Identification Of Alkaloids Research Articles

Identification of alkaloids from the methanol Leaf extract of Acalypha wilkesiana using HPLC/GC-MS

Identification of alkaloids from the methanol Leaf extract of Acalypha wilkesiana using HPLC/GC-MS

Characterization and identification of alkaloids in Phellodendri Chinensis Cortex and Phellodendri Amurensis Cortex based on UHPLC-IM-Q-TOF-MS

A strategy combining collision cross section(CCS) prediction and quantitative structure-retention relationship(QSRR) model for quinoline and isoquinoline alkaloids was established based on UHPLC-IM-Q-TOF-MS and applied to Phellodendri Chinensis Cortex and Phellodendri Amurensis Cortex. The strategy included the following three steps.(1) The molecular features were extracted by the "find features" algorithm.(2) The potential quinoline and isoquinoline alkaloids were screened by filtering the original characteristic ions extracted from Phellodendri Chinensis Cortex and Phellodendri Amurensis Cortex by the established CCS vs m/z prediction interval.(3) According to the retention time of candidate compounds predicted by QSRR model, the chemical constituents were identified in combination with the characteristic fragment ions and pyrolysis law of secondary mass spectrometry. With the strategy, a total of 80 compounds were predicted, and 15 were identified accurately. The strategy is effective for the identification of small analogs of traditional Chinese medicine.

Valorization of aromatic and Medicinal Plants of Ranomafana, District Ifanadiana, Region Vatovavy Fitovinany: Case of Vepris ampody and Vepris sp

For the conservation of the biodiversity of Ranomafana, the valorization of the aromatic and medicinal plants of Ranomafana is an alternative. Two plants of the RUTACEAE family were chosen Vepris ampody and Vepris sp. For this a multidisciplinary approach was adopted: an ethnobotanical survey for the traditional use, ecology of the plant in order to identify environmental conditions favorable to the development of the species, phytochemical screening and identification of the essential oils of the leaves, isolation of mycoendophytes and identification of the fatty acids resulting from the extracts of fermentation. Vepris ampody is used in traditional medicine, and the decoction of leaves and bark is used in case of fever, malaria, fatigue, and muscle pain. The leaves are rich in alkaloids and the essential oils in sabinene. Four strains have been isolated. After fermentation, these four strains produce fatty acids, mostly unsaturated. Vepri ssp. has no medicinal use, it is used to ward off a spell. The leaves are rich in alkaloids. The essential oil is rich in linalool. The perspectives of the study concern the popularization of culture and the identification of alkaloids.

Rapid identification of chemical components in vitro and in vivo of Menispermi Rhizoma by integrating UPLC-Q-TOF-MS with data post-processing strategy.

Menispermi Rhizoma (MR), the dried rhizome of Menispermum dauricum DC. (Menispermaceae), has been used to treat sore throat, enteritis, dysentery, and rheumatic arthralgia. Despite extensive research on its pharmacological effects, the chemical components in vitro and in vivo have not been thoroughly studied. To establish an efficient method for rapid classification and identification of alkaloids in MR and its preparations, as well as metabolites in vivo after oral administration of MR. Rapid identification of alkaloids and absorbed components of MR was performed using ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) coupled with UNIFI software. Moreover, the characteristic fragmentations and neutral losses of different types of alkaloids in MR were summarised to realise the rapid classification of alkaloids. A total of 55 components were unambiguously or tentatively identified in MR. Among them, 37 and 31 components were found in MR capsules and tablets, respectively. Meanwhile, 109 compounds were tentatively identified in rat plasma, urine and faeces, including 55 prototypes and 54 metabolites. Hydrogenation, hydroxylation, methylation, glucuronic acid and sulphate conjugations were the dominating metabolic fates of alkaloids. The data post-processing strategy established could greatly enhance the structural identification efficiency. The results obtained might lay the foundation for further interpretation of clinical effects, mechanism of action and quality control of MR.

