in preparing indenopyridines are indexed in separate sections including the use of ionic liquids heterogeneous catalysts and microwave- and ultrasonic-assisted synthetic routes. Some complex synthetic routes are explained by plausible mechanisms.
Antidiabetic and Antihyperlipidemic Effects of Hydroalcoholic Extract of Cuscuta reflexa on High-fat Diet and Streptozotocin-Induced Type 2 Diabetic Rats
Cuscuta reflexa Roxb. has been traditionally utilized as an ethnomedicinal agent for managing various ailments including diabetes jaundice and rheumatic issues. This investigation aimed to evaluate the oral hypoglycemic and hypolipidemic effects of the hydroalcoholic extract of the aerial parts of Cuscuta reflexa (HAECR) in rats with diabetes induced by a high-fat diet (HFD) and streptozotocin (STZ). Additionally the study sought to identify the bioactive compounds responsible for these effects in Cuscuta reflexa.
To date only a few attempts have been made to isolate the lead bioactive compound from Cuscuta reflexa highlighting the need for further exploration of this herb through bioactivity-guided fractionation. The isolation and characterization of the responsible lead molecules could pave the way for developing a new safer therapeutic option compared to conventionally used drugs.
The study aims to evaluate the oral hypoglycemic and hypolipidemic activity of hydroalcoholic extract of the aerial parts of Cuscuta reflexa (HAECR) in a high-fat diet (HFD) and streptozotocin (STZ) induced diabetic rats along with elucidating the responsible bioactive compounds of Cuscuta reflexa.
The hydroalcoholic plant extract was standardized by marker calibration by HPLC and subsequently phytochemical screening by LC-MS. Column chromatography was adopted to isolate bioactive compounds from the extract which NMR FT-IR and MS spectroscopy subsequently characterized. Oral antihyperglycemic activity and toxicity studies were performed and antioxidant activities were studied.
No deaths or behavioural changes were observed during the toxicity study up to 2000 mg/kg oral dosing. Other toxicological parameters such as deviations in organ weights and haematological and histological parameters were also not observed. 250 mg/kg dose of HAECR exhibited significant antihyperglycemic activity (56.9% reduction in blood glucose level) in diabetic rats. In the HAECR-treated groups significant reductions were observed compared to the control group with cholesterol levels decreasing by 57% triglycerides by 50% SGPT by 50% and SGOT by 30%. Considering the extensive analytical spectroscopy interpretation results Quercetin and Stigmasterol are the two possible isolated compounds from our extract.
Thus this study suggested the antihyperlipidemic and antihyperglycemic activity of HAECR which may be attributed to phytomolecules such as Stigmasterol and Quercetin. Therefore our findings from the investigated part of the herb could be regarded as an adjunctive agent for treating diabetes mellitus.
Αlpha-phellandrene Alleviates Lipopolysaccharide-induced Neurogenic Inflammation in Zebrafish Larvae
Stimulation of the sensory nerves in the trigeminal ganglion triggers CGRP as well as nitric oxide release leading to dilation of the cranial blood vessels and causing neurogenic inflammation. The release of these mediators is associated with several neuroinflammatory disorders. It is suggested that neuroinflammation can be alleviated by inhibiting the release of these inflammatory mediators.
The present study aimed to investigate the neuroprotective effect of α-Phellandrene in LPS-induced Zebrafish larvae.
Neurogenic inflammation refers to localized inflammation within the peripheral and central nervous systems which can lead to various neuroinflammatory disorders such as headache migraine Alzheimer’s disease Parkinson’s disease Huntington’s disease and multiple sclerosis. This condition is triggered by neuronal activation releasing neuropeptides inflammatory mediators cytokines interleukins and tumor necrosis factor-α. This study aimed to investigate the neuroprotective effects of α-Phellandrene by in-vivo experiment. The development of a drug to treat neurogenic inflammation is a prime task for managing the condition. Hence this study was undertaken to find out a CGRP antagonist from a natural source to alleviate the neuro inflammatory disorders.