Decoloration and alkaloid enrichment of Dactylicapnos scandens extracts based on the use of strong anion-exchange resins in tandem with strong cation-exchange silica-based materials

Alkaloids are natural bioactive ingredients but are usually present in low amounts in plant extracts. In addition, the dark color of plant extracts increases the difficulty in separation and identification of alkaloids. Therefore, effective decoloration and alkaloid enrichment methods are necessary for purification and further pharmacological studies of alkaloids. In this study, a simple and efficient strategy is developed for the decoloration and alkaloid enrichment of Dactylicapnos scandens (D. scandens) extracts. In feasibility experiments, we evaluated two anion-exchange resins and two cation-exchange silica-based materials with different functional groups using a standard mixture composed of alkaloids and nonalkaloids. By virtue of its high adsorbability of nonalkaloids, the strong anion-exchange resin PA408 is considered a better choice for the removal of nonalkaloids, and the strong cation-exchange silica-based material HSCX was selected for its great adsorption capacity for alkaloids. Furthermore, the optimized elution system was applied for the decoloration and alkaloid enrichment of D. scandens extracts. Nonalkaloid impurities in the extracts were removed by the use of PA408 in tandem with HSCX treatment, and the total alkaloid recovery, decoloration and impurity removal ratios are determined to be 98.74%, 81.45% and 87.33%, respectively. This strategy can contribute to further alkaloid purification and pharmacological profiling of D. scandens extracts, as well as other plants with medicinal value.

Aloe vera and its potency as antituberculosis against strains of Mycobacterium tuberculosis that is resistant to some tuberculosis drugs

Introduction: Aloe vera has anti-bacterial ability against Gram-positive and Gram-negative bacteria; however, anti-bacterial study, especially in multidrug resistant strain of Mycobacterium tuberculosis, has not been evaluated yet. This study aims to determine the potential of Aloe vera as an antituberculosis against drug-resistant strains of tuberculosis. Method: Stages of research include the production of ethanol extract of Aloe vera, then testing the phytochemicals (identification of alkaloids, steroids/triterpenoids, anthraquinone, flavonoids, saponins, tannins) and chemical content testing by thin layer chromatography (TLC). The anti-bacterial test for Mycobacterium tuberculosis was performed on the Lowenstein Jensen media. Results: Test results showed the qualitative identification, and TLC contains alkaloids, steroids/triterpenoids, anthraquinone, flavonoids, saponins, and tannins. Antioxidant activity against DPPH radical shows an IC50 value of 6927.133 ppm. Test of anti-bacterial activity to Mycobacterium Tuberculosis H37Rv and MDR TB strains HE (resistant to INH and Ethambutol), and SR (resistant to streptomycin and Rifampicin) showed inhibition ranging concentration of 50 mg/mL in all extracts as well as to test the sensitivity, a sensitive start to a concentration of 50 mg/mL in all extracts. Conclusions: Aloe vera contains alkaloids, steroids/triterpenoids, anthraquinone, flavonoids, saponins, and tannins that act as antioxidants and antituberculosis against strains of Mycobacterium tuberculosis that are not resistant and resistant to anti-tuberculosis drugs.

LC-MS/MS-based metabolomics approach revealed novel phytocompounds from sugarcane rind with promising pharmacological value.

Sugarcane provides many secondary metabolites for the pharmacological and cosmetic industries. Secondary metabolites, such as phenolic compounds, flavonoids, and anthocyanins, have been studied, but few reports focus on the identification of alkaloid and non-alkaloid phytocompounds in sugarcane. In this study, we identified 40 compounds in total from the rinds of cultivated sugarcane varieties (including eight alkaloids, 24 non-alkaloids, and eight others) by using the liquid chromatography-tandem mass spectrometry (LC-MS/MS) approach. Among these compounds, 31 were novel and are reported for the first time in sugarcane. Some alkaloids such as 3-indoleacrylic acid, N,N-dimethyl-5-methoxytryptamine, tryptamine, 6-hydroxynicotinic acid, and 6-deoxyfagomine are identified the first time in sugarcane rind. Four alkaloids such as trigonelline, piperidine, 3-indoleacrylic acid, and 6-deoxyfagomine are found abundantly in sugarcane rind and these compounds have promising pharmaceutical value. Some phytocompounds such as choline and acetylcholine (non-alkaloid compounds) were most common in the rind of ROC22 and Yuetang93/159 (YT93/159). Hierarchical cluster analysis and principal component analysis revealed that the ROC22, Taitang172 (F172), and Yuetang71/210 (YT71/210) varieties were quite similar in alkaloid composition when compared with other sugarcane varieties. We have also characterized the biosynthesis pathway of sugarcane alkaloids. The rind of F172, ROC22, and YT71/210 showed the highest total alkaloid content, whereas the rind of ROC16 revealed a minimum level. Interestingly, the rind extract from YT71/210 and F172 showed maximum antioxidant activity, followed by ROC22. Our results showed the diversity of alkaloid and non-alkaloid compounds in the rind of six cultivated sugarcanes and highlighted the promising phytocompounds that can be extracted, isolated, and utilized by the pharmacological industry. © 2022 Society of Chemical Industry.

Identification of Alkaloids from Terminalia chebula as Potent SARS- CoV-2 Main Protease Inhibitors: An In Silico Perspective.

Natural compounds in medicinal plants are best remedies for different diseases and are important to develop new drugs. This work was dedicated to understand the role of different natural compounds of Terminalia Chebula, a well‐known herbal plant, in the treating of Covid 19. In this article, we have investigated interactions of such natural compounds from Terminalia Chebula with the main protease (Mpro) of the SARS‐CoV‐2, which is a key component for cleavage of viral polyprotein, and an important target for the development of drugs towards COVID‐19. We have performed molecular docking study on 22 different molecules of Terminalia Chebula and proposed that 7 of the natural compounds (triterpenoids and sterols) interacts with a comparable or stronger interactions than the inhibitor N3. Molecular dynamics simulations (100 ns) revealed that 7 Mpro‐Terminalia Chebula complexes are stable, conformationally less fluctuated, slightly less compact, and marginally expanded than ligand‐free conformation of Mpro. The intermolecular H‐bonding and detailed MM/PBSA and MM‐GBSA analysis showed Daucosterol interaction to be the most strong, whereas comparable interactions were observed for Arjunetin, Maslinic acid, and Bellericoside. Our study suggested that these natural compounds can act as potent Mpro inhibitors for SARS‐CoV‐2, and may evolve as promising anti‐COVID‐19 drugs in the near future.

Determination of Alkaloids and Flavonoids in Sophora flavescens by UHPLC-Q-TOF/MS

This study is based on UHPLC-Q-TOF/MS and fragment ions to achieve classification and identification of alkaloids and flavonoids in Sophora flavescens. By reviewing the available and relevant literature, the mass fragmentation rules of alkaloids and flavonoids were summarized. 0.1% formic acid water (A) and acetonitrile (B) were used as mobile phases. 37 chemical constituents were identified, including 13 alkaloids and 24 flavonoids. This research method offers a complete strategy based on the fragmentation information of characteristic fragment ions and neutral loss obtained by MS/MS to characterize the chemical composition of Sophora flavescens.

A new N-oxide benzylisoquinoline alkaloid isolated from the leaves of atemoya (Annona cherimola × Annona squamosa)

Abstract Phytochemical investigation of the atemoya aerial parts was carried out by LC-MS-IT and cytotoxic activities were evaluated as well. These results led to the identification of a new N-oxide alkaloid (dehydroanomuricine-N-oxide) and eight other alkaloids: scoulerine, reticuline, isocorydine, norisocorydine, asimilobine, nornuciferine, anonaine, and liriodenine. The new alkaloid dehydroanomuricine-N-oxide and anomuricine were also isolated. The structures of these compounds were determined by spectroscopic and spectrometric techniques. The cytotoxic capacity of crude methanolic extract and the alkaloidal fraction were evaluated, showing moderate cytotoxicity. The isolation and identification of these alkaloids are an important contribution to the chemotaxonomy of the genus Annona and the Annonaceae family.

Phytochemical and high-performance thin-layer chromatography analysis of Ashawattha (Ficus religiosa Linn.) Kaanda Twaka (outer portion of stem bark) Churna (powder)

AIM: The aim of this study was to evaluate phytochemical constituent and high-performance thin-layer chromatography (HPTLC) analysis of Ashawattha Kandatwaka (the outer portion of stem bark) Churna (powder). INTRODUCTION: Ashawattha Kandatwaka Churna is a major constituent of numerous ayurvedic formulations. The plant has possessed their various pharmacological activities such as antifungal, anthelmintic, hypoglycemic, antibacterial, antioxidant, anticonvulsant, hypolipidemic, immunomodulatory, and wound healing activities. MATERIALS AND METHODS: Experiments were performed on authenticated plant materials following standard procedures. The methanol extract of stem bark of Ficus religiosa Linn. was used for the HPTLC study. Toluene (9 ml) and ethyl acetate (1 ml) were used for stem bark of F. religiosa Linn. as a mobile phase. RESULTS: Identification of alkaloids, steroids, and amino acids was confirmed through the phytochemical parameter. In the HPTLC study, the Rf values obtained at 254 nm were 0.02 and at 366 nm were 0.01, 0.17, and 0.53, respectively. CONCLUSION: Physiochemical analysis including HPTLC of Ashawattha Kaanda Twaka Churna will help in further standardization.