This study investigated the release of inflammatory mediators induced by lipopolysaccharides and the inhibitory effects of α-Phellandrene in zebrafish larvae. The inhibitory effect of α-Phellandrene on nitric acid production in larval fish homogenates was assessed using the Griess assay. Additionally the mRNA expression of TNF-α was quantified using RT-PCR.
The result of the behavioral study showed that treatment with α-Phellandrene (10 μg/mL) significantly (p<0.05) reduced the behavioral abnormalities as compared to LPS-treated animals. In addition α-Phellandrene-treated animals exhibited better nitric oxide inhibition activity as compared to the LPS-treated group. Further the molecular analysis revealed that the α-Phellandrene treatment significantly (p<0.05) reduced the mRNA expression of TNF-α as compared to LPS-treated group.
The results of behavioral study nitric oxide inhibition assay and molecular analysis suggest that α-Phellandrene prevents neuroinflammation in LPS-treated animals. It was concluded from the study that α-Phellandrene is used to treat neuroinflammation and it indicates that it possesses neuroprotective activity.
Bio-prospecting the Anti-oxidative and Radioprotective Role of Bioactive Pigment Isolated from Pontibacter indicus
To evaluate the anti-oxidative and radioprotective role of Pontibacter indicus SCG24 pigment during radiation exposure.
Radiation-induced cytotoxicity is quite common during cancer therapy. There is a need for naturally derived therapeutic molecules that can scavenge free radicals. They may act as substitutes for synthetic molecules. Hence there is a need for urgent evaluation of these potent compounds before therapeutic application.
The objective of this study is to examine the anti-oxidative and radioprotective role of P. indicus SCG24 pigment specifically to evaluate free radical scavenging X-ray irradiated HDF cells.
A radiotoleraent pigment-producing P. indicus SCG24 was isolated from pharmaceutical effluent. Chloroform was used as a primary solvent for pigment extraction. GCMS/MS analysed initial pigment composition. Various in-vitro antioxidant assays were performed using ABTS FRAP and DPPH assay. Flow cytometry was used to determine the rate of scavenging activity of pigment in HDF cells.
The GCMS/MS profile of the chloroform extract revealed twenty-two compounds. Furthermore based on the DPPH ABTS and FRAP assay the pigment was found to have significant antioxidant properties. The flow cytometry results indicate that the pigment possesses radioprotectant activity by neutralizing ROS species in HDF cells when exposed to X-ray radiation.
These observations on P. indicus SCG24 pigment suggested that the pigment may have potential therapeutic importance.
Effects of Silymarin on the Levels of Liver Enzymes and Hematological Parameters after Inguinal Hernia Repair: A Randomized Clinical Trial
Surgery can lead to local and systemic activation of oxidative and inflammatory systems. Therefore we aimed to evaluate the effects of silymarin on the levels of liver enzymes and hematological parameters after inguinal hernia repair.
In this randomized double-blind clinical trial 60 patients who were referred for hernia repair were included and randomly assigned into two groups. The intervention group was given silymarin three times a day and the control group received a placebo. The patient's vital signs hepatic enzymes blood and coagulation parameters were recorded before and after surgery. Data were analyzed by SPSSv18.
Hernia repair caused significant increases in the level of liver enzymes White Blood Cells (WBC) Platelet Count (PLT) and Poly Morphonuclear Neutrophils (PMN) (p<0.05) but did not cause significant alteration in the level of coagulation factors hematocrit (HCT) and hemoglobin (HB) (p>0.05). Supplementation of silymarin in patients significantly decreased the level of hepatic enzymes WBC PMN LYMPH and PLT (p<0.05). Furthermore the results for vital signs including Systolic Blood Pressure (SBP) Diastolic Blood Pressure (DBP) and PR were not changed after silymarin administration (p>0.05). Postoperative PTT levels in the intervention group were lower than those in the control group (p=0.023). Moreover a significant difference was observed between the International Normalized Ratio (INR) of the two groups after surgery (p=0.039).