Identification of alkaloids from Justicia adhatoda as potent SARS CoV-2 main protease inhibitors: An in silico perspective

The COVID-19 pandemic, caused by SARS CoV-2, is responsible for millions of death worldwide. No approved/proper therapeutics is currently available which can effectively combat this outbreak. Several attempts have been undertaken in the search of effective drugs to control the spread of SARS CoV-2 infection. The main protease (Mpro), key component for the cleavage of the viral polyprotein, is considered to be one of the important drug targets for treating COVID-19. Various phytochemicals, including polyphenols and alkaloids, have been proposed as potent inhibitors of Mpro. The alkaloids from leaf extracts of Justicia adhatoda have also been reported to possess anti-viral activity. But whether these alkaloids exhibit any inhibitory effect on SARS CoV-2 Mpro is far from clear. To explore this in detail, we have adopted computational approaches. Justicia adhatoda alkaloids possessing proper drug-likeness properties and two anti-HIV drugs (lopinavir and darunavir; having binding affinity -7.3 to -7.4 kcal/mol) were docked against SARS CoV-2 Mpro to study their binding properties. Only one alkaloid (anisotine) had interaction with both the catalytic residues (His41 and Cys145) of Mpro and exhibited good binding affinity (-7.9 kcal/mol). Molecular dynamic simulations (100 ns) revealed that Mpro-anisotine complex is more stable, conformationally less fluctuated; slightly less compact and marginally expanded than Mpro-darunavir/lopinavir complex. Even the number of intermolecular H-bonds and MM-GBSA analysis suggested that anisotine is a more potent Mpro inhibitor than the two previously recommended antiviral drugs (lopinavir and darunavir) and may evolve as a promising anti-COVID-19 drug if proven in animal experiments and on patients.

Screening of Extraction Process and The Estimation of Total Alkaloids in Carica papaya Linn. Leaf

The papaya leaf decoctions have been widely used as a traditional treatment for malaria. The alkaloid of papaya leaves, carpaine, is reported to have the antiplasmodial activity in vitro. The industrial-scale commercial product development requires the quantification of the carpaine, and total alkaloids in the papaya leave as the raw materials. This study aims to optimize the extraction process leading to the highest yield and total alkaloids. The extraction process was carried out using different methods and solvents. The first method was maceration with the water-miscible solvent of ethanol: distilled water: HCl 37% (89: 10: 1 v/v/v). The second method was maceration with the water-immiscible solvent of dichloromethane solvents in pH 8-9 with ammonium hydroxide. The third method was digestion with acid water solvent of 0.05 N HCl. The identification of alkaloids employed the analysis using Thin Layer Chromatography (TLC) and Dragendroff reagent. The quantification of carpaine used a densitometer, while the spectrophotometric method was used to estimate the total alkaloids. The results showed that despite the extraction methods used, the tested extracts confirm the alkaloids content with the highest yield of 3.09% (84.72% of total alkaloids).

Systematic characterization of alkaloids in Eomecon chionantha Hance using ultrahigh-performance liquid chromatography-tandem quadrupole Exactive Orbitrap mass spectrometry with a four-step screening strategy.

Eomecon chionantha Hance (ECH), a traditional folk herb, is commonly used to treat traumatic injuries based on its analgesic and anti-inflammatory properties. Previous studies have reported that alkaloids are the major bioactive components in ECH. Therefore, identification of alkaloids from ECH contributes to the discovery of its potential active ingredients and quality control in clinic treatments. A four-step screening strategy was performed as follows. (1) Extracting the accurate masses of ions related to different molecules. (2) Screening different types of compounds using their molecular cations, protonated molecules, diagnostic product ions and fragmentation pathways. (3) Comparing the characteristic product ion formulae to obtain the type and number of substituents. (4) Using the biosynthetic pathways of isoquinoline alkaloids to determine the concentration of alkaloids. Ultrahigh-performance liquid chromatography-tandem quadrupole Exactive Orbitrap mass spectrometry (UHPLC/Q-Exactive Orbitrap MS) analysis combined with the four-step screening strategy was used to profile the alkaloids in ECH. The structures of 95 alkaloids in ECH were unambiguously identified or reasonably assigned, of which 76 were reported in ECH for the first time. Six types of benzylisoquinoline alkaloids were identified in ECH: six benzyltetrahydroisoquinolines, nine protopines, five N-methyltetrahydroprotoberberines, six protoberberines, eight benzophenanthridines and sixty-one dihydrobenzophenanthridines. This comprehensive study identified the alkaloids in ECH, thus providing a practical reference for further research. The UHPLC/Q-Exactive Orbitrap MS method, combined with the four-step screening strategy, which was developed and successfully applied to identify the alkaloids in ECH, may also be applicable for the efficient screening of other herbal medicines.

Rapid Determination of Furoquinoline Alkaloids in Rutaceae Species by Ultra-Performance Liquid Chromatography (UPLC) with Photodiode Array (PDA) and Electrospray Ionization–Quadrupole Time-of-Flight Mass Spectrometry (ESI-Q-TOF/MS)

A qualitative and quantitative method based on ultra-performance liquid chromatography (UPLC) and photodiode array (PDA) and electrospray ionization–quadrupole time-of-flight mass spectrometry (ESI-Q-TOF/MS) was developed, verified, and used to determine the quinoline alkaloids in Dictamnus dasycarpus and Zanthoxylum schinifolium, belonging to the Rutaceae family. Excellent analyte peak resolution was achieved on both quaternary and binary pumps by using acetonitrile and water containing 0.1% formic acid as the mobile phase using a C18 column. All alkaloids exhibited maximum absorption wavelength from 239 to 244 nm. The analytes were ionized as quasi-molecular ions [M + H]+ in MS and were characterized by using fragmentation ions formed by collision-induced dissociation (CID). This information was included in a library that was used to qualitatively identify alkaloids. The proposed method showed excellent linearity (r2 > 0.9988), limits of detection (PDA ≤ 25 ng/mL, MS ≤ 1.2 ng/mL), limits of quantification (PDA ≤ 75 ng/mL, MS ≤ 3.6 ng/mL), precision (in terms of relative standard deviation) of PDA ≤ 1.81% and MS 5.7%,. Liquid–liquid extraction (LLE) and solid-phase extraction (SPE) were conducted to separate and purify the alkaloids from the extracts. The analyte recoveries were determined to be PDA ≤ 103.11% and MS ≤ 104.45%. The method proceeded to deliver the comparable results for the determination of alkaloid components in samples. The developed UPLC-PDA and UPLC-ESI-Q-TOF/MS protocol facilitated the rapid, qualitative and quantitative identification of alkaloids in plants.

The identification of alkaloids from the stems of Picrasma quassioides via computer-assisted structure elucidation and quantum chemical calculations

Four new alkaloids (1-4) and one known alkaloid were isolated from the stems of Picrasma quassioides. The structures of these isolated compounds were elucidated by spectroscopic analyses, a combination of computer-assisted structure elucidation software (ACD/Structure Elucidator) and gauge-including atomic orbital (GIAO) calculation of 1 D NMR data. All compounds were evaluated for their cytotoxic activities against hepatocellular carcinoma HepG2 and Hep3B cells. However, they did not show obvious inhibitory activities.

Isolation and identification of alkaloids from Macleaya microcarpa by UHPLC\u2013Q-TOF-MS and their cytotoxic activity in vitro, antiangiogenic activity in vivo

BackgroundExtensive bioactivities of alkaloids from the genus Macleaya (Macleaya cordata (Willd.) R. Br. and Macleaya microcarpa (Maxim.) Fedde) have been widely reported, as well as more and more concerned from the scientific communities. However, systematic research on the phytochemical information of M. microcarpa is incomplete. The aim of this study was to rapidly and conveniently qualitative analyze alkaloids from M. microcarpa by ultra-performance liquid chromatography/quadrupole-time-of-fight mass spectrometry (UHPLC–Q-TOF-MS) using accurate mass weight and characteristic fragment ions, furthermore separate and identify the main alkaloids, test antitumor activity in vitro and antiangiogenic activity in vivo.ResultsA total of 14 alkaloids from fruits of M. microcarpa were identified by UHPLC–Q-TOF-MS, including 5 protopines, 2 benzophenanthridines, 1 dimer, 1 dihydrobenzophenanthridines and 5 unknown structure compounds. Two major alkaloids were isolated by various column chromatographic methods. Their structures were determined by NMR data and related literatures. The two major alkaloids were evaluated for intro cytotoxic activities against HL-60, MCF-7, A-549, and in vivo antiangiogenic activity using transgenic zebrafish.ConclusionsCurrent qualitative method based on UHPLC–Q-TOF-MS technique provided a scientific basis for isolation, structural identification, and in vitro or in vivo pharmacological further study of alkaloids from M. microcarpa in the future.