Silymarin supplementation has the ability to attenuate hepatotoxicity induced by surgery; however further studies are needed to determine its exact mechanism of action.
1394-01-89-2449.
The Constituents Analysis and the Anti-inflammatory Activity of the Chinese Medicine: Kanglao Concoction
The Chinese medicine Kanglao concoction has been used clinically to treat tuberculosis. However its constituents and anti-inflammatory activity have not been fully understood.
In this study HPLC-MS2 has been employed to determine the main constituents in the concoction. The anti-inflammatory activity has been investigated by ELISA and Western Blot techniques.
The MS analysis revealed that tigogenin and afzelin were two main constituents in Kanglao concoction. Moreover the result of ELISA experiments showed that Kanglao concoction significantly reduced the expression of TNF-α and IL-1β at 5 mg/mL and 10 mg/mL to inhibit inflammation.
The expression of Notch pathway-related proteins in A549 cells increased under the stimulation of Mycobacterium tuberculosis and decreased dose-dependently upon the treatment of Kanglao concoction which was deduced to inhibit Notch pathway expression to impose anti-inflammatory activity.
A New Megastigmane Nor-sesquiterpene Isolated from Pourouma guianensis by High-Performance Countercurrent Chromatography
Pourouma guianensis (Urticaceae) is widespread throughout Brazil and is commonly known as “mapati”. Terpenes are common in Urticaceae species. However few studies have reported the isolation and characterisation of these compounds in Pourouma genus.
The aim of this study was to separate substances from stem barks of P. guianensis using a high-performance countercurrent chromatography gradient elution method. The dichloromethane extract of the P. guianensis stem bark was submitted to silica gel column chromatography yielding three fractions. Fraction 3 was submitted to a gradient elution system in high-performance countercurrent chromatography using two solvent systems hexane/ethyl acetate/methanol/water (1:2:x:1 x=1.0 and 1.5). Six compounds were isolated.
A new megastigmane nor-sesquiterpene named 2-acetyl-47-epoxy-3-oxy-559-trimethylhexahydrocoumaran (1) was obtained together with five known terpenes: vomifoliol (2) 2α3β19α23-tetrahydroxyurs-12-en-28-oic acid (3) 3-β-D-arabinopyranoside-19-hydroxyurs-12-en-28-oic acid (4) arjunolic acid (5) and tormentic acid (6). Fractions 1 and 2 were purified by binary gradient elution from hexane to ethyl acetate.
This process isolated three known compounds: friedelin (7) and 3β-friedelanol (8) from fraction 1 and β-sitosterol (9) from fraction 2. Gradient elution in countercurrent chromatography was a suitable alternative exploiting variations in the partition coefficient between substances with small structural differences.
Exploring Pharmacological Mechanisms, Clinical Trials and Patent Landscapes of Berberine: A Review
Traditional Chinese medicine has used berberine (BBR) for a long time. Berberine is a natural compound found in several plants including Berberis lyceum Royle Berberis thunbergii DC Berberis koreana Palib. Berberis vulgaris L. Mahonia aquifolium Mahonia bealei (Fort.) Carr. and Chelidonium majus L. Berberine is believed to help treat many diseases such as ovarian and colorectal cancer high blood pressure Parkinson's and Alzheimer's disease diabetes heart disorders depression viral infections and inflammatory diseases. However when taken orally berberine quickly breaks down in the body leading to low levels in the bloodstream. This means that its absorption in the intestines is limited which reduces its effectiveness despite its potential health benefits. The liver is the main organ that processes and uses berberine in both animals and humans and about 84% of berberine and its byproducts are excreted in the feces. We thoroughly reviewed the available research on berberine from reliable sources like PubMed ScienceDirect ClinicalTrials.gov and Scopus. Our study summarizes the latest findings on the therapeutic benefits of berberine and provides updated information on clinical research and patents. This review covers the various pharmacological effects of berberine including its use in treating Alzheimer's disease high blood pressure neuroprotective effects anti-arrhythmia Parkinson's disease diabetes cancer and depression.