Isolation and identification of alkaloids and glycosides active compound from Geranium lucidum and Geranium purpureum

The study aimed at isolating and identification of alkaloids and glycosides active compound from the Geranium lucidum and Geranium purpureum species Grananiaceae using HPLC technique. results Phytochemical analysis of the studied plant revealed the presence of four alkaloids compounds (Palmatine, Columbamine, pseudo columbamine, Geraniin) and Five glycosides compounds (Geranioside A, Geranioside B, Quercetin 4-O-β -glucopyranoside, Quercetin 3-O-β -glucopyranoside, Kaempferol- β-glucopyranoside). These compounds showed differences in their concentrations between and within species studied where Geraniin showed the highest concentration 96.05 ppm in G.purpureum. The highest concentration of glycoside content was recorded by Quercetin 4-O-β – glucopyranoside in G.lucidum With a concentration of 268.54 ppm

Antiplasmodial activity and cytotoxicity, isolation of active alkaloids, and dereplication of Xylopia sericea leaves ethanol extract by UPLC-DAD-ESI-MS/MS.

To assess the antiplasmodial activity of the ethanol extract of Xylopia sericea leaves, Annonaceae, often associated with antimalarial use and to perform a bioguided isolation of active compounds. Dereplication of ethanol extract by the UPLC-DAD-ESI-MS/MS technique allowed the identification of the major constituents, isolation and identification of alkaloids. The antiplasmodial and cytotoxic activity of the extract, fractions and isolated compounds was evaluated against the chloroquine-resistant W2 strain Plasmodium falciparum and HepG2 cells, respectively. Ethanol extract showed high reduction of parasitemia as well as moderate cytotoxicity (86.5±3.0% growth inhibition at 50μg/ml and CC50 72.1±5.1μg/ml, respectively). A total of eight flavonoids were identified, and two aporphine alkaloids, anonaine and O-methylmoschatoline, were isolated. Anonaine disclosed significant antiplasmodial effect and moderate cytotoxicity (IC50 23.2±2.7μg/ml, CC50 38.3±2.3μg/ml, SI 1.6) while O-methylmoschatoline was not active against P.falciparum and showed a low cytotoxicity (33.5±1.9% growth inhibition at 50μg/ml, CC50 274.4±0.5μg/ml). Characterization of Xylopia sericea leaves ethanol extract by UPLC-DAD-ESI-MS/MS as well as its antiplasmodial activity and the occurrence of anonaine and O-methylmoschatoline in this Xylopia species are reported by the first time.

Identification of Alkaloids from Corydalis yanhusuo W. T. Wang as Dopamine D₁ Receptor Antagonists by Using CRE-Luciferase Reporter Gene Assay.

Corydalis yanhusuo W. T. Wang (C. yanhusuo) has been traditionally used for drug addiction and pain relief in China. In our previous study, we showed that the extract of C. yanhusuo blocks dopamine receptors, demonstrating that its pharmacological activities are mostly due to the antagonistic effects of some of its components at dopamine receptors. As part of our ongoing project on C. yanhusuo, the aim of the present study is to establish a high-throughput and low-cost screening assay system and test the abilities of the isolated alkaloids from C. yanhusuo to inhibit dopamine-induced dopamine D1 receptor activity. By using our established cyclic adenosine monophosphate (cAMP)-response element (CRE)-luciferase reporter gene assay system, we identified eight alkaloids from C. yanhusuo with D1 receptor antagonistic activities. We next validated the activities of these compounds using fluorometric imaging plate reader (FLIPR) assay by measuring the intracellular Ca2+ change. Six out of eight compounds, including tetrahydropalmatine, corydaline, 13-methyldehydrocorydalmine, dehydrocorybubine, dehydrocorydaline, and columbamine, can be confirmed for their inhibitory activities. The dopamine-receptor-antagonistic effects of four compounds, including 13-methyldehydrocorydalmine, dehydrocorydaline, columbamine, and corydaline, are reported for the first time. The present study provides an important pharmacological basis to support the traditional use of C. yanhusuo in China.